Targeting Tubulin-colchicine Site for Cancer Therapy: Inhibitors, Antibody- Drug Conjugates and Degradation Agents

Author:

Duan Yongtao1,Liu Wei1,Tian Liang1,Mao Yanna1,Song Chuanjun2

Affiliation:

1. Henan Provincial Key Laboratory of Children's Genetics and Metabolic Diseases, Children's Hospital Affiliated to Zhengzhou University, Henan Children's Hospital, Zhengzhou Children's Hospital, Zhengzhou, 450018, China

2. College of Chemistry and Molecular Engineering, Zhengzhou University, Zhengzhou, 450001, China

Abstract

Microtubules are essential for the mitotic division of cells and have been an attractive target for antitumour drugs due to the increased incidence of cancer and significant mitosis rate of tumour cells. In the past few years, tubulin-colchicine binding site, as one of the three binding pockets including taxol-, vinblastine- and colchicine-binding sites, has been focused on to design tubulin-destabilizing agents including inhibitors, antibody-drug conjugates and degradation agents. The present review is the first to cover a systemic and recent synopsis of tubulin-colchicine binding site agents. We believe that it would provide an increase in our understanding of receptor-ligand interaction pattern and consciousness of a series of challenges about tubulin target druggability.

Funder

Henan Medical Science and Technology Program

Henan Province Postdoctoral Science Foundation

National Natural Science Foundation of China

Publisher

Bentham Science Publishers Ltd.

Subject

Drug Discovery,General Medicine

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