imatinib has been researched along with dasatinib in 51 studies
| Timeframe | Studies, this research(%) | All Research% |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 8 (15.69) | 29.6817 |
| 2010's | 30 (58.82) | 24.3611 |
| 2020's | 13 (25.49) | 2.80 |
| Authors | Studies |
|---|---|
| Atteridge, CE; Biggs, WH; Carter, TA; Edeen, PT; Fabian, MA; Floyd, M; Ford, JM; Grotzfeld, RM; Herrgard, S; Insko, DE; Lockhart, DJ; Mehta, SA; Milanov, ZV; Pao, W; Patel, HK; Sawyers, CL; Shah, NP; Treiber, DK; Varmus, H; Velasco, AM; Wodicka, LM; Zarrinkar, PP | 1 |
| Chu, JJ; Yang, PL | 1 |
| Bennett, KL; Bürckstümmer, T; Colinge, J; Ellmeier, W; Hantschel, O; Kneidinger, M; Rix, U; Schmidt, U; Schütze, G; Superti-Furga, G; Valent, P | 1 |
| Dalgarno, D; Keats, J; Lamore, S; Li, F; Parillon, L; Shakespeare, W; Wang, Y; Xu, Q; Zhou, T; Zhu, X | 1 |
| Atteridge, CE; Campbell, BT; Chan, KW; Ciceri, P; Davis, MI; Edeen, PT; Faraoni, R; Floyd, M; Gallant, P; Herrgard, S; Hunt, JP; Karaman, MW; Lockhart, DJ; Milanov, ZV; Morrison, MJ; Pallares, G; Patel, HK; Pritchard, S; Treiber, DK; Wodicka, LM; Zarrinkar, PP | 1 |
| Bradner, JE | 1 |
| Du-Cuny, L; Mash, EA; Meuillet, EJ; Moses, S; Powis, G; Song, Z; Zhang, S | 1 |
| Antczak, C; Calder, PA; Clarkson, B; Djaballah, H; Frattini, MG; Minchenko, MA; Ramirez, CN; Shum, D; Veach, DR | 1 |
| Ashman, LK; Griffith, R; Mashkani, B | 1 |
| Morphy, R | 1 |
| Hajduk, PJ; Johnson, EF; Kifle, L; Merta, PJ; Metz, JT; Soni, NB | 1 |
| Russu, WA; Shallal, HM | 1 |
| Ciceri, P; Davis, MI; Herrgard, S; Hocker, M; Hunt, JP; Pallares, G; Treiber, DK; Wodicka, LM; Zarrinkar, PP | 1 |
| Ballard, TE; Henderson, JL; Kalgutkar, AS; Obach, RS; Orr, ST; Ripp, SL; Scott, DO; Sun, H | 1 |
| Al-Mazaideh, GM; Erdmann, F; Göllner, C; Rohe, A; Schmidt, M; Sippl, W; Wichapong, K | 1 |
| Cantin, LD; Chen, H; Kenna, JG; Noeske, T; Stahl, S; Walker, CL; Warner, DJ | 1 |
| Ding, K; Leng, F; Li, Y; Long, H; Lu, X; Luo, J; Pan, X; Ren, X; Shen, M; Tu, Z; Wen, D; Zhang, F; Zhang, Z | 1 |
| Bai, Y; Ding, K; Feng, Y; Lang, X; Leng, F; Li, Y; Liu, J; Long, H; Lu, X; Luo, J; Pan, J; Pan, X; Ren, X; She, M; Tu, Z; Wang, D; Wen, D; Zhang, F; Zhang, Z; Zhuang, X | 1 |
| Hong, S; Hong, SS; Kim, J; Lee, H; Park, Y; Yun, SM | 1 |
| Davis, MI; Khan, J; Li, SQ; Patel, PR; Shen, M; Sun, H; Thomas, CJ | 1 |
| Cahya, S; Cummins, DJ; Gao, C; Iversen, PW; Nicolaou, CA; Vieth, M; Wang, J; Watson, IA | 1 |
| Afshari, CA; Chen, Y; Dunn, RT; Hamadeh, HK; Kalanzi, J; Kalyanaraman, N; Morgan, RE; van Staden, CJ | 1 |
| Choi, BS; Hong, S; Hong, SS; Kim, J; Kim, SJ; Lee, H; Lee, S | 1 |
| Bullock, AN; Canning, P; Choi, S; Cuny, GD; Mohedas, AH; Sanvitale, CE; Wang, Y; Xing, X; Yu, PB | 1 |
| Ding, K; Li, Y; Lu, X; Ren, X | 1 |
| Ding, K; Lu, X; Luo, J; Pan, X; Ren, X; Wang, D; Yu, R; Zhang, Z; Zhuang, X | 1 |
| Muthyala, R; Sham, YY; Shin, WS; Xie, J | 1 |
| Dong, J; Dong, Y; Pan, X; Shan, Y; Wang, M; Zhang, J; Zhang, L | 1 |
| Chen, C; Hu, Z; Liang, X; Liu, J; Liu, Q; Liu, X; Lv, F; Qi, S; Qi, Z; Wang, A; Wang, B; Wang, L; Wang, W; Zhang, S; Zhao, Z; Zou, F | 1 |
| Bai, C; Chen, Y; Ding, K; Ding, Y; Geng, Y; Li, LY; Liu, JW; Sang, F; Sun, B; Sun, J; Wang, J; Wu, LL; Yang, G; Zhang, Q; Zhang, Z | 1 |
| Beleh, OM; Brandvold, KR; Johnson, TK; Kwarcinski, FE; Meagher, JL; Phadke, S; Seeliger, MA; Soellner, MB; Stuckey, JA | 1 |
| Chen, M; Hu, C; Suzuki, A; Thakkar, S; Tong, W; Yu, K | 1 |
| Bestgen, B; Borjini, N; Chevé, G; Daydé-Cazals, B; Fauvel, B; Feneyrolles, C; Gassiot, F; Singer, M; Spenlinhauer, A; Van Hijfte, N; Warnault, P; Yasri, A | 1 |
| Jahnke, W; Skora, L | 1 |
| Bajić, M; Bistrović, A; Grbčić, P; Harej, A; Koštrun, S; Krstulović, L; Pavelić, SK; Raić-Malić, S; Sedić, M | 1 |
| Aiche, S; Bassermann, F; Becker, W; Canevari, G; Casale, E; Depaolini, SR; Ehrlich, HC; Felder, ER; Feuchtinger, A; Garz, AK; Gohlke, BO; Götze, K; Greif, PA; Hahne, H; Heinzlmeir, S; Helm, D; Huenges, J; Jeremias, I; Kayser, G; Klaeger, S; Koch, H; Koenig, PA; Kramer, K; Kuster, B; Médard, G; Meng, C; Petzoldt, S; Polzer, H; Preissner, R; Qiao, H; Reinecke, M; Reiter, K; Rueckert, L; Ruland, J; Ruprecht, B; Schlegl, J; Schmidt, T; Schneider, S; Schoof, M; Spiekermann, K; Tõnisson, N; Vick, B; Vooder, T; Walch, A; Wilhelm, M; Wu, Z; Zecha, J; Zolg, DP | 1 |
| Berellini, G; Buonamici, S; Cotesta, S; Cowan-Jacob, SW; Dodd, S; Drueckes, P; Fabbro, D; Furet, P; Gabriel, T; Groell, JM; Grotzfeld, RM; Hassan, AQ; Henry, C; Iyer, V; Jahnke, W; Jones, D; Lombardo, F; Loo, A; Manley, PW; Marzinzik, AL; Pellé, X; Rummel, G; Salem, B; Schoepfer, J; Warmuth, M; Wylie, AA; Zoller, T | 1 |
| Malarz, K; Mularski, J; Musiol, R; Pacholczyk, M | 1 |
| Abdolazimi, Y; Allegretti, PA; Annes, JP; Caffet, M; Horton, TM; Michel, G; Moeller, HP; Smith, M; Yeh, B | 1 |
| Cao, DS; Chen, AF; Chen, XS; Cheng, Y; Guan, YD; Jiang, SL; Yang, JM; Zhang, LX; Zhang, Y | 1 |
| Gao, H; Qiu, Y; Rao, Y; Sun, X; Sun, Y; Weng, Q; Yang, Y | 1 |
| Easwaran, M; Manickam, M; Pillaiyar, T; Wendt, LL | 1 |
| Abuo-Rahma, GEA; Badr, M; Bass, AKA; El-Zoghbi, MS; Mohamed, MFA; Nageeb, EM | 1 |
| Esaki, T; Kawashima, H; Komura, H; Kuroda, M; Mizuguchi, K; Natsume-Kitatani, Y; Ohashi, R; Watanabe, R | 1 |
| Caballero, E; García-Cárceles, J; Gil, C; Martínez, A | 1 |
| Laufer, S; Pillaiyar, T | 1 |
| Delabio, LC; Dutra, JP; Hembecker, M; Kita, DH; Moure, VR; Pereira, GDS; Scheiffer, G; Valdameri, G; Zattoni, IF | 1 |
| Hao, RR; Huang, WH; Liang, MH; Pan, YL; Shen, ZR; Zeng, SX | 1 |
| Bruyneel, AAN; Hnatiuk, AP; Malhotra, SV; Mercola, M; Pandrala, M | 1 |
| Allan, JM; Blair, HJ; Dannoura, A; Dueñas, ME; Heidenreich, O; Heunis, T; Inns, J; Marín-Rubio, JL; Martin, MP; Peltier-Heap, RE; Saxty, B; Scott, J; Simpson, AJ; Trost, M; Watt, JE | 1 |
| Dranchak, PK; Huang, R; Inglese, J; Lamy, L; Oliphant, E; Queme, B; Tao, D; Wang, Y; Xia, M | 1 |
10 review(s) available for imatinib and dasatinib
| Article | Year |
|---|---|
Selectively nonselective kinase inhibition: striking the right balance.
Topics: Animals; Antineoplastic Agents; Drug Design; Drug Discovery; Humans; Protein Binding; Protein Kinase Inhibitors; Structure-Activity Relationship | 2010 |
Mechanism-based inactivation (MBI) of cytochrome P450 enzymes: structure-activity relationships and discovery strategies to mitigate drug-drug interaction risks.
Topics: Animals; Apoproteins; Cytochrome P-450 Enzyme Inhibitors; Cytochrome P-450 Enzyme System; Drug Discovery; Drug Interactions; Heme; Humans; Models, Biological; Pharmacokinetics; Structure-Activity Relationship; Time Factors | 2012 |
Small molecule discoidin domain receptor kinase inhibitors and potential medical applications.
Topics: Amino Acid Sequence; Animals; Discoidin Domain Receptors; Drug Discovery; Humans; Inflammation; Ligands; Models, Molecular; Molecular Sequence Data; Neoplasms; Protein Conformation; Protein Kinase Inhibitors; Receptor Protein-Tyrosine Kinases; Receptors, Mitogen; Small Molecule Libraries | 2015 |
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
Topics: Chemical and Drug Induced Liver Injury; Databases, Factual; Drug Labeling; Humans; Pharmaceutical Preparations; Risk | 2016 |
The recent outbreaks of human coronaviruses: A medicinal chemistry perspective.
Topics: Antiviral Agents; Chemistry, Pharmaceutical; COVID-19; Disease Outbreaks; Drug Repositioning; Humans; Virus Internalization | 2021 |
Comprehensive review for anticancer hybridized multitargeting HDAC inhibitors.
Topics: Androgen Antagonists; Animals; Antineoplastic Agents; Benzimidazoles; Cyclic Nucleotide Phosphodiesterases, Type 5; Daunorubicin; Doxorubicin; fms-Like Tyrosine Kinase 3; Histone Deacetylase Inhibitors; Humans; Hydroxamic Acids; Molecular Targeted Therapy; Morpholines; Nicotinamide Phosphoribosyltransferase; Nitric Oxide; Pyrimidines; Quinazolines; Structure-Activity Relationship; Transcription Factors | 2021 |
Kinase Inhibitors as Underexplored Antiviral Agents.
Topics: Animals; Antiviral Agents; Drug Repositioning; Humans; Protein Kinase Inhibitors; Virus Diseases; Viruses | 2022 |
Kinases as Potential Therapeutic Targets for Anti-coronaviral Therapy.
Topics: Antiviral Agents; COVID-19; COVID-19 Drug Treatment; Humans; Protein Kinase Inhibitors; SARS-CoV-2; Signal Transduction; Virus Replication | 2022 |
Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
Topics: Antineoplastic Agents; ATP Binding Cassette Transporter, Subfamily G, Member 2; Breast Neoplasms; Drug Resistance, Multiple; Drug Resistance, Neoplasm; Female; Humans; Neoplasm Proteins; Neoplastic Stem Cells | 2022 |
The progress of small-molecules and degraders against BCR-ABL for the treatment of CML.
Topics: Antineoplastic Agents; Benzamides; Drug Resistance, Neoplasm; Fusion Proteins, bcr-abl; Humans; Imatinib Mesylate; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Piperazines; Protein Kinase Inhibitors; Pyrimidines | 2022 |
41 other study(ies) available for imatinib and dasatinib
| Article | Year |
|---|---|
Inhibition of drug-resistant mutants of ABL, KIT, and EGF receptor kinases.
Topics: Aminoquinolines; Aniline Compounds; Cell Line; Drug Resistance, Neoplasm; ErbB Receptors; Humans; Indoles; Kinetics; Morpholines; Mutation; Naphthalenes; Neoplasms; Oncogene Proteins v-abl; Organic Chemicals; Piperazines; Protein Kinase Inhibitors; Proto-Oncogene Proteins c-kit; Pyrazoles; Pyrroles; Sunitinib | 2005 |
c-Src protein kinase inhibitors block assembly and maturation of dengue virus.
Topics: Animals; Chlorocebus aethiops; CSK Tyrosine-Protein Kinase; Cytotoxicity Tests, Immunologic; Dasatinib; Dengue Virus; Fluorescent Antibody Technique, Indirect; Humans; Microscopy, Electron, Transmission; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidines; RNA Interference; src-Family Kinases; Thiazoles; Vero Cells; Virus Assembly | 2007 |
The Btk tyrosine kinase is a major target of the Bcr-Abl inhibitor dasatinib.
Topics: Animals; Basophils; Dasatinib; Enzyme-Linked Immunosorbent Assay; Fusion Proteins, bcr-abl; Histamine Release; Humans; K562 Cells; Mice; Mice, Inbred C57BL; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrimidines; Thiazoles; U937 Cells | 2007 |
Crystal structure of the T315I mutant of AbI kinase.
Topics: Animals; Cell Line; Crystallography, X-Ray; Mice; Models, Molecular; Mutation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-abl; Pyridines; Structural Homology, Protein; Threonine | 2007 |
A quantitative analysis of kinase inhibitor selectivity.
Topics: Binding Sites; Enzyme Activation; Humans; Phosphotransferases; Protein Binding; Protein Interaction Mapping; Protein Kinase Inhibitors; Proteome; Quantitative Structure-Activity Relationship | 2008 |
A pulse at the heart of targeted therapy.
Topics: Antineoplastic Agents; Benzamides; Clinical Trials as Topic; Drug Delivery Systems; Drug Design; Humans; Imatinib Mesylate; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Piperazines; Pyrimidines | 2009 |
Computational modeling of novel inhibitors targeting the Akt pleckstrin homology domain.
Topics: Antineoplastic Agents; Blood Proteins; Caco-2 Cells; Cell Membrane Permeability; Computer Simulation; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Phosphoproteins; Protein Binding; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-akt; Quantitative Structure-Activity Relationship | 2009 |
Structure-activity relationships of 6-(2,6-dichlorophenyl)-8-methyl-2-(phenylamino)pyrido[2,3-d]pyrimidin-7-ones: toward selective Abl inhibitors.
Topics: Antineoplastic Agents; Cell Line, Tumor; Humans; Oncogene Proteins v-abl; Pyridines; Pyridones; Pyrimidines; Pyrimidinones; Structure-Activity Relationship | 2009 |
Colony stimulating factor-1 receptor as a target for small molecule inhibitors.
Topics: Benzamides; Binding Sites; Carbazoles; Computer Simulation; Dasatinib; Drug Design; Furans; Humans; Hydrogen Bonding; Imatinib Mesylate; Indoles; Piperazines; Protein Kinase Inhibitors; Pyrimidines; Pyrroles; Receptor, Macrophage Colony-Stimulating Factor; Staurosporine; Sunitinib; Thiazoles | 2010 |
Navigating the kinome.
Topics: Drug Design; Pharmacogenetics; Protein Kinases; Proteome; Systems Biology | 2011 |
Discovery, synthesis, and investigation of the antitumor activity of novel piperazinylpyrimidine derivatives.
Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Humans; Models, Molecular; Molecular Structure; Piperazines; Protein Kinase Inhibitors; Protein Kinases; Pyrimidines; Stereoisomerism; Structure-Activity Relationship | 2011 |
Comprehensive analysis of kinase inhibitor selectivity.
Topics: Catalysis; Drug Design; Enzyme Stability; High-Throughput Screening Assays; Humans; Protein Binding; Protein Kinase Inhibitors; Protein Kinases; Proteomics; Signal Transduction; Substrate Specificity | 2011 |
Evaluation of potential Myt1 kinase inhibitors by TR-FRET based binding assay.
Topics: Dose-Response Relationship, Drug; Fluorescence Resonance Energy Transfer; Glycolipids; Humans; Membrane Proteins; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein-Tyrosine Kinases; Structure-Activity Relationship | 2013 |
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Bile Acids and Salts; Cell Line; Chemical and Drug Induced Liver Injury; Humans; Quantitative Structure-Activity Relationship | 2012 |
Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant.
Topics: Benzamides; Blotting, Western; Cell Line, Tumor; Cell Proliferation; Cells, Cultured; Drug Design; Drug Resistance, Neoplasm; Fusion Proteins, bcr-abl; Humans; Imatinib Mesylate; Isoleucine; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Models, Molecular; Molecular Structure; Mutation; Phosphorylation; Piperazines; Protein Kinase Inhibitors; Pyrimidines; Structure-Activity Relationship; Threonine | 2012 |
Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.
Topics: Administration, Oral; Animals; Antineoplastic Agents; Benzamides; Biological Availability; Cell Line, Tumor; Drug Resistance, Neoplasm; Fusion Proteins, bcr-abl; Humans; Imatinib Mesylate; Magnetic Resonance Spectroscopy; Models, Molecular; Mutation; Phosphorylation; Piperazines; Protein Kinase Inhibitors; Protein-Tyrosine Kinases; Pyrazoles; Pyrimidines; Spectrometry, Mass, Electrospray Ionization | 2013 |
Discovery of new benzothiazole-based inhibitors of breakpoint cluster region-Abelson kinase including the T315I mutant.
Topics: Animals; Benzothiazoles; Cell Line; Cell Proliferation; Drug Design; Fusion Proteins, bcr-abl; Mice; Molecular Docking Simulation; Mutation; Nocodazole; Protein Kinase Inhibitors; Protein Structure, Tertiary; Signal Transduction | 2013 |
Identification of potent Yes1 kinase inhibitors using a library screening approach.
Topics: Binding Sites; Cell Line; Cell Survival; Drug Design; Humans; Hydrogen Bonding; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein Structure, Tertiary; Proto-Oncogene Proteins c-yes; Small Molecule Libraries; Structure-Activity Relationship | 2013 |
Selectivity data: assessment, predictions, concordance, and implications.
Topics: Computer Simulation; Drug Discovery | 2013 |
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B; ATP Binding Cassette Transporter, Subfamily B, Member 11; ATP-Binding Cassette Transporters; Biological Transport; Chemical and Drug Induced Liver Injury; Cluster Analysis; Drug-Related Side Effects and Adverse Reactions; Humans; Liver; Male; Multidrug Resistance-Associated Proteins; Pharmacokinetics; Rats; Rats, Sprague-Dawley; Recombinant Proteins; Risk Assessment; Risk Factors; Toxicity Tests | 2013 |
Development and biological evaluation of potent and selective c-KIT(D816V) inhibitors.
Topics: Antineoplastic Agents; Apoptosis; Aza Compounds; Benzamides; Cell Cycle; Cell Line, Tumor; Drug Design; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Humans; Imatinib Mesylate; Indoles; Molecular Docking Simulation; Piperazines; Point Mutation; Proto-Oncogene Proteins c-kit; Pyrimidines; Structure-Activity Relationship | 2014 |
Structure-activity relationship of 3,5-diaryl-2-aminopyridine ALK2 inhibitors reveals unaltered binding affinity for fibrodysplasia ossificans progressiva causing mutants.
Topics: Activin Receptors, Type I; Aminopyridines; Humans; Mutation; Myositis Ossificans; Phenols; Protein Kinase Inhibitors; Structure-Activity Relationship | 2014 |
Hybrid pyrimidine alkynyls inhibit the clinically resistance related Bcr-Abl(T315I) mutant.
Topics: Cell Proliferation; Fusion Proteins, bcr-abl; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Models, Molecular; Mutation; Pyrimidines | 2015 |
Discovery of 1-hydroxypyridine-2-thiones as selective histone deacetylase inhibitors and their potential application for treating leukemia.
Topics: Animals; Cell Line, Tumor; Cell Proliferation; Cell Survival; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Histone Deacetylase Inhibitors; Histone Deacetylases; Humans; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Mice; Molecular Docking Simulation; Molecular Structure; Pyridines; Structure-Activity Relationship; Thiones | 2015 |
Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1H-indazol-3-amine.
Topics: Antineoplastic Agents; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Fusion Proteins, bcr-abl; Humans; Indazoles; K562 Cells; Molecular Docking Simulation; Molecular Structure; Piperazines; Protein Kinase Inhibitors; Structure-Activity Relationship | 2015 |
Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Le
Topics: Administration, Oral; Animals; Antineoplastic Agents; Apoptosis; Benzamides; Cell Line, Tumor; Cell Proliferation; Dose-Response Relationship, Drug; Drug Discovery; Drug Screening Assays, Antitumor; Female; Fusion Proteins, bcr-abl; Humans; K562 Cells; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Male; Mice; Mice, Nude; Models, Molecular; Molecular Structure; Neoplasms, Experimental; p38 Mitogen-Activated Protein Kinases; Protein Kinase Inhibitors; Pyrimidines; Rats; Rats, Sprague-Dawley; src-Family Kinases; Structure-Activity Relationship | 2016 |
Structure-Activity Relationship Study of Rakicidins: Overcoming Chronic Myeloid Leukemia Resistance to Imatinib with 4-Methylester-Rakicidin A.
Topics: Antineoplastic Agents; Apoptosis; Cell Proliferation; Dose-Response Relationship, Drug; Drug Resistance, Neoplasm; Drug Screening Assays, Antitumor; Humans; Imatinib Mesylate; K562 Cells; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Lipopeptides; Molecular Structure; Peptides, Cyclic; Structure-Activity Relationship | 2016 |
Conformation-Selective Analogues of Dasatinib Reveal Insight into Kinase Inhibitor Binding and Selectivity.
Topics: Animals; Chickens; Dasatinib; Drug Design; Humans; Molecular Docking Simulation; Protein Binding; Protein Conformation; Protein Kinase Inhibitors; Protein Kinases | 2016 |
Rational Design, Synthesis, and Biological Evaluation of 7-Azaindole Derivatives as Potent Focused Multi-Targeted Kinase Inhibitors.
Topics: Animals; Cell Proliferation; Drug Design; Human Umbilical Vein Endothelial Cells; Humans; Indoles; Male; Mice; Patch-Clamp Techniques; Protein Kinase Inhibitors | 2016 |
Topics: | 2017 |
Design, synthesis and biological evaluation of novel benzimidazole amidines as potent multi-target inhibitors for the treatment of non-small cell lung cancer.
Topics: Amidines; Antineoplastic Agents; Apoptosis; Benzimidazoles; Carcinoma, Non-Small-Cell Lung; Cell Proliferation; Cells, Cultured; Crystallography, X-Ray; Dose-Response Relationship, Drug; Drug Design; Drug Screening Assays, Antitumor; Humans; Lung Neoplasms; Models, Molecular; Molecular Structure; Protein Kinase Inhibitors; Protein Kinases; Structure-Activity Relationship; Triazoles | 2018 |
The target landscape of clinical kinase drugs.
Topics: Animals; Antineoplastic Agents; Cell Line, Tumor; Cytokines; Drug Discovery; fms-Like Tyrosine Kinase 3; Humans; Leukemia, Myeloid, Acute; Lung Neoplasms; Mice; Molecular Targeted Therapy; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Proteomics; Xenograft Model Antitumor Assays | 2017 |
Discovery of Asciminib (ABL001), an Allosteric Inhibitor of the Tyrosine Kinase Activity of BCR-ABL1.
Topics: Allosteric Regulation; Animals; Dogs; Drug Discovery; Fusion Proteins, bcr-abl; Humans; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Male; Mice; Models, Molecular; Molecular Structure; Mutation; Niacinamide; Phosphorylation; Protein Conformation; Protein Kinase Inhibitors; Pyrazoles; Rats; Rats, Sprague-Dawley; Tumor Cells, Cultured; Xenograft Model Antitumor Assays | 2018 |
The p53 stabilizing agent CP-31398 and multi-kinase inhibitors. Designing, synthesizing and screening of styrylquinazoline series.
Topics: Antineoplastic Agents; Cell Line, Tumor; Cell Proliferation; Drug Design; Drug Screening Assays, Antitumor; Humans; Molecular Docking Simulation; Protein Kinase Inhibitors; Protein Stability; Pyrimidines; Quinazolines; Tumor Suppressor Protein p53 | 2019 |
Generation of highly potent DYRK1A-dependent inducers of human β-Cell replication via Multi-Dimensional compound optimization.
Topics: Binding Sites; Cell Proliferation; Dyrk Kinases; Humans; Insulin; Insulin-Secreting Cells; Kinetics; Molecular Docking Simulation; Naphthyridines; Protein Kinase Inhibitors; Protein Serine-Threonine Kinases; Protein Structure, Tertiary; Protein-Tyrosine Kinases; Small Molecule Libraries; Structure-Activity Relationship | 2020 |
A multi-scale systems pharmacology approach uncovers the anti-cancer molecular mechanism of Ixabepilone.
Topics: Animals; Antineoplastic Agents; Apoptosis; Cell Proliferation; Dose-Response Relationship, Drug; Drug Screening Assays, Antitumor; Epothilones; Female; Humans; Mammary Neoplasms, Experimental; Mice; Mice, Inbred BALB C; Mice, Nude; Molecular Structure; Proto-Oncogene Proteins c-bcl-2; Structure-Activity Relationship; Tumor Cells, Cultured | 2020 |
Global PROTAC Toolbox for Degrading BCR-ABL Overcomes Drug-Resistant Mutants and Adverse Effects.
Topics: Antineoplastic Agents; Dasatinib; Drug Design; Fusion Proteins, bcr-abl; Humans; Imidazoles; Models, Molecular; Niacinamide; Proteolysis; Pyrazoles; Pyridazines | 2020 |
Development of an
Topics: Animals; ATP Binding Cassette Transporter, Subfamily B, Member 1; Biological Transport; Blood-Brain Barrier; Cell Line; Computer Simulation; Endothelial Cells; Gene Knockout Techniques; Humans; Organic Chemicals; Rats, Transgenic | 2021 |
Designing Novel BCR-ABL Inhibitors for Chronic Myeloid Leukemia with Improved Cardiac Safety.
Topics: Cell Line, Tumor; Drug Resistance, Neoplasm; Fusion Proteins, bcr-abl; Humans; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Mutation; Protein Kinase Inhibitors | 2022 |
A Matrix-Assisted Laser Desorption/Ionization Time-of-Flight Assay Identifies Nilotinib as an Inhibitor of Inflammation in Acute Myeloid Leukemia.
Topics: Cytokines; Drug Resistance, Neoplasm; Fusion Proteins, bcr-abl; Humans; Imatinib Mesylate; Inflammation; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Leukemia, Myeloid, Acute; Protein Kinase Inhibitors; Proteome; Pyrimidines; Spectrometry, Mass, Matrix-Assisted Laser Desorption-Ionization | 2022 |
In vivo quantitative high-throughput screening for drug discovery and comparative toxicology.
Topics: Animals; Caenorhabditis elegans; Drug Discovery; High-Throughput Screening Assays; Humans; Proteomics; Small Molecule Libraries | 2023 |