Advances in the development of Rho GTPase inhibitors

Yijing Zhang; Guanyi Li; Yaxue Zhao

doi:10.1016/j.bmc.2023.117337

Advances in the development of Rho GTPase inhibitors

Bioorg Med Chem. 2023 Jul 15:90:117337. doi: 10.1016/j.bmc.2023.117337. Epub 2023 May 18.

Authors

Yijing Zhang¹, Guanyi Li¹, Yaxue Zhao²

Affiliations

¹ School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China.
² School of Pharmacy, Shanghai Jiao Tong University, 800 Dongchuan Road, Shanghai 200240, China. Electronic address: yaxuezhao@sjtu.edu.cn.

PMID: 37253305
DOI: 10.1016/j.bmc.2023.117337

Abstract

Rho guanosine triphosphatases (Rho GTPases), as members of the Ras superfamily, are GDP/GTP binding proteins that behave as molecular switches for the transduction of signals from external stimuli. Rho GTPases play essential roles in a number of cellular processes including cell cycle, cell polarity as well as cell migration. The dysregulations of Rho GTPases are related with various diseases, especially with cancers. Accumulating evidence supports that Rho GTPases play important roles in cancer development and progression. Rho GTPases become potential therapeutic targets for cancer therapy. And a number of inhibitors targeting Rho GTPases have been developed. In this review, we discuss their structural features, summarize their roles in cancer, and focus on the recent progress of their inhibitors, which are beneficial for the drug discovery targeting Rho GTPases.

Keywords: Cancer; Docking; Inhibitor; Rho GTPase; Virtual screening.

Publication types

Review
Research Support, Non-U.S. Gov't

MeSH terms

Cell Cycle
Cell Movement
Drug Discovery
Humans
Neoplasms* / drug therapy
rho GTP-Binding Proteins* / metabolism
rho GTP-Binding Proteins* / therapeutic use

Substances

rho GTP-Binding Proteins