Targeting androgen receptor for prostate cancer therapy: From small molecules to PROTACs

被引：11

作者：

Avgeris, Ioannis ^{[1
]}

Pliatsika, Dimanthi ^{[1
,2
]}

Nikolaropoulos, Sotiris S. ^{[1
]}

Fousteris, Manolis A. ^{[1
]}

机构：

[1] Univ Patras, Dept Pharm, Lab Med Chem, GR-26500 Patras, Greece

[2] Zurich Univ Appl Sci ZHAW, Inst Chem & Biotechnol, Ctr Organ & Med Chem, Einsiedlerstr 3, CH-8820 Wadenswil, Switzerland

来源：

BIOORGANIC CHEMISTRY | 2022年 / 128卷

关键词：

Prostate cancer; Androgen receptor; Small molecules; PROTACs; SARDs; Structure-activity relationships; 3; BF3; SITE; BINDING-DOMAIN; ACTIVATION FUNCTION-1; PROTEIN-DEGRADATION; HIGHLY POTENT; DISCOVERY; ANTAGONISTS; INHIBITORS; ANTIANDROGEN; ABIRATERONE;

D O I：

10.1016/j.bioorg.2022.106089

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Prostate cancer (PCa) remains a serious type of cancer for men worldwide. The majority of new PCa cases are associated with androgen receptor (AR) hyperactivity. Various AR-targeting molecules that suppress its activity have been discovered. In this review, we present the already marketed antiandrogens and a selection of struc-turally and chemically interesting AR-targeting compounds, from a pharmacochemical perspective. Focus has been placed on the applied design approaches, structural evolution and structure-activity relationships of the most prominent compound classes. Passing from the traditional steroidal AR antagonists to the modern AR -targeting proteolysis targeting chimeras (PROTACs), we intend to provide a comprehensive overview on AR -targeting molecules for PCa treatment.

引用

页数：17

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