Vemurafenib: the first drug approved for BRAF-mutant cancer (Q28276886)

4

object named as

Chao Zhang

0 references

author name string

James Tsai

2

0 references

Jiazhong Zhang

3

0 references

Prabha Ibrahim

5

0 references

Keith Nolop

6

0 references

Peter Hirth

Nature Reviews Drug Discovery

7

0 references

language of work or name

English

0 references

publication date

November 2012

0 references

published in

0 references

volume

11

0 references

page(s)

873-86

0 references

issue

11

0 references

cites work

Structure and biological activity of v-raf, a unique oncogene transduced by a retrovirus

1 reference

The human homologs of the raf (mil) oncogene are located on human chromosomes 3 and 4

31 March 2020

1 reference

Serine- and threonine-specific protein kinase activities of purified gag-mil and gag-raf proteins

31 March 2020

1 reference

Characterization of murine A-raf, a new oncogene related to the v-raf oncogene

31 March 2020

1 reference

The complete coding sequence of the human A-raf-1 oncogene and transforming activity of a human A-raf carrying retrovirus

31 March 2020

1 reference

B-raf, a new member of the raf family, is activated by DNA rearrangement

31 March 2020

1 reference

Mutations of the BRAF gene in human cancer

31 March 2020

1 reference

A genome-based strategy uncovers frequent BRAF mutations in melanoma.

31 March 2020

1 reference

RAF/RAS oncogenes and mismatch-repair status

31 March 2020

1 reference

BRAF Mutation in Papillary Thyroid Carcinoma

31 March 2020

1 reference

BRAF mutations in papillary carcinomas of the thyroid

31 March 2020

1 reference

BRAF mutations in thyroid tumors are restricted to papillary carcinomas and anaplastic or poorly differentiated carcinomas arising from papillary carcinomas

31 March 2020

1 reference

Mutations in BRAF and KRAS characterize the development of low-grade ovarian serous carcinoma

31 March 2020

1 reference

BRAF and KRAS mutations in stomach cancer

31 March 2020

1 reference

Mutations of the BRAF gene in cholangiocarcinoma but not in hepatocellular carcinoma

31 March 2020

1 reference

Mutations of BRAF and KRAS2 in the development of Barrett's adenocarcinoma.

31 March 2020

1 reference

Mutations of the BRAF gene in squamous cell carcinoma of the head and neck.

31 March 2020

1 reference

BRAF and PIK3CA genes are somatically mutated in hepatocellular carcinoma among patients from South Italy

31 March 2020

1 reference

Recurrent BRAF mutations in Langerhans cell histiocytosis

31 March 2020

1 reference

Novel V600E BRAF mutations in imatinib-naive and imatinib-resistant gastrointestinal stromal tumors

31 March 2020

1 reference

Initial genome sequencing and analysis of multiple myeloma

31 March 2020

1 reference

Tandem duplication producing a novel oncogenic BRAF fusion gene defines the majority of pilocytic astrocytomas

31 March 2020

1 reference

BRAF gene duplication constitutes a mechanism of MAPK pathway activation in low-grade astrocytomas

31 March 2020

1 reference

Duplication of 7q34 in pediatric low-grade astrocytomas detected by high-density single-nucleotide polymorphism-based genotype arrays results in a novel BRAF fusion gene

31 March 2020

1 reference

BRAF V600E mutations are common in pleomorphic xanthoastrocytoma: diagnostic and therapeutic implications

31 March 2020

1 reference

Analysis of BRAF V600E mutation in 1,320 nervous system tumors reveals high mutation frequencies in pleomorphic xanthoastrocytoma, ganglioglioma and extra-cerebellar pilocytic astrocytoma

31 March 2020

1 reference

BRAF mutations in hairy-cell leukemia

31 March 2020

1 reference

High frequency of BRAF mutations in nevi

31 March 2020

1 reference

BRAFE600-associated senescence-like cell cycle arrest of human naevi

31 March 2020

1 reference

BRAF as a potential therapeutic target in melanoma and other malignancies

31 March 2020

1 reference

B-RAF is a therapeutic target in melanoma

31 March 2020

1 reference

V599EB-RAF is an oncogene in melanocytes

31 March 2020

1 reference

Oncogenic BRAF is required for tumor growth and maintenance in melanoma models

31 March 2020

1 reference

A new mouse model to explore the initiation, progression, and therapy of BRAFV600E-induced lung tumors

31 March 2020

1 reference

BRAF activation initiates but does not maintain invasive prostate adenocarcinoma

31 March 2020

1 reference

Braf(V600E) cooperates with Pten loss to induce metastatic melanoma

31 March 2020

1 reference

Melanocytic nevus-like hyperplasia and melanoma in transgenic BRAFV600E mice

31 March 2020

1 reference

Small-molecule MAPK inhibitors restore radioiodine incorporation in mouse thyroid cancers with conditional BRAF activation

31 March 2020

1 reference

Mutationally activated BRAF(V600E) elicits papillary thyroid cancer in the adult mouse

31 March 2020

1 reference

BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis

31 March 2020

1 reference

Sorafenib for the treatment of advanced renal cell carcinoma

31 March 2020

1 reference

Sorafenib for the treatment of unresectable hepatocellular carcinoma

31 March 2020

1 reference

Discovery and development of sorafenib: a multikinase inhibitor for treating cancer.

31 March 2020

1 reference

A phase I trial of the oral, multikinase inhibitor sorafenib in combination with carboplatin and paclitaxel

31 March 2020

1 reference

Results of a phase III, randomized, placebo-controlled study of sorafenib in combination with carboplatin and paclitaxel as second-line treatment in patients with unresectable stage III or stage IV melanoma

31 March 2020

1 reference

A phase II trial of sorafenib in metastatic melanoma with tissue correlates

31 March 2020

1 reference

Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF

31 March 2020

1 reference

Cutaneous manifestations of dabrafenib (GSK2118436): a selective inhibitor of mutant BRAF in patients with metastatic melanoma

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

RAF265 inhibits the growth of advanced human melanoma tumors

31 March 2020

1 reference

CEP-32496: a novel orally active BRAF(V600E) inhibitor with selective cellular and in vivo antitumor activity

31 March 2020

1 reference

Targeting cancer with small molecule kinase inhibitors

31 March 2020

1 reference

Targeting cancer with small-molecular-weight kinase inhibitors

31 March 2020

1 reference

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

31 March 2020

1 reference

Scaffold-based design of kinase inhibitors for cancer therapy

31 March 2020

1 reference

Fragment-based lead discovery using X-ray crystallography.

31 March 2020

1 reference

The rise of fragment-based drug discovery

31 March 2020

1 reference

Structural approaches to obtain kinase selectivity

31 March 2020

1 reference

Crystal structures of proto-oncogene kinase Pim1: a target of aberrant somatic hypermutations in diffuse large cell lymphoma

31 March 2020

1 reference

A family of phosphodiesterase inhibitors discovered by cocrystallography and scaffold-based drug design

31 March 2020

1 reference

Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent

31 March 2020

1 reference

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

31 March 2020

1 reference

BRAF mutation predicts sensitivity to MEK inhibition

31 March 2020

1 reference

PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells

31 March 2020

1 reference

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner

31 March 2020

1 reference

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

31 March 2020

1 reference

Targeting the mitogen-activated protein kinase pathway: physiological feedback and drug response

31 March 2020

1 reference

Differential sensitivity of melanoma cell lines with BRAFV600E mutation to the specific Raf inhibitor PLX4032.

31 March 2020

1 reference

Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma

31 March 2020

1 reference

RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models

31 March 2020

1 reference

BRAF silencing by short hairpin RNA or chemical blockade by PLX4032 leads to different responses in melanoma and thyroid carcinoma cells

31 March 2020

1 reference

Cytostatic activity of adenosine triphosphate-competitive kinase inhibitors in BRAF mutant thyroid carcinoma cells.

31 March 2020

1 reference

Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy.

31 March 2020

1 reference

Akt3-mediated resistance to apoptosis in B-RAF-targeted melanoma cells

31 March 2020

1 reference

Adaptive upregulation of FOXD3 and resistance to PLX4032/4720-induced cell death in mutant B-RAF melanoma cells

31 March 2020

1 reference

Role and therapeutic potential of PI3K-mTOR signaling in de novo resistance to BRAF inhibition

31 March 2020

1 reference

Hyperactivation of MEK-ERK1/2 signaling and resistance to apoptosis induced by the oncogenic B-RAF inhibitor, PLX4720, in mutant N-RAS melanoma cells.

31 March 2020

1 reference

Concurrent loss of the PTEN and RB1 tumor suppressors attenuates RAF dependence in melanomas harboring (V600E)BRAF

31 March 2020

1 reference

Wild-type and mutant B-RAF activate C-RAF through distinct mechanisms involving heterodimerization

31 March 2020

1 reference

Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF

31 March 2020

1 reference

Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer

31 March 2020

1 reference

A dimerization-dependent mechanism drives RAF catalytic activation

31 March 2020

1 reference

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

31 March 2020

1 reference

Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

31 March 2020

1 reference

Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib

31 March 2020

1 reference

Improved survival with vemurafenib in melanoma with BRAF V600E mutation

31 March 2020

1 reference

Marked, homogeneous, and early [18F]fluorodeoxyglucose-positron emission tomography responses to vemurafenib in BRAF-mutant advanced melanoma.

31 March 2020

1 reference

Apoptosis of human melanoma cells induced by inhibition of B-RAFV600E involves preferential splicing of bimS

31 March 2020

1 reference

Targeted therapy for BRAFV600E malignant astrocytoma.

31 March 2020

1 reference

Uncoupling of the LKB1-AMPKalpha energy sensor pathway by growth factors and oncogenic BRAF

31 March 2020

1 reference

Combination therapy with vemurafenib (PLX4032/RG7204) and metformin in melanoma cell lines with distinct driver mutations

31 March 2020

1 reference

DHODH modulates transcriptional elongation in the neural crest and melanoma

31 March 2020

1 reference

PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression

31 March 2020

1 reference

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR.

31 March 2020

1 reference

EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib

31 March 2020

1 reference

Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma

31 March 2020

1 reference

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

31 March 2020

1 reference

Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K

31 March 2020

1 reference

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

31 March 2020

1 reference

Amplification of the driving oncogene, KRAS or BRAF, underpins acquired resistance to MEK1/2 inhibitors in colorectal cancer cells.

31 March 2020

1 reference

BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells harboring the BRAF V600E mutation

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Resistance to BRAF inhibition in melanomas

31 March 2020

1 reference

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

31 March 2020

1 reference

Paradoxical activation of Raf by a novel Raf inhibitor

31 March 2020

1 reference

A negative feedback signaling network underlies oncogene-induced senescence

31 March 2020

1 reference

Regulation of Raf-1 by direct feedback phosphorylation.

31 March 2020

1 reference

Impact of feedback phosphorylation and Raf heterodimerization on normal and mutant B-Raf signaling

31 March 2020

1 reference

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

31 March 2020

1 reference

A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK

31 March 2020

1 reference

RAF inhibitor-induced KSR1/B-RAF binding and its effects on ERK cascade signaling

31 March 2020

1 reference

Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF

31 March 2020

1 reference

RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors

31 March 2020

1 reference

RAS mutations are associated with the development of cutaneous squamous cell tumors in patients treated with RAF inhibitors

31 March 2020

1 reference

BRAF inhibition in refractory hairy-cell leukemia.

31 March 2020

1 reference

A patient with BRAF V600E lung adenocarcinoma responding to vemurafenib.

31 March 2020

1 reference

The oncogenic BRAF kinase inhibitor PLX4032/RG7204 does not affect the viability or function of human lymphocytes across a wide range of concentrations

31 March 2020

1 reference

Selective BRAFV600E inhibition enhances T-cell recognition of melanoma without affecting lymphocyte function

31 March 2020

1 reference

Technology platforms for pharmacogenomic diagnostic assays

31 March 2020

1 reference

Analytical performance of a real-time PCR-based assay for V600 mutations in the BRAF gene, used as the companion diagnostic test for the novel BRAF inhibitor vemurafenib in metastatic melanoma

31 March 2020

1 reference

Cancer research. Melanoma drug vindicates targeted approach.

31 March 2020

1 reference

Activation of the MAP kinase pathway by the protein kinase raf

31 March 2020

1 reference

Transactivation of c-fos and beta-actin genes by raf as a step in early response to transmembrane signals

31 March 2020

1 reference

Hyperactive Ras in developmental disorders and cancer

31 March 2020

1 reference

Direct interaction of Ras and the amino-terminal region of Raf-1 in vitro

31 March 2020

1 reference

Requirement for Ras in Raf activation is overcome by targeting Raf to the plasma membrane

31 March 2020

1 reference

Oligomerization activates c-Raf-1 through a Ras-dependent mechanism

31 March 2020

1 reference

Constitutive mitogen-activated protein kinase activation in melanoma is mediated by both BRAF mutations and autocrine growth factor stimulation

31 March 2020

1 reference

12 December 2020

Suppression of BRAF(V599E) in human melanoma abrogates transformation

1 reference

12 December 2020

BRAF and RAS mutations in human lung cancer and melanoma

1 reference

12 December 2020

A novel oncogene related to c-mil is transduced in chicken neuroretina cells induced to proliferate by infection with an avian lymphomatosis virus

1 reference

12 December 2020

High prevalence of BRAF mutations in thyroid cancer: genetic evidence for constitutive activation of the RET/PTC-RAS-BRAF signaling pathway in papillary thyroid carcinoma

1 reference

12 December 2020

High prevalence of BRAF gene mutation in papillary thyroid carcinomas and thyroid tumor cell lines.

1 reference

12 December 2020

Raf pathway inhibitors in oncology

1 reference

12 December 2020

Active Ras induces heterodimerization of cRaf and BRaf

1 reference

12 December 2020