TLDR Researchers developed new compounds that target the androgen receptor effectively with fewer side effects.
The study designed, synthesized, and evaluated second-generation nonsteroidal selective androgen receptor modulators (SARMs) to improve metabolic stability and pharmacologic activity. Several new compounds showed high binding affinity to the androgen receptor (AR) and significant agonist activity, comparable to dihydrotestosterone (DHT). In vivo tests on castrated male rats demonstrated that compounds S-5, S-6, S-9, and S-10 exhibited strong anabolic activity with minimal androgenic effects. The research provided evidence of a new class of tissue-selective SARMs with favorable pharmacokinetic profiles, warranting further exploration of their dose-response and structure-activity relationships. The study was supported by the National Institute of Diabetes and Digestive and Kidney Diseases and the Van Vleet Professor funds.
204 citations,
February 2000 in “Current Medicinal Chemistry” Antiandrogens like flutamide are effective in treating conditions like prostate cancer and hair loss, but there's a need for more potent versions. Understanding their structure can help develop better treatments.
209 citations,
March 1998 in “Biochemical and biophysical research communications” Scientists found new nonsteroidal compounds that can act like natural male hormones and might help treat male fertility and hormone issues.
1 citations,
January 2013 in “MedChemComm” PF-05314882 selectively activates androgen receptors without much effect on prostate and may help in prostate cancer treatment and hair loss prevention.
658 citations,
June 2003 in “Endocrine reviews” Male hormones may play a role in the development of heart disease, and more research is needed to understand their effects.
35 citations,
October 2011 in “Medicine and science in sports and exercise” Muscles can make their own androgens, which may help muscle growth.
2 citations,
November 2017 in “Elsevier eBooks” Different substances that activate or block the androgen receptor can affect male development and treat conditions like prostate cancer.
2 citations,
December 2013 in “Cancer research” Enobosarm may effectively treat androgen receptor-positive breast cancer with fewer side effects.
