Development of inhibitors for uPAR: blocking the interaction of uPAR with its partners

Cai Yuan; Zhanzhi Guo; Shujuan Yu; Longguang Jiang; Mingdong Huang

doi:10.1016/j.drudis.2021.01.016

Development of inhibitors for uPAR: blocking the interaction of uPAR with its partners

Drug Discov Today. 2021 Apr;26(4):1076-1085. doi: 10.1016/j.drudis.2021.01.016. Epub 2021 Jan 21.

Authors

Cai Yuan¹, Zhanzhi Guo¹, Shujuan Yu², Longguang Jiang³, Mingdong Huang⁴

Affiliations

¹ College of Biological Science and Engineering, Fuzhou University, Fuzhou, Fujian, 350116, China.
² College of Chemistry, Fuzhou University, Fujian, 350116, China.
³ College of Chemistry, Fuzhou University, Fujian, 350116, China. Electronic address: jianglg@fzu.edu.cn.
⁴ College of Chemistry, Fuzhou University, Fujian, 350116, China. Electronic address: hmd_lab@fzu.edu.cn.

PMID: 33486111
DOI: 10.1016/j.drudis.2021.01.016

Abstract

Urokinase-type plasminogen activator receptor (uPAR) mediates a multitude of biological activities, has key roles in several clinical indications, including malignancies and inflammation, and, thus, has attracted intensive research over the past few decades. The pleiotropic functions of uPAR can be attributed to its interaction with an array of partners. Many inhibitors have been developed to intervene with the interaction of uPAR with these partners. Here, we review the development of these classes of uPAR inhibitor and their inhibitory mechanisms to promote the translation of these inhibitors to clinical applications.

Publication types

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

MeSH terms

Drug Discovery / methods*
Humans
Receptors, Urokinase Plasminogen Activator* / antagonists & inhibitors
Receptors, Urokinase Plasminogen Activator* / metabolism
Signal Transduction / drug effects*

Substances

Receptors, Urokinase Plasminogen Activator