Targeting the Androgen Receptor with Steroid Conjugates | Zendy

Paul M. Levine | Zendy; Michael J. Garabedian | Zendy; Kent Kirshenbaum | Zendy

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Targeting the Androgen Receptor with Steroid Conjugates

Author(s) -

Paul M. Levine,

Michael J. Garabedian,

Kent Kirshenbaum

Publication year - 2014

Publication title -

journal of medicinal chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 2.01

H-Index - 261

eISSN - 1520-4804

pISSN - 0022-2623

DOI - 10.1021/jm500101h

Subject(s) - androgen receptor , prostate cancer , chemistry , pharmacology , steroid , androgen receptor antagonists , cancer research , receptor , androgen , potency , prostate , cancer , medicine , hormone , in vitro , biochemistry

The androgen receptor (AR) is a major therapeutic target in prostate cancer pharmacology. Progression of prostate cancer has been linked to elevated expression of AR in malignant tissue, suggesting that AR plays a central role in prostate cancer cell biology. Potent therapeutic agents can be precisely crafted to specifically target AR, potentially averting systemic toxicities associated with nonspecific chemotherapies. In this review, we describe various strategies to generate steroid conjugates that can selectively engage AR with high potency. Analogies to recent developments in nonsteroidal conjugates targeting AR are also evaluated. Particular focus is placed on potential applications in AR pharmacology. The review culminates with a description of future prospects for targeting AR.

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