The mechanism of Raf activation through dimerization-Reference-Cited by-同舟云学术

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The mechanism of Raf activation through dimerization

Published:2021 Issue:47 Volume:12 Page:15609-15619
ISSN:2041-6520
Container-title:Chemical Science
language:en
Short-container-title:Chem. Sci.

Author:

Zhang Mingzhen¹^ORCID,Maloney Ryan¹^ORCID,Jang Hyunbum¹^ORCID,Nussinov Ruth¹²^ORCID

Affiliation:

1. Computational Structural Biology Section, Frederick National Laboratory for Cancer Research in the Laboratory of Cancer Immunometabolism, National Cancer Institute, Frederick, MD 21702, USA

2. Department of Human Molecular Genetics and Biochemistry, Sackler School of Medicine, Tel Aviv University, Tel Aviv 69978, Israel

Abstract

We decipher an atomic-level mechanism of Raf activation through dimerization, revealing that the disruption of intramolecular π–π stacking at the dimer interface promotes the OFF-to-ON transition.

Funder

National Cancer Institute

Publisher

Royal Society of Chemistry (RSC)

Subject

General Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2021/SC/D1SC03444H

Reference70 articles.

1. Regulation of RAF protein kinases in ERK signalling

2. Allosteric activation of RAF in the MAPK signaling pathway

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

4. Targeting Aberrant RAS/RAF/MEK/ERK Signaling for Cancer Therapy

5. Vemurafenib: the first drug approved for BRAF-mutant cancer

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1. Targeting the RAS upstream and downstream signaling pathway for cancer treatment;European Journal of Pharmacology;2024-09

2. An overview of RAF kinases and their inhibitors (2019–2023);European Journal of Medicinal Chemistry;2024-09

3. Slower CDK4 and faster CDK2 activation in the cell cycle;Structure;2024-08

4. Impact of protein and small molecule interactions on kinase conformations;eLife;2024-08-01

5. Impact of protein and small molecule interactions on kinase conformations;eLife;2024-08-01

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