Literature DB >> 18676143

Potent and selective pyrazole-based inhibitors of B-Raf kinase.

Joshua D Hansen1, Jonas Grina, Brad Newhouse, Mike Welch, George Topalov, Nicole Littman, Michele Callejo, Susan Gloor, Matthew Martinson, Ellen Laird, Barbara J Brandhuber, Guy Vigers, Tony Morales, Rich Woessner, Nikole Randolph, Joseph Lyssikatos, Alan Olivero.   

Abstract

Herein we describe a novel pyrazole-based class of ATP competitive B-Raf inhibitors. These inhibitors exhibit both excellent cellular potency and striking B-Raf selectivity. A subset of these inhibitors has demonstrated the ability to inhibit downstream ERK phosphorylation in LOX tumors from mouse xenograft studies.

Entities:  

Mesh：

Substances：

Year:  2008        PMID： 18676143     DOI： 10.1016/j.bmcl.2008.07.002

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  20 in total

1.  QM/MM based 3D QSAR models for potent B-Raf inhibitors.

Authors:  Jae Yoon Chung; Hwan Won Chung; Seung Joo Cho; Jung-Mi Hah; Art E Cho
Journal:  J Comput Aided Mol Des       Date:  2010-04-01       Impact factor: 3.686

2.  Scaffold mining of kinase hinge binders in crystal structure database.

Authors:  Li Xing; Brajesh Rai; Elizabeth A Lunney
Journal:  J Comput Aided Mol Des       Date:  2013-12-29       Impact factor: 3.686

3.  Development of a novel class of B-Raf(V600E)-selective inhibitors through virtual screening and hierarchical hit optimization.

Authors:  Xiangqian Kong; Jie Qin; Zeng Li; Adina Vultur; Linjiang Tong; Enguang Feng; Geena Rajan; Shien Liu; Junyan Lu; Zhongjie Liang; Mingyue Zheng; Weiliang Zhu; Hualiang Jiang; Meenhard Herlyn; Hong Liu; Ronen Marmorstein; Cheng Luo
Journal:  Org Biomol Chem       Date:  2012-09-28       Impact factor: 3.876

Review 4.  Targeted inhibition of BRAF kinase: opportunities and challenges for therapeutics in melanoma.

Authors:  Rolando Pérez-Lorenzo; Bin Zheng
Journal:  Biosci Rep       Date:  2012-02       Impact factor: 3.840

5.  Single-molecule superresolution imaging allows quantitative analysis of RAF multimer formation and signaling.

Authors:  Xiaolin Nan; Eric A Collisson; Sophia Lewis; Jing Huang; Tanja M Tamgüney; Jan T Liphardt; Frank McCormick; Joe W Gray; Steven Chu
Journal:  Proc Natl Acad Sci U S A       Date:  2013-10-24       Impact factor: 11.205

6.  Ligand-Binding-Site Refinement to Generate Reliable Holo Protein Structure Conformations from Apo Structures.

Authors:  Hugo Guterres; Sang-Jun Park; Wei Jiang; Wonpil Im
Journal:  J Chem Inf Model       Date:  2020-12-18       Impact factor: 4.956

Review 7.  A guide to picking the most selective kinase inhibitor tool compounds for pharmacological validation of drug targets.

Authors:  Joost C M Uitdehaag; Folkert Verkaar; Husam Alwan; Jos de Man; Rogier C Buijsman; Guido J R Zaman
Journal:  Br J Pharmacol       Date:  2012-06       Impact factor: 8.739

8.  Novel tricyclic pyrazole BRAF inhibitors with imidazole or furan central scaffolds.

Authors:  Dan Niculescu-Duvaz; Ion Niculescu-Duvaz; Bart M J M Suijkerbuijk; Delphine Ménard; Alfonso Zambon; Arnaud Nourry; Lawrence Davies; Helen A Manne; Frank Friedlos; Lesley Ogilvie; Douglas Hedley; Andrew K Takle; David M Wilson; Jean-Francois Pons; Tom Coulter; Ruth Kirk; Neus Cantarino; Steven Whittaker; Richard Marais; Caroline J Springer
Journal:  Bioorg Med Chem       Date:  2010-06-15       Impact factor: 3.641

9.  Subnanomolar inhibitor of cytochrome bc1 complex designed by optimizing interaction with conformationally flexible residues.

Authors:  Pei-Liang Zhao; Le Wang; Xiao-Lei Zhu; Xiaoqin Huang; Chang-Guo Zhan; Jia-Wei Wu; Guang-Fu Yang
Journal:  J Am Chem Soc       Date:  2010-01-13       Impact factor: 15.419

10.  GDC-0879, a BRAFV600E Inhibitor, Protects Kidney Podocytes from Death.

Authors:  Jonas Sieber; Nicolas Wieder; Abbe Clark; Manuel Reitberger; Sofia Matan; Jeannine Schoenfelder; Jianming Zhang; Anna Mandinova; Joshua Adam Bittker; Juan Gutierrez; Ozan Aygün; Namrata Udeshi; Steven Carr; Peter Mundel; Andreas Werner Jehle; Anna Greka
Journal:  Cell Chem Biol       Date:  2017-12-14       Impact factor: 8.116
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.