New perspectives for targeting RAF kinase in human cancer. (Q47688064)

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28984291 AND SRC:MED&resulttype=core&format=json

1 April 2020

title

New perspectives for targeting RAF kinase in human cancer (English)

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1 April 2020

author

Evripidis Gavathiotis

series ordinal

2

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1 April 2020

author name string

Zoi Karoulia

series ordinal

1

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1 April 2020

Poulikos I Poulikakos

series ordinal

3

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1 April 2020

language of work or name

English

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publication date

6 October 2017

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https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28984291 AND SRC:MED&resulttype=core&format=json

1 April 2020

published in

Nature Reviews Cancer

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volume

17

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issue

11

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1 April 2020

page(s)

676-691

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Regulation of RAF protein kinases in ERK signalling

1 April 2020

cites work

1 reference

MAP kinase signalling pathways in cancer

21 January 2018

1 reference

The RAF proteins take centre stage

21 January 2018

1 reference

Raf family kinases: old dogs have learned new tricks

21 January 2018

1 reference

Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer

21 January 2018

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Ras signaling and therapies

21 January 2018

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Inhibition of Ras for Cancer Treatment: The Search Continues

21 January 2018

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MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road

21 January 2018

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Mutations of the BRAF gene in human cancer

21 January 2018

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2

21 January 2018

1 reference

Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond

21 January 2018

1 reference

Genomic Classification of Cutaneous Melanoma

21 January 2018

1 reference

Comprehensive molecular profiling of lung adenocarcinoma

21 January 2018

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BRAF mutations in hairy-cell leukemia

21 January 2018

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Recurrent BRAF mutations in Langerhans cell histiocytosis

21 January 2018

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BRAF mutation predicts sensitivity to MEK inhibition

21 January 2018

1 reference

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

21 January 2018

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Improved survival with vemurafenib in melanoma with BRAF V600E mutation

21 January 2018

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

21 January 2018

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Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma

21 January 2018

1 reference

Combined vemurafenib and cobimetinib in BRAF-mutated melanoma

21 January 2018

1 reference

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

21 January 2018

1 reference

Tunable-combinatorial mechanisms of acquired resistance limit the efficacy of BRAF/MEK cotargeting but result in melanoma drug addiction

21 January 2018

1 reference

Concurrent MEK2 mutation and BRAF amplification confer resistance to BRAF and MEK inhibitors in melanoma

21 January 2018

1 reference

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

21 January 2018

1 reference

An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling

21 January 2018

1 reference

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

21 January 2018

1 reference

Effect of dabrafenib on melanoma cell lines harbouring the BRAF(V600D/R) mutations

21 January 2018

1 reference

Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

21 January 2018

1 reference

Safety and efficacy of vemurafenib in BRAF(V600E) and BRAF(V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study

21 January 2018

1 reference

BRAF inhibitor activity in V600R metastatic melanoma

21 January 2018

1 reference

BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Autoregulation of the Raf-1 serine/threonine kinase

21 January 2018

1 reference

Mammalian Ras interacts directly with the serine/threonine kinase Raf

21 January 2018

1 reference

Complexes of Ras.GTP with Raf-1 and mitogen-activated protein kinase kinase

21 January 2018

1 reference

Ras activation of the Raf kinase: tyrosine kinase recruitment of the MAP kinase cascade

21 January 2018

1 reference

Dynamics-Driven Allostery in Protein Kinases

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization

21 January 2018

1 reference

A dimerization-dependent mechanism drives RAF catalytic activation

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation

21 January 2018

1 reference

Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

RAF inhibitors activate the MAPK pathway by relieving inhibitory autophosphorylation

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Mechanism and consequences of RAF kinase activation by small-molecule inhibitors

21 January 2018

1 reference

Mutant BRAF Melanomas—Dependence and Resistance

21 January 2018

1 reference

Targeting RAS-ERK signalling in cancer: promises and challenges

21 January 2018

1 reference

Targeting cancer with small molecule kinase inhibitors

21 January 2018

1 reference

Allosteric activation of functionally asymmetric RAF kinase dimers

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Inhibitor hijacking of Akt activation

21 January 2018

1 reference

PKC maturation is promoted by nucleotide pocket occupation independently of intrinsic kinase activity.

21 January 2018

1 reference

Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1).

21 January 2018

1 reference

Modulation of Activation-Loop Phosphorylation by JAK Inhibitors Is Binding Mode Dependent

21 January 2018

1 reference

RAF inhibitors that evade paradoxical MAPK pathway activation

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Discrete cytosolic macromolecular BRAF complexes exhibit distinct activities and composition

21 January 2018

1 reference

The distribution of BRAF gene fusions in solid tumors and response to targeted therapy

21 January 2018

1 reference

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

21 January 2018

1 reference

Rearrangements of the RAF kinase pathway in prostate cancer, gastric cancer and melanoma

21 January 2018

1 reference

Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120.

21 January 2018

1 reference

Clinical detection and categorization of uncommon and concomitant mutations involving BRAF.

21 January 2018

1 reference

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

21 January 2018

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

21 January 2018

1 reference

Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy

21 January 2018

1 reference

Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling

21 January 2018

1 reference

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

21 January 2018

1 reference

Therapy-induced tumour secretomes promote resistance and tumour progression

21 January 2018

1 reference

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

21 January 2018

1 reference

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

21 January 2018

1 reference

Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer

21 January 2018

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Vemurafenib in Multiple Nonmelanoma Cancers with BRAF V600 Mutations

21 January 2018

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Paradoxical activation of Raf by a novel Raf inhibitor

21 January 2018

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Discovery of a novel Raf kinase inhibitor

21 January 2018

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Sorafenib in advanced clear-cell renal-cell carcinoma

21 January 2018

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Sorafenib in advanced hepatocellular carcinoma

21 January 2018

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Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885

21 January 2018

1 reference

Antitumor efficacy of the novel RAF inhibitor GDC-0879 is predicted by BRAFV600E mutational status and sustained extracellular signal-regulated kinase/mitogen-activated protein kinase pathway suppression.

21 January 2018

1 reference

Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation

21 January 2018

1 reference

The c-Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK-ERK and Akt-independent mechanism

21 January 2018

1 reference

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

21 January 2018

1 reference

Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives

21 January 2018

1 reference

Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells

21 January 2018

1 reference

BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers

21 January 2018

1 reference

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

21 January 2018

1 reference

Selective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib-resistant melanoma cells

21 January 2018

1 reference

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

21 January 2018

1 reference

A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

21 January 2018

1 reference

CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and In Vivo Antitumor Activity

21 January 2018

1 reference

Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma.

21 January 2018

1 reference

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

21 January 2018

1 reference

Safety, activity, and immune correlates of anti-PD-1 antibody in cancer

21 January 2018

1 reference

Improved Survival with Ipilimumab in Patients with Metastatic Melanoma

21 January 2018

1 reference

Pembrolizumab versus Ipilimumab in Advanced Melanoma

21 January 2018

1 reference

Development of immuno-oncology drugs - from CTLA4 to PD1 to the next generations

21 January 2018

1 reference

Genomic and Transcriptomic Features of Response to Anti-PD-1 Therapy in Metastatic Melanoma

21 January 2018

1 reference

Regulation and role of Raf-1/B-Raf heterodimerization

21 January 2018

1 reference

RAF/RAS oncogenes and mismatch-repair status

21 January 2018

1 reference

A Braf kinase-inactive mutant induces lung adenocarcinoma.

21 January 2018

1 reference

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Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS.

2 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6000833

BRAF-inhibitor Associated MEK Mutations Increase RAF-Dependent and -Independent Enzymatic Activity

2 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6000833

Immunotolerance as a Mechanism of Resistance to Targeted Therapies in Melanoma

2 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6000833

A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas.

2 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=6000833

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

2 November 2018

1 reference

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Active Ras induces heterodimerization of cRaf and BRaf

2 November 2018

1 reference

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CSIG-19. FHL2 INTERACTS WITH EGFRVIII TO PROMOTE GLIOBLASTOMA GROWTH

2 November 2018

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31 March 2020

Identifiers

DOI

10.1038/NRC.2017.79

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28984291 AND SRC:MED&resulttype=core&format=json

1 April 2020

1 reference

https://www.ebi.ac.uk/europepmc/webservices/rest/search?query=EXT_ID:28984291 AND SRC:MED&resulttype=core&format=json

1 April 2020

PubMed publication ID

28984291

1 reference