A critical update on the strategies towards modulators targeting androgen receptors

Hongyu Luan; Pengfei Xu; Ying Meng; Zhiyu Li; Jinlei Bian

doi:10.1016/j.bmc.2020.115554

A critical update on the strategies towards modulators targeting androgen receptors

Bioorg Med Chem. 2020 Jul 1;28(13):115554. doi: 10.1016/j.bmc.2020.115554. Epub 2020 May 12.

Authors

Hongyu Luan¹, Pengfei Xu¹, Ying Meng¹, Zhiyu Li², Jinlei Bian³

Affiliations

¹ Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China.
² Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China. Electronic address: zhiyuli@cpu.edu.cn.
³ Jiangsu Key Laboratory of Drug Design and Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, People's Republic of China. Electronic address: Bianjl@cpu.edu.cn.

PMID: 32546299
DOI: 10.1016/j.bmc.2020.115554

Abstract

Prostate cancer is the most common carcinoma of the male urinary system in developed countries. Androgen deprivation therapy has been commonly used in the treatment of prostate cancer for decades, but most patients will inevitably develop into more aggressive castration-resistant prostate cancer. Therefore, novel strategies are urgent to address this resistance mechanism. In this review, we discussed some new strategies for targeting androgen receptors through degradation pathways as potential treatments for prostate cancer.

Keywords: AR antagonists; Androgen Receptor; PROTACs; Prostate cancer; SARDs.

Publication types

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

MeSH terms

Androgen Receptor Antagonists / chemistry*
Androgen Receptor Antagonists / pharmacology
Animals
Antineoplastic Agents / chemistry*
Antineoplastic Agents / pharmacology
Drug Resistance, Neoplasm
Drug Screening Assays, Antitumor
Heat-Shock Proteins / metabolism
Humans
Male
Prostatic Neoplasms / drug therapy*
Proteolysis
Receptors, Androgen / metabolism*
Signal Transduction
Thiohydantoins / chemistry
Ubiquitination

Substances

Androgen Receptor Antagonists
Antineoplastic Agents
Heat-Shock Proteins
Receptors, Androgen
Thiohydantoins
apalutamide