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将Ras的激酶抑制因子捕获于非活性状态。

Arresting kinase suppressor of Ras in an inactive state.

作者信息

Badshah Syed Lal, Mabkhot Yahia

机构信息

Department of Chemistry, Islamia College University Peshawar, Peshawar, Khyber Pukhtoonkhwa, 25120, Pakistan.

Department of Chemistry, College of Science, King Saud University, Riyadh, 11451, Saudi Arabia.

出版信息

Chin J Cancer. 2017 Jan 9;36(1):5. doi: 10.1186/s40880-017-0181-z.

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.

摘要

Ras蛋白信号通路在控制不同类型癌症的状况中起着重要作用。在此,我们讨论了Dhawan等人发表在《自然》杂志上的题为《小分子稳定KSR非活性状态拮抗致癌Ras信号传导》的论文,该论文利用一种小分子作为抑制剂来使Ras激酶抑制蛋白(KSR)失活。喹唑啉的一种联苯醚类似物结合在KSR的一个结合口袋中,导致其非活性状态的稳定。在这种非活性状态下,KSR无法参与蛋白质关联的级联反应来执行信号传导过程。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/15cd/5223383/f18052e03558/40880_2017_181_Fig1_HTML.jpg

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