1. Arellano M, Moreno S. Regulation of CDK/cyclin complexes during the cell cycle. Int J Biochem Cell Biol. 1997;29:559–573. [PubMed] [Google Scholar]
2. Swaffer MP, Jones AW, Flynn HR, Snijders AP, Nurse P. CDK substrate phosphorylation and ordering the cell cycle. Cell. 2016;167:1750–1761. e1716. [PMC free article] [PubMed] [Google Scholar]
3. Lim S, Kaldis P. Cdks, cyclins and CKIs: roles beyond cell cycle regulation. Development. 2013;140:3079–3093. [PubMed] [Google Scholar]
4. Malumbres M, Harlow E, Hunt T, Hunter T, Lahti JM, Manning G, Morgan DO, Tsai LH, Wolgemuth DJ. Cyclin-dependent kinases: a family portrait. Nat Cell Biol. 2009;11:1275–1276. [PMC free article] [PubMed] [Google Scholar]
5. Morgan DO. Cyclin-dependent kinases: engines, clocks, and microprocessors. Annu Rev Cell Dev Biol. 1997;13:261–291. [PubMed] [Google Scholar]
6. Sherr CJ, Roberts JM. Living with or without cyclins and cyclin-dependent kinases. Genes Dev. 2004;18:2699–2711. [PubMed] [Google Scholar]
7. Akhtar MS, Heidemann M, Tietjen JR, Zhang DW, Chapman RD, Eick D, Ansari AZ. TFIIH kinase places bivalent marks on the carboxy-terminal domain of RNA polymerase II. Mol Cell. 2009;34:387–393. [PMC free article] [PubMed] [Google Scholar]
8. Larochelle S, Amat R, Glover-Cutter K, Sansó M, Zhang C, Allen JJ, Shokat KM, Bentley DL, Fisher RP. Cyclin-dependent kinase control of the initiation-to-elongation switch of RNA polymerase II. Nat Struct Mol Biol. 2012;19:1108–1115. [PMC free article] [PubMed] [Google Scholar]
9. Zhou Q, Li T, Price DH. RNA polymerase II elongation control. Annu Rev Biochem. 2012;81:119–143. [PMC free article] [PubMed] [Google Scholar]
10. Dhariwala FA, Rajadhyaksha MS. An unusual member of the Cdk family: Cdk5. Cell Mol Neurobiol. 2008;28:351–369. [PubMed] [Google Scholar]
11. Hellmich MR, Pant HC, Wada E, Battey JF. Neuronal cdc2-like kinase: a cdc2-related protein kinase with predominantly neuronal expression. Proc Natl Acad Sci U S A. 1992;89:10867–10871. [PMC free article] [PubMed] [Google Scholar]
12. Davidson G, Shen J, Huang YL, Su Y, Karaulanov E, Bartscherer K, Hassler C, Stannek P, Boutros M, Niehrs C. Cell cycle control of wnt receptor activation. Dev Cell. 2009;17:788–799. [PubMed] [Google Scholar]
13. Jiang M, Gao Y, Yang T, Zhu X, Chen J. Cyclin Y, a novel membrane-associated cyclin, interacts with PFTK1. FEBS Lett. 2009;583:2171–2178. [PubMed] [Google Scholar]
14. Meijer L, Borgne A, Mulner O, Chong JP, Blow JJ, Inagaki N, Inagaki M, Delcros JG, Moulinoux JP. Biochemical and cellular effects of roscovitine, a potent and selective inhibitor of the cyclin-dependent kinases cdc2, cdk2 and cdk5. Eur J Biochem. 1997;243:527–536. [PubMed] [Google Scholar]
15. Cicenas J, Kalyan K, Sorokinas A, Stankunas E, Levy J, Meskinyte I, Stankevicius V, Kaupinis A, Valius M. Roscovitine in cancer and other diseases. Ann Transl Med. 2015;3:135. [PMC free article] [PubMed] [Google Scholar]
16. Whittaker SR, Mallinger A, Workman P, Clarke PA. Inhibitors of cyclin-dependent kinases as cancer therapeutics. Pharmacol Ther. 2017;173:83–105. [PMC free article] [PubMed] [Google Scholar]
17. Asghar U, Witkiewicz AK, Turner NC, Knudsen ES. The history and future of targeting cyclin-dependent kinases in cancer therapy. Nat Rev Drug Discov. 2015;14:130–146. [PMC free article] [PubMed] [Google Scholar]
18. Zeidner JF, Karp JE. Clinical activity of alvocidib (flavopiridol) in acute myeloid leukemia. Leuk Res. 2015;39:1312–1318. [PubMed] [Google Scholar]
19. Parker BW, Kaur G, Nieves-Neira W, Taimi M, Kohlhagen G, Shimizu T, Losiewicz MD, Pommier Y, Sausville EA, Senderowicz AM. Early induction of apoptosis in hematopoietic cell lines after exposure to flavopiridol. Blood. 1998;91:458–465. [PubMed] [Google Scholar]
20. Phelps MA, Lin TS, Johnson AJ, Hurh E, Rozewski DM, Farley KL, Wu D, Blum KA, Fischer B, Mitchell SM, Moran ME, Brooker-McEldowney M, Heerema NA, Jarjoura D, Schaaf LJ, Byrd JC, Grever MR, Dalton JT. Clinical response and pharmaco*kinetics from a phase 1 study of an active dosing schedule of flavopiridol in relapsed chronic lymphocytic leukemia. Blood. 2009;113:2637–2645. [PMC free article] [PubMed] [Google Scholar]
21. Lin TS, Ruppert AS, Johnson AJ, Fischer B, Heerema NA, Andritsos LA, Blum KA, Flynn JM, Jones JA, Hu W, Moran ME, Mitchell SM, Smith LL, Wagner AJ, Raymond CA, Schaaf LJ, Phelps MA, Villalona-Calero MA, Grever MR, Byrd JC. Phase II study of flavopiridol in relapsed chronic lymphocytic leukemia demonstrating high response rates in genetically high-risk disease. J. Clin. Oncol. 2009;27:6012–6018. [PMC free article] [PubMed] [Google Scholar]
22. Bose P, Simmons GL, Grant S. Cyclin-dependent kinase inhibitor therapy for hematologic malignancies. Expert Opin Investig Drugs. 2013;22:723–738. [PMC free article] [PubMed] [Google Scholar]
23. Karp JE, Blackford A, Smith BD, Alino K, Seung AH, Bolaños-Meade J, Greer JM, Carraway HE, Gore SD, Jones RJ, Levis MJ, McDevitt MA, Doyle LA, Wright JJ. Clinical activity of sequential flavopiridol, cytosine arabinoside, and mitoxantrone for adults with newly diagnosed, poor-risk acute myelogenous leukemia. Leuk Res. 2010;34:877–882. [PMC free article] [PubMed] [Google Scholar]
24. Baker A, Gregory GP, Verbrugge I, Kats L, Hilton JJ, Vidacs E, Lee EM, Lock RB, Zuber J, Shortt J, Johnstone RW. The CDK9 inhibitor dinaciclib exerts potent apoptotic and antitumor effects in preclinical models of MLL-rearranged acute myeloid leukemia. Cancer Res. 2016;76:1158. [PubMed] [Google Scholar]
25. Johnson AJ, Yeh YY, Smith LL, Wagner AJ, Hessler J, Gupta S, Flynn J, Jones J, Zhang X, Bannerji R, Grever MR, Byrd JC. The novel cyclin-dependent kinase inhibitor dinaciclib (SCH727965) promotes apoptosis and abrogates microenvironmental cytokine protection in chronic lymphocytic leukemia cells. Leukemia. 2012;26:2554–2557. [PMC free article] [PubMed] [Google Scholar]
26. Hossain DMS, Javaid S, Cai M, Zhang C, Sawant A, Hinton M, Sathe M, Grein J, Blumenschein W, Pinheiro EM, Chackerian A. Dinaciclib induces immunogenic cell death and enhances anti-PD1-mediated tumor suppression. J Clin Invest. 2018;128:644–654. [PMC free article] [PubMed] [Google Scholar]
27. Shirsath NP, Manohar SM, Joshi KS. P276-00, a cyclin-dependent kinase inhibitor, modulates cell cycle and induces apoptosis in vitro and in vivo in mantle cell lymphoma cell lines. Mol Cancer. 2012;11:77. [PMC free article] [PubMed] [Google Scholar]
28. Cassaday RD, Goy A, Advani S, Chawla P, Nachankar R, Gandhi M, Gopal AK. 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. Clin Lymphoma Myeloma Leuk. 2015;15:392–397. [PMC free article] [PubMed] [Google Scholar]
29. Mishra PB, Lobo AS, Joshi KS, Rathos MJ, Kumar GA, Padigaru M. Molecular mechanisms of anti-tumor properties of P276-00 in head and neck squamous cell carcinoma. J Transl Med. 2013;11:42. [PMC free article] [PubMed] [Google Scholar]
30. Su YT, Chen R, Wang H, Song H, Zhang Q, Chen LY, Lappin H, Vasconcelos G, Lita A, Maric D, Li A, Celiku O, Zhang W, Meetze K, Estok T, Larion M, Abu-Asab M, Zhuang Z, Yang C, Gilbert MR, Wu J. Novel targeting of transcription and metabolism in glioblastoma. Clin Cancer Res. 2018;24:1124–1137. [PMC free article] [PubMed] [Google Scholar]
31. Goh KC, Novotny-Diermayr V, Hart S, Ong LC, Loh YK, Cheong A, Tan YC, Hu C, Jayaraman R, William AD, Sun ET, Dymock BW, Ong KH, Ethirajulu K, Burrows F, Wood JM. TG02, a novel oral multi-kinase inhibitor of CDKs, JAK2 and FLT3 with potent anti-leukemic properties. Leukemia. 2012;26:236–243. [PubMed] [Google Scholar]
32. Ponder KG, Matulis SM, Hitosugi S, Gupta VA, Sharp C, Burrows F, Nooka AK, Kaufman JL, Lonial S, Boise LH. Dual inhibition of Mcl-1 by the combination of carfilzomib and TG02 in multiple myeloma. Cancer Biol Ther. 2016;17:769–777. [PMC free article] [PubMed] [Google Scholar]
33. Dolman ME, Poon E, Ebus ME, den Hartog IJ, van Noesel CJ, Jamin Y, Hallsworth A, Robinson SP, Petrie K, Sparidans RW, Kok RJ, Versteeg R, Caron HN, Chesler L, Molenaar JJ. Cyclin-dependent kinase inhibitor AT7519 as a potential drug for MYCN-dependent neuroblastoma. Clin Cancer Res. 2015;21:5100–9. [PMC free article] [PubMed] [Google Scholar]
34. Dorward DA, Felton JM, Robb CT, Craven T, Kipari T, Walsh TS, Haslett C, Kefala K, Rossi AG, Lucas CD. The cyclin-dependent kinase inhibitor AT7519 accelerates neutrophil apoptosis in sepsis-related acute respiratory distress syndrome. Thorax. 2017;72:182–185. [PMC free article] [PubMed] [Google Scholar]
35. Chen EX, Hotte S, Hirte H, Siu LL, Lyons J, Squires M, Lovell S, Turner S, McIntosh L, Seymour L. A phase I study of cyclin-dependent kinase inhibitor, AT7519, in patients with advanced cancer: NCIC Clinical Trials Group IND 177. Br J Cancer. 2014;111:2262–2267. [PMC free article] [PubMed] [Google Scholar]
36. Syn NL, Lim PL, Kong LR, Wang L, Wong AL, Lim CM, Loh TKS, Siemeister G, Goh BC, Hsieh WS. Pan-CDK inhibition augments cisplatin lethality in nasopharyngeal carcinoma cell lines and xenograft models. Signal Transduct Target Ther. 2018;3:9. [PMC free article] [PubMed] [Google Scholar]
37. Lin SF, Lin JD, Hsueh C, Chou TC, Wong RJ. Activity of roniciclib in medullary thyroid cancer. Oncotarget. 2018;9:28030–28041. [PMC free article] [PubMed] [Google Scholar]
38. Bahleda R, Grilley-Olson JE, Govindan R, Barlesi F, Greillier L, Perol M, Ray-Coquard I, Strumberg D, Schultheis B, Dy GK, Zalcman G, Weiss GJ, Walter AO, Kornacker M, Rajagopalan P, Henderson D, Nogai H, Ocker M, Soria JC. Phase I dose-escalation studies of roniciclib, a pan-cyclin-dependent kinase inhibitor, in advanced malignancies. Br J Cancer. 2017;116:1505–1512. [PMC free article] [PubMed] [Google Scholar]
39. Cho BC, Dy GK, Govindan R, Kim DW, Pennell NA, Zalcman G, Besse B, Kim JH, Koca G, Rajagopalan P, Langer S, Ocker M, Nogai H, Barlesi F. Phase Ib/II study of the pan-cyclin-dependent kinase inhibitor roniciclib in combination with chemotherapy in patients with extensive-disease small-cell lung cancer. Lung Cancer. 2018;123:14–21. [PubMed] [Google Scholar]
40. Cirstea D, Hideshima T, Santo L, Eda H, Mishima Y, Nemani N, Hu Y, Mimura N, Cottini F, Gorgun G, Ohguchi H, Suzuki R, Loferer H, Munshi NC, Anderson KC, Raje N. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013;27:2366–2375. [PMC free article] [PubMed] [Google Scholar]
41. van der Biessen DA, Burger H, de Bruijn P, Lamers CH, Naus N, Loferer H, Wiemer EA, Mathijssen RH, de Jonge MJ. Phase I study of RGB-286638, a novel, multitargeted cyclin-dependent kinase inhibitor in patients with solid tumors. Clin Cancer Res. 2014;20:4776–83. [PubMed] [Google Scholar]
42. Locatelli G, Bosotti R, Ciomei M, Brasca MG, Calogero R, Mercurio C, Fiorentini F, Bertolotti M, Scacheri E, Scaburri A, Galvani A, Pesenti E, De Baere T, Soria JC, Lazar V, Isacchi A. Transcriptional analysis of an E2F gene signature as a biomarker of activity of the cyclin-dependent kinase inhibitor PHA-793887 in tumor and skin biopsies from a phase I clinical study. Mol Cancer Ther. 2010;9:1265–73. [PubMed] [Google Scholar]
43. Alzani R, Pedrini O, Albanese C, Ceruti R, Casolaro A, Patton V, Colotta F, Rambaldi A, Introna M, Pesenti E, Ciomei M, Golay J. Therapeutic efficacy of the pan-cdk inhibitor PHA-793887 in vitro and in vivo in engraftment and high-burden leukemia models. Exp Hematol. 2010;38:259–269. e252. [PubMed] [Google Scholar]
44. Massard C, Soria JC, Anthoney DA, Proctor A, Scaburri A, Pacciarini MA, Laffranchi B, Pellizzoni C, Kroemer G, Armand JP, Balheda R, Twelves CJ. A first in man, phase I dose-escalation study of PHA-793887, an inhibitor of multiple cyclin-dependent kinases (CDK2, 1 and 4) reveals unexpected hepatotoxicity in patients with solid tumors. Cell Cycle. 2011;10:963–970. [PubMed] [Google Scholar]
45. Fry DW, Harvey PJ, Keller PR, Elliott WL, Meade M, Trachet E, Albassam M, Zheng X, Leopold WR, Pryer NK, Toogood PL. Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts. Mol Cancer Ther. 2004;3:1427–1438. [PubMed] [Google Scholar]
46. Gelbert LM, Cai S, Lin X, Sanchez-Martinez C, Del Prado M, Lallena MJ, Torres R, Ajamie RT, Wishart GN, Flack RS, Neubauer BL, Young J, Chan EM, Iversen P, Cronier D, Kreklau E, de Dios A. Preclinical characterization of the CDK4/6 inhibitor LY2835219: in-vivo cell cycle-dependent/independent anti-tumor activities alone/in combination with gemcitabine. Invest New Drugs. 2014;32:825–837. [PMC free article] [PubMed] [Google Scholar]
47. Tripathy D, Bardia A, Sellers WR. Ribociclib (LEE011): mechanism of action and clinical impact of this selective cyclin-dependent kinase 4/6 inhibitor in various solid tumors. Clin Cancer Res. 2017;23:3251–3262. [PMC free article] [PubMed] [Google Scholar]
48. Klein ME, Kovatcheva M, Davis LE, Tap WD, Koff A. CDK4/6 inhibitors: the mechanism of action may not be as simple as once thought. Cancer Cell. 2018;34:9–20. [PMC free article] [PubMed] [Google Scholar]
49. Ali S, Heathcote DA, Kroll SH, Jogalekar AS, Scheiper B, Patel H, Brackow J, Siwicka A, Fuchter MJ, Periyasamy M, Tolhurst RS, Kanneganti SK, Snyder JP, Liotta DC, Aboagye EO, Barrett AG, Coombes RC. The development of a selective cyclin-dependent kinase inhibitor that shows antitumor activity. Cancer Res. 2009;69:6208–6215. [PMC free article] [PubMed] [Google Scholar]
50. Hazel P, Kroll SH, Bondke A, Barbazanges M, Patel H, Fuchter MJ, Coombes RC, Ali S, Barrett AG, Freemont PS. Inhibitor selectivity for cyclin-dependent kinase 7: a structural, thermodynamic, and modelling study. ChemMedChem. 2017;12:372–380. [PubMed] [Google Scholar]
51. Patel H, Periyasamy M, Sava GP, Bondke A, Slafer BW, Kroll SHB, Barbazanges M, Starkey R, Ottaviani S, Harrod A, Aboagye EO, Buluwela L, Fuchter MJ, Barrett AGM, Coombes RC, Ali S. ICEC0942, an orally bioavailable selective inhibitor of CDK7 for cancer treatment. Mol Cancer Ther. 2018;17:1156–1166. [PMC free article] [PubMed] [Google Scholar]
52. Chipumuro E, Marco E, Christensen CL, Kwiatkowski N, Zhang T, Hatheway CM, Abraham BJ, Sharma B, Yeung C, Altabef A, Perez-Atayde A, Wong KK, Yuan GC, Gray NS, Young RA, George RE. CDK7 inhibition suppresses super-enhancer-linked oncogenic transcription in MYCN-driven cancer. Cell. 2014;159:1126–1139. [PMC free article] [PubMed] [Google Scholar]
53. Christensen CL, Kwiatkowski N, Abraham BJ, Carretero J, Al-Shahrour F, Zhang T, Chipumuro E, Herter-Sprie GS, Akbay EA, Altabef A, Zhang J, Shimamura T, Capelletti M, Reibel JB, Cavanaugh JD, Gao P, Liu Y, Michaelsen SR, Poulsen HS, Aref AR, Barbie DA, Bradner JE, George RE, Gray NS, Young RA, Wong KK. Targeting transcriptional addictions in small cell lung cancer with a covalent CDK7 inhibitor. Cancer Cell. 2014;26:909–922. [PMC free article] [PubMed] [Google Scholar]
54. Kwiatkowski N, Zhang T, Rahl PB, Abraham BJ, Reddy J, Ficarro SB, Dastur A, Amzallag A, Ramaswamy S, Tesar B, Jenkins CE, Hannett NM, McMillin D, Sanda T, Sim T, Kim ND, Look T, Mitsiades CS, Weng AP, Brown JR, Benes CH, Marto JA, Young RA, Gray NS. Targeting transcription regulation in cancer with a covalent CDK7 inhibitor. Nature. 2014;511:616–620. [PMC free article] [PubMed] [Google Scholar]
55. Nagaraja S, Vitanza NA, Woo PJ, Taylor KR, Liu F, Zhang L, Li M, Meng W, Ponnuswami A, Sun W, Ma J, Hulleman E, Swigut T, Wysocka J, Tang Y, Monje M. Transcriptional dependencies in diffuse intrinsic pontine glioma. Cancer Cell. 2017;31:635–652. e636. [PMC free article] [PubMed] [Google Scholar]
56. Wang Y, Zhang T, Kwiatkowski N, Abraham BJ, Lee TI, Xie S, Yuzugullu H, Von T, Li H, Lin Z, Stover DG, Lim E, Wang ZC, Iglehart JD, Young RA, Gray NS, Zhao JJ. CDK7-dependent transcriptional addiction in triple-negative breast cancer. Cell. 2015;163:174–186. [PMC free article] [PubMed] [Google Scholar]
57. Zhang Y, Zhou L, Bandyopadhyay D, Sharma K, Allen AJ, Kmieciak M, Grant S. The covalent CDK7 inhibitor THZ1 potently induces apoptosis in multiple myeloma cells in vitro and in vivo. Clin Cancer Res. 2019;25:6195–6205. [PMC free article] [PubMed] [Google Scholar]
58. Olson CM, Liang Y, Leggett A, Park WD, Li L, Mills CE, Elsarrag SZ, Ficarro SB, Zhang T, Düster R, Geyer M, Sim T, Marto JA, Sorger PK, Westover KD, Lin CY, Kwiatkowski N, Gray NS. Development of a selective CDK7 covalent inhibitor reveals predominant cell-cycle phenotype. Cell Chem Biol. 2019;26:792–803. e710. [PMC free article] [PubMed] [Google Scholar]
59. Zhang H, Christensen CL, Dries R, Oser MG, Deng J, Diskin B, Li F, Pan Y, Zhang X, Yin Y, Papadopoulos E, Pyon V, Thakurdin C, Kwiatkowski N, Jani K, Rabin AR, Castro DM, Chen T, Silver H, Huang Q, Bulatovic M, Dowling CM, Sundberg B, Leggett A, Ranieri M, Han H, Li S, Yang A, Labbe KE, Almonte C, Sviderskiy VO, Quinn M, Donaghue J, Wang ES, Zhang T, He Z, Velcheti V, Hammerman PS, Freeman GJ, Bonneau R, Kaelin WG Jr, Sutherland KD, Kersbergen A, Aguirre AJ, Yuan GC, Rothenberg E, Miller G, Gray NS, Wong KK. CDK7 inhibition potentiates genome instability triggering anti-tumor immunity in small cell lung cancer. Cancer Cell. 2020;37:37–54. e9. [PMC free article] [PubMed] [Google Scholar]
60. Hu S, Marineau JJ, Rajagopal N, Hamman KB, Choi YJ, Schmidt DR, Ke N, Johannessen L, Bradley MJ, Orlando DA, Alnemy SR, Ren Y, Ciblat S, Winter DK, Kabro A, Sprott KT, Hodgson JG, Fritz CC, Carulli JP, di Tomaso E, Olson ER. Discovery and Characterization of SY-1365, a selective, covalent inhibitor of CDK7. Cancer Res. 2019;79:3479–3491. [PubMed] [Google Scholar]
61. Hu S, Marineau J, Hamman K, Bradley M, Savinainen A, Alnemy S, Rajagopal N, Orlando D, Chuaqui C, Olson E. Abstract 4421: SY-5609, an orally available selective CDK7 inhibitor demonstrates broad anti-tumor activity in vivo. Cancer Res. 2019;79:4421–4421. [Google Scholar]
62. Johannessen LH, Hu S, Ke N, D’Ippolito A, Rajagopal N, Marineau J, Savinainen A, Zamboni W, Hodgson G. Abstract C091: preclinical evaluation of PK, PD, and antitumor activity of the oral, non-covalent, potent and highly selective CDK7 inhibitor, SY-5609, provides rationale for clinical development in multiple solid tumor indications. Mol Cancer Ther. 2019;18:C091–C091. [Google Scholar]
63. Bacon CW, D’Orso I. CDK9: a signaling hub for transcriptional control. Transcription. 2019;10:57–75. [PMC free article] [PubMed] [Google Scholar]
64. Franco LC, Morales F, Boffo S, Giordano A. CDK9: a key player in cancer and other diseases. J Cell Biochem. 2018;119:1273–1284. [PubMed] [Google Scholar]
65. Poon E, Liang T, Jamin Y, Walz S, Kwok C, Hakkert A, Barker K, Urban Z, Thway K, Zeid R, Hallsworth A, Box G, Ebus ME, Licciardello MP, Sbirkov Y, Lazaro G, Calton E, Costa BM, Valenti M, De Haven Brandon A, Webber H, Tardif N, Almeida GS, Christova R, Boysen G, Richards MW, Barone G, Ford A, Bayliss R, Clarke PA, De Bono J, Gray NS, Blagg J, Robinson SP, Eccles SA, Zheleva D, Bradner JE, Molenaar J, Vivanco I, Eilers M, Workman P, Lin CY, Chesler L. Orally bioavailable CDK9/2 inhibitor shows mechanism-based therapeutic potential in MYCN-driven neuroblastoma. J Clin Invest. 2020;130:5875–5892. [PMC free article] [PubMed] [Google Scholar]
66. Cidado J, Boiko S, Proia T, Ferguson D, Criscione SW, San Martin M, Pop-Damkov P, Su N, Roamio Franklin VN, Sekhar Reddy Chilamakuri C, D’Santos CS, Shao W, Saeh JC, Koch R, Weinstock DM, Zinda M, Fawell SE, Drew L. AZD4573 is a highly selective CDK9 inhibitor that suppresses MCL-1 and induces apoptosis in hematologic cancer cells. Clin Cancer Res. 2020;26:922–934. [PubMed] [Google Scholar]
67. McLaughlin RP, He J, van der Noord VE, Redel J, Foekens JA, Martens JWM, Smid M, Zhang Y, van de Water B. A kinase inhibitor screen identifies a dual cdc7/CDK9 inhibitor to sensitise triple-negative breast cancer to EGFR-targeted therapy. Breast Cancer Res. 2019;21:77. [PMC free article] [PubMed] [Google Scholar]
68. Li J, Zhi X, Chen S, Shen X, Chen C, Yuan L, Guo J, Meng D, Chen M, Yao L. CDK9 inhibitor CDKI-73 is synergetic lethal with PARP inhibitor olaparib in BRCA1 wide-type ovarian cancer. Am J Cancer Res. 2020;10:1140–1155. [PMC free article] [PubMed] [Google Scholar]
69. Zhang H, Pandey S, Travers M, Sun H, Morton G, Madzo J, Chung W, Khowsathit J, Perez-Leal O, Barrero CA, Merali C, Okamoto Y, Sato T, Pan J, Garriga J, Bhanu NV, Simithy J, Patel B, Huang J, Raynal NJ, Garcia BA, Jacobson MA, Kadoch C, Merali S, Zhang Y, Childers W, Abou-Gharbia M, Karanicolas J, Baylin SB, Zahnow CA, Jelinek J, Graña X, Issa JJ. Targeting CDK9 reactivates epigenetically silenced genes in cancer. Cell. 2018;175:1244–1258. e1226. [PMC free article] [PubMed] [Google Scholar]
70. Wu T, Qin Z, Tian Y, Wang J, Xu C, Li Z, Bian J. Recent developments in the biology and medicinal chemistry of CDK9 inhibitors: an update. J Med Chem. 2020;63:13228–13257. [PubMed] [Google Scholar]
71. Anda S, Rothe C, Boye E, Grallert B. Consequences of abnormal CDK activity in S phase. Cell Cycle. 2016;15:963–973. [PMC free article] [PubMed] [Google Scholar]
72. Cherukupalli S, Chandrasekaran B, Aleti RR, Sayyad N, Hampannavar GA, Merugu SR, Rachamalla HR, Banerjee R, Karpoormath R. Synthesis of 4,6-disubstituted pyrazolo[3,4-d] pyrimidine analogues: cyclin-dependent kinase 2 (CDK2) inhibition, molecular docking and anticancer evaluation. Bioorg Chem. 2018;79:46–59. [PubMed] [Google Scholar]
73. Galbraith MD, Bender H, Espinosa JM. Therapeutic targeting of transcriptional cyclin-dependent kinases. Transcription. 2019;10:118–136. [PMC free article] [PubMed] [Google Scholar]
74. Cheng SW, Kuzyk MA, Moradian A, Ichu TA, Chang VC, Tien JF, Vollett SE, Griffith M, Marra MA, Morin GB. Interaction of cyclin-dependent kinase 12/CrkRS with cyclin K1 is required for the phosphorylation of the C-terminal domain of RNA polymerase II. Mol Cell Biol. 2012;32:4691–4704. [PMC free article] [PubMed] [Google Scholar]
75. Choi HJ, Jin S, Cho H, Won HY, An HW, Jeong GY, Park YU, Kim HY, Park MK, Son T, Min KW, Jang KS, Oh YH, Lee JY, Kong G. CDK12 drives breast tumor initiation and trastuzumab resistance via WNT and IRS1-ErbB-PI3K signaling. EMBO Rep. 2019;20:e48058. [PMC free article] [PubMed] [Google Scholar]
76. Henry KL, Kellner D, Bajrami B, Anderson JE, Beyna M, Bhisetti G, Cameron T, Capacci AG, Bertolotti-Ciarlet A, Feng J, Gao B, Hopkins B, Jenkins T, Li K, May-Dracka T, Murugan P, Wei R, Zeng W, Allaire N, Buckler A, Loh C, Juhasz P, Lucas B, Ennis KA, Vollman E, Cahir-McFarland E, Hett EC, Ols ML. CDK12-mediated transcriptional regulation of noncanonical NF-κB components is essential for signaling. Sci Signal. 2018;11:eaam8216. [PubMed] [Google Scholar]
77. Liu H, Shin SH, Chen H, Liu T, Li Z, Hu Y, Liu F, Zhang C, Kim DJ, Liu K, Dong Z. CDK12 and PAK2 as novel therapeutic targets for human gastric cancer. Theranostics. 2020;10:6201–6215. [PMC free article] [PubMed] [Google Scholar]
78. Naidoo K, Wai PT, Maguire SL, Daley F, Haider S, Kriplani D, Campbell J, Mirza H, Grigoriadis A, Tutt A, Moseley PM, Abdel-Fatah TMA, Chan SYT, Madhusudan S, Rhaka EA, Ellis IO, Lord CJ, Yuan Y, Green AR, Natrajan R. Evaluation of CDK12 protein expression as a potential novel biomarker for DNA damage response-targeted therapies in breast cancer. Mol Cancer Ther. 2018;17:306–315. [PMC free article] [PubMed] [Google Scholar]
79. Peng F, Yang C, Kong Y, Huang X, Chen Y, Zhou Y, Xie X, Liu P. CDK12 promotes breast cancer progression and maintains stemness by activating c-myc/β-catenin signaling. Curr Cancer Drug Targets. 2020;20:156–165. [PubMed] [Google Scholar]
80. Tien JF, Mazloomian A, Cheng SG, Hughes CS, Chow CCT, Canapi LT, Oloumi A, Trigo-Gonzalez G, Bashashati A, Xu J, Chang VC, Shah SP, Aparicio S, Morin GB. CDK12 regulates alternative last exon mRNA splicing and promotes breast cancer cell invasion. Nucleic Acids Res. 2017;45:6698–6716. [PMC free article] [PubMed] [Google Scholar]
81. Hopkins JL, Zou L. Induction of BRCAness in triple-negative breast cancer by a CDK12/13 inhibitor improves chemotherapy. Cancer Cell. 2019;36:461–463. [PubMed] [Google Scholar]
82. Quereda V, Bayle S, Vena F, Frydman SM, Monastyrskyi A, Roush WR, Duckett DR. Therapeutic targeting of CDK12/CDK13 in triple-negative breast cancer. Cancer Cell. 2019;36:545–558. e547. [PubMed] [Google Scholar]
83. Zhang T, Kwiatkowski N, Olson CM, Dixon-Clarke SE, Abraham BJ, Greifenberg AK, Ficarro SB, Elkins JM, Liang Y, Hannett NM, Manz T, Hao M, Bartkowiak B, Greenleaf AL, Marto JA, Geyer M, Bullock AN, Young RA, Gray NS. Covalent targeting of remote cysteine residues to develop CDK12 and CDK13 inhibitors. Nat Chem Biol. 2016;12:876–884. [PMC free article] [PubMed] [Google Scholar]
84. Wang C, Wang H, Lieftink C, du Chatinier A, Gao D, Jin G, Jin H, Beijersbergen RL, Qin W, Bernards R. CDK12 inhibition mediates DNA damage and is synergistic with sorafenib treatment in hepatocellular carcinoma. Gut. 2020;69:727–736. [PubMed] [Google Scholar]
85. Goel S, DeCristo MJ, Watt AC, BrinJones H, Sceneay J, Li BB, Khan N, Ubellacker JM, Xie S, Metzger-Filho O, Hoog J, Ellis MJ, Ma CX, Ramm S, Krop IE, Winer EP, Roberts TM, Kim HJ, McAllister SS, Zhao JJ. CDK4/6 inhibition triggers anti-tumour immunity. Nature. 2017;548:471–475. [PMC free article] [PubMed] [Google Scholar]
86. Schaer DA, Beckmann RP, Dempsey JA, Huber L, Forest A, Amaladas N, Li Y, Wang YC, Rasmussen ER, Chin D, Capen A, Carpenito C, Staschke KA, Chung LA, Litchfield LM, Merzoug FF, Gong X, Iversen PW, Buchanan S, de Dios A, Novosiadly RD, Kalos M. The CDK4/6 inhibitor abemaciclib induces a T Cell inflamed tumor microenvironment and enhances the efficacy of PD-L1 checkpoint blockade. Cell Rep. 2018;22:2978–2994. [PubMed] [Google Scholar]
87. Zhang J, Bu X, Wang H, Zhu Y, Geng Y, Nihira NT, Tan Y, Ci Y, Wu F, Dai X, Guo J, Huang YH, Fan C, Ren S, Sun Y, Freeman GJ, Sicinski P, Wei W. Cyclin D-CDK4 kinase destabilizes PD-L1 via cullin 3-SPOP to control cancer immune surveillance. Nature. 2018;553:91–95. [PMC free article] [PubMed] [Google Scholar]
88. Deng J, Wang ES, Jenkins RW, Li S, Dries R, Yates K, Chhabra S, Huang W, Liu H, Aref AR, Ivanova E, Paweletz CP, Bowden M, Zhou CW, Herter-Sprie GS, Sorrentino JA, Bisi JE, Lizotte PH, Merlino AA, Quinn MM, Bufe LE, Yang A, Zhang Y, Zhang H, Gao P, Chen T, Cavanaugh ME, Rode AJ, Haines E, Roberts PJ, Strum JC, Richards WG, Lorch JH, Parangi S, Gunda V, Boland GM, Bueno R, Palakurthi S, Freeman GJ, Ritz J, Haining WN, Sharpless NE, Arthanari H, Shapiro GI, Barbie DA, Gray NS, Wong KK. CDK4/6 inhibition augments antitumor immunity by Enhancing T-cell activation. Cancer Discov. 2018;8:216–233. [PMC free article] [PubMed] [Google Scholar]
89. Kruse U, Pallasch CP, Bantscheff M, Eberhard D, Frenzel L, Ghidelli S, Maier SK, Werner T, Wendtner CM, Drewes G. Chemoproteomics-based kinome profiling and target deconvolution of clinical multi-kinase inhibitors in primary chronic lymphocytic leukemia cells. Leukemia. 2011;25:89–100. [PubMed] [Google Scholar]
90. Gao N, Dai Y, Rahmani M, Dent P, Grant S. Contribution of disruption of the nuclear factor-κB pathway to induction of apoptosis in human leukemia cells by histone deacetylase Inhibitors and flavopiridol. Mol Pharmacol. 2004;66:956–63. [PubMed] [Google Scholar]
91. Dai Y, Rahmani M, Grant S. Proteasome inhibitors potentiate leukemic cell apoptosis induced by the cyclin-dependent kinase inhibitor flavopiridol through a SAPK/JNK- and NF-κB-dependent process. Oncogene. 2003;22:7108–7122. [PubMed] [Google Scholar]
92. Lin TS, Blum KA, Fischer DB, Mitchell SM, Ruppert AS, Porcu P, Kraut EH, Baiocchi RA, Moran ME, Johnson AJ, Schaaf LJ, Grever MR, Byrd JC. Flavopiridol, fludarabine, and rituximab in mantle cell lymphoma and indolent B-cell lymphoproliferative disorders. J. Clin. Oncol. 2010;28:418–423. [PMC free article] [PubMed] [Google Scholar]
93. Wu YM, Cieślik M, Lonigro RJ, Vats P, Reimers MA, Cao X, Ning Y, Wang L, Kunju LP, de Sarkar N, Heath EI, Chou J, Feng FY, Nelson PS, de Bono JS, Zou W, Montgomery B, Alva A, Robinson DR, Chinnaiyan AM. Inactivation of CDK12 delineates a distinct immunogenic class of advanced prostate cancer. Cell. 2018;173:1770–1782. e1714. [PMC free article] [PubMed] [Google Scholar]
94. Antonarakis ES. Cyclin-dependent kinase 12, immunity, and prostate cancer. N Engl J Med. 2018;379:1087–1089. [PubMed] [Google Scholar]
95. Li Y, Zhang H, Li Q, Zou P, Huang X, Wu C, Tan L. CDK12/13 inhibition induces immunogenic cell death and enhances anti-PD-1 anticancer activity in breast cancer. Cancer Lett. 2020;495:12–21. [PubMed] [Google Scholar]
96. Siemeister G, Luecking U, Wagner C, Detjen K, Mc Coy C, Bosslet K. Molecular and pharmacodynamic characteristics of the novel multi-target tumor growth inhibitor ZK 304709. Biomed Pharmacother. 2006;60:269–272. [PubMed] [Google Scholar]
97. Cho SJ, Lee SS, Kim YJ, Park BD, Choi JS, Liu L, Ham YM, Moon Kim B, Lee SK. Xylocydine, a novel Cdk inhibitor, is an effective inducer of apoptosis in hepatocellular carcinoma cells in vitro and in vivo. Cancer Lett. 2010;287:196–206. [PubMed] [Google Scholar]
98. Ham YM, Choi KJ, Song SY, Jin YH, Chun MW, Lee SK. Xylocydine, a novel inhibitor of cyclin-dependent kinases, prevents the tumor necrosis factor-related apoptosis-inducing ligand-induced apoptotic cell death of SK-HEP-1 cells. J Pharmacol Exp Ther. 2004;308:814–819. [PubMed] [Google Scholar]
99. Wu Y, Chen C, Sun X, Shi X, Jin B, Ding K, Yeung SC, Pan J. Cyclin-dependent kinase 7/9 inhibitor SNS-032 abrogates FIP1-like-1 platelet-derived growth factor receptor alpha and bcr-abl oncogene addiction in malignant hematologic cells. Clin Cancer Res. 2012;18:1966–1978. [PubMed] [Google Scholar]
100. Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ, Qian L, Chen BC, Zhao R, Bednarz MS, Kellar KA, Mulheron JG, Batorsky R, Roongta U, Kamath A, Marathe P, Ranadive SA, Sack JS, Tokarski JS, Pavletich NP, Lee FY, Webster KR, Kimball SD. Correction to N-(Cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-Dimethylethyl)-2-oxazolyl] methyl] thio] -2-thiazolyl] -4-piperidineca rboxamide (BMS-387032), a highly efficacious and selective antitumor agent. J Med Chem. 2015;58:7609. [PubMed] [Google Scholar]
101. Kamath AV, Chong S, Chang M, Marathe PH. P-glycoprotein plays a role in the oral absorption of BMS-387032, a potent cyclin-dependent kinase 2 inhibitor, in rats. Cancer Chemother Pharmacol. 2005;55:110–116. [PubMed] [Google Scholar]
102. Misra RN, Xiao HY, Kim KS, Lu S, Han WC, Barbosa SA, Hunt JT, Rawlins DB, Shan W, Ahmed SZ, Qian L, Chen BC, Zhao R, Bednarz MS, Kellar KA, Mulheron JG, Batorsky R, Roongta U, Kamath A, Marathe P, Ranadive SA, Sack JS, Tokarski JS, Pavletich NP, Lee FY, Webster KR, Kimball SD. N-(cycloalkylamino)acyl-2-aminothiazole inhibitors of cyclin-dependent kinase 2. N-[5-[[[5-(1,1-dimethylethyl)-2-oxazolyl]methyl]thio]-2-thiazolyl]-4-piperidinecarboxamide (BMS-387032), a highly efficacious and selective antitumor agent. J Med Chem. 2004;47:1719–1728. [PubMed] [Google Scholar]
103. Sorf A, Novotna E, Hofman J, Morell A, Staud F, Wsol V, Ceckova M. Cyclin-dependent kinase inhibitors AZD5438 and R547 show potential for enhancing efficacy of daunorubicin-based anticancer therapy: interaction with carbonyl-reducing enzymes and ABC transporters. Biochem Pharmacol. 2019;163:290–298. [PubMed] [Google Scholar]
104. DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R, Xiang Q, Tovar C, Blain R, Nevins T, Higgins B, Luistro L, Kolinsky K, Felix B, Hussain S, Heimbrook D. In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. Mol Cancer Ther. 2006;5:2644–2658. [PubMed] [Google Scholar]
105. Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N. Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6-methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity. J Med Chem. 2006;49:6549–6560. [PubMed] [Google Scholar]
106. Caligiuri M, Becker F, Murthi K, Kaplan F, Dedier S, Kaufmann C, Machl A, Zybarth G, Richard J, Bockovich N, Kluge A, Kley N. A proteome-wide CDK/CRK-specific kinase inhibitor promotes tumor cell death in the absence of cell cycle progression. Chem Biol. 2005;12:1103–1115. [PubMed] [Google Scholar]
107. Gray NS, Wodicka L, Thunnissen AM, Norman TC, Kwon S, Espinoza FH, Morgan DO, Barnes G, LeClerc S, Meijer L, Kim SH, Lockhart DJ, Schultz PG. Exploiting chemical libraries, structure, and genomics in the search for kinase inhibitors. Science. 1998;281:533–538. [PubMed] [Google Scholar]
108. Villerbu N, Gaben AM, Redeuilh G, Mester J. Cellular effects of purvalanol A: a specific inhibitor of cyclin-dependent kinase activities. Int J Cancer. 2002;97:761–769. [PubMed] [Google Scholar]
109. Echalier A, Cot E, Camasses A, Hodimont E, Hoh F, Jay P, Sheinerman F, Krasinska L, Fisher D. An integrated chemical biology approach provides insight into Cdk2 functional redundancy and inhibitor sensitivity. Chem Biol. 2012;19:1028–1040. [PubMed] [Google Scholar]
110. Raynaud FI, Whittaker SR, Fischer PM, McClue S, Walton MI, Barrie SE, Garrett MD, Rogers P, Clarke SJ, Kelland LR, Valenti M, Brunton L, Eccles S, Lane DP, Workman P. In vitro and in vivo pharmaco*kinetic-pharmacodynamic relationships for the trisubstituted aminopurine cyclin-dependent kinase inhibitors olomoucine, bohemine and CYC202. Clin Cancer Res. 2005;11:4875–4887. [PubMed] [Google Scholar]
111. McMillin DW, Delmore J, Negri J, Buon L, Jacobs HM, Laubach J, Jakubikova J, Ooi M, Hayden P, Schlossman R, Munshi NC, Lengauer C, Richardson PG, Anderson KC, Mitsiades CS. Molecular and cellular effects of multi-targeted cyclin-dependent kinase inhibition in myeloma: biological and clinical implications. Br J Haematol. 2011;152:420–432. [PMC free article] [PubMed] [Google Scholar]
112. Bettayeb K, Tirado OM, Marionneau-Lambot S, Ferandin Y, Lozach O, Morris JC, Mateo-Lozano S, Drueckes P, Schachtele C, Kubbutat MH, Liger F, Marquet B, Joseph B, Echalier A, Endicott JA, Notario V, Meijer L. Meriolins, a new class of cell death inducing kinase inhibitors with enhanced selectivity for cyclin-dependent kinases. Cancer Res. 2007;67:8325–8334. [PubMed] [Google Scholar]
113. Krystof V, Chamrad I, Jorda R, Kohoutek J. Pharmacological targeting of CDK9 in cardiac hypertrophy. Med Res Rev. 2010;30:646–666. [PubMed] [Google Scholar]
114. Zaharevitz DW, Gussio R, Leost M, Senderowicz AM, Lahusen T, Kunick C, Meijer L, Sausville EA. Discovery and initial characterization of the paullones, a novel class of small-molecule inhibitors of cyclin-dependent kinases. Cancer Res. 1999;59:2566–2569. [PubMed] [Google Scholar]
115. Lyssiotis CA, Foreman RK, Staerk J, Garcia M, Mathur D, Markoulaki S, Hanna J, Lairson LL, Charette BD, Bouchez LC, Bollong M, Kunick C, Brinker A, Cho CY, Schultz PG, Jaenisch R. Reprogramming of murine fibroblasts to induced pluripotent stem cells with chemical complementation of Klf4. Proc Natl Acad Sci U S A. 2009;106:8912–8917. [PMC free article] [PubMed] [Google Scholar]
116. Rodland GE, Melhus K, Generalov R, Gilani S, Bertoni F, Dahle J, Syljuasen RG, Patzke S. The dual cell cycle kinase inhibitor JNJ-7706621 reverses resistance to CD37-targeted radioimmunotherapy in activated B cell like diffuse Large B cell lymphoma cell lines. Front Oncol. 2019;9:1301. [PMC free article] [PubMed] [Google Scholar]
117. Zhong S, Wu B, Dong X, Han Y, Jiang S, Zhang Y, Bai Y, Luo SX, Chen Y, Zhang H, Zhao G. Identification of driver genes and key pathways of glioblastoma shows JNJ-7706621 as a novel antiglioblastoma drug. World Neurosurg. 2018;109:e329–e342. [PubMed] [Google Scholar]
118. Guo Q, Jin L, Zhu HY, Xing XX, Xuan MF, Luo QR, Zhang GL, Luo ZB, Wang JX, Yin XJ, Kang JD. The cyclin-dependent kinase inhibitor, JNJ-7706621, improves in vitro developmental competence of porcine parthenogenetic activation and somatic cell nuclear transfer embryos. Reprod Fertil Dev. 2018;30:1002–1010. [PubMed] [Google Scholar]
119. Matsuhashi A, Ohno T, Kimura M, Hara A, Saio M, Nagano A, Kawai G, Saitou M, Takigami I, Yamada K, Okano Y, Shimizu K. Growth suppression and mitotic defect induced by JNJ-7706621, an inhibitor of cyclin-dependent kinases and aurora kinases. Curr Cancer Drug Targets. 2012;12:625–639. [PubMed] [Google Scholar]
120. Danhier F, Ucakar B, Magotteaux N, Brewster ME, Preat V. Active and passive tumor targeting of a novel poorly soluble cyclin dependent kinase inhibitor, JNJ-7706621. Int J Pharm. 2010;392:20–28. [PubMed] [Google Scholar]
121. Emanuel S, Rugg CA, Gruninger RH, Lin R, Fuentes-Pesquera A, Connolly PJ, Wetter SK, Hollister B, Kruger WW, Napier C, Jolliffe L, Middleton SA. The in vitro and in vivo effects of JNJ-7706621: a dual inhibitor of cyclin-dependent kinases and aurora kinases. Cancer Res. 2005;65:9038–9046. [PubMed] [Google Scholar]
122. Hoessel R, Leclerc S, Endicott JA, Nobel ME, Lawrie A, Tunnah P, Leost M, Damiens E, Marie D, Marko D, Niederberger E, Tang W, Eisenbrand G, Meijer L. Indirubin, the active constituent of a Chinese antileukaemia medicine, inhibits cyclin-dependent kinases. Nat Cell Biol. 1999;1:60–67. [PubMed] [Google Scholar]
123. Heredia A, Davis C, Bamba D, Le N, Gwarzo MY, Sadowska M, Gallo RC, Redfield RR. Indirubin-3’-monoxime, a derivative of a Chinese antileukemia medicine, inhibits P-TEFb function and HIV-1 replication. AIDS. 2005;19:2087–2095. [PubMed] [Google Scholar]
124. Leclerc S, Garnier M, Hoessel R, Marko D, Bibb JA, Snyder GL, Greengard P, Biernat J, Wu YZ, Mandelkow EM, Eisenbrand G, Meijer L. Indirubins inhibit glycogen synthase kinase-3 beta and CDK5/p25, two protein kinases involved in abnormal tau phosphorylation in Alzheimer’s disease. A property common to most cyclin-dependent kinase inhibitors? J Biol Chem. 2001;276:251–260. [PubMed] [Google Scholar]
125. Byth KF, Thomas A, Hughes G, Forder C, McGregor A, Geh C, Oakes S, Green C, Walker M, Newcombe N, Green S, Growcott J, Barker A, Wilkinson RW. AZD5438, a potent oral inhibitor of cyclin-dependent kinases 1, 2, and 9, leads to pharmacodynamic changes and potent antitumor effects in human tumor xenografts. Mol Cancer Ther. 2009;8:1856–1866. [PubMed] [Google Scholar]
126. Jones CD, Andrews DM, Barker AJ, Blades K, Daunt P, East S, Geh C, Graham MA, Johnson KM, Loddick SA, McFarland HM, McGregor A, Moss L, Rudge DA, Simpson PB, Swain ML, Tam KY, Tucker JA, Walker M. The discovery of AZD5597, a potent imidazole pyrimidine amide CDK inhibitor suitable for intravenous dosing. Bioorg Med Chem Lett. 2008;18:6369–6373. [PubMed] [Google Scholar]
127. Vermeulen K, Strnad M, Krystof V, Havlicek L, Van der Aa A, Lenjou M, Nijs G, Rodrigus I, Stockman B, van Onckelen H, Van Bockstaele DR, Berneman ZN. Antiproliferative effect of plant cytokinin analogues with an inhibitory activity on cyclin-dependent kinases. Leukemia. 2002;16:299–305. [PubMed] [Google Scholar]
128. Kitagawa M, Higashi H, Takahashi IS, Okabe T, Ogino H, Taya Y, Hishimura S, Okuyama A. A cyclin-dependent kinase inhibitor, butyrolactone I, inhibits phosphorylation of RB protein and cell cycle progression. Oncogene. 1994;9:2549–2557. [PubMed] [Google Scholar]
129. Meijer L, Thunnissen AM, White AW, Garnier M, Nikolic M, Tsai LH, Walter J, Cleverley KE, Salinas PC, Wu YZ, Biernat J, Mandelkow EM, Kim SH, Pettit GR. Inhibition of cyclin-dependent kinases, GSK-3beta and CK1 by hymenialdisine, a marine sponge constituent. Chem Biol. 2000;7:51–63. [PubMed] [Google Scholar]
130. Jessen BA, Lee L, Koudriakova T, Haines M, Lundgren K, Price S, Nonomiya J, Lewis C, Stevens GJ. Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors. J Appl Toxicol. 2007;27:133–142. [PubMed] [Google Scholar]
131. Chen P, Lee NV, Hu W, Xu M, Ferre RA, Lam H, Bergqvist S, Solowiej J, Diehl W, He YA, Yu X, Nagata A, VanArsdale T, Murray BW. Spectrum and degree of CDK drug interactions predicts clinical performance. Mol Cancer Ther. 2016;15:2273–2281. [PubMed] [Google Scholar]
132. Mettey Y, Gompel M, Thomas V, Garnier M, Leost M, Ceballos-Picot I, Noble M, Endicott J, Vierfond JM, Meijer L. Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003;46:222–236. [PubMed] [Google Scholar]
133. Lahusen T, De Siervi A, Kunick C, Senderowicz AM. Alsterpaullone, a novel cyclin-dependent kinase inhibitor, induces apoptosis by activation of caspase-9 due to perturbation in mitochondrial membrane potential. Mol Carcinog. 2003;36:183–194. [PubMed] [Google Scholar]
134. Leost M, Schultz C, Link A, Wu YZ, Biernat J, Mandelkow EM, Bibb JA, Snyder GL, Greengard P, Zaharevitz DW, Gussio R, Senderowicz AM, Sausville EA, Kunick C, Meijer L. Paullones are potent inhibitors of glycogen synthase kinase-3beta and cyclin-dependent kinase 5/p25. Eur J Biochem. 2000;267:5983–5994. [PubMed] [Google Scholar]
135. Chang YT, Gray NS, Rosania GR, Sutherlin DP, Kwon S, Norman TC, Sarohia R, Leost M, Meijer L, Schultz PG. Synthesis and application of functionally diverse 2,6,9-trisubstituted purine libraries as CDK inhibitors. Chem Biol. 1999;6:361–375. [PubMed] [Google Scholar]
136. Kabadi SV, Stoica BA, Loane DJ, Luo T, Faden AI. CR8, a novel inhibitor of CDK, limits microglial activation, astrocytosis, neuronal loss, and neurologic dysfunction after experimental traumatic brain injury. J Cereb Blood Flow Metab. 2014;34:502–513. [PMC free article] [PubMed] [Google Scholar]
137. Bettayeb K, Oumata N, Echalier A, Ferandin Y, Endicott JA, Galons H, Meijer L. CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases. Oncogene. 2008;27:5797–5807. [PubMed] [Google Scholar]
138. Dey J, Deckwerth TL, Kerwin WS, Casalini JR, Merrell AJ, Grenley MO, Burns C, Ditzler SH, Dixon CP, Beirne E, Gillespie KC, Kleinman EF, Klinghoffer RA. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk Diffuse Large B-cell Lymphoma to BCL2 inhibition. Sci Rep. 2017;7:18007. [PMC free article] [PubMed] [Google Scholar]
139. Gupta S, Jain MM, Maru A, Nag SM, Somani N, Mehta AO, Kulkarni S, Acharya SA, Dhobe P, Jadhav N. A phase I study of selective cyclin dependent kinase inhibitor P1446A-05 administered on an intermittent schedule in patients with advanced refractory tumors. J. Clin. Oncol. 2012;30:3011–3011. [Google Scholar]
140. Hao D, Chu Q, Welch S, Yau CYF, Spratlin JL, Tang P, MacKenzie MJ, Townsley CA, Arndt D, Johnson L, Trapsa D, Degendorfer P, Kulkarni S, Jawlekar G, Dhobe P, Oza AM. A phase I and pharmaco*kinetic (PK) study of continuous daily administration of P1446A-05, a potent and specific oral Cdk4 inhibitor. J. Clin. Oncol. 2012;30:3013–3013. [Google Scholar]
141. Paiva C, Godbersen JC, Soderquist RS, Rowland T, Kilmarx S, Spurgeon SE, Brown JR, Srinivasa SP, Danilov AV. Cyclin-dependent kinase inhibitor P1446A induces apoptosis in a JNK/p38 MAPK-dependent manner in chronic lymphocytic leukemia B-Cells. PLoS One. 2015;10:e0143685. [PMC free article] [PubMed] [Google Scholar]
