Selected Approaches to Disrupting Protein-Protein Interactions within the MAPK/RAS Pathway

被引:9
作者
Harwood, Stephen J. [1 ]
Smith, Christopher R. [1 ]
Lawson, J. David [1 ]
Ketcham, John M. [1 ]
机构
[1] Mirati Therapeut, 3545 Cray Court, San Diego, CA 92121 USA
关键词
MAPK; KRAS; RAS; protein-protein interactions; X-ray crystallography; RAF INHIBITOR; DRUG DISCOVERY; COVALENT INHIBITOR; STRUCTURAL BASIS; SMALL MOLECULES; HUMAN CANCER; SH3; DOMAIN; BRAF; MELANOMA; SURVIVAL;
D O I
10.3390/ijms24087373
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Within the MAPK/RAS pathway, there exists a plethora of protein-protein interactions (PPIs). For many years, scientists have focused efforts on drugging KRAS and its effectors in hopes to provide much needed therapies for patients with KRAS-mutant driven cancers. In this review, we focus on recent strategies to inhibit RAS-signaling via disrupting PPIs associated with SOS1, RAF, PDE delta, Grb2, and RAS.
引用
收藏
页数:21
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