Probing Androgen Receptor Co-Factor Selectivity Profiles: A Chemical Tool to Determine Cross-Talk Between Androgen Receptor and Beta-Catenin In Vivo

January 2013 in “ MedChemComm ”

Edward J. Kilbourne, Thomas Kenney, Susan Chippari, Christopher J. McNally, Yihe Wang, Hieu Lam, Karthick Vishwanathan, Sunil Nagpal, Catherine C. Thompson, Eugene L. Piatnitski Chekler

androgen receptor Selective Androgen Receptor Modulator SARM PF-05314882 AR-mediated transcription Wnt reporter activity androgenic activity scalp hair loss β-catenin prostate seminal vesicles LH levels

TLDR PF-05314882 selectively activates androgen receptors without much effect on prostate and may help in prostate cancer treatment and hair loss prevention.

The document from 2013 detailed a study on a Selective Androgen Receptor Modulator (SARM) named PF-05314882, which demonstrated tissue-selective androgen receptor (AR) activity in rats without promoting interaction between AR and β-catenin. PF-05314882 bound to the AR with good affinity and activated AR-mediated transcription in vitro but showed weak activity on androgen-AR dependent inhibition of Wnt reporter activity. In castrated rats, PF-05314882 increased muscle weight and liver metabolic gene expression while minimally affecting the prostate, seminal vesicles, and LH levels. The study concluded that PF-05314882 could be a valuable tool to study AR and β-catenin cross-talk and may have therapeutic potential for conditions like prostate cancer and possibly avoiding androgenic activity in the scalp related to hair loss. The number of rats used in the study was not specified.

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