Literature DB >> 27326333

Design and Development of a Series of Potent and Selective Type II Inhibitors of CDK8.

Philippe Bergeron1, Michael F T Koehler1, Elizabeth M Blackwood1, Krista Bowman1, Kevin Clark1, Ron Firestein1, James R Kiefer1, Klaus Maskos2, Mark L McCleland1, Linda Orren1, Sreemathy Ramaswamy1, Laurent Salphati1, Steve Schmidt1, Elisabeth V Schneider3, Jiansheng Wu1, Maureen Beresini1.   

Abstract

Using Sorafenib as a starting point, a series of potent and selective inhibitors of CDK8 was developed. When cocrystallized with CDK8 and cyclin C, these compounds exhibit a Type-II (DMG-out) binding mode.

Entities:  

Keywords:  CDK8; DMG-out; Sorafenib; inhibitor

Year:  2016        PMID： 27326333      PMCID： PMC4904263          DOI： 10.1021/acsmedchemlett.6b00044

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


  18 in total

1.  A quantitative analysis of kinase inhibitor selectivity.

Authors:  Mazen W Karaman; Sanna Herrgard; Daniel K Treiber; Paul Gallant; Corey E Atteridge; Brian T Campbell; Katrina W Chan; Pietro Ciceri; Mindy I Davis; Philip T Edeen; Raffaella Faraoni; Mark Floyd; Jeremy P Hunt; Daniel J Lockhart; Zdravko V Milanov; Michael J Morrison; Gabriel Pallares; Hitesh K Patel; Stephanie Pritchard; Lisa M Wodicka; Patrick P Zarrinkar
Journal:  Nat Biotechnol       Date:  2008-01       Impact factor: 54.908

2.  An integrated suite of modeling tools that empower scientists in structure- and property-based drug design.

Authors:  Jianwen A Feng; Ignacio Aliagas; Philippe Bergeron; Jeff M Blaney; Erin K Bradley; Michael F T Koehler; Man-Ling Lee; Daniel F Ortwine; Vickie Tsui; Johnny Wu; Alberto Gobbi
Journal:  J Comput Aided Mol Des       Date:  2015-04-29       Impact factor: 3.686

3.  Development of a Potent, Specific CDK8 Kinase Inhibitor Which Phenocopies CDK8/19 Knockout Cells.

Authors:  Michael F T Koehler; Philippe Bergeron; Elizabeth M Blackwood; Krista Bowman; Kevin R Clark; Ron Firestein; James R Kiefer; Klaus Maskos; Mark L McCleland; Linda Orren; Laurent Salphati; Steve Schmidt; Elisabeth V Schneider; Jiansheng Wu; Maureen H Beresini
Journal:  ACS Med Chem Lett       Date:  2016-01-06       Impact factor: 4.345

4.  CDK8 maintains tumor dedifferentiation and embryonic stem cell pluripotency.

Authors:  Adam S Adler; Mark L McCleland; Tom Truong; Shari Lau; Zora Modrusan; Tim M Soukup; Merone Roose-Girma; Elizabeth M Blackwood; Ron Firestein
Journal:  Cancer Res       Date:  2012-02-16       Impact factor: 12.701

Review 5.  The mammalian Mediator complex and its role in transcriptional regulation.

Authors:  Ronald C Conaway; Shigeo Sato; Chieri Tomomori-Sato; Tingting Yao; Joan W Conaway
Journal:  Trends Biochem Sci       Date:  2005-05       Impact factor: 13.807

6.  Role of CDK8 and beta-catenin in colorectal adenocarcinoma.

Authors:  Jong-Og Seo; Song Iy Han; Sung-Chul Lim
Journal:  Oncol Rep       Date:  2010-07       Impact factor: 3.906

7.  Identification of N-(5-tert-butyl-isoxazol-3-yl)-N'-{4-[7-(2-morpholin-4-yl-ethoxy)imidazo[2,1-b][1,3]benzothiazol-2-yl]phenyl}urea dihydrochloride (AC220), a uniquely potent, selective, and efficacious FMS-like tyrosine kinase-3 (FLT3) inhibitor.

Authors:  Qi Chao; Kelly G Sprankle; Robert M Grotzfeld; Andiliy G Lai; Todd A Carter; Anne Marie Velasco; Ruwanthi N Gunawardane; Merryl D Cramer; Michael F Gardner; Joyce James; Patrick P Zarrinkar; Hitesh K Patel; Shripad S Bhagwat
Journal:  J Med Chem       Date:  2009-12-10       Impact factor: 7.446

8.  CDK8 expression in 470 colorectal cancers in relation to beta-catenin activation, other molecular alterations and patient survival.

Authors:  Ron Firestein; Kaori Shima; Katsuhiko Nosho; Natsumi Irahara; Yoshifumi Baba; Emeric Bojarski; Edward L Giovannucci; William C Hahn; Charles S Fuchs; Shuji Ogino
Journal:  Int J Cancer       Date:  2010-06-15       Impact factor: 7.396

9.  A selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.

Authors:  Trevor Dale; Paul A Clarke; Christina Esdar; Dennis Waalboer; Olajumoke Adeniji-Popoola; Maria-Jesus Ortiz-Ruiz; Aurélie Mallinger; Rahul S Samant; Paul Czodrowski; Djordje Musil; Daniel Schwarz; Klaus Schneider; Mark Stubbs; Ken Ewan; Elizabeth Fraser; Robert TePoele; Will Court; Gary Box; Melanie Valenti; Alexis de Haven Brandon; Sharon Gowan; Felix Rohdich; Florence Raynaud; Richard Schneider; Oliver Poeschke; Andree Blaukat; Paul Workman; Kai Schiemann; Suzanne A Eccles; Dirk Wienke; Julian Blagg
Journal:  Nat Chem Biol       Date:  2015-10-26       Impact factor: 15.040

10.  Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19.

Authors:  Aurélie Mallinger; Kai Schiemann; Christian Rink; Frank Stieber; Michel Calderini; Simon Crumpler; Mark Stubbs; Olajumoke Adeniji-Popoola; Oliver Poeschke; Michael Busch; Paul Czodrowski; Djordje Musil; Daniel Schwarz; Maria-Jesus Ortiz-Ruiz; Richard Schneider; Ching Thai; Melanie Valenti; Alexis de Haven Brandon; Rosemary Burke; Paul Workman; Trevor Dale; Dirk Wienke; Paul A Clarke; Christina Esdar; Florence I Raynaud; Suzanne A Eccles; Felix Rohdich; Julian Blagg
Journal:  J Med Chem       Date:  2016-01-21       Impact factor: 7.446
View more
  11 in total

1.  A precisely positioned MED12 activation helix stimulates CDK8 kinase activity.

Authors:  Felix Klatt; Alexander Leitner; Iana V Kim; Hung Ho-Xuan; Elisabeth V Schneider; Franziska Langhammer; Robin Weinmann; Melanie R Müller; Robert Huber; Gunter Meister; Claus-D Kuhn
Journal:  Proc Natl Acad Sci U S A       Date:  2020-01-27       Impact factor: 11.205

2.  Novel selective thiadiazine DYRK1A inhibitor lead scaffold with human pancreatic β-cell proliferation activity.

Authors:  Kunal Kumar; Peter Man-Un Ung; Peng Wang; Hui Wang; Hailing Li; Mary K Andrews; Andrew F Stewart; Avner Schlessinger; Robert J DeVita
Journal:  Eur J Med Chem       Date:  2018-08-22       Impact factor: 6.514

Review 3.  Structure-based discovery of cyclin-dependent protein kinase inhibitors.

Authors:  Mathew P Martin; Jane A Endicott; Martin E M Noble
Journal:  Essays Biochem       Date:  2017-11-08       Impact factor: 8.000

Review 4.  Inhibitors of cyclin-dependent kinases as cancer therapeutics.

Authors:  Steven R Whittaker; Aurélie Mallinger; Paul Workman; Paul A Clarke
Journal:  Pharmacol Ther       Date:  2017-02-05       Impact factor: 12.310

Review 5.  Structural insights into the functional diversity of the CDK-cyclin family.

Authors:  Daniel J Wood; Jane A Endicott
Journal:  Open Biol       Date:  2018-09       Impact factor: 6.411

Review 6.  Regulatory functions of the Mediator kinases CDK8 and CDK19.

Authors:  Charli B Fant; Dylan J Taatjes
Journal:  Transcription       Date:  2018-12-26

Review 7.  Therapeutic targeting of transcriptional cyclin-dependent kinases.

Authors:  Matthew D Galbraith; Heather Bender; Joaquín M Espinosa
Journal:  Transcription       Date:  2018-11-09

8.  Structure and noncanonical Cdk8 activation mechanism within an Argonaute-containing Mediator kinase module.

Authors:  Yi-Chuan Li; Ti-Chun Chao; Hee Jong Kim; Timothy Cholko; Shin-Fu Chen; Guojie Li; Laura Snyder; Kotaro Nakanishi; Chia-En Chang; Kenji Murakami; Benjamin A Garcia; Thomas G Boyer; Kuang-Lei Tsai
Journal:  Sci Adv       Date:  2021-01-15       Impact factor: 14.136

9.  Quantifying CDK inhibitor selectivity in live cells.

Authors:  Carrow I Wells; James D Vasta; Cesear R Corona; Jennifer Wilkinson; Chad A Zimprich; Morgan R Ingold; Julie E Pickett; David H Drewry; Kathryn M Pugh; Marie K Schwinn; Byounghoon Brian Hwang; Hicham Zegzouti; Kilian V M Huber; Mei Cong; Poncho L Meisenheimer; Timothy M Willson; Matthew B Robers
Journal:  Nat Commun       Date:  2020-06-02       Impact factor: 14.919

Review 10.  Cyclin-Dependent Kinases (CDK) and Their Role in Diseases Development-Review.

Authors:  Paweł Łukasik; Michał Załuski; Izabela Gutowska
Journal:  Int J Mol Sci       Date:  2021-03-13       Impact factor: 5.923
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.