Dual-target inhibitors based on COX-2: a review from medicinal chemistry perspectives

Author:

Zhang Fengmei12,Zhu Guonian12,Li Yangqian12,Qi Yawen12,Wang Zhoufeng1234,Li Weimin1234

Affiliation:

1. Department of Pulmonary & Critical Care Medicine, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China

2. State Key Laboratory of Respiratory Health & Multimorbidity, West China Hospital, Chengdu, 610041, Sichuan, China

3. Precision Medicine Center, Precision Medicine Key Laboratory of Sichuan Province, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China

4. The Research Units of West China, Chinese Academy of Medical Sciences, West China Hospital, Chengdu, 610041, Sichuan, China

Abstract

Inhibitors of COX-2 constitute a class of anti-inflammatory analgesics, showing potential against certain types of cancer. However, such inhibitors are associated with cardiovascular toxicity. Moreover, although single-target molecules possess specificity for particular targets, they often lead to poor safety, low efficacy and drug resistance due to compensatory mechanisms. A new generation of dual-target drugs that simultaneously inhibit COX-2 and another target is showing strong potential to treat cancer or reduce adverse cardiac effects. The present perspective focuses on the structure and functions of COX-2, and its role as a therapeutic target. It also explores the current state and future possibilities for dual-target strategies from a medicinal chemistry perspective.

Funder

Precision Medicine Key Laboratory of Sichuan Province

Natural Science Foundation of Sichuan Province

National Natural Science Foundation of China

Publisher

Future Science Ltd

Subject

Drug Discovery,Pharmacology,Molecular Medicine

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