Citation: | CHEN Ming, XIE Zhouling, LI Tinghan, WEI Zhihui, ZHAO Lu, LI Zhiyu. Advances in research on a novel antitumor target CDK9 and its inhibitors[J]. Journal of China Pharmaceutical University, 2017, 48(2): 233-241. DOI: 10.11665/j.issn.1000-5048.20170216 |
[1] |
Wang S,Fischer PM. Cyclin-dependent kinase 9:a key transcriptional regulator and potential drug target in oncology,virology and cardiology[J].Trends Pharmacol Sci, 2008,29(6):302-313.
|
[2] |
Heathcote DA,Patel H,Kroll SH,et al.A novel pyrazolo[1,5-a]pyrimidine is a potent inhibitor of cyclin-dependent protein kinases 1,2,and 9,which demonstrates antitumor effects in human tumor xenografts following oral administration[J].J Med Chem,2010,53(24):8508-8522.
|
[3] |
Wsierska-Gdek J,Chamrád I,Krytof V. Novel potent pharmacological cyclin-dependent kinase inhibitors[J].Future Med Chem,2009,1(9):1561-1581.
|
[4] |
Kryof V,Chamrád I,Jorda R,et al.Pharmacological targeting of CDK9 in cardiac hypertrophy[J].Med Res Rev,2010,30(4):646-666.
|
[5] |
Chen YJ,Dominguez-Brauer C,Wang Z,et al.A conserved phosphorylation site within the forkhead domain of FoxM1B is required for its activation by cyclin-CDK1[J].J Biol Chem,2009,284(44):30695-30707.
|
[6] |
Marais A,Ji Z,Child ES,et al.Cell cycle-dependent regulation of the forkhead transcription factor FOXK2 by CDK·cyclin complexes[J].J Biol Chem,2010,285(46):35728-35739.
|
[7] |
Tomashevski A, Webster DR, Grammas P, et al. Cyclin-C-dependent cell-cycle entry is required for activation of non-homologous end joining DNA repair in postmitotic neurons[J].Cell Death Differ,2010,17(7):1189-1198.
|
[8] |
Aggarwal P,Vaites LP,Kim JK,et al.Nuclear cyclin D1/CDK4 kinase regulates CUL4 expression and triggers neoplastic growth via activation of the PRMT5 methyltransferase[J].Cancer Cell,2010,18(4):329-340.
|
[9] |
Lavoie G,St-Pierre Y. Phosphorylation of human DNMT1:implication of cyclin-dependent kinases[J].Biochem Biophys Res Commun,2011,409(2):187-192.
|
[10] |
Tudhope SJ,Wang CC,Petrie JL,et al.A novel mechanism for regulating hepatic glycogen synthesis involving serotonin and cyclin-dependent kinase-5[J].Diabetes,2012,61(1):49-60.
|
[11] |
Firestein R,Bass AJ,Kim SY,et al.CDK8 is a colorectal cancer oncogene that regulates beta-catenin activity[J].Nature,2008,455(7212):547-551.
|
[12] |
Zhao X,Feng D,Wang Q,et al.Regulation of lipogenesis by cyclin-dependent kinase 8-mediated control of SREBP-1[J].J Clin Invest,2012,122(7):2417-2427.
|
[13] |
Yu DS,Zhao R,Hsu EL,et al.Cyclin-dependent kinase 9-cyclin K functions in the replication stress response[J].EMBO Rep,2010,11(11):876-882.
|
[14] |
Krytof V,Baumli S,Fürst R. Perspective of cyclin-dependent kinase 9(CDK9)as a drug target[J].Curr Pharm Des,2012,18(20):2883-2890.
|
[15] |
Stellrecht CM,Chen LS. Transcription inhibition as a therapeutic target for cancer[J].Cancers,2011,3(4):4170-4190.
|
[16] |
MacCallum DE,Melville J,Frame S,et al.Seliciclib(CYC202,R-roscovitine)induces cell death in multiple myeloma cells by inhibition of RNA polymerase II-dependent transcription and down-regulation of Mcl-1[J].Cancer Res,2005,65(12):5399-5407.
|
[17] |
Echalier A,Hole AJ,Lolli G,et al.An inhibitor′s-eye view of the ATP-binding site of CDKs in different regulatory states[J].ACS Chem Biol,2014,9(6):1251-1256.
|
[18] |
Echalier A,Endicott JA,Noble ME. Recent developments in cyclin-dependent kinase biochemical and structural studies[J].Biochim Biophys Acta,2010,1804(3):511-519.
|
[19] |
Nowicki MW,Walkinshaw MD. CDK9 inhibitors push cancer cells over the edge[J].Chem Biol,2010,17(10):1047-1048.
|
[20] |
Baumli S,Lolli G,Lowe ED,et al.The structure of P-TEFb(CDK9/cyclin T1),its complex with flavopiridol and regulation by phosphorylation[J].EMBO J,2008,27(13):1907-1918.
|
[21] |
Ahn YM,Vogeti L,Liu CJ,et al.Design,synthesis,and antiproliferative and CDK2-cyclin a inhibitory activity of novel flavopiridol analogues[J].Bioorg Med Chem,2007,15(2):702-713.
|
[22] |
Manohar SM, Rathos MJ, Sonawane V, et al. Cyclin-dependent kinase inhibitor,P276-00 induces apoptosis in multiple myeloma cells by inhibition of Cdk9-T1 and RNA polymerase II-dependent transcription[J].Leuk Res,2011,35(6):821-830.
|
[23] |
Cassaday RD,Goy A,Advani S,et al.A phase II,single-arm,open-label,multicenter study to evaluate the efficacy and safety of P276-00,a cyclin-dependent kinase inhibitor,in patients with relapsed or refractory mantle cell lymphoma[J].Clin Lymphoma Myeloma Leuk,2015,15(7):392-397.
|
[24] |
Houzé S, Hoang NT, Lozach O, et al. Several human cyclin-dependent kinase inhibitors,structurally related to roscovitine,are new anti-malarial agents[J].Molecules,2014,19(9):15237-15257.
|
[25] |
Benson C,White J,De Bono J,et al.A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib(CYC202;R-roscovitine),administered twice daily for 7 days every 21 days[J].Br J Cancer,2007,96(1):29-37.
|
[26] |
Mita MM,Joy AA,Mita A,et al.Randomized phase II trial of the cyclin-dependent kinase inhibitor dinaciclib(MK-7965)versus capecitabine in patients with advanced breast cancer[J].Clin Breast Cancer,2014,14(3):169-176.
|
[27] |
Mitri Z, Karakas C, Wei C, et al. A phase 1 study with dose expansion of the CDK inhibitor dinaciclib(SCH 727965)in combination with epirubicin in patients with metastatic triple negative breast cancer[J].Invest New Drugs,2015,33(4):890-894.
|
[28] |
Santo L,Vallet S,Hideshima T,et al.AT7519,a novel small molecule multi-cyclin-dependent kinase inhibitor,induces apoptosis in multiple myeloma via GSK-3beta activation and RNA polymerase II inhibition[J].Oncogene,2010,29(16):2325-2336.
|
[29] |
Chen EX, Hotte S, Hirte H, et al. A phase I study of cyclin-dependent kinase inhibitor,AT7519,in patients with advanced cancer:NCIC Clinical Trials Group IND 177[J].British J Cancer,2014,111(12):2262-2267.
|
[30] |
Diab S, Eckhardt S, Tan A, et al. A phase I study of R547,a novel,selective inhibitor of cell cycle and transcriptional cyclin dependent kinases(CDKs)[J].J Clin Oncol,2007,25(Suppl):3528.
|
[31] |
Baumli S, Endicott JA, Johnson LN. Halogen bonds form the basis for selective P-TEFb inhibition by DRB[J].Chem Biol,2010,17(9):931-936.
|
[32] |
Krytof V,Rárová L,Liebl J,et al.The selective P-TEFb inhibitor CAN508 targets angiogenesis[J].Eur J Med Chem,2011,46(9):4289-4294.
|
[33] |
Krytof V,Chamrád I,Jorda R,et al.Pharmacological targeting of CDK9 in cardiac hypertrophy[J].Med Res Rev,2010,30(4):646-666.
|
[34] |
Baumli S,Hole AJ,Noble ME,et al.The CDK9 C-helix exhibits conformational plasticity that may explain the selectivity of CAN508[J].ACS Chem Biol,2012,7(5):811-816.
|
[35] |
Shao H,Shi S,Huang S,et al.Substituted 4-(thiazol-5-yl)-2-(phenylamino)pyrimidines are highly active CDK9 inhibitors:synthesis,X-ray crystal structures,structure-activity relationship,and anticancer activities[J].J Med Chem,2013,<
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