Clinical Profiling of BCL-2 Family Members in the Setting of BRAF Inhibition Offers a Rationale for Targeting De Novo Resistance Using BH3 Mimetics

Tumor genetic analyses of patients with metastatic melanoma treated with the BRAF inhibitor GSK2118436 (GSK436).

(2017) K. L. Nathanson et al.   JOURNAL OF CLINICAL ONCOLOGY

Pharmacodynamic Characterization of the Efficacy Signals Due to Selective BRAF Inhibition with PLX4032 in Malignant Melanoma

(2015) William D. Tap et al.   NEOPLASIA

Pharmacodynamic Effects and Mechanisms of Resistance to Vemurafenib in Patients With Metastatic Melanoma

(2013) Kerstin Trunzer et al.   JOURNAL OF CLINICAL ONCOLOGY

CRM1 and BRAF Inhibition Synergize and Induce Tumor Regression in BRAF-Mutant Melanoma

(2013) R. A. Salas Fragomeni et al.   MOLECULAR CANCER THERAPEUTICS

Effects of BRAF inhibitors on human melanoma tissue before treatment, early during treatment, and on progression

(2013) Georgina V. Long et al.   Pigment Cell & Melanoma Research

BCL2A1is a lineage-specific antiapoptotic melanoma oncogene that confers resistance to BRAF inhibition

(2013) Rizwan Haq et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

A phase I trial of pan-Bcl-2 antagonist obatoclax administered as a 3-h or a 24-h infusion in combination with carboplatin and etoposide in patients with extensive-stage small cell lung cancer

(2012) A A Chiappori et al.   BRITISH JOURNAL OF CANCER

The BH3-mimetic ABT-737 sensitizes human melanoma cells to apoptosis induced by selective BRAF inhibitors but does not reverse acquired resistance

(2012) D. Wroblewski et al.   CARCINOGENESIS

Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial

(2012) Gerald S Falchook et al.   LANCET

Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial

(2012) Axel Hauschild et al.   LANCET

Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion

(2012) Ravid Straussman et al.   NATURE

Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors

(2012) Timothy R. Wilson et al.   NATURE

Survival in BRAF V600–Mutant Advanced Melanoma Treated with Vemurafenib

(2012) Jeffrey A. Sosman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Melanoma whole-exome sequencing identifies V600E B-RAF amplification-mediated acquired B-RAF inhibitor resistance

(2012) Hubing Shi et al.   Nature Communications

The MEK-ERK pathway negatively regulates bim expression through the 3' UTR in sympathetic neurons

(2011) Rosie Hughes et al.   BMC NEUROSCIENCE

Identification of the MEK1(F129L) Activating Mutation as a Potential Mechanism of Acquired Resistance to MEK Inhibition in Human Cancers Carrying the B-RafV600E Mutation

(2011) H. Wang et al.   CANCER RESEARCH

PTEN Loss Confers BRAF Inhibitor Resistance to Melanoma Cells through the Suppression of BIM Expression

(2011) K. H. T. Paraiso et al.   CANCER RESEARCH

Dissecting Therapeutic Resistance to RAF Inhibition in Melanoma by Tumor Genomic Profiling

(2011) Nikhil Wagle et al.   JOURNAL OF CLINICAL ONCOLOGY

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

(2011) Poulikos I. Poulikakos et al.   NATURE

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

(2011) Paul B. Chapman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Acquired Resistance to BRAF Inhibitors Mediated by a RAF Kinase Switch in Melanoma Can Be Overcome by Cotargeting MEK and IGF-1R/PI3K

(2010) Jessie Villanueva et al.   CANCER CELL

A phase I study of obatoclax mesylate, a Bcl-2 antagonist, plus topotecan in solid tumor malignancies

(2010) Paul K. Paik et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Drug Combination Studies and Their Synergy Quantification Using the Chou-Talalay Method

(2010) T.-C. Chou   CANCER RESEARCH

Phase I Dose Finding Studies of Obatoclax (GX15-070), a Small Molecule Pan-BCL-2 Family Antagonist, in Patients with Advanced Solid Tumors or Lymphoma

(2010) J. J. Hwang et al.   CLINICAL CANCER RESEARCH

Identification of Expression Signatures Predictive of Sensitivity to the Bcl-2 Family Member Inhibitor ABT-263 in Small Cell Lung Carcinoma and Leukemia/Lymphoma Cell Lines

(2010) S. K. Tahir et al.   MOLECULAR CANCER THERAPEUTICS

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

(2010) Gideon Bollag et al.   NATURE

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

(2010) Cory M. Johannessen et al.   NATURE

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation

(2010) Ramin Nazarian et al.   NATURE

The landscape of somatic copy-number alteration across human cancers

(2010) Rameen Beroukhim et al.   NATURE

PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas

(2010) John T. Lee et al.   Pigment Cell & Melanoma Research

ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor

(2008) C. Tse et al.   CANCER RESEARCH

Elevated CRAF as a Potential Mechanism of Acquired Resistance to BRAF Inhibition in Melanoma

(2008) C. Montagut et al.   CANCER RESEARCH

Oncogenic B-RafV600EInhibits Apoptosis and Promotes ERK-dependent Inactivation of Bad and Bim

(2008) Clare Sheridan et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Treatment of B-RAF mutant human tumor cells with a MEK inhibitor requires Bim and is enhanced by a BH3 mimetic

(2008) Mark S. Cragg et al.   JOURNAL OF CLINICAL INVESTIGATION

Down-Regulation of Mcl-1 by Small Interfering RNA Sensitizes Resistant Melanoma Cells to Fas-Mediated Apoptosis

(2008) N. Chetoui et al.   MOLECULAR CANCER RESEARCH

Increased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomas

(2008) K. S.M. Smalley et al.   MOLECULAR CANCER THERAPEUTICS

Mutant B-RAF mediates resistance to anoikis via Bad and Bim

(2008) K Boisvert-Adamo et al.   ONCOGENE

Oncogenic BRAFV600E inhibits BIM expression to promote melanoma cell survival

(2008) Robert A. Cartlidge et al.   Pigment Cell & Melanoma Research

The BCL-2 protein family: opposing activities that mediate cell death

(2007) Richard J. Youle et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY