2. Academic Validation
  3. Recent advances in the discovery and development of glyoxalase I inhibitors

Recent advances in the discovery and development of glyoxalase I inhibitors

  • Bioorg Med Chem. 2020 Feb 15;28(4):115243. doi: 10.1016/j.bmc.2019.115243.
Tian Jin 1,  Lu Zhao 2,  Hong-Ping Wang 3,  Mao-Lin Huang 4,  Yan Yue 4,  Chichong Lu 5,  Zhe-Bin Zheng 6
Affiliations

Affiliations

  • 1 Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052, People's Republic of China. Electronic address: jintian@cdu.edu.cn.
  • 2 Sichuan Institute for Food and Drug Control, Chengdu 611731, People's Republic of China. Electronic address: zhaolu0309@126.com.
  • 3 Sichuan Institute for Food and Drug Control, Chengdu 611731, People's Republic of China.
  • 4 Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052, People's Republic of China.
  • 5 Department of Chemistry, School of Science, Beijing Technology and Business University, Beijing 100048, People's Republic of China. Electronic address: luchichong@btbu.edu.cn.
  • 6 Antibiotics Research and Re-evaluation Key Laboratory of Sichuan Province, Sichuan Industrial Institute of Antibiotics, Chengdu University, Chengdu 610052, People's Republic of China. Electronic address: zhebinzheng@hotmail.com.
PMID: 31879183 DOI: 10.1016/j.bmc.2019.115243
Abstract

Glyoxalase I (GLO1) is a homodimeric Zn2+-metalloenzyme that catalyses the transformation of methylglyoxal (MG) to d-lacate through the intermediate S-d-lactoylglutathione. Growing evidence indicates that GLO1 has been identified as a potential target for the treatment Cancer and Other Diseases. Various inhibitors of GLO1 have been discovered or developed over the past several decades including natural or natural product-based inhibitors, GSH-based inhibitors, non-GSH-based inhibitors, etc. The aim of this review is to summarize recent achievements of concerning discovery, design strategies, as well as pharmacological aspects of GLO1 inhibitors with the target of promoting their development toward clinical application.

Keywords

Fragment-based drug discovery strategy; GSH-based inhibitors; High throughput screening; Natural or natural product-based inhibitors; Non-GSH-based inhibitors; Photo-affinity labeling and affinity pull-down protocols.

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