Bioactive modulators targeting STING adaptor in cGAS-STING pathway

Xi Feng; Dongyu Liu; Zhiyu Li; Jinlei Bian

doi:10.1016/j.drudis.2019.11.007

Bioactive modulators targeting STING adaptor in cGAS-STING pathway

Drug Discov Today. 2020 Jan;25(1):230-237. doi: 10.1016/j.drudis.2019.11.007. Epub 2019 Nov 20.

Authors

Xi Feng¹, Dongyu Liu¹, Zhiyu Li², Jinlei Bian³

Affiliations

¹ Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China.
² Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China. Electronic address: zhiyuli@cpu.edu.cn.
³ Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China. Electronic address: bianjl@cpu.edu.cn.

PMID: 31758915
DOI: 10.1016/j.drudis.2019.11.007

Abstract

The cyclic GMP-AMP synthase (cGAS)-stimulator of interferon genes (STING)-pathway triggers innate immune responses by recognizing cytosolic DNA. Recent studies revealed that STING adaptor associates with various diseases, and several modulators targeting STING have been identified including three agonists that have entered clinical trials for treating cancer over the past 2 years. In particular, the efficacy of STING agonists and/or antagonists suggests adaptor STING as a potential therapeutic target for diverse diseases. Herein, we summarize the latest advances in understanding STING functioning and provide an overview of recent STING modulator discoveries, including structural details and the potential therapeutic applications of these modulators.

Publication types

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

MeSH terms

Animals
Humans
Membrane Proteins / agonists
Membrane Proteins / antagonists & inhibitors
Membrane Proteins / metabolism*
Nucleotidyltransferases / metabolism*
Signal Transduction

Substances

Membrane Proteins
STING1 protein, human
Nucleotidyltransferases
cGAS protein, human