Literature DB >> 26396681

Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma.

Teresa E Williams1, Sharadha Subramanian1, Joelle Verhagen1, Christopher M McBride1, Abran Costales1, Leonard Sung1, William Antonios-McCrea1, Maureen McKenna1, Alicia K Louie1, Savithri Ramurthy1, Barry Levine1, Cynthia M Shafer1, Timothy Machajewski1, Paul A Renhowe1, Brent A Appleton1, Payman Amiri1, James Chou1, Darrin Stuart1, Kimberly Aardalen1, Daniel Poon1.   

Abstract

Abrogation of errant signaling along the MAPK pathway through the inhibition of B-RAF kinase is a validated approach for the treatment of pathway-dependent cancers. We report the development of imidazo-benzimidazoles as potent B-RAF inhibitors. Robust in vivo efficacy coupled with correlating pharmacokinetic/pharmacodynamic (PKPD) and PD-efficacy relationships led to the identification of RAF265, 1, which has advanced into clinical trials.

Entities:  

Keywords:  B-RAF; MAP; VEGF; serine/threonine kinases; tyrosine kinases

Year:  2015        PMID： 26396681      PMCID： PMC4569875          DOI： 10.1021/ml500526p

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


  17 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

Review 2.  Targeting cancer with small molecule kinase inhibitors.

Authors:  Jianming Zhang; Priscilla L Yang; Nathanael S Gray
Journal:  Nat Rev Cancer       Date:  2009-01       Impact factor: 60.716

Review 3.  The influence of lipophilicity in drug discovery and design.

Authors:  John A Arnott; Sonia Lobo Planey
Journal:  Expert Opin Drug Discov       Date:  2012-09-19       Impact factor: 6.098

4.  Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers.

Authors:  Sriram Tyagarajan; Prasun K Chakravarty; Bishan Zhou; Michael H Fisher; Mathew J Wyvratt; Kathy Lyons; Tracy Klatt; Xiaohua Li; Sanjeev Kumar; Brande Williams; John Felix; Birgit T Priest; Richard M Brochu; Vivien Warren; McHardy Smith; Maria Garcia; Gregory J Kaczorowski; William J Martin; Catherine Abbadie; Erin McGowan; Nina Jochnowitz; William H Parsons
Journal:  Bioorg Med Chem Lett       Date:  2010-07-21       Impact factor: 2.823

Review 5.  Targeting the MAPK-RAS-RAF signaling pathway in cancer therapy.

Authors:  Libero Santarpia; Scott M Lippman; Adel K El-Naggar
Journal:  Expert Opin Ther Targets       Date:  2012-01-12       Impact factor: 6.902

6.  4-Trifluoromethylimidazoles and 5-(4-pyridyl)-1,2,4-triazoles, new classes of xanthine oxidase inhibitors.

Authors:  J J Baldwin; P A Kasinger; F C Novello; J M Sprague; D E Duggan
Journal:  J Med Chem       Date:  1975-09       Impact factor: 7.446

Review 7.  Vemurafenib: the first drug approved for BRAF-mutant cancer.

Authors:  Gideon Bollag; James Tsai; Jiazhong Zhang; Chao Zhang; Prabha Ibrahim; Keith Nolop; Peter Hirth
Journal:  Nat Rev Drug Discov       Date:  2012-10-12       Impact factor: 84.694

8.  Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity.

Authors:  James Tsai; John T Lee; Weiru Wang; Jiazhong Zhang; Hanna Cho; Shumeye Mamo; Ryan Bremer; Sam Gillette; Jun Kong; Nikolas K Haass; Katrin Sproesser; Ling Li; Keiran S M Smalley; Daniel Fong; Yong-Liang Zhu; Adhirai Marimuthu; Hoa Nguyen; Billy Lam; Jennifer Liu; Ivana Cheung; Julie Rice; Yoshihisa Suzuki; Catherine Luu; Calvin Settachatgul; Rafe Shellooe; John Cantwell; Sung-Hou Kim; Joseph Schlessinger; Kam Y J Zhang; Brian L West; Ben Powell; Gaston Habets; Chao Zhang; Prabha N Ibrahim; Peter Hirth; Dean R Artis; Meenhard Herlyn; Gideon Bollag
Journal:  Proc Natl Acad Sci U S A       Date:  2008-02-19       Impact factor: 11.205

9.  Design and Synthesis of Orally Bioavailable Benzimidazole Reverse Amides as Pan RAF Kinase Inhibitors.

Authors:  Sharadha Subramanian; Abran Costales; Teresa E Williams; Barry Levine; Christopher M McBride; Daniel Poon; Payman Amiri; Paul A Renhowe; Cynthia M Shafer; Darrin Stuart; Joelle Verhagen; Savithri Ramurthy
Journal:  ACS Med Chem Lett       Date:  2014-07-17       Impact factor: 4.345

10.  Mutations of the BRAF gene in human cancer.

Authors:  Helen Davies; Graham R Bignell; Charles Cox; Philip Stephens; Sarah Edkins; Sheila Clegg; Jon Teague; Hayley Woffendin; Mathew J Garnett; William Bottomley; Neil Davis; Ed Dicks; Rebecca Ewing; Yvonne Floyd; Kristian Gray; Sarah Hall; Rachel Hawes; Jaime Hughes; Vivian Kosmidou; Andrew Menzies; Catherine Mould; Adrian Parker; Claire Stevens; Stephen Watt; Steven Hooper; Rebecca Wilson; Hiran Jayatilake; Barry A Gusterson; Colin Cooper; Janet Shipley; Darren Hargrave; Katherine Pritchard-Jones; Norman Maitland; Georgia Chenevix-Trench; Gregory J Riggins; Darell D Bigner; Giuseppe Palmieri; Antonio Cossu; Adrienne Flanagan; Andrew Nicholson; Judy W C Ho; Suet Y Leung; Siu T Yuen; Barbara L Weber; Hilliard F Seigler; Timothy L Darrow; Hugh Paterson; Richard Marais; Christopher J Marshall; Richard Wooster; Michael R Stratton; P Andrew Futreal
Journal:  Nature       Date:  2002-06-09       Impact factor: 49.962
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  8 in total

1.  RAF1 amplification drives a subset of bladder tumors and confers sensitivity to MAPK-directed therapeutics.

Authors:  Raie T Bekele; Amruta S Samant; Amin H Nassar; Jonathan So; Elizabeth P Garcia; Catherine R Curran; Justin H Hwang; David L Mayhew; Anwesha Nag; Aaron R Thorner; Judit Börcsök; Zsofia Sztupinszki; Chong-Xian Pan; Joaquim Bellmunt; David J Kwiatkowski; Guru P Sonpavde; Eliezer M Van Allen; Kent W Mouw
Journal:  J Clin Invest       Date:  2021-11-15       Impact factor: 19.456

2.  Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode.

Authors:  Jun Fujimoto; Osamu Kurasawa; Terufumi Takagi; Xin Liu; Hiroshi Banno; Takuto Kojima; Yasutomi Asano; Akito Nakamura; Tadahiro Nambu; Akito Hata; Tsuyoshi Ishii; Tomoya Sameshima; Yasuyuki Debori; Maki Miyamoto; Michael G Klein; Richard Tjhen; Bi-Ching Sang; Irena Levin; Scott Weston Lane; Gyorgy P Snell; Ke Li; Georgia Kefala; Isaac D Hoffman; Steve C Ding; Douglas R Cary; Ryo Mizojiri
Journal:  ACS Med Chem Lett       Date:  2019-09-19       Impact factor: 4.345

3.  Exploring Molecular Mechanisms of Paradoxical Activation in the BRAF Kinase Dimers: Atomistic Simulations of Conformational Dynamics and Modeling of Allosteric Communication Networks and Signaling Pathways.

Authors:  Amanda Tse; Gennady M Verkhivker
Journal:  PLoS One       Date:  2016-11-18       Impact factor: 3.240

4.  A first-in-human phase I, multicenter, open-label, dose-escalation study of the oral RAF/VEGFR-2 inhibitor (RAF265) in locally advanced or metastatic melanoma independent from BRAF mutation status.

Authors:  Benjamin Izar; William Sharfman; F Stephen Hodi; Donald Lawrence; Keith T Flaherty; Ravi Amaravadi; Kevin B Kim; Igor Puzanov; Jeffrey Sosman; Reinhard Dummer; Simone M Goldinger; Lyhping Lam; Shefali Kakar; Zhongwen Tang; Oliver Krieter; David F McDermott; Michael B Atkins
Journal:  Cancer Med       Date:  2017-07-18       Impact factor: 4.452

5.  Positioning High-Throughput CETSA in Early Drug Discovery through Screening against B-Raf and PARP1.

Authors:  Joseph Shaw; Ian Dale; Paul Hemsley; Lindsey Leach; Nancy Dekki; Jonathan P Orme; Verity Talbot; Ana J Narvaez; Michal Bista; Daniel Martinez Molina; Michael Dabrowski; Martin J Main; Davide Gianni
Journal:  SLAS Discov       Date:  2018-12-13       Impact factor: 3.341

6.  Cross-species analysis of viral nucleic acid interacting proteins identifies TAOKs as innate immune regulators.

Authors:  Friederike L Pennemann; Assel Mussabekova; Christian Urban; Alexey Stukalov; Line Lykke Andersen; Vincent Grass; Teresa Maria Lavacca; Cathleen Holze; Lila Oubraham; Yasmine Benamrouche; Enrico Girardi; Rasha E Boulos; Rune Hartmann; Giulio Superti-Furga; Matthias Habjan; Jean-Luc Imler; Carine Meignin; Andreas Pichlmair
Journal:  Nat Commun       Date:  2021-12-01       Impact factor: 14.919

7.  New tools for evaluating protein tyrosine sulfation: tyrosylprotein sulfotransferases (TPSTs) are novel targets for RAF protein kinase inhibitors.

Authors:  Dominic P Byrne; Yong Li; Pawin Ngamlert; Krithika Ramakrishnan; Claire E Eyers; Carrow Wells; David H Drewry; William J Zuercher; Neil G Berry; David G Fernig; Patrick A Eyers
Journal:  Biochem J       Date:  2018-08-14       Impact factor: 3.857

Review 8.  Targeting Aberrant RAS/RAF/MEK/ERK Signaling for Cancer Therapy.

Authors:  Ufuk Degirmenci; Mei Wang; Jiancheng Hu
Journal:  Cells       Date:  2020-01-13       Impact factor: 6.600
  8 in total

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