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.

View this study on pubs.rsc.org →

Discuss this study in the Community →

Research cited in this study

1 / 1 results

research A Mouse Model of Androgenetic Alopecia

42 citations, March 2010 in “Endocrinology”

Mice with human gene experienced hair loss when treated with DHT.

Similar Research

5 / 1000+ results

research The Selective Androgen Receptor Modulator GTx-024 (Enobosarm) Improves Lean Body Mass and Physical Function in Healthy Elderly Men and Postmenopausal Women: Results of a Double-Blind, Placebo-Controlled Phase II Trial

306 citations, August 2011 in “Journal of cachexia, sarcopenia and muscle”

Enobosarm significantly increased muscle mass and improved physical function in elderly men and postmenopausal women without serious side effects.

research Recent Discoveries and Developments of Androgen Receptor-Based Therapy for Prostate Cancer

17 citations, January 2015 in “MedChemComm”

New treatments for prostate cancer are less toxic and show promise, but more research is needed to enhance their effectiveness and reduce side effects.

research New Approaches to the Treatment of Osteoporosis

28 citations, August 2000 in “Current Opinion in Chemical Biology”

Future osteoporosis treatments should focus on increasing bone growth, with many promising options available.

research Androgen Receptor: A Promising Therapeutic Target in Breast Cancer

21 citations, March 2019 in “Critical Reviews in Clinical Laboratory Sciences”

The androgen receptor is a promising target for breast cancer treatment, especially in triple-negative cases, but more research is needed for personalized therapies.

research Androgen Receptor Modulators: A Review of Recent Patents and Reports (2012-2018)

23 citations, May 2019 in “Expert Opinion on Therapeutic Patents”

New androgen receptor modulators show promise for treating diseases like prostate cancer and muscle wasting.

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

Research cited in this study

research A Mouse Model of Androgenetic Alopecia

Related Community Posts Join

community Could a reversed SARM designed for the scalp serve as a replacement for oral Dut and Fin?

community If Minoxidil Beards are permanent, why should Finasteride be unable to keep Minoxidil Gains on the scalp?

community Why is Kevin Mann (Haircafe) Hated?

community Would there be ANY reason to still take 5AR inhibitors if pyrilutamide does what is intended?

community PSA: Most men who stay on Fin will see the sexual side effects go away. Stop the fear mongering