(Q38272894)

1 September 2017

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title

Targeting RAS-ERK signalling in cancer: promises and challenges (English)

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1 September 2017

Ahmed A Samatar

1

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1 September 2017

Poulikos I Poulikakos

series ordinal

2

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1 September 2017

publication date

1 December 2014

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Nature Reviews Drug Discovery

1 September 2017

published in

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1 September 2017

volume

13

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1 September 2017

issue

12

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1 September 2017

page(s)

928-942

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Targeting the RAF-MEK-ERK pathway in cancer therapy

1 September 2017

cites work

1 reference

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MAP kinase signalling pathways in cancer

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Mutations of the BRAF gene in human cancer

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BRAFV600E: implications for carcinogenesis and molecular therapy

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Inhibition of Ras for cancer treatment: the search continues

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RAS Interaction with PI3K: More Than Just Another Effector Pathway

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Targeting RAS and PI3K in lung cancer.

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The RalGEF-Ral Effector Signaling Network: The Road Less Traveled for Anti-Ras Drug Discovery

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Ras signaling and therapies

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31 March 2020

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K- and N-Ras are geranylgeranylated in cells treated with farnesyl protein transferase inhibitors

31 March 2020

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Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling

31 March 2020

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Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity

31 March 2020

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Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

31 March 2020

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Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

31 March 2020

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In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction

31 March 2020

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K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

31 March 2020

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The RAF proteins take centre stage

31 March 2020

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Autoregulation of the Raf-1 serine/threonine kinase

31 March 2020

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

31 March 2020

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Mutations of C-RAF are rare in human cancer because C-RAF has a low basal kinase activity compared with B-RAF

31 March 2020

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

31 March 2020

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Conditionally oncogenic forms of the A-Raf and B-Raf protein kinases display different biological and biochemical properties in NIH 3T3 cells

31 March 2020

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Oncogenic and sorafenib-sensitive ARAF mutations in lung adenocarcinoma

31 March 2020

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Somatic activating ARAF mutations in Langerhans cell histiocytosis.

31 March 2020

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Raf-1 promotes cell survival by antagonizing apoptosis signal-regulating kinase 1 through a MEK-ERK independent mechanism

31 March 2020

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Role of the kinase MST2 in suppression of apoptosis by the proto-oncogene product Raf-1.

31 March 2020

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Raf-1 physically interacts with Rb and regulates its function: a link between mitogenic signaling and cell cycle regulation

31 March 2020

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Raf-1 regulates Rho signaling and cell migration

31 March 2020

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Recurrent BRAF mutations in Langerhans cell histiocytosis

31 March 2020

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High prevalence of BRAF V600E mutations in Erdheim-Chester disease but not in other non-Langerhans cell histiocytoses.

31 March 2020

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Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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C-Raf inhibits MAPK activation and transformation by B-Raf(V600E).

31 March 2020

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Improved survival with vemurafenib in melanoma with BRAF V600E mutation

31 March 2020

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Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

31 March 2020

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Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy

31 March 2020

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Dramatic efficacy of vemurafenib in both multisystemic and refractory Erdheim-Chester disease and Langerhans cell histiocytosis harboring the BRAF V600E mutation

31 March 2020

1 reference

RAF inhibitors activate the MAPK pathway by relieving inhibitory autophosphorylation

31 March 2020

1 reference

Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling

31 March 2020

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Increased BRAF heterodimerization is the common pathogenic mechanism for noonan syndrome-associated RAF1 mutants

31 March 2020

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Allosteric activation of functionally asymmetric RAF kinase dimers

31 March 2020

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A dimerization-dependent mechanism drives RAF catalytic activation

31 March 2020

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Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization

31 March 2020

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

31 March 2020

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

31 March 2020

1 reference

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

31 March 2020

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Progression of RAS-mutant leukemia during RAF inhibitor treatment

31 March 2020

1 reference

Efficacy of intermittent combined RAF and MEK inhibition in a patient with concurrent BRAF- and NRAS-mutant malignancies

31 March 2020

1 reference

New RAS-mutant pancreatic adenocarcinoma with combined BRAF and MEK inhibition for metastatic melanoma.

31 March 2020

1 reference

Mutant BRAF melanomas--dependence and resistance

31 March 2020

1 reference

Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma

31 March 2020

1 reference

Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors

31 March 2020

1 reference

Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas

31 March 2020

1 reference

MEK1/2 dual-specificity protein kinases: structure and regulation

31 March 2020

1 reference

MEK inhibitors: a therapeutic approach to targeting the Ras-MAP kinase pathway in tumors

31 March 2020

1 reference

Novel MEK1 mutation identified by mutational analysis of epidermal growth factor receptor signaling pathway genes in lung adenocarcinoma

31 March 2020

1 reference

MEK1 mutations, but not ERK2 mutations, occur in melanomas and colon carcinomas, but none in thyroid carcinomas

31 March 2020

1 reference

A phase II study of PD-0325901, an oral MEK inhibitor, in previously treated patients with advanced non-small cell lung cancer

31 March 2020

1 reference

Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancer

31 March 2020

1 reference

The first-in-human study of the hydrogen sulfate (Hyd-sulfate) capsule of the MEK1/2 inhibitor AZD6244 (ARRY-142886): a phase I open-label multicenter trial in patients with advanced cancer

31 March 2020

1 reference

Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies

31 March 2020

1 reference

Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration

31 March 2020

1 reference

Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo

31 March 2020

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BRAF mutation predicts sensitivity to MEK inhibition

31 March 2020

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Phase I pharmacokinetic and pharmacodynamic study of the oral MAPK/ERK kinase inhibitor PD-0325901 in patients with advanced cancers

31 March 2020

1 reference

Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor

31 March 2020

1 reference

AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in precl

31 March 2020

1 reference

Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancers

31 March 2020

1 reference

A phase I, open-label, randomized crossover study to assess the effect of dosing of the MEK 1/2 inhibitor Selumetinib (AZD6244; ARRY-142866) in the presence and absence of food in patients with advanced solid tumors

31 March 2020

1 reference

Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma

31 March 2020

1 reference

Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: a randomised, multicentre, placebo-controlled, phase 2 study

31 March 2020

1 reference

GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition

31 March 2020

1 reference

A phase 1b study of trametinib, an oral Mitogen-activated protein kinase kinase (MEK) inhibitor, in combination with gemcitabine in advanced solid tumours

31 March 2020

1 reference

Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial

31 March 2020

1 reference

Improved survival with MEK inhibition in BRAF-mutated melanoma

31 March 2020

1 reference

Differential activity of MEK and ERK inhibitors in BRAF inhibitor resistant melanoma.

31 March 2020

1 reference

Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations

31 March 2020

1 reference

Blockade of the MEK/ERK signalling cascade by AS703026, a novel selective MEK1/2 inhibitor, induces pleiotropic anti-myeloma activity in vitro and in vivo

31 March 2020

1 reference

Preclinical disposition of GDC-0973 and prospective and retrospective analysis of human dose and efficacy predictions

31 March 2020

1 reference

RDEA119/BAY 869766: a potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer

31 March 2020

1 reference

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

31 March 2020

1 reference

Discovery of TAK-733, a potent and selective MEK allosteric site inhibitor for the treatment of cancer

31 March 2020

1 reference

First-in-human, phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of RO5126766, a first-in-class dual MEK/RAF inhibitor in patients with solid tumors.

31 March 2020

1 reference

Phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of the MEK inhibitor RO4987655 (CH4987655) in patients with advanced solid tumors.

31 March 2020

1 reference

MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study

31 March 2020

1 reference

Phase II study of the MEK1/MEK2 inhibitor Trametinib in patients with metastatic BRAF-mutant cutaneous melanoma previously treated with or without a BRAF inhibitor

31 March 2020

1 reference

Regulation of Raf-1 by direct feedback phosphorylation.

31 March 2020

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

31 March 2020

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Strong negative feedback from Erk to Raf confers robustness to MAPK signalling.

31 March 2020

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Oncogenic and wild-type Ras play divergent roles in the regulation of mitogen-activated protein kinase signaling

31 March 2020

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Enhanced inhibition of ERK signaling by a novel allosteric MEK inhibitor, CH5126766, that suppresses feedback reactivation of RAF activity

31 March 2020

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Disruption of CRAF-mediated MEK activation is required for effective MEK inhibition in KRAS mutant tumors

31 March 2020

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ERKs: a family of protein-serine/threonine kinases that are activated and tyrosine phosphorylated in response to insulin and NGF

31 March 2020

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Ordered phosphorylation of p42mapk by MAP kinase kinase

31 March 2020

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Structure-guided design of potent and selective pyrimidylpyrrole inhibitors of extracellular signal-regulated kinase (ERK) using conformational control

31 March 2020

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ERK inhibition overcomes acquired resistance to MEK inhibitors.

31 March 2020

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Identification of a selective ERK inhibitor and structural determination of the inhibitor-ERK2 complex

31 March 2020

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Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors

31 March 2020

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Resistance to BRAF-targeted therapy in melanoma

31 March 2020

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

31 March 2020

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

31 March 2020

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Relief of feedback inhibition of HER3 transcription by RAF and MEK inhibitors attenuates their antitumor effects in BRAF-mutant thyroid carcinomas.

31 March 2020

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

31 March 2020

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

31 March 2020

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

31 March 2020

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Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma

31 March 2020

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A genome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition

31 March 2020

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Elucidating distinct roles for NF1 in melanomagenesis

31 March 2020

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Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence

31 March 2020

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Mapping the molecular determinants of BRAF oncogene dependence in human lung cancer.

31 March 2020

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

31 March 2020

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

31 March 2020

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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

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Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma

31 March 2020

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

31 March 2020

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COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

31 March 2020

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Mixed lineage kinases activate MEK independently of RAF to mediate resistance to RAF inhibitors

31 March 2020

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MEK1 mutations confer resistance to MEK and B-RAF inhibition

31 March 2020

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MAP kinase pathway alterations in BRAF-mutant melanoma patients with acquired resistance to combined RAF/MEK inhibition

31 March 2020

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Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance

31 March 2020

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Antiproliferative effects of continued mitogen-activated protein kinase pathway inhibition following acquired resistance to BRAF and/or MEK inhibition in melanoma.

31 March 2020

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Discovery of novel, dual mechanism ERK inhibitors by affinity selection screening of an inactive kinase

31 March 2020

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A unique inhibitor binding site in ERK1/2 is associated with slow binding kinetics.

31 March 2020

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Active Ras induces heterodimerization of cRaf and BRaf

31 March 2020

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/25435214

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1038/NRD4281

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1 September 2017

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