The androgen receptor amino-terminal domain: structure, function and therapeutic potential

Signalling by the steroid hormone testosterone involves the androgen receptor (AR), a structurally dynamic protein. The amino-terminal domain of the AR makes up more than half of the protein and has been found to be intrinsically disordered. This structural plasticity mediates receptor-dependent tra...

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Published inEndocrine oncology Vol. 5; no. 1; p. e240061
Main Authors Hunter, Irene, Jamieson, Craig, McEwan, Iain J
Format Journal Article
LanguageEnglish
Published England Bioscientifica Ltd 01.01.2025
Bioscientifica
Subjects
androgen receptor
endocrine therapy resistance
prostate
Review
endocrine therapy resistance
prostate
androgen receptor
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Summary:Signalling by the steroid hormone testosterone involves the androgen receptor (AR), a structurally dynamic protein. The amino-terminal domain of the AR makes up more than half of the protein and has been found to be intrinsically disordered. This structural plasticity mediates receptor-dependent transcription, intradomain interactions and allosteric regulation. AR activity is a primary drug target in advanced and metastatic prostate cancer, a leading cause of cancer-related death in men. Recent research has focused on the amino-terminal domain as a novel drug target. In this review, we discuss the structural properties of the receptor and highlight some promising preclinical and clinical studies that aim to develop a drug discovery pipeline of small-molecule inhibitors targeting the amino-terminal domain.
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ISSN:2634-4793
2634-4793
DOI:10.1530/EO-24-0061