Open AccessRho Family Proteins: Covalent Inhibitors Allosterically Block the Activation of Rho Family Proteins and Suppress Cancer Cell Invasion (Adv. Sci. 14/2020)
Author(s) -
Sun Zhongya,
Zhang Hao,
Zhang Yuanyuan,
Liao Liping,
Zhou Wen,
Zhang Fengcai,
Lian Fulin,
Huang Jing,
Xu Pan,
Zhang Rukang,
Lu Wenchao,
Zhu Mingrui,
Tao Hongru,
Yang Feng,
Ding Hong,
Chen Shijie,
Yue Liyan,
Zhou Bing,
Zhang Naixia,
Tan Minjia,
Jiang Hualiang,
Chen Kaixian,
Liu Bo,
Liu Chuanpeng,
Dang Yongjun,
Luo Cheng
Publication year - 2020
Publication title -
advanced science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.388
H-Index - 100
ISSN - 2198-3844
DOI - 10.1002/advs.202070079
Subject(s) - allosteric regulation , chemistry , covalent bond , rhoa , drug discovery , protein family , computational biology , biochemistry , biology , enzyme , signal transduction , gene , organic chemistry
In article number 2000098, Bo Liu, Chuanpeng Liu, Yongjun Dang, Cheng Luo, and co‐workers describe the fi rst covalent and allosteric inhibitors targeting RhoA, which had been deemed as an “undruggable” protein target. This study reveals a novel allosteric regulatory site within the Rho family, which could be exploited for anti‐metastasis drug development, and also provides a novel strategy for inhibitor discovery toward “undruggable” proteins.