Literature DB >> 26373275

Path Forward for RAF Therapies: Inhibition of Monomers and Dimers.

Robert L Kortum1, Deborah K Morrison2.   

Abstract

Current BRAF inhibitors block signaling from monomeric BRAF(V600E), but not from oncogenic RAS, which requires RAF dimerization. In this issue of Cancer Cell, Yao and colleagues investigate why current drugs are ineffective against RAF dimers, while Peng and colleagues describe a pan-RAF inhibitor targeting both monomeric and dimeric RAF.
Copyright © 2015 Elsevier Inc. All rights reserved.

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Year:  2015        PMID： 26373275      PMCID： PMC7394233          DOI： 10.1016/j.ccell.2015.08.006

Source DB:  PubMed          Journal:  Cancer Cell        ISSN： 1535-6108            Impact factor:   31.743


  10 in total

Review 1.  Acquired and intrinsic BRAF inhibitor resistance in BRAF V600E mutant melanoma.

Authors:  Inna V Fedorenko; Kim H T Paraiso; Keiran S M Smalley
Journal:  Biochem Pharmacol       Date:  2011-05-25       Impact factor: 5.858

Review 2.  Paradoxical oncogenesis--the long-term effects of BRAF inhibition in melanoma.

Authors:  Geoffrey T Gibney; Jane L Messina; Inna V Fedorenko; Vernon K Sondak; Keiran S M Smalley
Journal:  Nat Rev Clin Oncol       Date:  2013-05-28       Impact factor: 66.675

Review 3.  Emerging insights into resistance to BRAF inhibitors in melanoma.

Authors:  Amanda D Bucheit; Michael A Davies
Journal:  Biochem Pharmacol       Date:  2013-11-28       Impact factor: 5.858

4.  Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas.

Authors:  Piro Lito; Christine A Pratilas; Eric W Joseph; Madhavi Tadi; Ensar Halilovic; Matthew Zubrowski; Alan Huang; Wai Lin Wong; Margaret K Callahan; Taha Merghoub; Jedd D Wolchok; Elisa de Stanchina; Sarat Chandarlapaty; Poulikos I Poulikakos; James A Fagin; Neal Rosen
Journal:  Cancer Cell       Date:  2012-11-13       Impact factor: 31.743

5.  Effects of Raf dimerization and its inhibition on normal and disease-associated Raf signaling.

Authors:  Alyson K Freeman; Daniel A Ritt; Deborah K Morrison
Journal:  Mol Cell       Date:  2013-01-24       Impact factor: 17.970

6.  Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers.

Authors:  Sheng-Bin Peng; James R Henry; Michael D Kaufman; Wei-Ping Lu; Bryan D Smith; Subha Vogeti; Thomas J Rutkoski; Scott Wise; Lawrence Chun; Youyan Zhang; Robert D Van Horn; Tinggui Yin; Xiaoyi Zhang; Vipin Yadav; Shih-Hsun Chen; Xueqian Gong; Xiwen Ma; Yue Webster; Sean Buchanan; Igor Mochalkin; Lysiane Huber; Lisa Kays; Gregory P Donoho; Jennie Walgren; Denis McCann; Phenil Patel; Ilaria Conti; Gregory D Plowman; James J Starling; Daniel L Flynn
Journal:  Cancer Cell       Date:  2015-09-03       Impact factor: 31.743

7.  BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition.

Authors:  Zhan Yao; Neilawattie M Torres; Anthony Tao; Yijun Gao; Lusong Luo; Qi Li; Elisa de Stanchina; Omar Abdel-Wahab; David B Solit; Poulikos I Poulikakos; Neal Rosen
Journal:  Cancer Cell       Date:  2015-09-03       Impact factor: 31.743

8.  Allosteric activation of functionally asymmetric RAF kinase dimers.

Authors:  Jiancheng Hu; Edward C Stites; Haiyang Yu; Elizabeth A Germino; Hiruy S Meharena; Philip J S Stork; Alexandr P Kornev; Susan S Taylor; Andrey S Shaw
Journal:  Cell       Date:  2013-08-29       Impact factor: 41.582

9.  Paradox-breaking RAF inhibitors that also target SRC are effective in drug-resistant BRAF mutant melanoma.

Authors:  Maria Romina Girotti; Filipa Lopes; Natasha Preece; Dan Niculescu-Duvaz; Alfonso Zambon; Lawrence Davies; Steven Whittaker; Grazia Saturno; Amaya Viros; Malin Pedersen; Bart M J M Suijkerbuijk; Delphine Menard; Robert McLeary; Louise Johnson; Laura Fish; Sarah Ejiama; Berta Sanchez-Laorden; Juliane Hohloch; Neil Carragher; Kenneth Macleod; Garry Ashton; Anna A Marusiak; Alberto Fusi; John Brognard; Margaret Frame; Paul Lorigan; Richard Marais; Caroline Springer
Journal:  Cancer Cell       Date:  2014-12-11       Impact factor: 31.743

10.  Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization.

Authors:  Hugo Lavoie; Neroshan Thevakumaran; Gwenaëlle Gavory; John J Li; Abbas Padeganeh; Sébastien Guiral; Jean Duchaine; Daniel Y L Mao; Michel Bouvier; Frank Sicheri; Marc Therrien
Journal:  Nat Chem Biol       Date:  2013-05-19       Impact factor: 15.040
  10 in total
  5 in total

Review 1.  KSR as a therapeutic target for Ras-dependent cancers.

Authors:  Beth K Neilsen; Danielle E Frodyma; Robert E Lewis; Kurt W Fisher
Journal:  Expert Opin Ther Targets       Date:  2017-04-07       Impact factor: 6.902

Review 2.  Therapeutic approach to treating patients with BRAF-mutant lung cancer: latest evidence and clinical implications.

Authors:  Adrianus J de Langen; Egbert F Smit
Journal:  Ther Adv Med Oncol       Date:  2016-10-03       Impact factor: 8.168

3.  Pan-Raf co-operates with PI3K-dependent signalling and critically contributes to myeloma cell survival independently of mutated RAS.

Authors:  E Müller; S Bauer; T Stühmer; A Mottok; C-J Scholz; T Steinbrunn; D Brünnert; A Brandl; H Schraud; S Kreßmann; A Beilhack; A Rosenwald; R C Bargou; M Chatterjee
Journal:  Leukemia       Date:  2016-09-30       Impact factor: 11.528

Review 4.  Treatment of NRAS-mutated advanced or metastatic melanoma: rationale, current trials and evidence to date.

Authors:  Amélie Boespflug; Julie Caramel; Stephane Dalle; Luc Thomas
Journal:  Ther Adv Med Oncol       Date:  2017-05-29       Impact factor: 8.168

5.  A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma.

Authors:  Filemon S Dela Cruz; Daniel Diolaiti; Andrew T Turk; Allison R Rainey; Alberto Ambesi-Impiombato; Stuart J Andrews; Mahesh M Mansukhani; Peter L Nagy; Mariano J Alvarez; Andrea Califano; Farhad Forouhar; Beata Modzelewski; Chelsey M Mitchell; Darrell J Yamashiro; Lianna J Marks; Julia L Glade Bender; Andrew L Kung
Journal:  Genome Med       Date:  2016-10-31       Impact factor: 11.117
  5 in total

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