Literature DB >> 24900428

Structure-Based Design of Potent and Selective CK1γ Inhibitors.

Hongbing Huang1, Lisa Acquaviva1, Virginia Berry1, Howard Bregman1, Nagasree Chakka1, Anne O'Connor1, Erin F DiMauro1, Jennifer Dovey1, Oleg Epstein1, Barbara Grubinska1, Jon Goldstein1, Hakan Gunaydin1, Zihao Hua1, Xin Huang1, Liyue Huang1, Jason Human1, Alex Long1, John Newcomb1, Vinod F Patel1, Doug Saffran1, Randy Serafino1, Steve Schneider1, Craig Strathdee1, Jin Tang1, Susan Turci1, Ryan White1, Violeta Yu1, Huilin Zhao1, Cindy Wilson1, Matthew W Martin1.   

Abstract

Aberrant activation of the Wnt pathway is believed to drive the development and growth of some cancers. The central role of CK1γ in Wnt signal transduction makes it an attractive target for the treatment of Wnt-pathway dependent cancers. We describe a structure-based approach that led to the discovery of a series of pyridyl pyrrolopyridinones as potent and selective CK1γ inhibitors. These compounds exhibited good enzyme and cell potency, as well as selectivity against other CK1 isoforms. A single oral dose of compound 13 resulted in significant inhibition of LRP6 phosphorylation in a mouse tumor PD model.

Entities:  

Keywords:  CK1γ; Wnt pathway; cancer; pyridyl pyrrolopyridinone

Year:  2012        PMID： 24900428      PMCID： PMC4025826          DOI： 10.1021/ml300278f

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


  17 in total

1.  The casein kinase I family in Wnt signaling.

Authors:  R M McKay; J M Peters; J M Graff
Journal:  Dev Biol       Date:  2001-07-15       Impact factor: 3.582

2.  Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor.

Authors:  Alexander Long; Huilin Zhao; Xin Huang
Journal:  J Med Chem       Date:  2012-01-05       Impact factor: 7.446

3.  Small-molecule inhibition of Wnt signaling through activation of casein kinase 1α.

Authors:  Curtis A Thorne; Alison J Hanson; Judsen Schneider; Emilios Tahinci; Darren Orton; Christopher S Cselenyi; Kristin K Jernigan; Kelly C Meyers; Brian I Hang; Alex G Waterson; Kwangho Kim; Bruce Melancon; Victor P Ghidu; Gary A Sulikowski; Bonnie LaFleur; Adrian Salic; Laura A Lee; David M Miller; Ethan Lee
Journal:  Nat Chem Biol       Date:  2010-10-03       Impact factor: 15.040

Review 4.  Wnt signaling: multiple pathways, multiple receptors, and multiple transcription factors.

Authors:  Michael D Gordon; Roel Nusse
Journal:  J Biol Chem       Date:  2006-06-22       Impact factor: 5.157

5.  A beta-catenin/TCF-coordinated chromatin loop at MYC integrates 5' and 3' Wnt responsive enhancers.

Authors:  Gregory S Yochum; Colette M Sherrick; Mary Macpartlin; Richard H Goodman
Journal:  Proc Natl Acad Sci U S A       Date:  2009-12-04       Impact factor: 11.205

6.  Beta-catenin regulates expression of cyclin D1 in colon carcinoma cells.

Authors:  O Tetsu; F McCormick
Journal:  Nature       Date:  1999-04-01       Impact factor: 49.962

7.  Axin-mediated CKI phosphorylation of beta-catenin at Ser 45: a molecular switch for the Wnt pathway.

Authors:  Sharon Amit; Ada Hatzubai; Yaara Birman; Jens S Andersen; Etti Ben-Shushan; Matthias Mann; Yinon Ben-Neriah; Irit Alkalay
Journal:  Genes Dev       Date:  2002-05-01       Impact factor: 11.361

8.  Control of beta-catenin phosphorylation/degradation by a dual-kinase mechanism.

Authors:  Chunming Liu; Yiming Li; Mikhail Semenov; Chun Han; Gyeong Hun Baeg; Yi Tan; Zhuohua Zhang; Xinhua Lin; Xi He
Journal:  Cell       Date:  2002-03-22       Impact factor: 41.582

Review 9.  Mining the Wnt pathway for cancer therapeutics.

Authors:  Nick Barker; Hans Clevers
Journal:  Nat Rev Drug Discov       Date:  2006-12       Impact factor: 84.694

10.  β-catenin/cyclin D1 mediated development of suture mesenchyme in calvarial morphogenesis.

Authors:  Anthony J Mirando; Takamitsu Maruyama; Jiang Fu; Hsiao-Man Ivy Yu; Wei Hsu
Journal:  BMC Dev Biol       Date:  2010-11-26       Impact factor: 1.978
View more
  6 in total

1.  A monoclinic crystal form of casein kinase 1 δ.

Authors:  Nicholas A Zeringo; Lea Murphy; Eric A McCloskey; Loren Rohal; John J Bellizzi
Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun       Date:  2013-09-28

2.  Structure-based design of 2-aminopyridine oxazolidinones as potent and selective tankyrase inhibitors.

Authors:  Hongbing Huang; Angel Guzman-Perez; Lisa Acquaviva; Virginia Berry; Howard Bregman; Jennifer Dovey; Hakan Gunaydin; Xin Huang; Liyue Huang; Doug Saffran; Randy Serafino; Steve Schneider; Cindy Wilson; Erin F DiMauro
Journal:  ACS Med Chem Lett       Date:  2013-10-21       Impact factor: 4.345

3.  Targeting Casein Kinase 1 Delta Sensitizes Pancreatic and Bladder Cancer Cells to Gemcitabine Treatment by Upregulating Deoxycytidine Kinase.

Authors:  Francesca Vena; Simon Bayle; Ainhoa Nieto; Victor Quereda; Massimiliano Aceti; Sylvia M Frydman; Samer S Sansil; Wayne Grant; Andrii Monastyrskyi; Patricia McDonald; William R Roush; Mingxiang Teng; Derek Duckett
Journal:  Mol Cancer Ther       Date:  2020-05-19       Impact factor: 6.261

4.  Discovery and Optimization of Macrocyclic Quinoxaline-pyrrolo-dihydropiperidinones as Potent Pim-1/2 Kinase Inhibitors.

Authors:  Victor J Cee; Frank Chavez; Bradley Herberich; Brian A Lanman; Liping H Pettus; Anthony B Reed; Bin Wu; Ryan P Wurz; Kristin L Andrews; Jie Chen; Dean Hickman; Jimmy Laszlo; Matthew R Lee; Nadia Guerrero; Bethany K Mattson; Yen Nguyen; Christopher Mohr; Karen Rex; Christine E Sastri; Paul Wang; Qiong Wu; Tian Wu; Yang Xu; Yihong Zhou; Jeffrey T Winston; J Russell Lipford; Andrew S Tasker; Hui-Ling Wang
Journal:  ACS Med Chem Lett       Date:  2016-02-12       Impact factor: 4.345

Review 5.  Targeting Casein Kinase 1 (CK1) in Hematological Cancers.

Authors:  Pavlína Janovská; Emmanuel Normant; Hari Miskin; Vítězslav Bryja
Journal:  Int J Mol Sci       Date:  2020-11-27       Impact factor: 5.923

6.  Identification of lead anti-human cytomegalovirus compounds targeting MAP4K4 via machine learning analysis of kinase inhibitor screening data.

Authors:  Blair L Strang; Christopher R M Asquith; Hanan F Moshrif; Catherine M-K Ho; William J Zuercher; Hassan Al-Ali
Journal:  PLoS One       Date:  2018-07-26       Impact factor: 3.240
  6 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.