The androgen receptor-targeted proteolysis targeting chimera and other alternative therapeutic choices in overcoming the resistance to androgen deprivation treatment in prostate cancer

Androgen receptor (AR) plays a vital role in prostate cancer (PCa), including castration-resistant PCa, by retaining AR signalling. Androgen deprivation treatment (ADT) has been the standard treatment in the past decades. A great number of AR antagonists initially had been found effective in tumour...

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Bibliographic Details
Published in:Clinical & translational oncology 2023-02, Vol.25 (2), p.352-363
Main Authors: Li, Liuxun, Xu, Jiangli
Format: Article
Language:English
Subjects:
Androgen Antagonists - therapeutic use
Androgens - genetics
Androgens - metabolism
Androgens - therapeutic use
Drug Resistance, Neoplasm - genetics
Humans
Male
Medicine
Medicine & Public Health
Oncology
Prostatic Neoplasms - drug therapy
Prostatic Neoplasms, Castration-Resistant - drug therapy
Prostatic Neoplasms, Castration-Resistant - pathology
Proteolysis Targeting Chimera
Receptors, Androgen - metabolism
Review
Review Article
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Summary:Androgen receptor (AR) plays a vital role in prostate cancer (PCa), including castration-resistant PCa, by retaining AR signalling. Androgen deprivation treatment (ADT) has been the standard treatment in the past decades. A great number of AR antagonists initially had been found effective in tumour remission; however, most PCa relapsed that caused by pre-translational resistance such as AR mutations to turn antagonist into agonist, and AR variants to bypass the androgen binding. Recently, several alternative therapeutic choices have been proposed. Among them, proteolysis targeting chimera (PROTAC) acts different from traditional drugs that usually function as inhibitors or antagonists, and it degrades oncogenic protein and does not disrupt the transcription of an oncogene. This review first discussed some essential mechanisms of ADT resistance, and then introduced the application of AR-targeted PROTAC in PCa cells, as well as other AR-targeted therapeutic choices.
ISSN:1699-3055
1699-048X
1699-3055
DOI:10.1007/s12094-022-02957-x