Arresting kinase suppressor of Ras in an inactive state

Chinese Journal of Cancer

Yahia Mabkhot¹  Syed Lal Badshah² 

[1] Department of Chemistry, College of Science, King Saud University;Department of Chemistry, Islamia College University Peshawar;

关键词: Ras;    Cancer;    Quinazoline analogues;    Structure–activity relationship;    Kinase inhibitors;   

DOI  :  10.1186/s40880-017-0181-z

来源: DOAJ

【 摘 要 】

Abstract Ras protein signaling pathways are important in controlling the plight of different types of cancer. Here we discussed the paper entitled “Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling” published in Nature journal on inactivating the kinase suppressor of Ras (KSR) protein using a small molecule as an inhibitor by Dhawan et al. A biphenyl ether analogue of a quinazoline binds in one of the binding pockets of KSR and results in stabilization of its inactive state. In this inactive state, KSR is unable to take part in the cascade of protein association to perform the signalling process.

【 授权许可】

Unknown