重塑 KRAS。

Remodeling KRAS.

机构信息

Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, 20 North Pine St., Baltimore, MD 21201, USA.

出版信息

Structure. 2017 Sep 5;25(9):1323-1324. doi: 10.1016/j.str.2017.08.012.

DOI:10.1016/j.str.2017.08.012

PMID:28877504

Abstract

Mutations in members of the RAS family of small GTPases have been associated with numerous human cancers. However, RAS family members are notoriously difficult to target. In this issue of Structure, Lu et al. (2017) examine the effects of two compounds with distinct chemical scaffolds on the structure and dynamics of an oncogenic KRAS mutant, thus highlighting the usefulness of HDX-MS for drug development.

摘要

RAS 家族小 GTP 酶成员的突变与许多人类癌症有关。然而，RAS 家族成员是出了名的难以靶向。在本期结构杂志中，Lu 等人（2017 年）研究了两种具有不同化学支架的化合物对致癌 KRAS 突变体结构和动力学的影响，从而突出了 HDX-MS 在药物开发中的有用性。