pteridines has been researched along with bi 2536 in 140 studies
Timeframe | Studies, this research(%) | All Research% |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 0 (0.00) | 18.2507 |
2000's | 12 (8.57) | 29.6817 |
2010's | 114 (81.43) | 24.3611 |
2020's | 14 (10.00) | 2.80 |
Authors | Studies |
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Adolf, GR; Baum, A; Garin-Chesa, P; Grauert, M; Gürtler, U; Hoffmann, M; Kraut, N; Krssák, M; Lénárt, P; Lieb, S; Peters, JM; Petronczki, M; Quant, J; Rettig, WJ; Steegmaier, M | 1 |
Di Fiore, B; Hoffmann, M; Kraut, N; Lénárt, P; Lipp, JJ; Peters, JM; Petronczki, M; Rettig, WJ; Steegmaier, M | 1 |
Musacchio, A; Plyte, S | 1 |
Glotzer, M; Kraut, N; Peters, JM; Petronczki, M | 1 |
Giranda, VL; Johnson, EF; Luo, Y; Stewart, KD; Woods, KW | 1 |
Coli, R; Ding, YH; Feru, F; Kohls, D; Kothe, M; Kuhn, C; Low, S; Rennie, GR | 1 |
Frost, A; Hedbom, S; Hoesl, CE; Kaiser, R; Mross, K; Munzert, G; Rentschler, J; Rouyrre, N; Steinbild, S; Trommeshauser, D | 1 |
Carlomagno, F; Nappi, TC; Salerno, P; Salvatore, G; Santoro, M; Zitzelsberger, H | 1 |
Bunz, F; Diaz, LA; Kinzler, KW; Pagliarini, R; Papadopoulos, N; Rago, C; Sur, S; Vogelstein, B | 1 |
Bailly, C; Créancier, L; Dos Santos, C; Kruczynski, A; Manenti, S; Payrastre, B; Recher, C; Renner, AG | 1 |
Schöffski, P | 1 |
He, B; Li, Z; Luthra, P; Sun, D | 1 |
Fritsch, H; Munzert, G; Soto, E; Staab, A; Tillmann, C; Trocóniz, IF; Trommeshauser, D | 1 |
Lorenz, J; Mössner, J; Wiedmann, M; Wolf, S | 1 |
Hasskarl, J; Lübbert, M; Schnerch, D; Wäsch, R | 1 |
Cerny-Reiterer, S; Ferenc, V; Gleixner, KV; Gruze, A; Hadzijusufovic, E; Mayerhofer, M; Meyer, RA; Peter, B; Pickl, WF; Sillaber, C; Valent, P | 1 |
Aerts, C; Allgeier, A; Blay, JY; Bogaerts, J; Brain, E; De Greve, J; Fontaine, C; Fritsch, H; Hanft, G; Lacombe, D; Machiels, JP; Munzert, G; Rapion, J; Ray-Coquard, I; Schöffski, P; Sleijfer, S; Soria, JC; Wolter, P | 1 |
Frickhofen, N; Fritsch, H; Gaschler-Markefski, B; Hanft, G; Kortsik, C; Munzert, G; Reck, M; Schuler, M; Sebastian, M; von Pawel, J; Waller, CF | 1 |
Choi, E; Jeong, JY; Jeong, K; Lee, H; Lee, HO | 1 |
Al-Batran, SE; Fritsch, H; Hochhaus, A; Hofheinz, RD; Jäger, E; Munzert, G; Reichardt, VL; Trommeshauser, D | 1 |
de Boer, RA; Lu, B; Maass, AH; Mahmud, H; Silljé, HH; van Gilst, WH; Yu, B | 1 |
Döge, C; Freiwald, M; Fritsch, H; Munzert, G; Soto, E; Staab, A; Trocóniz, IF | 1 |
Ackermann, S; Berthold, F; Eggert, A; Ehemann, V; Fischer, M; Goeser, F; Hero, B; Schramm, A; Schulte, JH | 1 |
Chevassut, TJ; Kishikova, L; Powell, FL; Stewart, HJ; Wheatley, SP | 1 |
Cerny-Reiterer, S; Ferenc, V; Gleixner, KV; Hadzijusufovic, E; Herrmann, H; Horny, HP; Mirkina, I; Müllauer, L; Peter, B; Pickl, WF; Schuch, K; Valent, P; Willmann, M; Winter, V | 1 |
Matsumura, F; Yamakita, Y; Yamashiro, S | 1 |
Al-Awar, R; Datti, A; Fujitani, M; Grinshtein, N; Irwin, MS; Isaac, M; Kaplan, DR; Prakesch, M; Uehling, D; Wrana, JL | 1 |
Choy, E; Duan, Z; Harmon, D; Hornicek, FJ; Liu, X; Mankin, H; Yang, C; Yang, S | 1 |
Posern, G | 1 |
Eckerdt, F | 1 |
Bar-On, O; Ganoth, D; Hershko, A; Moshe, Y | 1 |
Doege, C; Freiwald, M; Munzert, G; Soto, E; Staab, A; Trocóniz, IF | 1 |
Ding, Y; Feenstra, K; Furge, KA; Huang, D; Looyenga, BD; Mackeigan, JP; Petillo, D; Smith, J; Teh, BT; Zhang, Z | 1 |
Anderson, KC; Delmore, J; Gray, NS; Klippel, S; Kung, AL; McMillin, DW; Miduturu, CV; Mitsiades, CS; Negri, J; Ooi, M; Richardson, PG | 1 |
Brassesco, MS; Montaldi, AP; Morales, AG; Oliveira, JC; Pezuk, JA; Sakamoto-Hojo, ET; Scrideli, CA; Tone, LG | 2 |
Dong, MQ; Han, Y; Hou, W; Jing, Z; Li, J; Liao, J; Tian, C; Wang, J; Xu, X | 1 |
Foley, EA; Kapoor, TM; Maldonado, M | 1 |
Budin, G; Reiner, T; Weissleder, R; Yang, KS | 1 |
Lorenz, J; Mössner, J; Thrum, S; Wiedmann, M | 1 |
Cui, JL; Du, XL; Feng, YB; Huo, YQ; Lin, DC; Peng, H; Ruan, X; Wang, CJ; Wang, MR; Wang, YQ; Zhan, QM; Zhang, H; Zhang, TT; Zhang, Y | 1 |
Chang, YC; Ouyang, P; Wu, CH; Yen, TC | 1 |
Dunn, SE; Fotovati, A; Hu, K; Law, JH | 1 |
Elemento, O; Houghtaling, BR; Kapoor, TM; Wacker, SA | 1 |
Alimova, I; Birks, DK; Donson, AM; Dubuc, A; Foreman, NK; Handler, MH; Harris, PS; Knipstein, J; Taylor, MD; Venkataraman, S; Vibhakar, R | 1 |
Chen, J; Dunham, C; Dunn, SE; Fotovati, A; Jayanthan, A; Jones, C; Kerr, JM; Lee, C; Narendran, A; Singh, SK; Singhal, A; Triscott, J; Venugopal, C; Verreault, M; Wakimoto, H; Yip, S | 1 |
Burkard, ME; Jallepalli, PV; Santamaria, A | 1 |
Brassesco, MS; de Oliveira, JC; Montaldi, AP; Morales, AG; Pezuk, JA; Sakamoto-Hojo, ET; Scrideli, CA; Tone, LG; Valera, ET | 1 |
Chu, QS; Ellis, PM; Fritsch, H; Gaschler-Markefski, B; Gyorffy, S; Laurie, SA; Leighl, N; Munzert, G | 1 |
Gray, NS; Kwiatkowski, N; Lim, SM; Yang, PL; Zeng, H; Zhang, W; Zhang, Z | 1 |
Aulitzky, WE; Dittrich, C; Fleischer, F; Hollerbach, S; Merger, M; Mross, K; Munzert, G; Scheulen, ME; Schmid, RM; Schutte, J; Strumberg, D | 1 |
Benz, A; Bihrer, V; Canamero, M; Engels, K; Haupenthal, J; Kollmar, O; Korkusuz, H; Kriener, S; Kronenberger, B; Longerich, T; Piiper, A; Pleli, T; Richter, S; Schmithals, C; Vogl, TJ; Waidmann, O; Zeuzem, S | 1 |
Baiocchi, M; Biffoni, M; De Maria, R; Di Franco, S; Federici, G; Francescangeli, F; Pagliuca, A; Patrizii, M; Ricci Vitiani, L; Signore, M; Todaro, M; Zeuner, A | 1 |
Handel, MA; Jordan, PW; Karppinen, J | 1 |
Ang, BT; Brooks, HB; Campbell, RM; Chong, YK; Foong, CS; Sandanaraj, E; Tang, C | 1 |
Cheson, BD; Friedberg, JW; Fritsch, H; Juvvigunta, V; Munzert, G; Petit, C; Vose, JM; Waller, EK; Younes, A | 1 |
Barillot, E; Cruzalegui, F; De Koning, L; Decaudin, D; Depil, S; Dubois, T; Dumont, A; Gentien, D; Gravier, E; Lang, G; Maire, V; Marangoni, E; Marty-Prouvost, B; Némati, F; Pierré, A; Richardson, M; Rigaill, G; Roman-Roman, S; Tesson, B; Tucker, GC; Vincent-Salomon, A | 1 |
Albitar, L; Brachova, P; Dai, D; Ianzini, F; Kosmacek, EA; Laidler, LL; Leslie, KK; Liu, D; Mackey, MA; Meng, X; Wang, X; Xiong, Z; Yang, S; Zhang, Y; Zhu, D | 1 |
Chiorean, EG; Elzey, BD; Hazbun, T; Konieczny, SF; Kuang, S; Liu, X; Liu, XS; Ratliff, TL; Rice, SJ; Song, B | 1 |
Baran, V; Kovarikova, V; Rehak, P; Solc, P; Sutovsky, P | 1 |
Brassesco, MS; de Oliveira, HF; de Oliveira, JC; Morales, AG; Pezuk, JA; Scrideli, CA; Tone, LG | 1 |
Beato, M; Di Croce, L; Font-Mateu, J; Molina, H; Pisano, P; Verde, G; Wierer, M | 1 |
Benes, C; Florian, S; Mitchison, TJ; Moerke, N; Shamu, C; Tang, Y; Xie, T | 1 |
Biankin, AV; Caldon, CE; Clark, SJ; Cowley, MJ; Gallego-Ortega, D; Gee, JM; McCloy, RA; Musgrove, EA; Nicholson, RI; Ormandy, CJ; Print, CG; Sergio, CM; Stone, A; Valdes-Mora, F | 1 |
Carducci, MA; Gonzalez, M; Hammers, H; Kachhap, SK; Kaelber, NS; Kim, E; Kortenhorst, MS; Mendonca, J; van Diest, PJ; Wissing, MD | 1 |
Yim, H | 1 |
Ambudkar, SV; Cheng, HW; Hsiao, SH; Huang, YH; Li, YQ; Luo, SY; Sim, HM; Tuo, WC; Wu, CP | 1 |
Berns, R; Bouffet, E; Dunham, C; Dunn, SE; Foster, C; Fotovati, A; Hawkins, C; Hukin, J; Lee, C; Manoranjan, B; Narendran, A; Northcott, P; O'Halloran, K; Pambid, MR; Ramaswamy, V; Rassekh, R; Singh, SK; Singhal, A; Taylor, MD; Triscott, J; Venugopal, C; Yip, S | 1 |
Berdel, WE; Bug, G; Döhner, H; Fleischer, F; Fritsch, H; Garin-Chesa, P; Krämer, A; Krauter, J; Lübbert, M; Müller-Tidow, C; Munzert, G; Nachbaur, D; Ottmann, OG; Taube, T; Valent, P | 1 |
Anderson, JP; Babcock, M; Bergeron, M; Chiou, SS; Fauss, D; Motter, R; Nelson, S; San Pablo, F; Tanaka, P | 1 |
Cassimeris, L; Silva, VC | 1 |
Bertomeu, T; Bucur, O; Dewar, R; Goganau, I; Khosravi-Far, R; Pennarun, B; Petrescu, SM; Stancu, AL | 1 |
Abbott, NJ; Bertone, P; Danovi, D; Elbatsh, AM; Ender, C; Engström, PG; Ferretti, P; Folarin, A; Gagrica, S; Georgian, A; Gogolok, S; Harvey, KJ; Paddison, PJ; Pollard, SM; Preston, JE; Smith, A; Stricker, SH; U, KP; Yu, D | 1 |
Hayashi, A; Kondo, T; Tabuchi, Y; Yunoki, T | 1 |
Lund-Andersen, C; Nähse-Kumpf, V; Patzke, S; Syljuåsen, RG | 1 |
Brassesco, MS; Morales, AG; Oliveira, JC; Pezuk, JA; Queiroz, RG; Scrideli, CA; Tone, LG | 1 |
Ciceri, P; Fedorov, O; Filippakopoulos, P; Hunt, JP; Knapp, S; Lasater, EA; Martin, S; Müller, S; O'Mahony, A; Pallares, G; Picaud, S; Shah, NP; Treiber, DK; Wells, C; Wodicka, LM | 1 |
Callaini, G; Glover, DM; Gottardo, M; Riparbelli, MG | 1 |
Kaur, P; Kumar, M; Pydi, SP; Sharma, S; Singh, TP | 1 |
Becker, S; Dötsch, C; Knecht, R; Krämer, A; Kurunci-Csacsko, E; Kuster, B; Pachl, F; Raab, M; Strebhardt, K | 1 |
Ahmad, N; Bi, P; Burcham, G; Elzey, BD; Konieczny, SF; Kuang, S; Li, J; Li, Z; Liu, X; Lu, Y; Ratliff, T | 1 |
Becker, S; Bug, G; Dötsch, C; Hehlgans, S; Krämer, A; Kurunci-Csacsko, E; Kuster, B; Ottmann, O; Pachl, F; Raab, M; Sanhaji, M; Strebhardt, K | 1 |
Fujiwara, K; Hirose, M; Ito, J; Kamoshita, M; Kashiwazaki, N; Kato, T; Parys, JB; Sathanawongs, A; Wojcikiewicz, RJ | 1 |
Ember, SW; Mishra, NK; Pomerantz, WC; Schönbrunn, E; Urick, AK | 1 |
Ahmad, N; Hodges, K; Kuang, S; Liu, X; Ratliff, T; Shao, C | 1 |
Cheon, MG; Choi, M; Kim, JE; Kim, W; Lee, CW | 1 |
Brehm, K; Koziol, U | 1 |
Astrinidis, A; Cox, AM; Hartley, S; Paladhi, UR; Pichette, B; Valianou, M | 1 |
Christensen, MD; Eaton, S; Elmer, JJ; Gonzalez-Malerva, L; LaBaer, J; Rege, K | 1 |
Bogatyreva, L; Dragoi, D; Frey, AV; Hauschke, D; Lassmann, S; Lübbert, M; May, AM; Münch, C; Thurig, K; Wäsch, R; Werner, M | 1 |
Cassinelli, G; De Cesare, M; Lanzi, C; Zaffaroni, N; Zuco, V | 1 |
Chow, JP; Hong, MJ; Li, J; Ma, HT; Mak, JP; Man, WY; Poon, RY | 1 |
Cohen, P; Gray, N; Lopez-Pelaez, M; Malik, N; Nanda, SK; Prescott, A; Vollmer, S | 1 |
Fulda, S; Hugle, M; Stehle, A | 1 |
Chen, BP; Lee, KJ; Lin, YF; Morotomi-Yano, K; Saha, D; Shang, ZF; Sun, J | 1 |
Ahmad, N; Chen, L; Liu, X; Wang, H; Zhang, Z | 1 |
Shin, SB; Woo, SU; Yim, H | 1 |
Belz, K; Fulda, S; Hugle, M | 1 |
Baran, V; Brzakova, A; Kovarikova, V; Rehak, P; Solc, P | 1 |
Cozza, G; Hanson, PI; Negro, A; Pinna, LA; Salvi, M; Trashi, E | 1 |
Chen, Q; Guo, X; Jiang, Q; Jing, G; Liu, J; Wang, Y; Zhang, C; Zhang, X; Zhuo, X | 1 |
Bharti, R; Mandal, M; Parida, S; Prashanth Kumar, BN; Rajput, S | 1 |
Ahmad, N; Hodges, KB; Karki, A; Konieczny, SF; Li, J; Liu, X; Ratliff, TL; Strebhardt, K; Zoubeidi, A | 1 |
Haines, DS; Hess, S; Lee, CM; Moradian, A; Ramkumar, P; Reddy, EP; Sharrocks, AD; Sweredoski, MJ | 1 |
Aspinall, CF; Taylor, SS; Tighe, A; Zheleva, D | 1 |
Byers, LA; Diao, L; Ferrarotto, R; Gibbons, DL; Girard, L; Giri, U; Glisson, BS; Goonatilake, R; Heymach, JV; Johnson, FM; Li, L; Minna, J; Peng, DH; Peng, S; Tong, P; Wang, J; Wang, L; Wang, Y; Yoo, SY | 1 |
Cao, Y; Chen, D; Du, J; Liu, X; Ma, W; Wang, Q; Xu, Q; Zhang, N | 1 |
Bigenzahn, J; Birner, P; Erovic, BM; Heiduschka, G; Kadletz, L; Schmid, R; Schneider, S; Seemann, R; Stanisz, I; Thurnher, D | 1 |
Ahmad, N; Chen, L; Liu, X | 1 |
Friemel, A; Kreis, NN; Louwen, F; Ritter, A; Yuan, J | 1 |
Bradner, JE; Buckley, DL; Ember, SW; Fitzgerald, ME; Koblan, LW; Liu, S; Ott, CJ; Remillard, D; Roberts, JM; Schonbrunn, E; Vittori, S; Zhang, W; Zhu, JY | 1 |
Awad, MM; Bonomi, PD; Bradford, DS; Chu, QS; Eaton, KD; Ellison, DM; Fritsch, H; Gandhi, L; Govindan, R; Johnson, BE; Munzert, G; Socinski, MA; Stephenson, JJ | 1 |
Lee, YJ; Shin, SB; Woo, SU; Yim, H | 1 |
Burdova, K; Lindqvist, A; Macurek, L; Müllers, E; Silva Cascales, H | 1 |
Albaladejo, J; Bravo, I; Fernández-Sainz, J; Garzón, A; Granadino-Roldán, JM; Pacheco-Liñán, PJ; Rubio-Martínez, J | 1 |
Breitenbuecher, F; Gaschler-Markefski, B; Kasper, S; Kortsik, C; Morresi-Hauf, A; Munzert, G; Schad, A; Schmid, KW; Schuler, M; Sebastian, M; Ting, S; von Pawel, J; Wehler, B; Werner, M; Westerwick, D; Wohlschläger, J; Worm, K | 1 |
Chanda, SK; Lanz, C; Pohl, MO; Rodriguez-Frandsen, A; Soonthornvacharin, S; Stertz, S; von Recum-Knepper, J; Wolff, T; Yángüez, E | 1 |
Chen, M; Dai, T; Guo, X; Jing, C; Li, L; Lian, G; Liu, J; Shi, Y; Wang, Y; Ye, F; Zhang, Q | 1 |
Bui, QT; Hong, J; Im, JH; Jeong, SB; Kang, KW; Lim, SC; Shim, Y; Song, JM; Yoon, JH; Yun, J | 1 |
Gohda, J; Inoue, JI; Ishida, T; Kawaguchi, Y; Liu, K; Suzuki, K; Takeuchi, H; Xie, X | 1 |
Chan, JR; Jiang, M; Lu, QR; Rao, R; Wang, H; Wang, J; Wu, LM; Xu, L | 1 |
Moon, J; Roh, S | 1 |
Chai, Y; Chen, Z; He, F; Ju, H; Lang, Y; Li, P; Qin, J; Zhao, L; Zhao, T | 1 |
Chu, XY; Fu, XF; He, JF; Li, HY; Li, XY; Luo, F; Tian, YZ; Zhao, HL; Zhu, JJ | 1 |
Chen, J; Danna, Y; Fan, J; Gong, Y; Li, J; Liu, R; Rao, F; Wang, Y; Wu, M; Yang, D; Zhan, Q; Zhang, W | 1 |
Aitken, MJL; Burks, JK; Chandra, J; Golfman, LS; Hall, MG; Herbrich, SM; Kannan, S; Konopleva, M; Mak, DH; Mullighan, CG; Song, G; Zweidler-McKay, PA | 1 |
Bai, L; Lu, H; Mu, X; Wang, J; Xu, Y | 1 |
Burkart, MD; La Clair, JJ; Trieger, KA | 1 |
Dong, H; Guo, X; Han, B; Hong, X; Jiang, W; Liu, K; Lu, S; Qiu, F; Qiu, X; Qu, L; Shi, T; Tian, L; Wu, Z; Yao, K; Zhao, J; Zhao, W; Zhong, L; Zhong, M; Zhou, B | 1 |
Jemaà, M; Kifagi, C; Massoumi, R; Serrano, SS | 1 |
Fu, Z; Gheghiani, L; Shang, S | 1 |
Deng, Z; Du, Z; Li, X; Tao, Z; Wang, H; Zhou, Y | 1 |
Chen, G; Deng, Z; Feng, M; Feng, Z; Li, X; Li, Y; Pan, T; Tao, Z; Wang, H; Yin, H; Zhao, G; Zhou, Y | 1 |
He, JC; Huang, J; Lee, K; Li, Z; Lin, J; Liu, R; Ma'ayan, A; Wang, Z; Wojciechowicz, ML; Zhang, L | 1 |
Ann Matthews, A; Cheong, I; Goh, SMP; Ng, CZ; Sum, R; Xu, A; Yap, LW | 1 |
Harris, RC; Terker, AS; Zhang, MZ | 1 |
Begley, KL; Chen, X; Evers, BM; Gao, T; Guo, L; He, D; Kril, LM; Lee, EY; Liu, C; Liu, X; Sviripa, VM; Wang, C; Watt, DS; Xie, Y; Zhang, W | 1 |
Cheng, J; Lu, L; Shou, Z; Tuo, Z; Yang, Q; Zhou, J | 1 |
Albaladejo, J; Bravo, I; Fernández-Sainz, J; Garzón-Ruiz, A; Granadino-Roldán, JM; Pacheco-Liñán, PJ; Rubio-Martínez, J | 1 |
Jemaà, M; Lang, F; Mokdad Gargouri, R | 1 |
4 review(s) available for pteridines and bi 2536
Article | Year |
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Polo-like kinase (PLK) inhibitors in preclinical and early clinical development in oncology.
Topics: Aniline Compounds; Animals; Cell Cycle Proteins; Clinical Trials as Topic; Cyclic N-Oxides; Drug Evaluation, Preclinical; Glycine; Humans; Neoplasms; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyridines; Sulfonamides; Sulfones; Thiazolidines | 2009 |
BI_2536--targeting the mitotic kinase Polo-like kinase 1 (Plk1).
Topics: Animals; Cell Cycle Proteins; Clinical Trials as Topic; Humans; Neoplasms; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2010 |
Current clinical trials with polo-like kinase 1 inhibitors in solid tumors.
Topics: Animals; Antineoplastic Agents; Cell Cycle Proteins; Clinical Trials as Topic; Humans; Molecular Targeted Therapy; Neoplasms; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Thiophenes | 2013 |
On the importance of targeting parasite stem cells in anti-echinococcosis drug development.
Topics: Animals; Anthelmintics; Benzimidazoles; Cell Division; Drug Design; Drug Evaluation, Preclinical; Echinococcosis; Echinococcus; Echinococcus multilocularis; Genomics; Helminth Proteins; Hydroxyurea; Larva; Molecular Targeted Therapy; Parasitology; Pluripotent Stem Cells; Pteridines; Transcriptome; Tubulin | 2014 |
13 trial(s) available for pteridines and bi 2536
Article | Year |
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Phase I dose escalation and pharmacokinetic study of BI 2536, a novel Polo-like kinase 1 inhibitor, in patients with advanced solid tumors.
Topics: Adult; Aged; Antineoplastic Agents; Cell Cycle Proteins; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Humans; Infusions, Intravenous; Male; Maximum Tolerated Dose; Middle Aged; Neoplasms; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Protein Structure, Tertiary; Proto-Oncogene Proteins; Pteridines | 2008 |
Semi-mechanistic population pharmacokinetic/pharmacodynamic model for neutropenia following therapy with the Plk-1 inhibitor BI 2536 and its application in clinical development.
Topics: Algorithms; Cell Cycle Proteins; Chromatography, High Pressure Liquid; Data Interpretation, Statistical; Half-Life; Humans; Leukocyte Count; Mass Spectrometry; Maximum Tolerated Dose; Models, Statistical; Neutropenia; Neutrophils; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2010 |
Multicentric parallel phase II trial of the polo-like kinase 1 inhibitor BI 2536 in patients with advanced head and neck cancer, breast cancer, ovarian cancer, soft tissue sarcoma and melanoma. The first protocol of the European Organization for Research
Topics: Adult; Aged; Antineoplastic Agents; Breast Neoplasms; Feasibility Studies; Female; Head and Neck Neoplasms; Humans; Infusions, Intravenous; Male; Melanoma; Middle Aged; Neoplasms; Ovarian Neoplasms; Patient Compliance; Pteridines; Sarcoma; Treatment Outcome; Young Adult | 2010 |
The efficacy and safety of BI 2536, a novel Plk-1 inhibitor, in patients with stage IIIB/IV non-small cell lung cancer who had relapsed after, or failed, chemotherapy: results from an open-label, randomized phase II clinical trial.
Topics: Adenocarcinoma; Adult; Aged; Aged, 80 and over; Carcinoma, Non-Small-Cell Lung; Cell Cycle Proteins; Drug Resistance, Neoplasm; Female; Humans; Lung Neoplasms; Male; Middle Aged; Neoplasm Recurrence, Local; Neoplasm Staging; Neoplasms, Squamous Cell; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Salvage Therapy; Survival Rate; Treatment Failure; Treatment Outcome | 2010 |
An open-label, phase I study of the polo-like kinase-1 inhibitor, BI 2536, in patients with advanced solid tumors.
Topics: Adult; Aged; Aged, 80 and over; Antineoplastic Agents; Cell Cycle Proteins; Disease Progression; Dose-Response Relationship, Drug; Drug Administration Schedule; Female; Humans; Male; Middle Aged; Neoplasms; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Treatment Outcome | 2010 |
Comparison of different semi-mechanistic models for chemotherapy-related neutropenia: application to BI 2536 a Plk-1 inhibitor.
Topics: Antineoplastic Agents; Carcinoma, Non-Small-Cell Lung; Cell Cycle Proteins; Humans; Lung Neoplasms; Models, Biological; Neutropenia; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2011 |
A phase I open-label dose-escalation study of intravenous BI 2536 together with pemetrexed in previously treated patients with non-small-cell lung cancer.
Topics: Administration, Intravenous; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Cell Cycle Proteins; Disease-Free Survival; Drug Eruptions; Drug Interactions; Enzyme Inhibitors; Fatigue; Female; Glutamates; Guanine; Humans; Lung Neoplasms; Male; Maximum Tolerated Dose; Middle Aged; Nausea; Neutropenia; Pemetrexed; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pruritus; Pteridines; Treatment Outcome | 2013 |
A randomised phase II trial of the Polo-like kinase inhibitor BI 2536 in chemo-naïve patients with unresectable exocrine adenocarcinoma of the pancreas - a study within the Central European Society Anticancer Drug Research (CESAR) collaborative network.
Topics: Adenocarcinoma; Aged; Cell Cycle Proteins; Cohort Studies; Confidence Intervals; Disease-Free Survival; Female; Follow-Up Studies; Humans; Male; Middle Aged; Pancreatic Neoplasms; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2012 |
The Plk1 inhibitor BI 2536 in patients with refractory or relapsed non-Hodgkin lymphoma: a phase I, open-label, single dose-escalation study.
Topics: Adult; Aged; Aged, 80 and over; Cell Cycle Proteins; Female; Humans; Lymphoma, Non-Hodgkin; Male; Middle Aged; Neoplasm Staging; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Treatment Outcome; Young Adult | 2013 |
A randomized, open-label, phase I/II trial to investigate the maximum tolerated dose of the Polo-like kinase inhibitor BI 2536 in elderly patients with refractory/relapsed acute myeloid leukaemia.
Topics: Age Factors; Aged; Aged, 80 and over; Antineoplastic Agents; Cell Cycle Proteins; Drug Administration Schedule; Female; Humans; Leukemia, Myeloid, Acute; Male; Maximum Tolerated Dose; Middle Aged; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Recurrence; Treatment Outcome | 2013 |
PLK1 expression and BI 2536 effects in childhood acute lymphoblastic leukemia.
Topics: Adolescent; Bone Marrow; Cell Cycle Proteins; Child; Child, Preschool; Disease-Free Survival; Female; G2 Phase Cell Cycle Checkpoints; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Leukemic; Humans; Infant; Jurkat Cells; M Phase Cell Cycle Checkpoints; Male; Polo-Like Kinase 1; Precursor Cell Lymphoblastic Leukemia-Lymphoma; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Retrospective Studies; RNA, Messenger; RNA, Neoplasm; Survival Rate | 2014 |
An open-label, phase II study of the polo-like kinase-1 (Plk-1) inhibitor, BI 2536, in patients with relapsed small cell lung cancer (SCLC).
Topics: Administration, Intravenous; Adult; Aged; Cell Cycle Proteins; Disease-Free Survival; Female; Humans; Lung Neoplasms; Male; Middle Aged; Neoplasm Recurrence, Local; Neoplasm Staging; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Recurrence; Small Cell Lung Carcinoma; Smoking; Treatment Failure; Treatment Outcome | 2017 |
Comprehensive Biomarker Analyses in Patients with Advanced or Metastatic Non-Small Cell Lung Cancer Prospectively Treated with the Polo-Like Kinase 1 Inhibitor BI2536.
Topics: Antimitotic Agents; Biomarkers, Tumor; Carcinoma, Non-Small-Cell Lung; Cohort Studies; Disease Progression; Disease-Free Survival; DNA Mutational Analysis; Lung Neoplasms; Neoplasm Metastasis; Prospective Studies; Proto-Oncogene Proteins p21(ras); Pteridines; Sequence Analysis, DNA; Up-Regulation | 2017 |
123 other study(ies) available for pteridines and bi 2536
Article | Year |
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BI 2536, a potent and selective inhibitor of polo-like kinase 1, inhibits tumor growth in vivo.
Topics: Animals; Apoptosis; Body Weight; Cell Cycle; Cell Cycle Proteins; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Flow Cytometry; HeLa Cells; Humans; Immunohistochemistry; Magnetic Resonance Imaging; Mice; Microscopy, Fluorescence; Neoplasms; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Signal Transduction; Spectrometry, Fluorescence; Xenograft Model Antitumor Assays | 2007 |
The small-molecule inhibitor BI 2536 reveals novel insights into mitotic roles of polo-like kinase 1.
Topics: Cell Cycle Proteins; Dose-Response Relationship, Drug; Enzyme Inhibitors; F-Box Proteins; HeLa Cells; Humans; Image Processing, Computer-Assisted; Microscopy, Electron, Transmission; Microscopy, Fluorescence; Microtubules; Mitosis; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Spindle Apparatus | 2007 |
PLK1 inhibitors: setting the mitotic death trap.
Topics: Animals; Antineoplastic Agents; Cell Cycle Proteins; Enzyme Inhibitors; Humans; Mitosis; Neoplasms; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2007 |
Polo-like kinase 1 triggers the initiation of cytokinesis in human cells by promoting recruitment of the RhoGEF Ect2 to the central spindle.
Topics: Aurora Kinase B; Aurora Kinases; Catalysis; CDC2 Protein Kinase; Cell Cycle Proteins; Chromosomes, Human; Cytokinesis; Enzyme Activation; Guanine Nucleotide Exchange Factors; HeLa Cells; Humans; Microtubule-Associated Proteins; Models, Biological; Polo-Like Kinase 1; Protein Binding; Protein Serine-Threonine Kinases; Protein Transport; Proto-Oncogene Proteins; Pteridines; Rho Guanine Nucleotide Exchange Factors; rhoA GTP-Binding Protein; Spindle Apparatus | 2007 |
Pharmacological and functional comparison of the polo-like kinase family: insight into inhibitor and substrate specificity.
Topics: Adenosine Triphosphate; Amino Acid Sequence; Androstadienes; Binding Sites; Cell Cycle Proteins; Humans; Models, Molecular; Molecular Sequence Data; Peptide Library; Polo-Like Kinase 1; Protein Conformation; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Substrate Specificity; Wortmannin | 2007 |
Selectivity-determining residues in Plk1.
Topics: Adenylyl Imidodiphosphate; Animals; Cell Cycle; Cell Cycle Proteins; Clinical Trials as Topic; Crystallography, X-Ray; Drug Design; Humans; Models, Molecular; Neoplasm Proteins; Neoplasms; Polo-Like Kinase 1; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein Structure, Tertiary; Proto-Oncogene Proteins; Pteridines; Structure-Activity Relationship | 2007 |
Identification of Polo-like kinase 1 as a potential therapeutic target in anaplastic thyroid carcinoma.
Topics: Animals; Carcinoma; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cyclin B; Cyclin B1; Female; Humans; Mice; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Thyroid Neoplasms; Tumor Suppressor Protein p53 | 2009 |
A panel of isogenic human cancer cells suggests a therapeutic approach for cancers with inactivated p53.
Topics: Alleles; Animals; Antineoplastic Agents; Cell Line, Tumor; Cyclin-Dependent Kinase Inhibitor p21; G1 Phase; Gene Expression Profiling; Gene Targeting; Genotype; Humans; Imidazoles; Mice; Neoplasms; Piperazines; Pteridines; Transcription, Genetic; Tumor Suppressor Protein p53; Xenograft Model Antitumor Assays | 2009 |
Polo-like kinase 1 is overexpressed in acute myeloid leukemia and its inhibition preferentially targets the proliferation of leukemic cells.
Topics: Cell Cycle Proteins; Cell Proliferation; Gene Expression Regulation, Leukemic; Humans; Leukemia, Myeloid, Acute; Neoplasm Proteins; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA, Small Interfering; Tumor Cells, Cultured | 2009 |
PLK1 down-regulates parainfluenza virus 5 gene expression.
Topics: Amino Acid Motifs; Amino Acid Substitution; Apoptosis; Cell Cycle Proteins; Cytokines; Down-Regulation; Gene Expression Regulation, Viral; HeLa Cells; Humans; Parainfluenza Virus 5; Phosphoproteins; Phosphorylation; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Respirovirus; Respirovirus Infections; Transfection; Viral Proteins | 2009 |
Treatment of biliary tract cancer with NVP-AEW541: mechanisms of action and resistance.
Topics: Antineoplastic Agents; Biliary Tract Neoplasms; Cell Line, Tumor; Cell Proliferation; Deoxycytidine; Drug Resistance, Neoplasm; Drug Synergism; Drug Therapy, Combination; Fluorouracil; Gallbladder Neoplasms; Gemcitabine; Humans; Proto-Oncogene Proteins c-akt; Pteridines; Pyrimidines; Pyrroles; Receptor, IGF Type 1 | 2010 |
Polo-like kinase 1 (Plk1) as a novel drug target in chronic myeloid leukemia: overriding imatinib resistance with the Plk1 inhibitor BI 2536.
Topics: Adolescent; Adult; Aged; Antineoplastic Combined Chemotherapy Protocols; Benzamides; Cell Cycle Proteins; Drug Delivery Systems; Drug Evaluation, Preclinical; Drug Resistance, Neoplasm; Female; Fusion Proteins, bcr-abl; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Leukemic; Humans; Imatinib Mesylate; K562 Cells; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Male; Middle Aged; Piperazines; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrimidines | 2010 |
Inhibition of Plk1 induces mitotic infidelity and embryonic growth defects in developing zebrafish embryos.
Topics: Amino Acid Sequence; Animals; Animals, Genetically Modified; Apoptosis; Cell Cycle Proteins; Cell Proliferation; Chromosome Segregation; Embryo, Nonmammalian; Gene Expression Regulation, Developmental; Gene Knockdown Techniques; Green Fluorescent Proteins; Histones; In Situ Hybridization; Kinetics; Microscopy, Video; Mitosis; Molecular Sequence Data; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Reverse Transcriptase Polymerase Chain Reaction; Sequence Homology, Amino Acid; Zebrafish; Zebrafish Proteins | 2010 |
The Plk1 inhibitor BI 2536 temporarily arrests primary cardiac fibroblasts in mitosis and generates aneuploidy in vitro.
Topics: Aneuploidy; Animals; Cell Cycle Proteins; Cell Differentiation; Cells, Cultured; Fibroblasts; Heart; HeLa Cells; Humans; Mitosis; Myocardium; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Rats; Rats, Sprague-Dawley | 2010 |
Prediction of neutropenia-related effects of a new combination therapy with the anticancer drugs BI 2536 (a Plk1 inhibitor) and pemetrexed.
Topics: Antimetabolites, Antineoplastic; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Non-Small-Cell Lung; Cell Cycle Proteins; Clinical Trials, Phase I as Topic; Computer Simulation; Feasibility Studies; Glutamates; Guanine; Humans; Lung Neoplasms; Models, Biological; Neutropenia; Pemetrexed; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Treatment Outcome | 2010 |
Polo-like kinase 1 is a therapeutic target in high-risk neuroblastoma.
Topics: Adolescent; Animals; Antineoplastic Agents; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cell Survival; Child; Child, Preschool; Female; Genetic Association Studies; Humans; Infant; Infant, Newborn; Kaplan-Meier Estimate; Mice; Mice, Nude; Multivariate Analysis; Neoplasm Transplantation; Neuroblastoma; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Transcription, Genetic; Transplantation, Heterologous; Tumor Burden; Up-Regulation; Young Adult | 2011 |
The polo-like kinase inhibitor BI 2536 exhibits potent activity against malignant plasma cells and represents a novel therapy in multiple myeloma.
Topics: Apoptosis; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Drug Screening Assays, Antitumor; Humans; Multiple Myeloma; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2011 |
Polo-like kinase-1 as a novel target in neoplastic mast cells: demonstration of growth-inhibitory effects of small interfering RNA and the Polo-like kinase-1 targeting drug BI 2536.
Topics: Animals; Apoptosis; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Flow Cytometry; HL-60 Cells; Humans; Immunohistochemistry; K562 Cells; Mast Cells; Mastocytosis, Systemic; Phosphorylation; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Reverse Transcriptase Polymerase Chain Reaction; RNA Interference; Thymidine; Tumor Cells, Cultured; U937 Cells | 2011 |
Myosin phosphatase-targeting subunit 1 controls chromatid segregation.
Topics: Cell Cycle Proteins; Centromere; Chromosome Segregation; Chromosomes, Human; HeLa Cells; Humans; Mutation; Myosin-Light-Chain Phosphatase; Phosphorylation; Polo-Like Kinase 1; Protein Phosphatase 2; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2011 |
Small molecule kinase inhibitor screen identifies polo-like kinase 1 as a target for neuroblastoma tumor-initiating cells.
Topics: Algorithms; Animals; Brain Neoplasms; Cell Cycle Proteins; Cells, Cultured; High-Throughput Screening Assays; Humans; Mice; Mice, Inbred NOD; Mice, SCID; Molecular Targeted Therapy; Neoplastic Stem Cells; Neuroblastoma; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Small Molecule Libraries; Xenograft Model Antitumor Assays | 2011 |
Inhibition of polo-like kinase 1 leads to the suppression of osteosarcoma cell growth in vitro and in vivo.
Topics: Animals; Bone Neoplasms; Cell Cycle Proteins; Cell Division; Cell Growth Processes; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Female; G2 Phase; Humans; Mice; Mice, Nude; Mitosis; Osteosarcoma; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Xenograft Model Antitumor Assays | 2011 |
Should I stall or should I cycle? An inhibitor for Polo-like Kinase 1 with distinct roles in primary cells.
Topics: Animals; Benzylamines; Cell Cycle; Cell Cycle Proteins; Cell Proliferation; Cells, Cultured; Humans; Mice; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyridines; Substrate Specificity | 2011 |
Polo-like kinase 1 inhibitors SBE13 and BI 2536 induce different responses in primary cells.
Topics: Apoptosis; Benzylamines; Cell Cycle; Cell Cycle Proteins; Cells, Cultured; Neoplasms; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyridines; Substrate Specificity | 2011 |
Regulation of the action of early mitotic inhibitor 1 on the anaphase-promoting complex/cyclosome by cyclin-dependent kinases.
Topics: Anaphase-Promoting Complex-Cyclosome; Cell Cycle Proteins; Cyclin-Dependent Kinases; F-Box Proteins; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Neoplastic; HeLa Cells; Humans; MAP Kinase Signaling System; Mitosis; Models, Biological; Phosphorylation; Prophase; Pteridines; Ubiquitin-Protein Ligase Complexes; Ubiquitin-Protein Ligases | 2011 |
Combined gene expression profiling and RNAi screening in clear cell renal cell carcinoma identify PLK1 and other therapeutic kinase targets.
Topics: Animals; Antineoplastic Agents; Carcinoma, Renal Cell; Cell Cycle Proteins; Cell Line, Tumor; Female; Gene Expression Profiling; Humans; Kidney Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; Molecular Targeted Therapy; Neoplasm Invasiveness; Neoplasm Proteins; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA Interference; RNA, Small Interfering; Xenograft Model Antitumor Assays | 2011 |
Microenvironmental influence on pre-clinical activity of polo-like kinase inhibition in multiple myeloma: implications for clinical translation.
Topics: Blotting, Western; Bone and Bones; Caspase 3; Cell Cycle; Cell Cycle Proteins; Cell Line; Cell Line, Tumor; Cell Survival; Coculture Techniques; Dose-Response Relationship, Drug; Humans; Inhibitory Concentration 50; Multiple Myeloma; Osteoclasts; Polo-Like Kinase 1; Poly(ADP-ribose) Polymerases; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Stromal Cells; Time Factors; Tumor Burden; Tumor Microenvironment; Xenograft Model Antitumor Assays | 2011 |
BI 2536-mediated PLK1 inhibition suppresses HOS and MG-63 osteosarcoma cell line growth and clonogenicity.
Topics: Antineoplastic Agents; Caspase 3; Cell Cycle Proteins; Cell Death; Cell Line, Tumor; Chromosomal Instability; Dose-Response Relationship, Drug; Enzyme Inhibitors; Humans; Mitosis; Osteosarcoma; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2011 |
Phosphorylation of Ataxin-10 by polo-like kinase 1 is required for cytokinesis.
Topics: Ataxin-10; Binding Sites; Cell Cycle Proteins; Cytokinesis; Gene Knockdown Techniques; Giant Cells; HeLa Cells; Humans; Nerve Tissue Proteins; Phosphorylation; Polo-Like Kinase 1; Protein Interaction Domains and Motifs; Protein Serine-Threonine Kinases; Protein Stability; Proto-Oncogene Proteins; Pteridines; RNA, Small Interfering; Serine; Signal Transduction; Threonine; Transfection; Ubiquitination | 2011 |
Formation of stable attachments between kinetochores and microtubules depends on the B56-PP2A phosphatase.
Topics: Aurora Kinase B; Aurora Kinases; Benzamides; Cell Cycle Proteins; Chromosome Segregation; HeLa Cells; Humans; Indoles; Kinetochores; Leupeptins; Microscopy, Fluorescence; Microtubules; Nocodazole; Phosphorylation; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Phosphatase 2; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Quinazolines; Recombinant Fusion Proteins; RNA Interference; Sulfonamides; Time Factors; Transfection; Tumor Suppressor Proteins | 2011 |
Bioorthogonal probes for polo-like kinase 1 imaging and quantification.
Topics: Cell Cycle Proteins; Cell Division; Cell Line, Tumor; Cell Nucleus; Enzyme Inhibitors; Fluorescent Dyes; G2 Phase; Humans; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Recombinant Proteins; Xanthenes | 2011 |
Polo-like kinase 1 inhibition as a new therapeutic modality in therapy of cholangiocarcinoma.
Topics: Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cholangiocarcinoma; Deoxycytidine; Fluorouracil; Gemcitabine; Gene Expression Regulation, Neoplastic; Humans; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrimidines; Pyrroles; RNA, Messenger | 2011 |
Antiproliferative in vitro effects of BI 2536-mediated PLK1 inhibition on cervical adenocarcinoma cells.
Topics: Antineoplastic Agents; Apoptosis; Cell Cycle; Cell Cycle Proteins; Cell Proliferation; Epithelial Cells; Female; HeLa Cells; Humans; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2013 |
Reciprocal activation between PLK1 and Stat3 contributes to survival and proliferation of esophageal cancer cells.
Topics: Animals; Antineoplastic Agents; beta Catenin; Blotting, Western; Carcinoma, Squamous Cell; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cell Separation; Cell Survival; Chromatin Immunoprecipitation; Electrophoretic Mobility Shift Assay; Enzyme Activation; Esophageal Neoplasms; Feedback, Physiological; Female; Flow Cytometry; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Neoplastic; Genes, Reporter; Humans; Immunohistochemistry; In Situ Nick-End Labeling; Mice; Mice, Nude; NIH 3T3 Cells; Phosphorylation; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA Interference; Signal Transduction; STAT3 Transcription Factor; Time Factors; Transcriptional Activation; Transfection; Xenograft Model Antitumor Assays | 2012 |
Centrosomal protein 55 (Cep55) stability is negatively regulated by p53 protein through Polo-like kinase 1 (Plk1).
Topics: Cell Cycle Proteins; Centrosome; Down-Regulation; Female; Gene Expression Regulation, Neoplastic; Gene Knockdown Techniques; HeLa Cells; Humans; Male; Neoplasms; Nuclear Proteins; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Protein Stability; Proto-Oncogene Proteins; Pteridines; Tumor Suppressor Protein p53 | 2012 |
Small interfering RNA library screen identified polo-like kinase-1 (PLK1) as a potential therapeutic target for breast cancer that uniquely eliminates tumor-initiating cells.
Topics: Antineoplastic Agents; Apoptosis; Breast Neoplasms; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cyclin B1; Doxorubicin; Female; Fluorouracil; Gene Expression; Gene Knockdown Techniques; Gene Library; Humans; Hyaluronan Receptors; Molecular Targeted Therapy; Neoplastic Stem Cells; Paclitaxel; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA Interference; RNA, Small Interfering | 2012 |
Using transcriptome sequencing to identify mechanisms of drug action and resistance.
Topics: Antineoplastic Agents; Boronic Acids; Bortezomib; Cell Cycle Proteins; Cell Line, Tumor; Drug Resistance, Neoplasm; Humans; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrazines; Sequence Analysis, DNA; Transcriptome | 2012 |
Polo-like kinase 1 (PLK1) inhibition suppresses cell growth and enhances radiation sensitivity in medulloblastoma cells.
Topics: Apoptosis; Blotting, Western; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cerebellar Neoplasms; Child; Child, Preschool; Cohort Studies; Enzyme Inhibitors; Female; Humans; Male; Medulloblastoma; Microarray Analysis; Neoplasm Proteins; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Radiation Tolerance; RNA; RNA, Mitochondrial | 2012 |
Polo-like kinase 1 inhibition kills glioblastoma multiforme brain tumor cells in part through loss of SOX2 and delays tumor progression in mice.
Topics: Animals; Apoptosis; Brain Neoplasms; Cell Cycle Proteins; Cell Growth Processes; Cell Line, Tumor; Disease Progression; Glioblastoma; Humans; Mice; Molecular Targeted Therapy; Neural Stem Cells; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; SOXB1 Transcription Factors; Survival Analysis; Transfection | 2012 |
Enabling and disabling polo-like kinase 1 inhibition through chemical genetics.
Topics: Aniline Compounds; Cell Cycle; Cell Cycle Proteins; Cell Line; Drug Resistance; Humans; Mutation; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Thiazolidines | 2012 |
In vitro PLK1 inhibition by BI 2536 decreases proliferation and induces cell-cycle arrest in melanoma cells.
Topics: Antineoplastic Agents; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Disease Progression; Dose-Response Relationship, Drug; G2 Phase Cell Cycle Checkpoints; Humans; M Phase Cell Cycle Checkpoints; Melanoma; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Skin Neoplasms | 2012 |
Leveraging kinase inhibitors to develop small molecule tools for imaging kinases by fluorescence microscopy.
Topics: Boron Compounds; Cell Cycle; Cell Cycle Proteins; Centrosome; Chromosome Structures; Fluorescent Dyes; HeLa Cells; Humans; Microscopy, Fluorescence; Molecular Imaging; Molecular Probes; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Proto-Oncogene Proteins; Pteridines | 2012 |
Reduced efficacy of the Plk1 inhibitor BI 2536 on the progression of hepatocellular carcinoma due to low intratumoral drug levels.
Topics: Animals; Antineoplastic Agents; Carcinoma, Hepatocellular; Cell Cycle Proteins; Cell Line, Tumor; Cell Transformation, Neoplastic; Disease Progression; Drug Resistance, Neoplasm; Humans; Liver; Liver Neoplasms; Magnetic Resonance Imaging; Male; Mice; Mice, Nude; Mice, Transgenic; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2012 |
Proliferation state and polo-like kinase1 dependence of tumorigenic colon cancer cells.
Topics: AC133 Antigen; Animals; Antigens, CD; Cell Cycle; Cell Cycle Proteins; Cell Growth Processes; Cell Line, Tumor; Colonic Neoplasms; Female; Gene Expression Regulation, Neoplastic; Glycoproteins; Humans; Immunohistochemistry; Mice; Mice, Inbred NOD; Mitochondria; Peptides; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA, Small Interfering; Transplantation, Heterologous | 2012 |
Polo-like kinase is required for synaptonemal complex disassembly and phosphorylation in mouse spermatocytes.
Topics: Animals; Cell Cycle Proteins; Cells, Cultured; Chromosomal Proteins, Non-Histone; DNA-Binding Proteins; G2 Phase Cell Cycle Checkpoints; Gene Expression; Kinetics; Male; Meiotic Prophase I; Mice; Mice, Inbred C57BL; Nuclear Proteins; Phosphorylation; Polo-Like Kinase 1; Protein Multimerization; Protein Processing, Post-Translational; Protein Serine-Threonine Kinases; Protein Transport; Proteolysis; Proto-Oncogene Proteins; Pteridines; Spermatocytes; Spermatogenesis; Synaptonemal Complex | 2012 |
Glioma-propagating cells as an in vitro screening platform: PLK1 as a case study.
Topics: Animals; Brain Neoplasms; Cell Cycle Proteins; Cell Proliferation; Cell Survival; Computational Biology; Databases, Genetic; Disease Progression; Drug Screening Assays, Antitumor; Glioma; Humans; Inhibitory Concentration 50; Mice; Microarray Analysis; Neoplastic Stem Cells; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Small Molecule Libraries; Spheroids, Cellular; Tumor Cells, Cultured | 2012 |
Polo-like kinase 1: a potential therapeutic option in combination with conventional chemotherapy for the management of patients with triple-negative breast cancer.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Breast Neoplasms; Cell Cycle Proteins; Cell Line, Tumor; Female; Humans; Mice; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Up-Regulation; Xenograft Model Antitumor Assays | 2013 |
Induction of mitotic cell death by overriding G2/M checkpoint in endometrial cancer cells with non-functional p53.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Cell Cycle Checkpoints; Cell Death; Cell Line, Tumor; Endometrial Neoplasms; Female; G2 Phase Cell Cycle Checkpoints; Gefitinib; Humans; M Phase Cell Cycle Checkpoints; Mice; Mice, Nude; Mitosis; Paclitaxel; Pteridines; Quinazolines; Tumor Suppressor Protein p53; Xenograft Model Antitumor Assays | 2013 |
Plk1 phosphorylation of orc2 and hbo1 contributes to gemcitabine resistance in pancreatic cancer.
Topics: Animals; Antimetabolites, Antineoplastic; Carcinoma, Pancreatic Ductal; Cell Cycle Proteins; Cell Line, Tumor; Deoxycytidine; DNA Replication; Drug Resistance, Neoplasm; Female; Gemcitabine; Histone Acetyltransferases; Humans; Inhibitory Concentration 50; Mice; Mice, Nude; Origin Recognition Complex; Pancreatic Neoplasms; Phosphorylation; Polo-Like Kinase 1; Protein Processing, Post-Translational; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-fos; Pteridines; Tissue Array Analysis; Xenograft Model Antitumor Assays | 2013 |
Polo-like kinase 1 is essential for the first mitotic division in the mouse embryo.
Topics: Animals; Blastocyst; Blotting, Western; Cell Cycle Proteins; Female; Fluorescent Antibody Technique; Gene Expression Regulation, Developmental; Male; Mice; Microtubule-Organizing Center; Mitosis; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Spindle Apparatus; Time-Lapse Imaging | 2013 |
Inhibition of polo-like kinase 1 induces cell cycle arrest and sensitizes glioblastoma cells to ionizing radiation.
Topics: Apoptosis; Cell Cycle Checkpoints; Cell Cycle Proteins; Cell Growth Processes; Cell Line, Tumor; Glioblastoma; Humans; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Radiation-Sensitizing Agents | 2013 |
PLK1 signaling in breast cancer cells cooperates with estrogen receptor-dependent gene transcription.
Topics: Benzamides; Breast Neoplasms; Cell Cycle Proteins; Cell Growth Processes; Cell Line, Tumor; Chromatin; Female; Gene Expression Regulation, Neoplastic; Heterocyclic Compounds, 2-Ring; Humans; MCF-7 Cells; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Receptors, Estrogen; Signal Transduction; Transcription, Genetic; Tumor Cells, Cultured | 2013 |
Differential determinants of cancer cell insensitivity to antimitotic drugs discriminated by a one-step cell imaging assay.
Topics: Antimitotic Agents; Apoptosis; Benzamides; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Dose-Response Relationship, Drug; Drug Discovery; Drug Resistance, Neoplasm; Fluorescent Dyes; Heterocyclic Compounds, 2-Ring; High-Throughput Screening Assays; Humans; Molecular Imaging; Paclitaxel; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Small Molecule Libraries; Structure-Activity Relationship | 2013 |
BCL-2 hypermethylation is a potential biomarker of sensitivity to antimitotic chemotherapy in endocrine-resistant breast cancer.
Topics: Antimitotic Agents; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Benzamides; Biomarkers; Biphenyl Compounds; Breast Neoplasms; DNA Methylation; Drug Resistance, Neoplasm; Female; Gene Expression Regulation, Neoplastic; Genes, bcl-2; Heterocyclic Compounds, 2-Ring; Humans; MCF-7 Cells; Neoplasm Metastasis; Nitrophenols; Nocodazole; Paclitaxel; Piperazines; Prognosis; Pteridines; Sulfonamides | 2013 |
Targeting prostate cancer cell lines with polo-like kinase 1 inhibitors as a single agent and in combination with histone deacetylase inhibitors.
Topics: Antineoplastic Agents; Cell Cycle Proteins; Cell Line, Tumor; Drug Therapy, Combination; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Male; Polo-Like Kinase 1; Prostatic Neoplasms; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Valproic Acid; Vorinostat | 2013 |
Human ABCB1 (P-glycoprotein) and ABCG2 mediate resistance to BI 2536, a potent and selective inhibitor of Polo-like kinase 1.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 1; ATP Binding Cassette Transporter, Subfamily G, Member 2; ATP-Binding Cassette Transporters; Biological Transport; Cell Cycle Proteins; Cell Line, Tumor; Dose-Response Relationship, Drug; Drug Resistance, Multiple; Drug Resistance, Neoplasm; G2 Phase Cell Cycle Checkpoints; Humans; Lapatinib; Mice; Neoplasm Proteins; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrimidines; Quinazolines | 2013 |
Personalizing the treatment of pediatric medulloblastoma: Polo-like kinase 1 as a molecular target in high-risk children.
Topics: Adolescent; Animals; Antineoplastic Agents; Brain Neoplasms; Cell Cycle Proteins; Child; Child, Preschool; Cohort Studies; Humans; Infant; Medulloblastoma; Mice; Mice, Inbred C57BL; Mice, Inbred NOD; Mice, SCID; Molecular Targeted Therapy; Polo-Like Kinase 1; Precision Medicine; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Risk Factors; Tumor Cells, Cultured; Xenograft Model Antitumor Assays | 2013 |
In vivo modulation of polo-like kinases supports a key role for PLK2 in Ser129 α-synuclein phosphorylation in mouse brain.
Topics: alpha-Synuclein; Analysis of Variance; Animals; Brain; Enzyme Inhibitors; Enzyme-Linked Immunosorbent Assay; G-Protein-Coupled Receptor Kinase 5; G-Protein-Coupled Receptor Kinases; Gene Expression Regulation; Mice; Mice, Knockout; Phosphorylation; Protein Serine-Threonine Kinases; Pteridines; RNA, Messenger; Serine | 2014 |
Stathmin and microtubules regulate mitotic entry in HeLa cells by controlling activation of both Aurora kinase A and Plk1.
Topics: Aurora Kinase A; CDC2 Protein Kinase; cdc25 Phosphatases; Cell Cycle Proteins; Cell Line, Tumor; Centrosome; Cyclin B; G2 Phase Cell Cycle Checkpoints; HeLa Cells; Humans; Microtubules; Mitosis; Nocodazole; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA Interference; RNA, Small Interfering; Stathmin; Tubulin; Tubulin Modulators | 2013 |
Combination of bortezomib and mitotic inhibitors down-modulate Bcr-Abl and efficiently eliminates tyrosine-kinase inhibitor sensitive and resistant Bcr-Abl-positive leukemic cells.
Topics: Benzamides; Boronic Acids; Bortezomib; Caspases; Cell Death; Cell Line, Tumor; Dasatinib; Down-Regulation; Drug Resistance, Neoplasm; Drug Synergism; Enzyme Activation; Fusion Proteins, bcr-abl; Heterocyclic Compounds, 2-Ring; Humans; Imatinib Mesylate; JNK Mitogen-Activated Protein Kinases; Leukemia; Mitosis; Models, Biological; p38 Mitogen-Activated Protein Kinases; Paclitaxel; Phosphorylation; Piperazines; Protein Kinase Inhibitors; Pteridines; Pyrazines; Pyrimidines; Signal Transduction; STAT5 Transcription Factor; Thiazoles | 2013 |
A high-content small molecule screen identifies sensitivity of glioblastoma stem cells to inhibition of polo-like kinase 1.
Topics: Animals; Benzimidazoles; Blood-Brain Barrier; Blotting, Western; Brain Neoplasms; Cell Cycle Checkpoints; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Cells, Cultured; Drug Screening Assays, Antitumor; Glioblastoma; Humans; Indans; Mice; Mice, Knockout; Neoplastic Stem Cells; Neural Stem Cells; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrazoles; Reverse Transcriptase Polymerase Chain Reaction; Small Molecule Libraries; Swine; Thiophenes; Tumor Suppressor Protein p53 | 2013 |
Inhibition of polo-like kinase 1 promotes hyperthermia sensitivity via inactivation of heat shock transcription factor 1 in human retinoblastoma cells.
Topics: Adaptor Proteins, Signal Transducing; Apoptosis; Apoptosis Regulatory Proteins; Blotting, Western; Cell Cycle; Cell Cycle Proteins; Cell Proliferation; Cell Survival; DNA-Binding Proteins; Enzyme Inhibitors; Flow Cytometry; Gene Knockdown Techniques; Heat Shock Transcription Factors; HSP40 Heat-Shock Proteins; HSP70 Heat-Shock Proteins; Humans; Hyperthermia, Induced; Phosphorylation; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Real-Time Polymerase Chain Reaction; Retinal Neoplasms; Retinoblastoma; RNA, Small Interfering; Transcription Factors; Tumor Cells, Cultured | 2013 |
PLK1-inhibition can cause radiosensitization or radioresistance dependent on the treatment schedule.
Topics: Bone Neoplasms; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Chemoradiotherapy; Colonic Neoplasms; DNA Damage; DNA Repair; Flow Cytometry; HT29 Cells; Humans; Osteosarcoma; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Radiation Tolerance | 2014 |
Dual kinase-bromodomain inhibitors for rationally designed polypharmacology.
Topics: Antineoplastic Combined Chemotherapy Protocols; Blotting, Western; Calorimetry; Cell Line, Tumor; Crystallization; Drug Design; Drug Interactions; Drug Screening Assays, Antitumor; Epigenesis, Genetic; High-Throughput Screening Assays; Humans; Neoplasms; Polypharmacology; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-myc; Pteridines; Pyrrolidines; Recombinant Proteins; Signal Transduction; Structure-Activity Relationship; Sulfonamides | 2014 |
Inhibition of Polo kinase by BI2536 affects centriole separation during Drosophila male meiosis.
Topics: Animals; Axoneme; Centrioles; Chromatids; Drosophila; Drosophila Proteins; Male; Meiosis; Protein Serine-Threonine Kinases; Pteridines; Pupa; Spermatocytes; Tubulin | 2014 |
Identification of a high affinity selective inhibitor of Polo-like kinase 1 for cancer chemotherapy by computational approach.
Topics: Antineoplastic Agents; Catalytic Domain; Cell Cycle Proteins; Humans; Hydrogen Bonding; Molecular Docking Simulation; Molecular Dynamics Simulation; Polo-Like Kinase 1; Protein Binding; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Thermodynamics | 2014 |
Quantitative chemical proteomics reveals a Plk1 inhibitor-compromised cell death pathway in human cells.
Topics: Cell Cycle Proteins; Cell Death; Death-Associated Protein Kinases; HeLa Cells; Humans; Mitosis; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Proto-Oncogene Proteins; Pteridines | 2014 |
Plk1 phosphorylation of PTEN causes a tumor-promoting metabolic state.
Topics: Animals; Antineoplastic Agents; Benzamides; Cell Cycle Proteins; Cell Line, Tumor; Cell Transformation, Neoplastic; Endosomal Sorting Complexes Required for Transport; Gene Expression Regulation; Glucose; Glycolysis; HEK293 Cells; Heterocyclic Compounds, 2-Ring; Humans; Lactic Acid; Liver; Mice; Mice, Nude; Nedd4 Ubiquitin Protein Ligases; Neoplasms, Experimental; Nocodazole; Phosphatidylinositol 3-Kinase; Phosphorylation; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; PTEN Phosphohydrolase; Pteridines; Signal Transduction; Ubiquitin-Protein Ligases | 2014 |
Mitotic arrest and slippage induced by pharmacological inhibition of Polo-like kinase 1.
Topics: Cell Cycle Proteins; Cell Line, Tumor; Female; Human Umbilical Vein Endothelial Cells; Humans; M Phase Cell Cycle Checkpoints; Male; Neoplasm Proteins; Neoplasms; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2015 |
The effect of M-phase stage-dependent kinase inhibitors on inositol 1,4,5-trisphosphate receptor 1 (IP3 R1) expression and localization in pig oocytes.
Topics: Animals; Butadienes; Calcium; Cell Cycle Proteins; Cells, Cultured; Dose-Response Relationship, Drug; Gene Expression; Inositol 1,4,5-Trisphosphate Receptors; Mice; Nitriles; Oocytes; Phosphorylation; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Purines; Roscovitine; Swine | 2015 |
Fluorinated aromatic amino acids are sensitive 19F NMR probes for bromodomain-ligand interactions.
Topics: Acetaminophen; Amino Acids, Aromatic; Antigens, Nuclear; Azepines; Binding Sites; Bridged Bicyclo Compounds, Heterocyclic; Cell Cycle Proteins; Crystallography, X-Ray; Cyclic N-Oxides; Escherichia coli; Gene Expression; Halogenation; Humans; Indolizines; Ligands; Magnetic Resonance Spectroscopy; Molecular Docking Simulation; Molecular Probes; Nerve Tissue Proteins; Nuclear Proteins; Oncogene Proteins, Fusion; Protein Binding; Pteridines; Pyridinium Compounds; Pyrrolidines; Recombinant Proteins; Staining and Labeling; Sulfonamides; Transcription Factors; Triazoles | 2014 |
Inhibition of polo-like kinase 1 (Plk1) enhances the antineoplastic activity of metformin in prostate cancer.
Topics: Animals; Antineoplastic Agents; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cell Separation; Cell Survival; Disease Progression; Flow Cytometry; Glycolysis; Humans; Male; Metformin; Mice; Mitosis; Neoplasm Transplantation; Polo-Like Kinase 1; Prostate-Specific Antigen; Prostatic Neoplasms; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA Interference; Signal Transduction; Tumor Suppressor Protein p53 | 2015 |
Polo-like kinase 1 inhibitor BI2536 causes mitotic catastrophe following activation of the spindle assembly checkpoint in non-small cell lung cancer cells.
Topics: Antimitotic Agents; Apoptosis; Blotting, Western; Carcinoma, Non-Small-Cell Lung; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Humans; Lung Neoplasms; M Phase Cell Cycle Checkpoints; Microscopy, Fluorescence; Mitosis; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Spindle Apparatus; Time-Lapse Imaging | 2015 |
Pharmacological inhibition of Polo-like kinase 1 (PLK1) by BI-2536 decreases the viability and survival of hamartin and tuberin deficient cells via induction of apoptosis and attenuation of autophagy.
Topics: Animals; Apoptosis; Autophagy; Cell Cycle Proteins; Cell Survival; Clone Cells; Gene Expression Regulation; HeLa Cells; Humans; Mice; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-bcl-2; Pteridines; Sirolimus; Tuberous Sclerosis Complex 1 Protein; Tuberous Sclerosis Complex 2 Protein; Tumor Suppressor Proteins | 2015 |
Kinome-level screening identifies inhibition of polo-like kinase-1 (PLK1) as a target for enhancing non-viral transgene expression.
Topics: Cell Culture Techniques; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Cyclic N-Oxides; Dose-Response Relationship, Drug; Drug Carriers; Gene Silencing; Gene Transfer Techniques; Green Fluorescent Proteins; Humans; Luciferases; Male; Plasmids; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyridines; Small Molecule Libraries; Sulfonamides; Transgenes | 2015 |
Therapeutic polo-like kinase 1 inhibition results in mitotic arrest and subsequent cell death of blasts in the bone marrow of AML patients and has similar effects in non-neoplastic cell lines.
Topics: Aged; Aged, 80 and over; Antimitotic Agents; Apoptosis; Blast Crisis; Blotting, Western; Bone Marrow; Cell Cycle Proteins; Cell Proliferation; Female; Humans; Immunoenzyme Techniques; Leukemia, Myeloid, Acute; Male; Mitosis; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Messenger; Tumor Cells, Cultured | 2015 |
PLK1 is a critical determinant of tumor cell sensitivity to CPT11 and its inhibition enhances the drug antitumor efficacy in squamous cell carcinoma models sensitive and resistant to camptothecins.
Topics: Activation, Metabolic; Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Camptothecin; Carcinoma, Squamous Cell; Cell Cycle Proteins; Cell Line, Tumor; Child; Drug Resistance, Neoplasm; Female; G2 Phase Cell Cycle Checkpoints; Humans; Irinotecan; Mice; Mice, Nude; Molecular Targeted Therapy; Neoplasm Proteins; Polo-Like Kinase 1; Prodrugs; Protein Kinase Inhibitors; Protein Processing, Post-Translational; Protein Serine-Threonine Kinases; Proteolysis; Proto-Oncogene Proteins; Pteridines; Rhabdomyosarcoma, Embryonal; Sarcoma, Ewing; Skin Neoplasms; Topoisomerase I Inhibitors; Ubiquitination; Uterine Cervical Neoplasms; Xenograft Model Antitumor Assays | 2015 |
Co-inhibition of polo-like kinase 1 and Aurora kinases promotes mitotic catastrophe.
Topics: Animals; Antineoplastic Agents; Aurora Kinase A; Aurora Kinase B; Carcinoma; Cell Cycle Proteins; Cyclohexanecarboxylic Acids; Drug Synergism; Female; HeLa Cells; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Mitosis; Molecular Targeted Therapy; Nasopharyngeal Carcinoma; Nasopharyngeal Neoplasms; Organophosphates; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Quinazolines; Thiazoles; Tumor Cells, Cultured | 2015 |
Suppression of interferon β gene transcription by inhibitors of bromodomain and extra-terminal (BET) family members.
Topics: Animals; Antimitotic Agents; Cell Cycle Proteins; Cell Line, Transformed; Dendritic Cells; Humans; Interferon Regulatory Factor-3; Interferon-beta; Ligands; Macrophages; Mice; Nuclear Proteins; Promoter Regions, Genetic; Protein Isoforms; Proto-Oncogene Proteins c-jun; Pteridines; Signal Transduction; Toll-Like Receptor 7; Toll-Like Receptor 9; Transcription Factors; Transcription, Genetic | 2015 |
Eribulin synergizes with Polo-like kinase 1 inhibitors to induce apoptosis in rhabdomyosarcoma.
Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Caspases; Cell Cycle Checkpoints; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Chick Embryo; Dose-Response Relationship, Drug; Drug Synergism; Endodeoxyribonucleases; Furans; Humans; Ketones; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Rhabdomyosarcoma; RNA Interference; Signal Transduction; Time Factors; Transfection; Tubulin Modulators; Tumor Burden | 2015 |
The Catalytic Subunit of DNA-Dependent Protein Kinase Coordinates with Polo-Like Kinase 1 to Facilitate Mitotic Entry.
Topics: CDC2 Protein Kinase; Cell Cycle Proteins; Cell Division; Cell Line, Tumor; Cyclin-Dependent Kinases; DNA Breaks, Double-Stranded; DNA-Activated Protein Kinase; G2 Phase; HCT116 Cells; HeLa Cells; Humans; Mitosis; Nuclear Proteins; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2015 |
Inhibition of Plk1 represses androgen signaling pathway in castration-resistant prostate cancer.
Topics: Animals; Cell Cycle Proteins; HEK293 Cells; Humans; Male; Mice; Mice, Nude; Polo-Like Kinase 1; Prostatic Neoplasms, Castration-Resistant; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Receptors, Androgen; Signal Transduction; Xenograft Model Antitumor Assays | 2015 |
Differential Cellular Effects of Plk1 Inhibitors Targeting the ATP-binding Domain or Polo-box Domain.
Topics: Adenosine Triphosphate; Antineoplastic Agents; Apoptosis; Benzimidazoles; Benzoates; Benzoquinones; Binding Sites; Catalytic Domain; Cell Cycle Proteins; Cell Proliferation; Cyclin-Dependent Kinase Inhibitor p21; Dose-Response Relationship, Drug; Drug Design; Female; G2 Phase Cell Cycle Checkpoints; HeLa Cells; Humans; Inhibitory Concentration 50; Mitosis; Molecular Targeted Therapy; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein Structure, Tertiary; Proto-Oncogene Proteins; Pteridines; Quinones; S Phase Cell Cycle Checkpoints; Signal Transduction; Thiophenes; Time Factors; Uterine Cervical Neoplasms | 2015 |
Identification of synthetic lethality of PLK1 inhibition and microtubule-destabilizing drugs.
Topics: Animals; Apoptosis; bcl-2 Homologous Antagonist-Killer Protein; Cell Cycle Checkpoints; Cell Cycle Proteins; Disease Models, Animal; Drug Synergism; Humans; Mice; Mitochondria; Myeloid Cell Leukemia Sequence 1 Protein; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-bcl-2; Pteridines; Reactive Oxygen Species; Rhabdomyosarcoma; Signal Transduction; Transplantation, Heterologous; Tubulin Modulators; Tumor Cells, Cultured | 2015 |
PLK1 regulates spindle formation kinetics and APC/C activation in mouse zygote.
Topics: Anaphase; Anaphase-Promoting Complex-Cyclosome; Animals; Blastocyst; Cell Cycle Proteins; Centrosome; Female; Kinetics; Kinetochores; Male; Mice; Microscopy, Confocal; Mitosis; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Spindle Apparatus; Time-Lapse Imaging; Zygote | 2016 |
Tools to discriminate between targets of CK2 vs PLK2/PLK3 acidophilic kinases.
Topics: Buffers; HEK293 Cells; Humans; Hydrogen-Ion Concentration; Naphthyridines; Phenazines; Phosphorylation; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Pteridines; Transfection | 2012 |
Usp16 regulates kinetochore localization of Plk1 to promote proper chromosome alignment in mitosis.
Topics: Cell Cycle Proteins; Cell Line, Tumor; Chromosome Segregation; Chromosomes; HEK293 Cells; HeLa Cells; Humans; Kinetochores; Microtubules; Mitosis; Nocodazole; Phosphorylation; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA Interference; RNA, Small Interfering; Ubiquitin Thiolesterase; Ubiquitination | 2015 |
BI2536--A PLK inhibitor augments paclitaxel efficacy in suppressing tamoxifen induced senescence and resistance in breast cancer cells.
Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Breast Neoplasms; Cell Line, Tumor; Cellular Senescence; Down-Regulation; Drug Resistance, Neoplasm; Female; Humans; In Situ Nick-End Labeling; NF-kappa B; p38 Mitogen-Activated Protein Kinases; Paclitaxel; Pteridines; Signal Transduction; Tamoxifen; Up-Regulation; Vascular Endothelial Growth Factor A | 2015 |
Cotargeting Polo-Like Kinase 1 and the Wnt/β-Catenin Signaling Pathway in Castration-Resistant Prostate Cancer.
Topics: Animals; Antimitotic Agents; Axin Protein; beta Catenin; Cdc20 Proteins; Cell Cycle Proteins; Cell Line, Tumor; Glycogen Synthase Kinase 3; Glycogen Synthase Kinase 3 beta; HEK293 Cells; Humans; Male; Mice; Neoplasm Transplantation; Phosphorylation; Polo-Like Kinase 1; Prostatic Neoplasms, Castration-Resistant; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Transplantation, Heterologous; Wnt Proteins; Wnt Signaling Pathway | 2015 |
JNK-associated Leucine Zipper Protein Functions as a Docking Platform for Polo-like Kinase 1 and Regulation of the Associating Transcription Factor Forkhead Box Protein K1.
Topics: Adaptor Proteins, Signal Transducing; Animals; Antimitotic Agents; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Forkhead Transcription Factors; Gene Expression Regulation; HEK293 Cells; HeLa Cells; Humans; Mass Spectrometry; Mice; Mitosis; Phosphorylation; Polo-Like Kinase 1; Protein Binding; Protein Interaction Mapping; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Signal Transduction; Tandem Mass Spectrometry | 2015 |
Mitotic entry: Non-genetic heterogeneity exposes the requirement for Plk1.
Topics: Antimitotic Agents; Cell Cycle Proteins; Cell Line, Tumor; Genetic Heterogeneity; HeLa Cells; Humans; Mitosis; Phosphorylation; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrazoles; Pyrimidines; Pyrimidinones; Small Molecule Libraries | 2015 |
Epithelial-Mesenchymal Transition Predicts Polo-Like Kinase 1 Inhibitor-Mediated Apoptosis in Non-Small Cell Lung Cancer.
Topics: Animals; Apoptosis; Benzimidazoles; Carcinoma, Non-Small-Cell Lung; Cell Cycle Checkpoints; Cell Cycle Proteins; Cell Line, Tumor; Chromosomal Instability; Disease Models, Animal; Drug Resistance, Neoplasm; Epithelial-Mesenchymal Transition; Humans; Lung Neoplasms; Mice; Mutation; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Proto-Oncogene Proteins p21(ras); Pteridines; Thiophenes; Tumor Burden; Xenograft Model Antitumor Assays | 2016 |
Unique subcellular distribution of phosphorylated Plk1 (Ser137 and Thr210) in mouse oocytes during meiotic division and pPlk1(Ser137) involvement in spindle formation and REC8 cleavage.
Topics: Animals; Antigens; Antimitotic Agents; Cell Cycle Proteins; Chromosome Segregation; Cumulus Cells; Cytokinesis; Female; Gene Expression Regulation, Developmental; Meiosis; Mice; Mice, Inbred BALB C; Mice, Inbred C57BL; Microtubule-Organizing Center; Nuclear Proteins; Okadaic Acid; Oocytes; Phosphoproteins; Phosphorylation; Polo-Like Kinase 1; Protein Phosphatase 2; Protein Serine-Threonine Kinases; Proteolysis; Proto-Oncogene Proteins; Pteridines; Signal Transduction; Spindle Apparatus; Tubulin | 2015 |
Evaluation of Polo-like kinase 1 as a potential therapeutic target in Merkel cell carcinoma.
Topics: Adult; Aged; Aged, 80 and over; Carcinoma, Merkel Cell; Cell Cycle Proteins; Cell Line, Tumor; Female; Humans; Male; Middle Aged; Molecular Targeted Therapy; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Skin Neoplasms | 2016 |
Combining p53 stabilizers with metformin induces synergistic apoptosis through regulation of energy metabolism in castration-resistant prostate cancer.
Topics: Acetanilides; Antineoplastic Agents; Apoptosis; Cell Cycle Proteins; Cell Line, Tumor; Drug Synergism; Drug Therapy, Combination; Gene Expression Regulation, Neoplastic; Glycolysis; Humans; Male; Metformin; Mitochondria; Mitosis; Oxidative Phosphorylation; Polo-Like Kinase 1; Prostate; Prostatic Neoplasms, Castration-Resistant; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Signal Transduction; Sirtuin 1; Thiourea; Tumor Suppressor Protein p53 | 2016 |
Impact of Polo-like kinase 1 inhibitors on human adipose tissue-derived mesenchymal stem cells.
Topics: Adipose Tissue; Adult; Apoptosis; Benzoates; Cell Cycle Proteins; Cell Line, Tumor; Cell Movement; Cell Proliferation; Cells, Cultured; Cellular Senescence; Female; Humans; MCF-7 Cells; Mesenchymal Stem Cells; Mitosis; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Quinones | 2016 |
Assessment of Bromodomain Target Engagement by a Series of BI2536 Analogues with Miniaturized BET-BRET.
Topics: Cell Cycle Checkpoints; Cell Cycle Proteins; Cell Survival; Drug Design; Fluorescence Resonance Energy Transfer; Fluorescent Dyes; HEK293 Cells; Humans; Luminescent Measurements; Nuclear Proteins; Polo-Like Kinase 1; Protein Binding; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Transcription Factors | 2016 |
Comparative Analysis of a FRET-based PLK1 Kinase Assay to Identify PLK1 inhibitors for Chemotherapy.
Topics: Animals; Antineoplastic Agents; Benzimidazoles; Biological Assay; Biomarkers, Tumor; Cell Cycle Proteins; Drug Evaluation, Preclinical; Fluorescence Resonance Energy Transfer; Fluorescent Dyes; Genistein; Glutathione Transferase; Humans; Insecta; Peptides; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Radioisotopes; Thiophenes; Tumor Protein, Translationally-Controlled 1 | 2017 |
Residual Cdk1/2 activity after DNA damage promotes senescence.
Topics: Antigens, CD; Cadherins; CDC2 Protein Kinase; Cell Line; Cell Line, Tumor; Cell Size; Cell Survival; Cellular Senescence; Cyclin B1; Cyclin-Dependent Kinase 2; Cyclin-Dependent Kinase Inhibitor p21; DNA Damage; Epithelial Cells; Etoposide; G2 Phase Cell Cycle Checkpoints; Gene Expression Regulation; Humans; Osteoblasts; Pteridines; Purines; Quinolines; Retinal Pigment Epithelium; Signal Transduction; Single-Cell Analysis; Thiazoles | 2017 |
Binding of the anticancer drug BI-2536 to human serum albumin. A spectroscopic and theoretical study.
Topics: Antineoplastic Agents; Binding Sites; Humans; Molecular Docking Simulation; Protein Binding; Protein Structure, Secondary; Pteridines; Quantum Theory; Serum Albumin; Spectrometry, Fluorescence; Spectroscopy, Fourier Transform Infrared; Thermodynamics | 2017 |
Identification of Polo-like kinases as potential novel drug targets for influenza A virus.
Topics: A549 Cells; Animals; Antimitotic Agents; Cell Cycle Proteins; Dogs; Glycine; HEK293 Cells; Humans; Influenza A virus; Influenza, Human; Madin Darby Canine Kidney Cells; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA Interference; Sulfones; Tumor Suppressor Proteins; Virus Replication | 2017 |
BI2536, a potent and selective inhibitor of polo-like kinase 1, in combination with cisplatin exerts synergistic effects on gastric cancer cells.
Topics: Antineoplastic Combined Chemotherapy Protocols; Apoptosis; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cell Survival; Cisplatin; Drug Resistance, Neoplasm; Drug Synergism; Humans; Polo-Like Kinase 1; Protein Array Analysis; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Signal Transduction; Stomach Neoplasms; Up-Regulation | 2018 |
Essential Role of Polo-like Kinase 1 (Plk1) Oncogene in Tumor Growth and Metastasis of Tamoxifen-Resistant Breast Cancer.
Topics: Animals; Antineoplastic Agents, Hormonal; Apoptosis; Biomarkers, Tumor; Breast Neoplasms; Cell Cycle; Cell Cycle Proteins; Cell Movement; Cell Proliferation; Drug Resistance, Neoplasm; Female; Gene Expression Regulation, Neoplastic; Humans; Liver Neoplasms; Mice; Mice, Inbred BALB C; Mice, Nude; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Splenic Neoplasms; Tamoxifen; Tumor Cells, Cultured; Xenograft Model Antitumor Assays | 2018 |
BI-2536 and BI-6727, dual Polo-like kinase/bromodomain inhibitors, effectively reactivate latent HIV-1.
Topics: Cell Line, Tumor; Drug Combinations; Gene Expression Regulation, Viral; Histone Deacetylase Inhibitors; HIV-1; Host-Pathogen Interactions; Humans; Inhibitory Concentration 50; Leukocytes, Mononuclear; Lymphocytes; Monocytes; Phorbol Esters; Primary Cell Culture; Protein Domains; Protein Kinase Inhibitors; Pteridines; RNA, Messenger; RNA, Viral; THP-1 Cells; Transcription, Genetic; Virus Activation; Virus Latency; Vorinostat | 2018 |
The TSC1-mTOR-PLK axis regulates the homeostatic switch from Schwann cell proliferation to myelination in a stage-specific manner.
Topics: Animals; Cell Cycle; Cell Cycle Proteins; Cell Proliferation; Female; Homeostasis; Male; Mice, 129 Strain; Mice, Inbred C57BL; Mice, Transgenic; Neural Stem Cells; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Schwann Cells; Sciatic Nerve; TOR Serine-Threonine Kinases; Transcriptome; Tuberous Sclerosis Complex 1 Protein | 2018 |
Expression of polo-like kinase 1 in pre-implantation stage murine somatic cell nuclear transfer embryos.
Topics: Animals; Antimitotic Agents; Cell Cycle Proteins; Embryo, Mammalian; Embryonic Development; Gene Expression; Gene Expression Profiling; Mice; Mice, Inbred C57BL; Mice, Inbred DBA; Nuclear Transfer Techniques; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2019 |
Effect of PLK1 inhibition on cisplatin-resistant gastric cancer cells.
Topics: Antineoplastic Agents; Apoptosis; Autophagy; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Cisplatin; Gene Expression Regulation, Enzymologic; Gene Expression Regulation, Neoplastic; Humans; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA Interference; RNA, Small Interfering; Signal Transduction; Stomach Neoplasms | 2019 |
Inhibition of Polo-Like Kinase 1 by BI2536 Reverses the Multidrug Resistance of Human Hepatoma Cells In Vitro and In Vivo.
Topics: Animals; Antineoplastic Agents; Carcinoma, Hepatocellular; Cell Cycle Proteins; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Humans; Liver Neoplasms; Liver Neoplasms, Experimental; Male; Mice; Mice, Nude; Molecular Structure; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Structure-Activity Relationship; Tumor Cells, Cultured | 2019 |
A PLK1 kinase inhibitor enhances the chemosensitivity of cisplatin by inducing pyroptosis in oesophageal squamous cell carcinoma.
Topics: Animals; Antineoplastic Agents; Antineoplastic Combined Chemotherapy Protocols; Carcinoma, Squamous Cell; Cell Cycle Proteins; Cell Line, Tumor; Cisplatin; Esophageal Neoplasms; Female; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyroptosis | 2019 |
Antileukemia Effects of Notch-Mediated Inhibition of Oncogenic PLK1 in B-Cell Acute Lymphoblastic Leukemia.
Topics: Animals; Cell Cycle Proteins; Cell Line; Cell Line, Tumor; Humans; Mice, Inbred NOD; Mice, Knockout; Mice, SCID; Oncogenes; Polo-Like Kinase 1; Precursor B-Cell Lymphoblastic Leukemia-Lymphoma; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Receptors, Notch; RNA Interference; Xenograft Model Antitumor Assays | 2019 |
Protein targeting chimeric molecules specific for dual bromodomain 4 (BRD4) and Polo-like kinase 1 (PLK1) proteins in acute myeloid leukemia cells.
Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Cycle Proteins; Cell Line, Tumor; Cell Movement; Cell Survival; Gene Expression Regulation, Leukemic; Genes, myc; Humans; Leukemia, Myeloid, Acute; Mice, SCID; Molecular Targeted Therapy; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proteolysis; Proto-Oncogene Proteins; Pteridines; Small Molecule Libraries; Transcription Factors; Xenograft Model Antitumor Assays | 2020 |
Splice Modulation Synergizes Cell Cycle Inhibition.
Topics: Antineoplastic Agents; Aurora Kinases; Benzamides; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Proliferation; Drug Screening Assays, Antitumor; Heterocyclic Compounds, 3-Ring; Humans; Macrolides; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Pyrazoles; Pyrimidines; Structure-Activity Relationship; Substrate Specificity | 2020 |
PLK1/NF-κB feedforward circuit antagonizes the mono-ADP-ribosyltransferase activity of PARP10 and facilitates HCC progression.
Topics: Animals; Antineoplastic Agents; Carcinogenesis; Carcinoma, Hepatocellular; Cell Cycle Proteins; Disease Progression; Feedback, Physiological; Female; HEK293 Cells; Hepatectomy; Humans; Kaplan-Meier Estimate; Liver; Liver Neoplasms; Male; Mice; Middle Aged; Mutagenesis, Site-Directed; Neoplasm Staging; Nitriles; Phosphorylation; Polo-Like Kinase 1; Poly(ADP-ribose) Polymerases; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Signal Transduction; Staurosporine; Sulfones; Transcription Factor RelA; Xenograft Model Antitumor Assays | 2020 |
Preferential Killing of Tetraploid Colon Cancer Cells by Targeting the Mitotic Kinase PLK1.
Topics: Antimitotic Agents; Antineoplastic Agents, Phytogenic; Apoptosis; Cell Cycle; Cell Cycle Proteins; Cell Line, Tumor; Cell Survival; Colchicine; Colonic Neoplasms; Drug Synergism; Humans; Microtubules; Mitochondria; Mitosis; Paclitaxel; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; RNA, Small Interfering; Tetraploidy; Tubulin Modulators; Vincristine | 2020 |
Targeting the PLK1-FOXO1 pathway as a novel therapeutic approach for treating advanced prostate cancer.
Topics: Apoptosis; Cell Cycle Proteins; Cell Line, Tumor; Cell Nucleus; Cell Survival; Drug Synergism; Forkhead Box Protein O1; Humans; Male; Molecular Targeted Therapy; Neoplasm Staging; Nocodazole; Phosphorylation; Polo-Like Kinase 1; Prostatic Neoplasms; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Signal Transduction; Transcription, Genetic | 2020 |
Dual inhibition of Src and PLK1 regulate stemness and induce apoptosis through Notch1-SOX2 signaling in EGFRvIII positive glioma stem cells (GSCs).
Topics: Animals; Antineoplastic Agents; Apoptosis; Benzodioxoles; Brain Neoplasms; Cell Cycle Proteins; Cell Line, Tumor; ErbB Receptors; Female; Gene Expression Regulation, Neoplastic; Glioma; Humans; Injections, Intraventricular; Mice; Mice, Inbred BALB C; Mice, Nude; Neoplastic Stem Cells; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Quinazolines; Receptor, Notch1; Signal Transduction; SOXB1 Transcription Factors; src-Family Kinases; Stereotaxic Techniques; Survival Analysis; Tumor Burden; Xenograft Model Antitumor Assays | 2020 |
Dual PLK1 and STAT3 inhibition promotes glioblastoma cells apoptosis through MYC.
Topics: Animals; Antineoplastic Agents; Apoptosis; Brain Neoplasms; Carcinogenesis; Cell Cycle Proteins; Cell Line, Tumor; Cell Movement; Cell Proliferation; Cyclic S-Oxides; Female; Gene Expression Regulation, Neoplastic; Glioblastoma; Humans; Mice; Mice, Nude; Neuroglia; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-myc; Pteridines; RNA, Small Interfering; Signal Transduction; STAT3 Transcription Factor; Survival Analysis; Tumor Burden; Xenograft Model Antitumor Assays | 2020 |
Connectivity Mapping Identifies BI-2536 as a Potential Drug to Treat Diabetic Kidney Disease.
Topics: Animals; Diabetes Mellitus; Diabetic Nephropathies; Kidney; Mice; Pharmaceutical Preparations; Pteridines; Transcriptome | 2021 |
Calibrated liposomal release of the anti-mitotic agent BI-2536 increases the targeting of mitotic tumor cells.
Topics: Animals; Antimitotic Agents; Cell Proliferation; Colonic Neoplasms; Drug Compounding; Drug Liberation; Female; HCT116 Cells; Humans; Kinetics; Lipids; Liposomes; Mice, Nude; Mitosis; Pteridines; Tumor Burden; Xenograft Model Antitumor Assays | 2020 |
Staying Connected: Transcriptomics in the Search for Novel Diabetic Kidney Disease Treatments.
Topics: Diabetes Mellitus; Diabetic Nephropathies; Humans; Pharmaceutical Preparations; Pteridines; Transcriptome | 2021 |
Potent Synergistic Effect on C-Myc-Driven Colorectal Cancers Using a Novel Indole-Substituted Quinoline with a Plk1 Inhibitor.
Topics: Amodiaquine; Animals; Apoptosis; Cell Cycle Proteins; Cell Proliferation; Colorectal Neoplasms; Drug Synergism; Female; Humans; Male; Mice; Mice, Nude; Polo-Like Kinase 1; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Proto-Oncogene Proteins c-myc; Pteridines; Tumor Cells, Cultured; Xenograft Model Antitumor Assays | 2021 |
PLK1 Inhibition Induces Immunogenic Cell Death and Enhances Immunity against NSCLC.
Topics: Animals; Carcinoma, Non-Small-Cell Lung; Cell Cycle Proteins; Cell Line, Tumor; Humans; Immunogenic Cell Death; Lung Neoplasms; Mice; Polo-Like Kinase 1; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines; Tumor Microenvironment | 2021 |
Shedding light on the binding mechanism of kinase inhibitors BI-2536, Volasetib and Ro-3280 with their pharmacological target PLK1.
Topics: Adenosine Triphosphate; Cell Cycle Proteins; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proto-Oncogene Proteins; Pteridines | 2022 |
Polo-like kinase inhibitor BI2536 induces eryptosis.
Topics: Calcium; Ceramides; Eryptosis; Erythrocytes; Hemolysis; Humans; Protein Serine-Threonine Kinases; Pteridines | 2023 |