Compounds > quinazolines
Page last updated: 2024-08-21

quinazolines and bix 01294

quinazolines has been researched along with bix 01294 in 97 studies

Research

Studies (97)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (3.09)29.6817
2010's81 (83.51)24.3611
2020's13 (13.40)2.80

Authors

AuthorsStudies
August, EM; Hickey, ER; Homon, CA; Jenuwein, T; Kelly, TA; Kowalski, JA; Kubicek, S; Mechtler, K; O'Sullivan, RJ; Rea, S; Teodoro, ML; Zhang, Q1
Desponts, C; Ding, S; Do, JT; Hahm, HS; Schöler, HR; Shi, Y1
Bedford, MT; Chang, Y; Cheng, X; Horton, JR; Liu, J; Snyder, JP; Spannhoff, A; Upadhyay, AK; Zhang, X1
Müller, AM; Obier, N1
Imai, K; Okamoto, T; Togami, H1
Bedford, MT; Chang, Y; Cheng, X; Ganesh, T; Horton, JR; Liu, J; Shinkai, Y; Snyder, JP; Spannhoff, A; Sun, A; Zhang, X1
Allali-Hassani, A; Quinn, AM; Simeonov, A; Vedadi, M1
Hauser, AT; Jung, M1
Cho, HS; Field, HI; Hamamoto, R; Hayami, S; Kelly, JD; Nakamura, Y; Neal, DE; Ponder, BA; Takawa, M; Toyokawa, G; Tsunoda, T; Yoshimatsu, M1
Berkova, Z; Koblas, T; Leontovyč, I; Pektorova, L; Saudek, F; Zacharovova, K1
Abbas, W; Herbein, G; Tripathy, MK1
Chang, Y; Cheng, X; Han, JW; Hu, R; Labella, D; Mai, A; Rotili, D; Upadhyay, AK; Yoon, YS; Zhang, X1
Igarashi, Y; Ito, A; Kawasaki, H; Shimazu, T; Shin-ya, K; Shinkai, Y; Tachibana, M; Takagi, M; Takahashi, M; Takemoto, Y; Yoshida, M1
Atadja, P; Fan, H; Frederiksen, M; Gao, J; Gu, XJ; Guo, W; Harrington, E; Jiang, L; Li, E; Li, S; Lin, Y; Lu, C; Meier, P; Scheufler, C; Wang, Z; Xu, YC; Zhao, K; Zhou, S1
Davis, RL; Deramus, T; Franklin, AV; Gupta-Agarwal, S; Lubin, FD; McMahon, LL; Wheelock, M1
Bouchat, S; Cardona, C; Clumeck, N; Colin, L; De Wit, S; Gatot, JS; Herbein, G; Kabeya, K; Lambotte, O; Rohr, O; Rouzioux, C; Van Lint, C1
Lu, Z; Raj, JU; Singh, D; Yang, Q1
Cabot, RA; Johnson, CM; Park, KE1
Eisenberg, CA; Eisenberg, LM; Iaffaldano, G; Kaur, K; Mezentseva, NV; Rémond, MC; Yang, J1
Fuchter, MJ; Malmquist, NA; Mecheri, S; Moss, TA; Scherf, A1
An, XR; Fu, L; Guan, H; Hou, J; Yan, FX; Zhang, J1
Burgkart, R; Culmes, M; Eckstein, HH; Guenther, M; Nüssler, AK; Pelisek, J; Wagner, E1
Appadurai, DA; Manning, J; May, JM; Mitchell, B; Nganga, V; Pierce, LJ; Shakya, A; Spangrude, GJ; Swanson, PC; Tantin, D; Wang, H1
Chen, Y; Fu, S; He, Y; Jiang, H; Li, H; Lin, Q; Shou, J; Sun, S; Wang, Y; Yu, H; Yu, Y1
Chlenski, A; Godley, LA; Lu, Z; Raj, JU; Salwen, HR; Tian, Y; Yang, Q1
Fiszbein, A; Kornblihtt, AR; Petrillo, E; Schor, IE1
Itoi, F; Li, C; Sato, E; Tanemura, K; Terashita, Y; Tokoro, M; Wakayama, S; Wakayama, T; Yamagata, K1
Imai, K; Ochiai, K; Suzuki, N; Tsuda, H; Yang, P; Zhao, N1
Asara, JM; Choi, JH; Cui, H; Ding, HF; Ding, J; Dong, Z; Huang, S; Li, T; Wang, X; Yang, L; Zha, Y; Zhao, E1
Cho, DH; Hwang, JJ; Jang, SJ; Jeong, SY; Jin, DH; Kim, CS; Kim, DE; Kim, HG; Kim, Y; Kim, YS; Koh, JY; Lee, JS; Lee, SJ; Seol, HS; Song, JH; Suh, YA1
Arimondo, PB; Ausseil, F; Bouvy, C; Chang, Y; Cheng, X; Cosconati, S; Di Maro, S; Diederich, M; Grandjenette, C; Gros, C; Labella, D; Mai, A; Marrocco, B; Masson, V; Novellino, E; Poughon, V; Rotili, D; Schnekenburger, M; Tarantino, D1
Navakauskiene, R; Savickiene, J; Stirblyte, I; Treigyte, G; Valiuliene, G1
Feng, D; Hu, Q; Li, H; Ma, H; Su, Y; Tao, H; Wang, X; Zhang, C1
Kaminska, B; Maleszewska, M; Steranka, A1
Basavarajappa, BS; Subbanna, S1
Ea, CK; Lim, YY; Loh, SW; Ng, WL; Yeo, KS1
Angulo-Barturen, I; Avery, VM; Caron, J; Chen, P; Delves, MJ; Duffy, S; Ferrer, S; Fuchter, MJ; Gamo, FJ; Jiménez-Díaz, MB; Malmquist, NA; Menard, D; Nosten, F; Renia, L; Ruecker, A; Santos Martínez, M; Sanz, LM; Scherf, A; Sinden, RE; Sundriyal, S; Suwanarusk, R; Witkowski, B; Wittlin, S1
Fan, JD; He, YL; Lei, PJ; Li, LY; Li, S; Liu, H; Wang, X; Wang, ZN; Wei, G; Wu, M; Zhang, X; Zheng, JY1
Cui, H; Fu, G; Qiu, Y; Ren, A1
Chang, JW; Cho, DH; Hwang, JJ; Jo, YK; Kim, ES; Kim, PS; Park, SJ; Park, TJ; Seo, JH; Shin, JH1
Geutskens, SB; Goedhart, M; Haasnoot, GW; Miggelbrink, XM; Muggen, AF; van den Elsen, PJ; van Eggermond, MC; van Zwet, E; Wierda, RJ1
Chen, Q; Deitsch, KW; Heinberg, AR; Ukaegbu, UE; Wele, M; Zhang, X1
Bae, JS; Choi, YS; Lee, SH; Lee, YM; Oh, SY; Seok, JY1
Chen, J; Chen, P; Chen, X; Huang, HF; Huang, RF; Huang, YF; Jiang, XH; Jiang, YP; Li, M; Yang, XY; Yao, JF; Zheng, FF1
Arihiro, K; Doi, S; Doi, T; Irifuku, T; Kohno, N; Masaki, T; Nakashima, A; Sasaki, K; Ueno, T; Yamada, K1
Cao, C; Huang, J; Luo, A; Qin, G; Wang, F; Wang, X; Yao, J; Zhang, H; Zhao, J; Zheng, Q1
Chao, SB; Huang, XJ; Lin, F; Liu, HL; Ma, XS; Meng, TG; Qin, L; Schatten, H; Sun, QY; Wang, XG; Zhu, CC1
Cho, GW; Jeong, SG; Kim, HT1
Berardino, BG; Caramelo, JJ; Enriqué Steinberg, JH; Fiszbein, A; Giono, LE; Kornblihtt, AR; Pietrasanta, LI; Quaglino, A; Rossi, M; Schor, IE; Sigaut, L; Srebrow, A; von Bilderling, C1
Chen, C; Feng, W; He, M; Li, M; Liu, C; Lu, Y; Pi, H; Yang, L; Yu, Z; Zhang, L; Zhang, Y; Zhong, M; Zhou, Z1
Edwards, JG; Eisenberg, CA; Eisenberg, LM; Kaur, K; Yang, J1
Chen, WL; Guo, XK; Li, DD; Sun, HP; Wang, ZH; You, QD1
Cho, DH; Hwang, JJ; Jeong, SY; Kim, CS; Koh, JY; Park, SE; Park, YY; Suh, N; Yi, HJ1
Razali, NB; Sajikumar, S; Sharma, M1
Bataba, E; Huang, K; Kondengaden, SM; Li, KK; Luo, C; Luo, LF; Wang, B; Wang, PG; Wang, R; Zang, L; Zhu, M1
Ahmad, F; Dixit, D; Joshi, SD; Sen, E1
Huang, R; Huang, Y; Jiang, X; Li, M; Yang, X; Yao, J; Yu, M; Zheng, F1
Bao, S; Feng, SW; Guo, X; Lei, L; Liu, Y; Shen, R; Shen, X; Wang, F; Wang, N; Wang, W; Wang, X; Wang, Y; Wu, H; Xu, S1
Guo, AS; Huang, YQ; Lin, RS; Ma, XD1
Ciechomska, IA; Jackl, J; Kaminska, B; Przanowski, P; Wojtas, B1
Barat, C; Dental, C; Ouellet, M; Proust, A; Tremblay, MJ1
Cao, Z; Ding, B; Ding, J; Hong, R; Huang, W; Li, H; Li, Y; Zhang, Y; Zuo, X1
Doi, S; Irifuku, T; Maeda, K; Masaki, T; Nagai, T; Nakashima, A; Ueno, T1
Gu, JK; Hao, M; Jiang, HD; Jim Wang, ZJ; Ju, HX; Li, L; Xu, MC; Yang, ZZ; Yu, LS; Zeng, S1
Aoyama, K; Chiba, T; Inoue, M; Iwama, A; Koide, S; Kusakabe, Y; Mimura, N; Miyagi, S; Miyazaki, M; Noguchi, Y; Ogasawara, S; Ooka, Y; Oshima, M; Otsuka, M; Saito, T; Saraya, A; Suzuki, E; Tara, S; Tawada, A; Wakamatsu, T; Yokosuka, O; Yokoyama, M; Yuki, K; Zen, Y1
Dierkes, T; Sajikumar, S; Sharma, M1
Diao, HL; Liao, HQ; Ma, N; Tian, L; Yang, H; Zhang, CJ1
Huang, X; Huang, Y; Lin, L; Ma, X; Zou, Y1
Balcerczyk, A; Macierzyńska-Piotrowska, E; Pirola, L; Rybaczek, D; Wojtala, M1
Abdullah, LN; Chow, EK; Ho, JC; Jha, S; Kato, H; Lee, KL; Pang, QY; Poellinger, L; Ueda, J; Yang, H1
Deng, J; Hou, Z; Lai, D; Liang, H; Liu, D; Wang, Q; Wang, X1
Koh, KARP; Tan, KSW; Yason, JA1
Heo, SH; Hong, M; Kim, I; Kim, SY; Kwon, TK; Lee, S; Oh, Y; Park, S; Sung, YH; Yi, GS1
Alsalim, H; Jafarpour, F; Nasr-Esfahani, MH; Niasari-Naslaji, A; Tanhaei Vash, N1
Baksiene, S; Borutinskaite, V; Navakauskiene, R; Vitkeviciene, A1
Chae, YC; Kim, JY; Kim, KB; Lee, KH; Oh, H; Park, JW; Seo, SB1
Chatterjee, M; Dworak, N; Jividen, K; Johnson, IG; Kelley, JB; Makosa, D; Paschal, BM; Simke, WC; Snow, C; Yang, CS1
Fang, Q; Hill, K; Lai, R; Long, H; Pan, S; Sha, SH; Wang, X; Xiong, H; Zheng, Y; Zhu, Y1
Chase, KA; Feiner, B; Hu, E; Ramaker, MJ; Rosen, C; Sharma, RP1
Kim, I; Kim, SY; Namgung, Y1
Cui, Y; Dai, M; Hu, Y; Kong, W; Wang, X; Wu, H; Wu, J; Yu, B; Yu, X; Zhang, H; Zheng, Y1
Farrukh, A; Kiesow, MJ; Llinás, M; Ngwa, CJ; Orchard, LM; Pradel, G1
Cui, H; Dong, Z; Hou, J; Ke, X; Wang, F; Yang, L; Yin, C; Zhang, K; Zhang, R; Zhong, X1
Barmada, SJ; Flores, BN; Green, KM; Ivanova, MI; Kearse, MG; Sheth, UJ; Sutter, AB; Todd, PK; Wright, SE1
Charles, MRC; Coumar, MS; Dhayalan, A; Hsieh, HP; Lin, SY; Mahesh, A1
Chen, TQ; Chen, YJ; Guo, X; Hu, N; Huo, B; Jiang, DS; Masau, JF; Wei, X; Yi, X; Zhong, XX; Zhu, XH1
Deng, BB; Jiao, BP; Li, YR; Liu, YJ; Wang, GJ1
Hwang, S; Kim, I; Kim, K; Kim, S; Park, S; Yeom, J1
Bao, X; Deng, A; Li, Q; Wang, L; Wang, M; Xiang, Y; Yu, W; Zhang, B; Zhang, Y1
Nagaraja, SS; Nagarajan, D; Subramanian, U1
Bao, X; Chen, C; Deng, A; Deng, P; He, M; Ji, D; Li, Q; Liang, X; Lu, Y; Pi, H; Tan, G; Wang, L; Yu, Z; Zhang, L; Zhou, Z1
Sun, J; Wu, JC; Xu, JC; Zhang, YF; Zhou, ZY1
Guillou, JL; Lassalle, J; Mons, N; Nicolay-Kritter, K1
Beizer, A; Belitsky, G; Bugaeva, P; Fedorov, D; Katz, R; Kirsanov, K; Lesovaya, E; Lizogub, O; Maksimova, V; Shalginskikh, N; Usalka, O; Vlasova, O; Yakubovskaya, M1
Gu, X; Li, B; Li, H; Li, M; Sun, X; Xu, P; Zhu, Y; Zuo, Q1
Chang, EJ; Hwang, S; Im, SS; Kim, J; Kim, JH; Lee, JH; Rho, JK; Shin, DM; Son, J1
Han, Y; Hua, Z; Jiang, Y; Liu, S; Nie, S; Shu, X; Wang, X; Xu, G; Xu, S; Yang, H; Zhou, C1

Reviews

2 review(s) available for quinazolines and bix 01294

ArticleYear
Epigenetic regulation of HIV-1 transcription.
    Epigenomics, 2011, Volume: 3, Issue:4

    Topics: Azepines; DNA Methylation; Epigenesis, Genetic; Gene Expression Regulation, Viral; Histone Acetyltransferases; Histone Deacetylase Inhibitors; Histone Deacetylases; Histone-Lysine N-Methyltransferase; Histones; HIV Infections; HIV-1; Humans; Nucleosomes; Phorbol Esters; Piperazines; Quinazolines; tat Gene Products, Human Immunodeficiency Virus; Transcription, Genetic; Virus Integration

2011
G9a - An Appealing Antineoplastic Target.
    Current cancer drug targets, 2017, Volume: 17, Issue:6

    Topics: Adenosine; Animals; Antineoplastic Agents; Azepines; Benzimidazoles; DNA Methylation; Enzyme Inhibitors; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Molecular Targeted Therapy; Quinazolines

2017

Trials

1 trial(s) available for quinazolines and bix 01294

ArticleYear
Examining the effects of the histone methyltransferase inhibitor BIX-01294 on histone modifications and gene expression in both a clinical population and mouse models.
    PloS one, 2019, Volume: 14, Issue:6

    Topics: Animals; Azepines; Brain-Derived Neurotrophic Factor; Cerebral Cortex; Enzyme Inhibitors; Female; Gene Expression Regulation; Histone Code; Histone Methyltransferases; Histones; Humans; Kruppel-Like Factor 4; Leukocytes, Mononuclear; Male; Mice; Mutation; Quinazolines; Reelin Protein; RNA, Messenger; Schizophrenia

2019

Other Studies

94 other study(ies) available for quinazolines and bix 01294

ArticleYear
Reversal of H3K9me2 by a small-molecule inhibitor for the G9a histone methyltransferase.
    Molecular cell, 2007, Feb-09, Volume: 25, Issue:3

    Topics: Animals; Azepines; Cell Line; Enzyme Inhibitors; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Histones; Humans; Lysine; Methylation; Mice; Promoter Regions, Genetic; Protein Methyltransferases; Quinazolines

2007
Induction of pluripotent stem cells from mouse embryonic fibroblasts by Oct4 and Klf4 with small-molecule compounds.
    Cell stem cell, 2008, Nov-06, Volume: 3, Issue:5

    Topics: 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester; Animals; Azepines; Cell Culture Techniques; Cell Differentiation; Cells, Cultured; Embryo, Mammalian; Fibroblasts; Gene Expression Profiling; Gene Expression Regulation, Developmental; Kruppel-Like Factor 4; Kruppel-Like Transcription Factors; Mice; Microarray Analysis; Octamer Transcription Factor-3; Pluripotent Stem Cells; Quinazolines; Small Molecule Libraries; Transcriptional Activation

2008
Structural basis for G9a-like protein lysine methyltransferase inhibition by BIX-01294.
    Nature structural & molecular biology, 2009, Volume: 16, Issue:3

    Topics: Azepines; Binding Sites; Crystallography, X-Ray; Enzyme Inhibitors; Histone-Lysine N-Methyltransferase; Models, Molecular; Protein Conformation; Protein Structure, Tertiary; Quinazolines; S-Adenosylhomocysteine

2009
Chromatin flow cytometry identifies changes in epigenetic cell states.
    Cells, tissues, organs, 2010, Volume: 191, Issue:3

    Topics: Acetylation; Animals; Azepines; Cell Differentiation; Cells, Cultured; Chromatin; Embryonic Stem Cells; Epigenesis, Genetic; Flow Cytometry; Histone Deacetylase Inhibitors; Histone-Lysine N-Methyltransferase; Histones; Hydroxamic Acids; Methylation; Mice; Quinazolines

2010
Involvement of histone H3 lysine 9 (H3K9) methyltransferase G9a in the maintenance of HIV-1 latency and its reactivation by BIX01294.
    The Journal of biological chemistry, 2010, May-28, Volume: 285, Issue:22

    Topics: Antigens, Viral; Azepines; Cell Line; Chromatin Immunoprecipitation; Gene Expression Regulation, Viral; HeLa Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; HIV Long Terminal Repeat; HIV-1; Humans; Protein Structure, Tertiary; Quinazolines; RNA Interference; T-Lymphocytes; Virus Replication

2010
Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferases.
    Journal of molecular biology, 2010, Jul-02, Volume: 400, Issue:1

    Topics: Azepines; Histone Code; Histone-Lysine N-Methyltransferase; Lysine; Models, Molecular; Molecular Sequence Data; Molecular Structure; Protein Processing, Post-Translational; Quinazolines

2010
A chemiluminescence-based method for identification of histone lysine methyltransferase inhibitors.
    Molecular bioSystems, 2010, Volume: 6, Issue:5

    Topics: Azepines; Enzyme Inhibitors; Histone-Lysine N-Methyltransferase; Histones; Humans; Luminescent Measurements; Methylation; Models, Theoretical; Quinazolines

2010
Chemical probes: sharpen your epigenetic tools.
    Nature chemical biology, 2011, Jul-18, Volume: 7, Issue:8

    Topics: Autoantigens; Azepines; Drug Delivery Systems; Enzyme Inhibitors; Epigenesis, Genetic; Golgi Matrix Proteins; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Molecular Structure; Proteins; Quinazolines; Signal Transduction; Structure-Activity Relationship

2011
Enhanced expression of EHMT2 is involved in the proliferation of cancer cells through negative regulation of SIAH1.
    Neoplasia (New York, N.Y.), 2011, Volume: 13, Issue:8

    Topics: Apoptosis; Azepines; Cell Line, Transformed; Cell Line, Tumor; Cell Proliferation; Gene Expression Regulation, Neoplastic; HEK293 Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Neoplasms; Nuclear Proteins; Quinazolines; Ubiquitin-Protein Ligases

2011
The effect of epigenetic factors on differentiation of pancreatic progenitor cells into insulin-producing cells.
    Transplantation proceedings, 2011, Volume: 43, Issue:9

    Topics: Azacitidine; Azepines; C-Peptide; Cell Culture Techniques; Cell Differentiation; Decitabine; Epigenesis, Genetic; Humans; Hydroxamic Acids; Immunohistochemistry; Insulin-Secreting Cells; Islets of Langerhans; Keratin-19; Models, Biological; Models, Genetic; Pancreas; Pyrroles; Quinazolines; Stem Cells; Transcription Factors

2011
An analog of BIX-01294 selectively inhibits a family of histone H3 lysine 9 Jumonji demethylases.
    Journal of molecular biology, 2012, Feb-24, Volume: 416, Issue:3

    Topics: Animals; Azepines; Cells, Cultured; Crystallography, X-Ray; Enzyme Inhibitors; Fibroblasts; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Histones; Humans; Jumonji Domain-Containing Histone Demethylases; Mice; Protein Structure, Tertiary; Quinazolines

2012
Inhibition of histone H3K9 methyltransferases by gliotoxin and related epipolythiodioxopiperazines.
    The Journal of antibiotics, 2012, Volume: 65, Issue:5

    Topics: Azepines; Crystallization; Disulfides; Drug Design; Enzyme Inhibitors; Gliotoxin; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Indole Alkaloids; Methylation; Piperazines; Quinazolines

2012
Detecting S-adenosyl-L-methionine-induced conformational change of a histone methyltransferase using a homogeneous time-resolved fluorescence-based binding assay.
    Analytical biochemistry, 2012, Apr-01, Volume: 423, Issue:1

    Topics: Adenosine; Azepines; Catalytic Domain; Chromatography, High Pressure Liquid; Fluorescent Dyes; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Humans; Kinetics; Protein Binding; Quinazolines; Recombinant Proteins; S-Adenosylhomocysteine; Tandem Mass Spectrometry; Time Factors

2012
G9a/GLP histone lysine dimethyltransferase complex activity in the hippocampus and the entorhinal cortex is required for gene activation and silencing during memory consolidation.
    The Journal of neuroscience : the official journal of the Society for Neuroscience, 2012, Apr-18, Volume: 32, Issue:16

    Topics: Analysis of Variance; Animals; Azepines; Brain-Derived Neurotrophic Factor; Chromatin Immunoprecipitation; Conditioning, Psychological; Cues; DNA (Cytosine-5-)-Methyltransferases; DNA Methyltransferase 3A; Electric Stimulation; Entorhinal Cortex; Enzyme Inhibitors; Excitatory Postsynaptic Potentials; Fear; Gene Silencing; Hippocampus; Histone-Lysine N-Methyltransferase; Histones; In Vitro Techniques; Long-Term Potentiation; Male; Memory; Methylation; Patch-Clamp Techniques; Polymers; Proto-Oncogene Proteins c-fyn; Quinazolines; Rats; Rats, Sprague-Dawley; Transcriptional Activation

2012
Histone methyltransferase inhibitors induce HIV-1 recovery in resting CD4(+) T cells from HIV-1-infected HAART-treated patients.
    AIDS (London, England), 2012, Jul-31, Volume: 26, Issue:12

    Topics: Antiretroviral Therapy, Highly Active; Azepines; CD4-Positive T-Lymphocytes; Disease Reservoirs; Histocompatibility Antigens; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; HIV Infections; HIV-1; Humans; Leukocytes, Mononuclear; Methyltransferases; Piperazines; Quinazolines; Repressor Proteins; Virus Latency

2012
BIX-01294 treatment blocks cell proliferation, migration and contractility in ovine foetal pulmonary arterial smooth muscle cells.
    Cell proliferation, 2012, Volume: 45, Issue:4

    Topics: Animals; Azepines; Base Sequence; Blotting, Western; Cell Movement; Cell Proliferation; Chromatography, Liquid; DNA Methylation; DNA Primers; Mass Spectrometry; Muscle, Smooth, Vascular; Platelet-Derived Growth Factor; Pulmonary Artery; Quinazolines; Real-Time Polymerase Chain Reaction; Sheep

2012
IVMBIX-01294, an inhibitor of the histone methyltransferase EHMT2, disrupts histone H3 lysine 9 (H3K9) dimethylation in the cleavage-stage porcine embryo.
    Reproduction, fertility, and development, 2012, Volume: 24, Issue:6

    Topics: Animals; Azepines; Cleavage Stage, Ovum; Dose-Response Relationship, Drug; Embryo Culture Techniques; Embryo Transfer; Embryo, Mammalian; Embryonic Development; Enzyme Inhibitors; Female; Fertilization in Vitro; Gene Expression Regulation, Developmental; Histone-Lysine N-Methyltransferase; Histones; Lysine; Methylation; Pregnancy; Pregnancy Rate; Quinazolines; RNA, Messenger; Swine; Time Factors; Transcription, Genetic

2012
The histone methyltransferase inhibitor BIX01294 enhances the cardiac potential of bone marrow cells.
    Stem cells and development, 2013, Feb-15, Volume: 22, Issue:4

    Topics: Animals; Antigens, Differentiation; Azepines; Bone Marrow Cells; Gene Expression Regulation; Histone-Lysine N-Methyltransferase; Mice; Muscle Proteins; Myocardium; Myocytes, Cardiac; Quinazolines

2013
Small-molecule histone methyltransferase inhibitors display rapid antimalarial activity against all blood stage forms in Plasmodium falciparum.
    Proceedings of the National Academy of Sciences of the United States of America, 2012, Oct-09, Volume: 109, Issue:41

    Topics: Amino Acid Sequence; Animals; Antimalarials; Azepines; Blotting, Western; Cells, Cultured; Dose-Response Relationship, Drug; Erythrocytes; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Histones; Humans; Life Cycle Stages; Lysine; Malaria; Methylation; Mice; Mice, Inbred C57BL; Molecular Sequence Data; Parasitemia; Plasmodium berghei; Plasmodium falciparum; Quinazolines; Sequence Homology, Amino Acid

2012
Abnormal histone H3K9 dimethylation but normal dimethyltransferase EHMT2 expression in cloned sheep embryos.
    Theriogenology, 2012, Volume: 78, Issue:9

    Topics: Animals; Azepines; Cloning, Organism; Gene Expression Regulation, Developmental; Gene Expression Regulation, Enzymologic; Histone-Lysine N-Methyltransferase; Nuclear Transfer Techniques; Quinazolines; Sheep

2012
Endothelial differentiation of adipose-derived mesenchymal stem cells is improved by epigenetic modifying drug BIX-01294.
    European journal of cell biology, 2013, Volume: 92, Issue:2

    Topics: Azepines; Biomarkers; Blotting, Western; Cell Differentiation; Cells, Cultured; Culture Media; DNA Methylation; Endothelial Cells; Epigenesis, Genetic; Homeodomain Proteins; Humans; Immunohistochemistry; Kruppel-Like Factor 4; Kruppel-Like Transcription Factors; Mesenchymal Stem Cells; Nanog Homeobox Protein; Octamer Transcription Factor-3; Quinazolines; Real-Time Polymerase Chain Reaction; RNA, Messenger; Subcutaneous Fat; Time Factors; Vascular Cell Adhesion Molecule-1; Vascular Endothelial Growth Factor Receptor-2

2013
Vitamin C promotes maturation of T-cells.
    Antioxidants & redox signaling, 2013, Dec-10, Volume: 19, Issue:17

    Topics: Animals; Ascorbic Acid; Azepines; Cells, Cultured; Culture Media; Epigenesis, Genetic; Gene Expression; Gene Rearrangement, T-Lymphocyte; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Histones; Immunologic Factors; Methylation; Mice; Mice, Inbred C57BL; Phthalimides; Protein Processing, Post-Translational; Quinazolines; Receptors, Antigen, T-Cell; T-Lymphocytes; Tryptophan

2013
Inhibition of H3K9 methyltransferases G9a/GLP prevents ototoxicity and ongoing hair cell death.
    Cell death & disease, 2013, Feb-21, Volume: 4

    Topics: Animals; Anti-Bacterial Agents; Apoptosis; Azepines; Cells, Cultured; Cochlea; Hair Cells, Auditory; Histone-Lysine N-Methyltransferase; Histones; Methylation; Mice; Mice, Inbred C57BL; Models, Animal; Neomycin; Organ of Corti; Quinazolines

2013
Histone-lysine methyltransferase EHMT2 is involved in proliferation, apoptosis, cell invasion, and DNA methylation of human neuroblastoma cells.
    Anti-cancer drugs, 2013, Volume: 24, Issue:5

    Topics: Apoptosis; Azepines; Caspase 3; Caspase 8; Cell Line, Tumor; Cell Movement; Cell Proliferation; Cyclin D1; DNA Methylation; Doxorubicin; Enzyme Inhibitors; Epigenesis, Genetic; Gene Expression Regulation, Neoplastic; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; N-Myc Proto-Oncogene Protein; Neuroblastoma; Nuclear Proteins; Oncogene Proteins; Quinazolines

2013
Intragenic epigenetic changes modulate NCAM alternative splicing in neuronal differentiation.
    The EMBO journal, 2013, Aug-14, Volume: 32, Issue:16

    Topics: Alternative Splicing; Animals; Azacitidine; Azepines; Cell Differentiation; Cell Line, Tumor; Chromatin; Chromatin Immunoprecipitation; DNA Methylation; DNA Primers; Epigenesis, Genetic; Exons; Mice; Neural Cell Adhesion Molecules; Neurons; Quinazolines; Real-Time Polymerase Chain Reaction; Reverse Transcriptase Polymerase Chain Reaction; RNA, Small Interfering; Sequence Analysis, DNA

2013
Latrunculin A treatment prevents abnormal chromosome segregation for successful development of cloned embryos.
    PloS one, 2013, Volume: 8, Issue:10

    Topics: Actins; Animals; Azepines; Bridged Bicyclo Compounds, Heterocyclic; Chromosome Segregation; Cloning, Organism; Embryo, Mammalian; Embryonic Development; Epigenesis, Genetic; Female; Fertilization in Vitro; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Histones; Lysine; Methylation; Mice; Mice, Inbred C57BL; Mice, Inbred DBA; Nuclear Transfer Techniques; Oocytes; Quinazolines; Thiazolidines

2013
BIX01294 suppresses osteoclast differentiation on mouse macrophage-like Raw264.7 cells.
    Bosnian journal of basic medical sciences, 2013, Volume: 13, Issue:4

    Topics: Animals; Azepines; Cell Differentiation; Cell Line; Enzyme Inhibitors; Histone-Lysine N-Methyltransferase; Histones; Macrophages; Methylation; Mice; NFATC Transcription Factors; Osteoclasts; Quinazolines; RANK Ligand

2013
The histone H3 methyltransferase G9A epigenetically activates the serine-glycine synthesis pathway to sustain cancer cell survival and proliferation.
    Cell metabolism, 2013, Dec-03, Volume: 18, Issue:6

    Topics: Animals; Autophagy; Azepines; Bone Neoplasms; Cell Line, Tumor; Cell Proliferation; Cell Survival; Epigenomics; Glycine; HeLa Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Methylation; Mice; Microtubule-Associated Proteins; Quinazolines; Ribosomes; Serine; Transcription, Genetic

2013
BIX-01294 induces autophagy-associated cell death via EHMT2/G9a dysfunction and intracellular reactive oxygen species production.
    Autophagy, 2013, Volume: 9, Issue:12

    Topics: Animals; Autophagy; Azepines; Breast Neoplasms; Cells, Cultured; Colon; Enzyme Inhibitors; Female; HCT116 Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; MCF-7 Cells; Mice; Primary Cell Culture; Quinazolines; Reactive Oxygen Species; Signal Transduction

2013
Properly substituted analogues of BIX-01294 lose inhibition of G9a histone methyltransferase and gain selective anti-DNA methyltransferase 3A activity.
    PloS one, 2014, Volume: 9, Issue:5

    Topics: Azepines; Catalytic Domain; Cell Line, Tumor; Cell Proliferation; Cell Survival; DNA (Cytosine-5-)-Methyltransferases; DNA Methyltransferase 3A; Enzyme Inhibitors; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Molecular Docking Simulation; Quinazolines; Structure-Activity Relationship

2014
Euchromatic histone methyltransferase 2 inhibitor, BIX-01294, sensitizes human promyelocytic leukemia HL-60 and NB4 cells to growth inhibition and differentiation.
    Leukemia research, 2014, Volume: 38, Issue:7

    Topics: Azepines; Cell Differentiation; Cell Proliferation; Cell Survival; Dose-Response Relationship, Drug; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; HL-60 Cells; Humans; Leukemia, Promyelocytic, Acute; Quinazolines; Tretinoin

2014
Histone methyltransferase G9a and H3K9 dimethylation inhibit the self-renewal of glioma cancer stem cells.
    Molecular and cellular biochemistry, 2014, Volume: 394, Issue:1-2

    Topics: AC133 Antigen; Antigens, CD; Azepines; Brain Neoplasms; Cell Line, Tumor; Cell Proliferation; Enzyme Inhibitors; Gene Expression Regulation, Neoplastic; Glioma; Glycoproteins; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Lysine; Methylation; Neoplastic Stem Cells; Peptides; Promoter Regions, Genetic; Quinazolines; Signal Transduction; SOXB1 Transcription Factors; Transfection

2014
The effects of selected inhibitors of histone modifying enzyme on C6 glioma cells.
    Pharmacological reports : PR, 2014, Volume: 66, Issue:1

    Topics: Acetylation; Adenosine; Animals; Azepines; Brain Neoplasms; Cell Line, Tumor; Cell Survival; Enzyme Inhibitors; Epigenesis, Genetic; Glioma; Histones; Hydroxamic Acids; Piperazines; Quinazolines; Rats; Valproic Acid

2014
Pre-administration of G9a/GLP inhibitor during synaptogenesis prevents postnatal ethanol-induced LTP deficits and neurobehavioral abnormalities in adult mice.
    Experimental neurology, 2014, Volume: 261

    Topics: Animals; Animals, Newborn; Azepines; Central Nervous System Depressants; Drug Administration Schedule; Electric Stimulation; Enzyme Inhibitors; Ethanol; Gene Expression Regulation, Developmental; Histone-Lysine N-Methyltransferase; In Vitro Techniques; Long-Term Potentiation; Male; Maze Learning; Memory Disorders; Mice; Mice, Inbred C57BL; Neurogenesis; Quinazolines; Recognition, Psychology; Social Behavior

2014
Inhibition of euchromatic histone methyltransferase 1 and 2 sensitizes chronic myeloid leukemia cells to interferon treatment.
    PloS one, 2014, Volume: 9, Issue:7

    Topics: Antineoplastic Agents; Apoptosis; Azepines; Benzamides; Cell Proliferation; Drug Synergism; Gene Expression; HeLa Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Imatinib Mesylate; Interferon Type I; K562 Cells; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Piperazines; Pyrimidines; Quinazolines

2014
Histone methyltransferase inhibitors are orally bioavailable, fast-acting molecules with activity against different species causing malaria in humans.
    Antimicrobial agents and chemotherapy, 2015, Volume: 59, Issue:2

    Topics: Animals; Antimalarials; Azepines; Female; Hep G2 Cells; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Humans; Malaria; Malaria, Falciparum; Mice; Mice, SCID; Plasmodium berghei; Plasmodium falciparum; Quinazolines

2015
The selective activation of p53 target genes regulated by SMYD2 in BIX-01294 induced autophagy-related cell death.
    PloS one, 2015, Volume: 10, Issue:1

    Topics: Apoptosis; Autophagy; Autophagy-Related Proteins; Azepines; Cell Line, Tumor; Cyclin-Dependent Kinase Inhibitor p21; Cysteine Endopeptidases; HCT116 Cells; Histone-Lysine N-Methyltransferase; Histones; Humans; Membrane Proteins; Methylation; Microtubule-Associated Proteins; Quinazolines; RNA Interference; RNA, Small Interfering; Sirolimus; Transcriptome; Tumor Suppressor Protein p53; Vesicular Transport Proteins

2015
Inhibition of H3K9 methyltransferase G9a induces autophagy and apoptosis in oral squamous cell carcinoma.
    Biochemical and biophysical research communications, 2015, Mar-27, Volume: 459, Issue:1

    Topics: Animals; Apoptosis; Autophagy; Azepines; Carcinoma, Squamous Cell; Cell Line, Tumor; Cell Proliferation; Enzyme Inhibitors; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Mice, SCID; Mouth Neoplasms; Quinazolines; Xenograft Model Antitumor Assays

2015
BIX-01294-induced autophagy regulates elongation of primary cilia.
    Biochemical and biophysical research communications, 2015, May-01, Volume: 460, Issue:2

    Topics: Autophagy; Azepines; Cell Line, Transformed; Cilia; Histone-Lysine N-Methyltransferase; Humans; Quinazolines; Retinal Pigment Epithelium

2015
A role for KMT1c in monocyte to dendritic cell differentiation: Epigenetic regulation of monocyte differentiation.
    Human immunology, 2015, Volume: 76, Issue:6

    Topics: Acetylation; Adenosine; Azepines; Cell Adhesion Molecules; Cell Differentiation; Chromatin; Chromatin Assembly and Disassembly; Dendritic Cells; Epigenesis, Genetic; Gene Expression Profiling; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Lectins, C-Type; Methylation; Monocytes; Primary Cell Culture; Quinazolines; Receptors, Cell Surface; Signal Transduction; Transcription, Genetic

2015
A Unique Virulence Gene Occupies a Principal Position in Immune Evasion by the Malaria Parasite Plasmodium falciparum.
    PLoS genetics, 2015, Volume: 11, Issue:5

    Topics: Antigenic Variation; Antigens, Protozoan; Azepines; Chloroquine; Gene Expression Regulation; Genetic Loci; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Humans; Hydroxamic Acids; Immune Evasion; Inhibitory Concentration 50; Malaria, Falciparum; Models, Theoretical; Piperazines; Plasmodium falciparum; Promoter Regions, Genetic; Protozoan Proteins; Quinazolines; RNA Polymerase II; Terpenes; Transcriptional Activation; Transcriptome

2015
The Histone Methyltransferase Inhibitor BIX01294 Inhibits HIF-1α Stability and Angiogenesis.
    Molecules and cells, 2015, Volume: 38, Issue:6

    Topics: Animals; Azepines; Carcinoma, Hepatocellular; Chick Embryo; Enzyme Inhibitors; Hep G2 Cells; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Humans; Hypoxia-Inducible Factor 1, alpha Subunit; Liver Neoplasms; Mice; Neovascularization, Pathologic; Quinazolines; Signal Transduction

2015
Effect of BIX-01294 on H3K9me2 levels and the imprinted gene Snrpn in mouse embryonic fibroblast cells.
    Bioscience reports, 2015, Aug-18, Volume: 35, Issue:5

    Topics: Animals; Azepines; Cells, Cultured; DNA Methylation; Fibroblasts; Gene Expression Regulation, Developmental; Genomic Imprinting; Histone-Lysine N-Methyltransferase; Histones; Mice; Quinazolines; Ribonucleoproteins, Small Nuclear

2015
Inhibition of H3K9 histone methyltransferase G9a attenuates renal fibrosis and retains klotho expression.
    Kidney international, 2016, Volume: 89, Issue:1

    Topics: Actins; Animals; Antibodies, Neutralizing; Azepines; Cell Line; Enzyme Inhibitors; Fibroblasts; Fibronectins; Fibrosis; Glomerulonephritis, IGA; Glucuronidase; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Kidney; Klotho Proteins; Lysine; Male; Methylation; Mice; Quinazolines; Rats; RNA, Messenger; RNA, Small Interfering; Transforming Growth Factor beta1; Ureteral Obstruction

2016
BIX-01294 increases pig cloning efficiency by improving epigenetic reprogramming of somatic cell nuclei.
    Reproduction (Cambridge, England), 2016, Volume: 151, Issue:1

    Topics: Animals; Azepines; Blastocyst; Cellular Reprogramming; Cloning, Organism; Embryo Culture Techniques; Embryo Transfer; Embryonic Development; Epigenesis, Genetic; Female; Gene Expression; Histone-Lysine N-Methyltransferase; Histones; Homeodomain Proteins; Nuclear Transfer Techniques; Octamer Transcription Factor-3; Pluripotent Stem Cells; Quinazolines; RNA, Messenger; SOXB1 Transcription Factors; Sus scrofa

2016
The Dynamics and Regulatory Mechanism of Pronuclear H3k9me2 Asymmetry in Mouse Zygotes.
    Scientific reports, 2015, Dec-07, Volume: 5

    Topics: Animals; Azepines; Cell Nucleus; Fertilization in Vitro; Histone-Lysine N-Methyltransferase; Histones; Kruppel-Like Transcription Factors; Lysine; Methylation; Mice; Microinjections; Models, Biological; Nerve Tissue Proteins; Quinazolines; RNA, Small Interfering; Zygote

2015
G9a inhibition promotes neuronal differentiation of human bone marrow mesenchymal stem cells through the transcriptional induction of RE-1 containing neuronal specific genes.
    Neurochemistry international, 2016, Volume: 96

    Topics: Azepines; Bone Marrow Cells; Cell Differentiation; Cells, Cultured; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Mesenchymal Stem Cells; Neurons; Quinazolines; Repressor Proteins; Transcription, Genetic

2016
Alternative Splicing of G9a Regulates Neuronal Differentiation.
    Cell reports, 2016, 03-29, Volume: 14, Issue:12

    Topics: Alternative Splicing; Animals; Azepines; Brain; Cell Differentiation; Cell Line; Cell Nucleus; Exons; Fluorescence Resonance Energy Transfer; Genes, Reporter; HeLa Cells; Histone-Lysine N-Methyltransferase; Histones; Humans; Methylation; Mice; Mice, Inbred C57BL; Microscopy, Fluorescence; Neurons; Protein Isoforms; Quinazolines; Real-Time Polymerase Chain Reaction; RNA Interference; RNA Precursors; RNA, Small Interfering; Tretinoin

2016
G9a-mediated histone methylation regulates cadmium-induced male fertility damage in pubertal mice.
    Toxicology letters, 2016, Jun-11, Volume: 252

    Topics: Age Factors; Animals; Apoptosis; Apoptosis Regulatory Proteins; Azepines; Blotting, Western; Cadmium Chloride; Dose-Response Relationship, Drug; Enzyme Inhibitors; Female; Fertility; Fluorescent Antibody Technique; Histone-Lysine N-Methyltransferase; Histones; In Situ Nick-End Labeling; Infertility, Male; Litter Size; Male; Methylation; Mice, Inbred C57BL; Quinazolines; Sexual Development; Sperm Count; Testis; Time Factors

2016
G9a histone methyltransferase inhibitor BIX01294 promotes expansion of adult cardiac progenitor cells without changing their phenotype or differentiation potential.
    Cell proliferation, 2016, Volume: 49, Issue:3

    Topics: Adult Stem Cells; Animals; Azepines; Cell Differentiation; Cell Proliferation; Coculture Techniques; Enzyme Inhibitors; Histone-Lysine N-Methyltransferase; Mice; Mice, Inbred C57BL; Myocytes, Cardiac; Quinazolines; Rats, Wistar

2016
Inhibition of EHMT2/G9a epigenetically increases the transcription of Beclin-1 via an increase in ROS and activation of NF-κB.
    Oncotarget, 2016, Jun-28, Volume: 7, Issue:26

    Topics: Azepines; Beclin-1; Breast Neoplasms; Epigenesis, Genetic; Female; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; MCF-7 Cells; Microtubule-Associated Proteins; NF-kappa B; Prognosis; Promoter Regions, Genetic; Quinazolines; Reactive Oxygen Species; RNA Interference; Transcription, Genetic

2016
Inhibition of G9a/GLP Complex Promotes Long-Term Potentiation and Synaptic Tagging/Capture in Hippocampal CA1 Pyramidal Neurons.
    Cerebral cortex (New York, N.Y. : 1991), 2017, 06-01, Volume: 27, Issue:6

    Topics: Animals; Azepines; Brain-Derived Neurotrophic Factor; CA1 Region, Hippocampal; Chromatin Immunoprecipitation; Electric Stimulation; Enzyme Inhibitors; Histone-Lysine N-Methyltransferase; In Vitro Techniques; Long-Term Potentiation; Male; Models, Biological; Pyramidal Cells; Quinazolines; Rats; Rats, Wistar; Synapses

2017
Discovery of novel small molecule inhibitors of lysine methyltransferase G9a and their mechanism in leukemia cell lines.
    European journal of medicinal chemistry, 2016, Oct-21, Volume: 122

    Topics: Animals; Apoptosis; Azepines; Binding, Competitive; Cell Cycle; Cell Proliferation; Drug Discovery; Histone-Lysine N-Methyltransferase; Humans; K562 Cells; Mice; Molecular Docking Simulation; Protein Conformation; Quinazolines; Small Molecule Libraries

2016
G9a inhibition induced PKM2 regulates autophagic responses.
    The international journal of biochemistry & cell biology, 2016, Volume: 78

    Topics: Adaptor Proteins, Signal Transducing; Autophagy; Azepines; Carrier Proteins; Cell Line, Tumor; Cell Proliferation; Cell Transformation, Neoplastic; Enzyme Inhibitors; Epigenesis, Genetic; Gene Expression Regulation, Neoplastic; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Hypoxia-Inducible Factor 1, alpha Subunit; Membrane Proteins; Microtubule-Associated Proteins; Phosphoproteins; Quinazolines; Thyroid Hormone-Binding Proteins; Thyroid Hormones; Transcription Factors; Tumor Protein p73; YAP-Signaling Proteins

2016
Beneficial effects of diazepin-quinazolin-amine derivative (BIX-01294) on preimplantation development and molecular characteristics of cloned mouse embryos.
    Reproduction, fertility, and development, 2017, Volume: 29, Issue:6

    Topics: Animals; Azepines; Blastocyst; Cloning, Organism; CpG Islands; DNA Methylation; Ectogenesis; Embryo, Mammalian; Enzyme Inhibitors; Epigenesis, Genetic; Female; Gene Expression Regulation, Developmental; GRB10 Adaptor Protein; Histone-Lysine N-Methyltransferase; Histones; Lysine; Male; Methylation; Mice; Nuclear Transfer Techniques; Parthenogenesis; Protein Processing, Post-Translational; Quinazolines

2017
Dopaminergic inhibition by G9a/Glp complex on tyrosine hydroxylase in nerve injury-induced hypersensitivity.
    Molecular pain, 2016, Volume: 12

    Topics: Animals; Azepines; Brain; Chromatography, High Pressure Liquid; CpG Islands; Disease Models, Animal; DNA Methylation; Dopamine; Down-Regulation; Histone-Lysine N-Methyltransferase; Hypersensitivity; Male; Mice; Mice, Inbred C57BL; Pain Measurement; Pain Threshold; Quinazolines; Sciatic Neuropathy; Signal Transduction; Tyrosine 3-Monooxygenase

2016
Mechanism of G9a inhibitor BIX‑01294 acting on U251 glioma cells.
    Molecular medicine reports, 2016, Volume: 14, Issue:5

    Topics: Adult; Apoptosis; Azepines; Cell Line, Tumor; Cell Proliferation; DNA Methylation; Female; Gene Expression Regulation, Neoplastic; Glioma; Histocompatibility Antigens; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Humans; Male; Middle Aged; Neoplasm Proteins; Quinazolines

2016
BIX01294, an inhibitor of histone methyltransferase, induces autophagy-dependent differentiation of glioma stem-like cells.
    Scientific reports, 2016, 12-09, Volume: 6

    Topics: Autophagy; Azepines; Brain Neoplasms; Cell Differentiation; Dose-Response Relationship, Drug; Enzyme Inhibitors; Glioblastoma; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Histones; Humans; Neoplastic Stem Cells; Quinazolines; Tumor Cells, Cultured

2016
HIV-1 Latency-Reversing Agents Prostratin and Bryostatin-1 Induce Blood-Brain Barrier Disruption/Inflammation and Modulate Leukocyte Adhesion/Transmigration.
    Journal of immunology (Baltimore, Md. : 1950), 2017, 02-01, Volume: 198, Issue:3

    Topics: Acetamides; Azacitidine; Azepines; Blood-Brain Barrier; Bryostatins; Cell Adhesion; Cell Adhesion Molecules; Cell Movement; Cells, Cultured; Chemokine CCL2; Cytokines; Decitabine; HIV-1; Humans; Inflammation; Intercellular Adhesion Molecule-1; Leukocytes; Phorbol Esters; Quinazolines; Receptors, Cell Surface; Virus Latency

2017
TSA and BIX-01294 Induced Normal DNA and Histone Methylation and Increased Protein Expression in Porcine Somatic Cell Nuclear Transfer Embryos.
    PloS one, 2017, Volume: 12, Issue:1

    Topics: Animals; Azepines; Blastocyst; Cell Lineage; DNA; DNA Methylation; Embryo, Mammalian; Histones; Hydroxamic Acids; Nuclear Transfer Techniques; Quinazolines; Swine

2017
Inhibition of H3K9 methyltransferase G9a ameliorates methylglyoxal-induced peritoneal fibrosis.
    PloS one, 2017, Volume: 12, Issue:3

    Topics: Animals; Azepines; Case-Control Studies; Cells, Cultured; DNA Methylation; Gene Expression Regulation, Enzymologic; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Male; Mice; Mice, Inbred C57BL; Peritoneal Fibrosis; Pyruvaldehyde; Quinazolines

2017
Brain-derived neurotrophic factor involved epigenetic repression of UGT2B7 in colorectal carcinoma: A mechanism to alter morphine glucuronidation in tumor.
    Oncotarget, 2017, Apr-25, Volume: 8, Issue:17

    Topics: Adult; Aged; Aged, 80 and over; Analgesics, Opioid; Azepines; Brain-Derived Neurotrophic Factor; Cancer Pain; Cell Line, Tumor; Colorectal Neoplasms; Drug Tolerance; Epigenetic Repression; Female; Gene Expression Regulation, Neoplastic; Gene Knockdown Techniques; Glucuronosyltransferase; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Immunohistochemistry; Male; Middle Aged; Morphine; Morphine Derivatives; Neoplasm Proteins; Polycomb Repressive Complex 1; Polycomb Repressive Complex 2; Promoter Regions, Genetic; Quinazolines; RNA Interference; RNA, Small Interfering; Transcription Factors; Up-Regulation

2017
Histone lysine methyltransferase G9a is a novel epigenetic target for the treatment of hepatocellular carcinoma.
    Oncotarget, 2017, Mar-28, Volume: 8, Issue:13

    Topics: Adult; Aged; Aged, 80 and over; Animals; Azepines; Blotting, Western; Carcinoma, Hepatocellular; Chromatin Immunoprecipitation; DNA Methylation; Enzyme Inhibitors; Epigenesis, Genetic; Female; Gene Expression Regulation, Neoplastic; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Immunohistochemistry; Liver Neoplasms; Male; Mice; Mice, Inbred NOD; Mice, SCID; Middle Aged; Quinazolines; Real-Time Polymerase Chain Reaction; Xenograft Model Antitumor Assays

2017
Epigenetic regulation by G9a/GLP complex ameliorates amyloid-beta 1-42 induced deficits in long-term plasticity and synaptic tagging/capture in hippocampal pyramidal neurons.
    Aging cell, 2017, Volume: 16, Issue:5

    Topics: Amyloid beta-Peptides; Animals; Azepines; Brain-Derived Neurotrophic Factor; CA1 Region, Hippocampal; Cognitive Dysfunction; Epigenesis, Genetic; Histone-Lysine N-Methyltransferase; Long-Term Potentiation; Male; Microtomy; Peptide Fragments; Pyramidal Cells; Quinazolines; Rats; Rats, Wistar; Receptor, trkB; Synapses; Tissue Culture Techniques

2017
[Methyltransferase inhibitor BIX01294 promotes the migration and inhibits decidualization of mouse uterine stromal cells in vitro].
    Nan fang yi ke da xue xue bao = Journal of Southern Medical University, 2017, Jun-20, Volume: 37, Issue:6

    Topics: Animals; Azepines; Cell Movement; Cells, Cultured; Decidua; Embryo Implantation; Endometrium; Female; Histone-Lysine N-Methyltransferase; Mice; Pregnancy; Quinazolines; Stromal Cells

2017
Effect of BIX-01294 on proliferation, apoptosis and histone methylation of acute T lymphoblastic leukemia cells.
    Leukemia research, 2017, Volume: 62

    Topics: Antineoplastic Agents; Apoptosis; Azepines; Cell Line, Tumor; Cell Proliferation; DNA Methylation; Histones; Humans; Precursor T-Cell Lymphoblastic Leukemia-Lymphoma; Quinazolines

2017
Pharmacological and transcriptional inhibition of the G9a histone methyltransferase suppresses proliferation and modulates redox homeostasis in human microvascular endothelial cells.
    Pharmacological research, 2018, Volume: 128

    Topics: Azepines; Cell Line; Cell Proliferation; Endothelial Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Homeostasis; Humans; Microvessels; Oxidation-Reduction; Quinazolines; RNA, Small Interfering

2018
Inhibition of the H3K9 methyltransferase G9A attenuates oncogenicity and activates the hypoxia signaling pathway.
    PloS one, 2017, Volume: 12, Issue:11

    Topics: Apoptosis; Azepines; Cell Cycle; Cell Hypoxia; Cell Movement; Cell Proliferation; HeLa Cells; Histone-Lysine N-Methyltransferase; Humans; Hypoxia-Inducible Factor 1, alpha Subunit; MCF-7 Cells; Methylation; Neoplasms; Oncogenes; Prognosis; Quinazolines; Signal Transduction

2017
BIX-01294 promotes the differentiation of adipose mesenchymal stem cells into adipocytes and neural cells in Arbas Cashmere goats.
    Research in veterinary science, 2018, Volume: 119

    Topics: Adipocytes; Animals; Azepines; Cell Differentiation; Goats; Histones; Mesenchymal Stem Cells; Quinazolines

2018
Viability Screen of LOPAC
    Antimicrobial agents and chemotherapy, 2018, Volume: 62, Issue:8

    Topics: Antiprotozoal Agents; Antirheumatic Agents; Apoptosis; Auranofin; Azepines; Blastocystis; Blastocystis Infections; Drug Repositioning; Enzyme Inhibitors; High-Throughput Screening Assays; Humans; Hypoglycemic Agents; Inhibitory Concentration 50; Onium Compounds; Phosphorylation; Quinazolines; Small Molecule Libraries

2018
Inhibition of euchromatin histone-lysine N-methyltransferase 2 sensitizes breast cancer cells to tumor necrosis factor-related apoptosis-inducing ligand through reactive oxygen species-mediated activating transcription factor 4-C/EBP homologous protein-de
    Molecular carcinogenesis, 2018, Volume: 57, Issue:11

    Topics: Activating Transcription Factor 4; Animals; Apoptosis; Azepines; Breast Neoplasms; Caspase 8; CCAAT-Enhancer-Binding Proteins; Cell Line, Tumor; Cell Survival; Disease Models, Animal; Female; Heterografts; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Mice; Models, Biological; Quinazolines; Reactive Oxygen Species; Receptors, TNF-Related Apoptosis-Inducing Ligand; TNF-Related Apoptosis-Inducing Ligand; Transcription Factor CHOP

2018
Effect of DNA and Histone Methyl Transferase Inhibitors on Outcomes of Buffalo-Bovine Interspecies Somatic Cell Nuclear Transfer.
    Cellular reprogramming, 2018, Volume: 20, Issue:4

    Topics: Acetylation; Animals; Azepines; Blastocyst; Buffaloes; Cattle; Cell Survival; Cells, Cultured; Cellular Reprogramming; Cytidine; DNA; DNA Modification Methylases; Embryo, Mammalian; Embryonic Development; Epigenesis, Genetic; Female; Histone-Lysine N-Methyltransferase; Histones; Nuclear Transfer Techniques; Quinazolines

2018
Epigallocatechin-3-gallate and BIX-01294 have different impact on epigenetics and senescence modulation in acute and chronic myeloid leukemia cells.
    European journal of pharmacology, 2018, Nov-05, Volume: 838

    Topics: Antineoplastic Agents; Azepines; Catechin; Cellular Senescence; Chromobox Protein Homolog 5; Drug Screening Assays, Antitumor; Epigenesis, Genetic; G1 Phase Cell Cycle Checkpoints; Gene Expression Regulation, Neoplastic; Humans; K562 Cells; Leukemia, Myelogenous, Chronic, BCR-ABL Positive; Leukemia, Promyelocytic, Acute; Quinazolines

2018
FOXO1 degradation via G9a-mediated methylation promotes cell proliferation in colon cancer.
    Nucleic acids research, 2019, 02-28, Volume: 47, Issue:4

    Topics: Apoptosis; Azepines; Cell Proliferation; Colonic Neoplasms; CRISPR-Cas Systems; DNA Methylation; Female; Flow Cytometry; Forkhead Box Protein O1; Gene Expression Regulation, Neoplastic; Gene Knockout Techniques; HCT116 Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Male; Quinazolines; S-Phase Kinase-Associated Proteins; Tissue Array Analysis; Ubiquitination

2019
A nuclear lamina-chromatin-Ran GTPase axis modulates nuclear import and DNA damage signaling.
    Aging cell, 2019, Volume: 18, Issue:1

    Topics: Active Transport, Cell Nucleus; Azepines; Chromatin; DNA Damage; Fibroblasts; Histones; Humans; Interphase; Lamin Type A; Lysine; Methylation; Nuclear Lamina; Progeria; Quinazolines; ran GTP-Binding Protein; Signal Transduction

2019
Inhibition of Histone Methyltransferase G9a Attenuates Noise-Induced Cochlear Synaptopathy and Hearing Loss.
    Journal of the Association for Research in Otolaryngology : JARO, 2019, Volume: 20, Issue:3

    Topics: 3T3 Cells; Animals; Auditory Threshold; Azepines; Drug Evaluation, Preclinical; Hair Cells, Auditory; Hearing Loss, Noise-Induced; Histone-Lysine N-Methyltransferase; KCNQ Potassium Channels; Male; Mice; Mice, Inbred CBA; Quinazolines

2019
Down-regulation of Survivin by BIX-01294 Pretreatment Overcomes Resistance of Hepatocellular Carcinoma Cells to TRAIL.
    Anticancer research, 2019, Volume: 39, Issue:7

    Topics: Azepines; Carcinoma, Hepatocellular; Cell Line, Tumor; Down-Regulation; Drug Resistance, Neoplasm; Humans; Liver Neoplasms; Quinazolines; Survivin; TNF-Related Apoptosis-Inducing Ligand

2019
G9a and histone deacetylases are crucial for Snail2-mediated E-cadherin repression and metastasis in hepatocellular carcinoma.
    Cancer science, 2019, Volume: 110, Issue:11

    Topics: Acetylation; Animals; Azepines; Cadherins; Carcinoma, Hepatocellular; Cell Movement; Disease Progression; Down-Regulation; Epigenesis, Genetic; Epithelial-Mesenchymal Transition; Female; Histocompatibility Antigens; Histone Deacetylase Inhibitors; Histone Deacetylases; Histone-Lysine N-Methyltransferase; Humans; Hydroxamic Acids; Liver; Liver Neoplasms; Methylation; Mice; Mice, Inbred BALB C; Mice, Nude; Neoplasm Invasiveness; Neoplasm Metastasis; Quinazolines; Snail Family Transcription Factors; Transcription, Genetic; Transforming Growth Factor beta

2019
The G9a Histone Methyltransferase Inhibitor BIX-01294 Modulates Gene Expression during
    International journal of molecular sciences, 2019, Oct-14, Volume: 20, Issue:20

    Topics: Animals; Anopheles; Antimalarials; Azepines; Gene Expression Regulation, Developmental; Germ Cells; Histone-Lysine N-Methyltransferase; Humans; Malaria, Falciparum; Plasmodium falciparum; Quinazolines

2019
G9a promotes cell proliferation and suppresses autophagy in gastric cancer by directly activating mTOR.
    FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 2019, Volume: 33, Issue:12

    Topics: Animals; Autophagy; Azepines; Cell Cycle; Cell Line; Cell Proliferation; Cell Survival; Down-Regulation; Female; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Mice, SCID; Neoplasms, Experimental; Quinazolines; Stomach Neoplasms; TOR Serine-Threonine Kinases

2019
High-throughput screening yields several small-molecule inhibitors of repeat-associated non-AUG translation.
    The Journal of biological chemistry, 2019, 12-06, Volume: 294, Issue:49

    Topics: Amyotrophic Lateral Sclerosis; Animals; Ataxia; Azepines; Cells, Cultured; Circular Dichroism; DNA Repeat Expansion; Drug Evaluation, Preclinical; Fragile X Syndrome; HEK293 Cells; Humans; Neurodegenerative Diseases; Propidium; Pyrimidines; Quinazolines; Rats; Tremor; Trinucleotide Repeat Expansion

2019
Identification of novel quinoline inhibitor for EHMT2/G9a through virtual screening.
    Biochimie, 2020, Volume: 168

    Topics: Azepines; Catalytic Domain; Databases, Chemical; Enzyme Inhibitors; HEK293 Cells; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Methylation; Protein Binding; Quinazolines; Quinolines

2020
EHMT2/G9a Inhibits Aortic Smooth Muscle Cell Death by Suppressing Autophagy Activation.
    International journal of biological sciences, 2020, Volume: 16, Issue:7

    Topics: Aorta; Autophagy; Azepines; Blotting, Western; Cells, Cultured; Flow Cytometry; Fluorescent Antibody Technique; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Muscle, Smooth, Vascular; Myocytes, Smooth Muscle; Quinazolines; Signal Transduction

2020
BIX-01294 enhanced chemotherapy effect in gastric cancer by inducing GSDME-mediated pyroptosis.
    Cell biology international, 2020, Volume: 44, Issue:9

    Topics: Animals; Apoptosis; Autophagy; Azepines; Cell Death; Cell Line, Tumor; Cell Survival; Male; Mice; Mice, Inbred BALB C; Mice, Nude; Neoplasm Proteins; Pyroptosis; Quinazolines; Stomach Neoplasms

2020
Euchromatin histone methyltransferase II (EHMT2) regulates the expression of ras-related GTP binding C (RRAGC) protein.
    BMB reports, 2020, Volume: 53, Issue:11

    Topics: Apoptosis; Azepines; Carcinoma, Hepatocellular; Cell Line, Tumor; Cell Proliferation; Chromatin Immunoprecipitation; Euchromatin; Gene Expression; Gene Expression Regulation; Histocompatibility Antigens; Histone Methyltransferases; Histone-Lysine N-Methyltransferase; Histones; Humans; Liver Neoplasms; Monomeric GTP-Binding Proteins; Proteomics; Quinazolines; Reactive Oxygen Species; Stress, Physiological; Transcriptome

2020
BIX-01294-enhanced chemosensitivity in nasopharyngeal carcinoma depends on autophagy-induced pyroptosis.
    Acta biochimica et biophysica Sinica, 2020, Oct-19, Volume: 52, Issue:10

    Topics: Animals; Antineoplastic Combined Chemotherapy Protocols; Autophagy; Autophagy-Related Protein 5; Azepines; bcl-2-Associated X Protein; Caspase 3; Cell Line, Tumor; Cell Survival; Chloroquine; Cisplatin; CRISPR-Cas Systems; Gene Knockout Techniques; Humans; Mice; Mice, Inbred BALB C; Mice, Nude; Microtubule-Associated Proteins; Nasopharyngeal Carcinoma; Nasopharyngeal Neoplasms; Pyroptosis; Quinazolines; Receptors, Estrogen; Signal Transduction

2020
Radiation-induced H3K9 methylation on E-cadherin promoter mediated by ROS/Snail axis : Role of G9a signaling during lung epithelial-mesenchymal transition.
    Toxicology in vitro : an international journal published in association with BIBRA, 2021, Volume: 70

    Topics: Azepines; Cadherins; Cell Line; Cell Movement; Cell Survival; Epithelial Cells; Epithelial-Mesenchymal Transition; Glycogen Synthase Kinase 3 beta; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Histones; Humans; Lung; Methylation; Promoter Regions, Genetic; Quinazolines; Reactive Oxygen Species; Signal Transduction; Snail Family Transcription Factors; X-Rays

2021
BIX-01294, a G9a inhibitor, suppresses cell proliferation by inhibiting autophagic flux in nasopharyngeal carcinoma cells.
    Investigational new drugs, 2021, Volume: 39, Issue:3

    Topics: Antineoplastic Agents; Autophagosomes; Azepines; Cell Line, Tumor; Cell Physiological Phenomena; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Lysosomal Membrane Proteins; Lysosomal-Associated Membrane Protein 2; Lysosomes; Nasopharyngeal Carcinoma; Nasopharyngeal Neoplasms; Quinazolines; RNA, Small Interfering

2021
Down-regulated microRNA-199a-3p enhances osteogenic differentiation of bone marrow mesenchymal stem cells by targeting Kdm3a in ovariectomized rats.
    The Biochemical journal, 2021, 02-26, Volume: 478, Issue:4

    Topics: Animals; Antigens, CD; Azepines; Bone and Bones; Disease Models, Animal; Down-Regulation; Female; Gene Expression Regulation; Gene Knockdown Techniques; Gene Regulatory Networks; Genes, Reporter; Histone Demethylases; Humans; Kruppel-Like Transcription Factors; Mesenchymal Stem Cells; MicroRNAs; Mitogen-Activated Protein Kinase 1; Osteogenesis; Osteoporosis; Osteoporosis, Postmenopausal; Ovariectomy; Quinazolines; Rats; Rats, Sprague-Dawley

2021
The histone H3 lysine 9 methyltransferase G9a/GLP complex activity is required for long-term consolidation of spatial memory in mice.
    Neurobiology of learning and memory, 2021, Volume: 179

    Topics: Animals; Azepines; Corpus Striatum; Hippocampus; Histone Code; Histone-Lysine N-Methyltransferase; Male; Memory Consolidation; Memory, Long-Term; Memory, Short-Term; Mice; Morris Water Maze Test; Quinazolines; Spatial Memory

2021
HeLa TI cell-based assay as a new approach to screen for chemicals able to reactivate the expression of epigenetically silenced genes.
    PloS one, 2021, Volume: 16, Issue:6

    Topics: Azacitidine; Azepines; DNA Methylation; Epigenesis, Genetic; HeLa Cells; Histone Deacetylase Inhibitors; Humans; Phthalimides; Quinazolines; Tryptophan

2021
H3K9me2 regulates early transcription factors to promote mesenchymal stem‑cell differentiation into cardiomyocytes.
    Molecular medicine reports, 2021, Volume: 24, Issue:2

    Topics: Animals; Azacitidine; Azepines; Cell Differentiation; Female; GATA4 Transcription Factor; Gene Knockdown Techniques; Histone Demethylases; Histone-Lysine N-Methyltransferase; Histones; Homeobox Protein Nkx-2.5; Male; MEF2 Transcription Factors; Mesenchymal Stem Cells; Myocytes, Cardiac; Primary Cell Culture; Quinazolines; Rats, Wistar; Transcription Factors; Troponin T

2021
BIX01294 inhibits EGFR signaling in EGFR-mutant lung adenocarcinoma cells through a BCKDHA-mediated reduction in the EGFR level.
    Experimental & molecular medicine, 2021, Volume: 53, Issue:12

    Topics: 3-Methyl-2-Oxobutanoate Dehydrogenase (Lipoamide); Adenocarcinoma of Lung; Apoptosis; Azepines; Biomarkers; Cell Line, Tumor; Citric Acid Cycle; Disease Susceptibility; Drug Resistance, Neoplasm; Energy Metabolism; ErbB Receptors; Histone Demethylases; Humans; Immunohistochemistry; Mitochondria; Models, Biological; Protein Kinase Inhibitors; Quinazolines; Signal Transduction

2021
BIX-01294 enhances the effect of chemotherapy on colorectal cancer by inhibiting the expression of stemness genes.
    Biochemical and biophysical research communications, 2022, 01-29, Volume: 590

    Topics: Animals; Azepines; Biomarkers, Tumor; Cell Line, Tumor; Cell Movement; Cell Proliferation; Colorectal Neoplasms; Female; Fluorouracil; Gene Expression Regulation, Neoplastic; Histocompatibility Antigens; Histone-Lysine N-Methyltransferase; Humans; Mice, Inbred BALB C; Mice, Nude; Neoplastic Stem Cells; Quinazolines; Receptors, G-Protein-Coupled

2022