Varaico: Literature-Extracted Genetic Variants

Gene:MAP2K1
Variant:p.K97R
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MAP2K1

NM_002755.4:p.K97R

Associated Papers

RAS-dependent RAF-MAPK hyperactivation by pathogenic RIT1 is a therapeutic target in Noonan syndrome-associated cardiac hypertrophy.

Cuevas-Navarro A et al.

Science Advances, 2023

ARAF protein kinase activates RAS by antagonizing its binding to RASGAP NF1.

Su W et al.

Molecular Cell, 2022

Discovery of MAP855, an Efficacious and Selective MEK1/2 Inhibitor with an ATP-Competitive Mode of Action.

Poddutoori R et al.

Journal of Medicinal Chemistry, 2022

LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors.

Monaco KA et al.

Clinical Cancer Research : an Official Journal of the American Association for Cancer Research, 2021

KRAS interaction with RAF1 RAS-binding domain and cysteine-rich domain provides insights into RAS-mediated RAF activation.

Tran TH et al.

Nature Communications, 2021

RAF dimer inhibition enhances the antitumor activity of MEK inhibitors in K-RAS mutant tumors.

Yuan X et al.

Molecular Oncology, 2020

Allele-Specific Mechanisms of Activation of MEK1 Mutants Determine Their Properties.

Gao Y et al.

Cancer Discovery, 2018

MEK drives BRAF activation through allosteric control of KSR proteins.

Lavoie H et al.

Nature, 2018

Inhibition of oncogenic BRAF activity by indole-3-carbinol disrupts microphthalmia-associated transcription factor expression and arrests melanoma cell proliferation.

Kundu A et al.

Molecular Carcinogenesis, 2017

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

Tang Z et al.

Molecular Cancer Therapeutics, 2015

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

Yao Z et al.

Cancer Cell, 2015

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

Peng SB et al.

Cancer Cell, 2015

U0126, a mitogen-activated protein kinase kinase 1 and 2 (MEK1 and 2) inhibitor, selectively up-regulates main isoforms of CYP3A subfamily via a pregnane X receptor (PXR) in HepG2 cells.

Smutny T et al.

Archives of Toxicology, 2014

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

Hatzivassiliou G et al.

Nature, 2013

Mammalian Ste20-like kinase (Mst2) indirectly supports Raf-1/ERK pathway activity via maintenance of protein phosphatase-2A catalytic subunit levels and consequent suppression of inhibitory Raf-1 phosphorylation.

Kilili GK et al.

The Journal of Biological Chemistry, 2010

Diacylglycerol kinase eta augments C-Raf activity and B-Raf/C-Raf heterodimerization.

Yasuda S et al.

The Journal of Biological Chemistry, 2009

Evidence for an important role of serine 16 and its phosphorylation in the stabilization of c-Mos.

Pham CD et al.

Oncogene, 1999

Evidence of a functional interaction between serine 3 and serine 25 Mos phosphorylation sites. A dominant inhibitory role of serine 25 phosphorylation on Mos protein kinase.

Yang Y et al.

The Journal of Biological Chemistry, 1998

Mutations of critical amino acids affect the biological and biochemical properties of oncogenic A-Raf and Raf-1.

Bosch E et al.

Oncogene, 1997

Negative regulation of Raf activity by binding of 14-3-3 to the amino terminus of Raf in vivo.

Rommel C et al.

Mechanisms of Development, 1997

Identification of 2 serine residues of MEK-1 that are differentially phosphorylated during activation by raf and MEK kinase.

Yan M et al.

The Journal of Biological Chemistry, 1994

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Regarding the variants extracted from papers and shown text snippets from research papers, the following holds: "Some rights reserved. This work permits non-commercial use, distribution and reproduction in any medium, provided the original author and source are credited."