Literature DB >> 24900195

Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases.

Kamil Paruch1, Michael P Dwyer1, Carmen Alvarez1, Courtney Brown1, Tin-Yau Chan1, Ronald J Doll1, Kerry Keertikar1, Chad Knutson1, Brian McKittrick1, Jocelyn Rivera1, Randall Rossman1, Greg Tucker1, Thierry Fischmann1, Alan Hruza1, Vincent Madison1, Amin A Nomeir1, Yaolin Wang1, Paul Kirschmeier1, Emma Lees2, David Parry2, Nicole Sgambellone2, Wolfgang Seghezzi2, Lesley Schultz2, Frances Shanahan2, Derek Wiswell2, Xiaoying Xu1, Quiao Zhou1, Ray A James3, Vidyadhar M Paradkar3, Haengsoon Park3, Laura R Rokosz3, Tara M Stauffer3, Timothy J Guzi1.   

Abstract

Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncology therapeutics. Herein is described the utilization of an in vivo screening approach with integrated efficacy and tolerability parameters to identify candidate CDK inhibitors with a suitable balance of activity and tolerability. This approach has resulted in the identification of SCH 727965, a potent and selective CDK inhibitor that is currently undergoing clinical evaluation.

Keywords:  Cyclin-dependent kinase; SCH 727965; oncology therapeutics

Year:  2010        PMID： 24900195      PMCID： PMC4007794          DOI： 10.1021/ml100051d

Source DB:  PubMed          Journal:  ACS Med Chem Lett        ISSN： 1948-5875            Impact factor:   4.345


  27 in total

Review 1.  Regulation of RNA polymerase II activity by CTD phosphorylation and cell cycle control.

Authors:  Thomas Oelgeschläger
Journal:  J Cell Physiol       Date:  2002-02       Impact factor: 6.384

Review 2.  Recycling the cell cycle: cyclins revisited.

Authors:  Andrew W Murray
Journal:  Cell       Date:  2004-01-23       Impact factor: 41.582

3.  Unmasking the redundancy between Cdk1 and Cdk2 at G2 phase in human cancer cell lines.

Authors:  Lawrence L'Italien; Marcel Tanudji; Loren Russell; Xiao Min Schebye
Journal:  Cell Cycle       Date:  2006-05-01       Impact factor: 4.534

Review 4.  Regulation of the cell cycle by the Rb tumor suppressor family.

Authors:  M E Ewen
Journal:  Results Probl Cell Differ       Date:  1998

5.  Combined depletion of cell cycle and transcriptional cyclin-dependent kinase activities induces apoptosis in cancer cells.

Authors:  Dongpo Cai; Vaughan M Latham; Xinxin Zhang; Geoffrey I Shapiro
Journal:  Cancer Res       Date:  2006-09-15       Impact factor: 12.701

Review 6.  Cyclin-dependent kinase pathways as targets for cancer treatment.

Authors:  Geoffrey I Shapiro
Journal:  J Clin Oncol       Date:  2006-04-10       Impact factor: 44.544

7.  In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials.

Authors:  Wanda DePinto; Xin-Jie Chu; Xuefeng Yin; Melissa Smith; Kathryn Packman; Petra Goelzer; Allen Lovey; Yingsi Chen; Hong Qian; Rachid Hamid; Qing Xiang; Christian Tovar; Roger Blain; Tom Nevins; Brian Higgins; Leopoldo Luistro; Kenneth Kolinsky; Bernardo Felix; Sazzad Hussain; David Heimbrook
Journal:  Mol Cancer Ther       Date:  2006-11       Impact factor: 6.261

8.  Dinaciclib (SCH 727965), a novel and potent cyclin-dependent kinase inhibitor.

Authors:  David Parry; Timothy Guzi; Frances Shanahan; Nicole Davis; Deepa Prabhavalkar; Derek Wiswell; Wolfgang Seghezzi; Kamil Paruch; Michael P Dwyer; Ronald Doll; Amin Nomeir; William Windsor; Thierry Fischmann; Yaolin Wang; Martin Oft; Taiying Chen; Paul Kirschmeier; Emma M Lees
Journal:  Mol Cancer Ther       Date:  2010-07-27       Impact factor: 6.261

Review 9.  Flavopiridol in the treatment of chronic lymphocytic leukemia.

Authors:  Beth A Christian; Michael R Grever; John C Byrd; Thomas S Lin
Journal:  Curr Opin Oncol       Date:  2007-11       Impact factor: 3.645

10.  Pyrazolo[1,5-a]pyrimidines as orally available inhibitors of cyclin-dependent kinase 2.

Authors:  Kamil Paruch; Michael P Dwyer; Carmen Alvarez; Courtney Brown; Tin-Yau Chan; Ronald J Doll; Kerry Keertikar; Chad Knutson; Brian McKittrick; Jocelyn Rivera; Randall Rossman; Greg Tucker; Thierry O Fischmann; Alan Hruza; Vincent Madison; Amin A Nomeir; Yaolin Wang; Emma Lees; David Parry; Nicole Sgambellone; Wolfgang Seghezzi; Lesley Schultz; Fran Shanahan; Derek Wiswell; Xiaoying Xu; Quiao Zhou; Ray A James; Vidyadhar M Paradkar; Haengsoon Park; Laura R Rokosz; Tara M Stauffer; Timothy J Guzi
Journal:  Bioorg Med Chem Lett       Date:  2007-09-08       Impact factor: 2.823
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  43 in total

1.  Initial testing (stage 1) of the cyclin dependent kinase inhibitor SCH 727965 (dinaciclib) by the pediatric preclinical testing program.

Authors:  Richard Gorlick; E Anders Kolb; Peter J Houghton; Christopher L Morton; Geoffrey Neale; Stephen T Keir; Hernan Carol; Richard Lock; Doris Phelps; Min H Kang; C Patrick Reynolds; John M Maris; Catherine Billups; Malcolm A Smith
Journal:  Pediatr Blood Cancer       Date:  2012-02-07       Impact factor: 3.167

2.  The cyclin-dependent kinase inhibitor SCH 727965 (dinacliclib) induces the apoptosis of osteosarcoma cells.

Authors:  Wei Fu; Le Ma; Baoky Chu; Xue Wang; Marilyn M Bui; Jennifer Gemmer; Soner Altiok; W Jackson Pledger
Journal:  Mol Cancer Ther       Date:  2011-04-13       Impact factor: 6.261

3.  Discovery of Widespread Host Protein Interactions with the Pre-replicated Genome of CHIKV Using VIR-CLASP.

Authors:  Byungil Kim; Sarah Arcos; Katherine Rothamel; Jeffrey Jian; Kristie L Rose; W Hayes McDonald; Yuqi Bian; Seth Reasoner; Nicholas J Barrows; Shelton Bradrick; Mariano A Garcia-Blanco; Manuel Ascano
Journal:  Mol Cell       Date:  2020-05-06       Impact factor: 17.970

4.  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.

Authors:  Zahi Mitri; Cansu Karakas; Caimiao Wei; Brian Briones; Holly Simmons; Nuhad Ibrahim; Ricardo Alvarez; James L Murray; Khandan Keyomarsi; Stacy Moulder
Journal:  Invest New Drugs       Date:  2015-05-07       Impact factor: 3.850

5.  Cyclin-dependent kinase inhibitor dinaciclib interacts with the acetyl-lysine recognition site of bromodomains.

Authors:  Mathew P Martin; Sanne H Olesen; Gunda I Georg; Ernst Schönbrunn
Journal:  ACS Chem Biol       Date:  2013-09-10       Impact factor: 5.100

Review 6.  Chronic Lymphocytic Leukemia: Exploiting Vulnerabilities with Targeted Agents.

Authors:  Joseph Maly; James S Blachly
Journal:  Curr Hematol Malig Rep       Date:  2016-02       Impact factor: 3.952

Review 7.  Small Molecule Inhibitors in Chronic Lymphocytic Lymphoma and B Cell Non-Hodgkin Lymphoma.

Authors:  Allison Rosenthal
Journal:  Curr Hematol Malig Rep       Date:  2017-06       Impact factor: 3.952

Review 8.  Arrested Developments: CDK4/6 Inhibitor Resistance and Alterations in the Tumor Immune Microenvironment.

Authors:  Jessica L F Teh; Andrew E Aplin
Journal:  Clin Cancer Res       Date:  2018-10-04       Impact factor: 12.531

Review 9.  Emerging drug profile: cyclin-dependent kinase inhibitors.

Authors:  James S Blachly; John C Byrd
Journal:  Leuk Lymphoma       Date:  2013-07-29

10.  Development of highly potent and selective diaminothiazole inhibitors of cyclin-dependent kinases.

Authors:  Ernst Schonbrunn; Stephane Betzi; Riazul Alam; Mathew P Martin; Andreas Becker; Huijong Han; Rawle Francis; Ramappa Chakrasali; Sudhakar Jakkaraj; Aslamuzzaman Kazi; Said M Sebti; Christopher L Cubitt; Anthony W Gebhard; Lori A Hazlehurst; Joseph S Tash; Gunda I Georg
Journal:  J Med Chem       Date:  2013-05-06       Impact factor: 7.446
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