(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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PubMed ID

25435214

1 September 2017

Poulikos I Poulikakos

series ordinal

2

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1 September 2017

1 December 2014

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Nature Reviews Drug Discovery

1 September 2017

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1 September 2017

13

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1 September 2017

12

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1 September 2017

928-942

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https://scigraph.springernature.com/pub.10.1038/nrd4281

1 September 2017

0 references

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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

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Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization

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

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

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31 March 2020

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31 March 2020

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31 March 2020

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

31 March 2020

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31 March 2020

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31 March 2020

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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

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31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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Improved survival with MEK inhibition in BRAF-mutated melanoma

31 March 2020

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31 March 2020

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Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations

31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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31 March 2020

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

31 March 2020

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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

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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

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31 March 2020

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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

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Ordered phosphorylation of p42mapk by MAP kinase kinase

31 March 2020

1 reference

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

31 March 2020

1 reference

ERK inhibition overcomes acquired resistance to MEK inhibitors.

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Resistance to BRAF-targeted therapy in melanoma

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

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

Elucidating distinct roles for NF1 in melanomagenesis

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

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

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

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

31 March 2020

1 reference

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

31 March 2020

1 reference

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

31 March 2020

1 reference

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

31 March 2020

1 reference

MEK1 mutations confer resistance to MEK and B-RAF inhibition

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

31 March 2020

1 reference

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

1 reference

1 September 2017

1 reference

PubMed ID

25435214