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Updated: Dec 14, 2025

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
Published on: March 21, 2017
Retinoic acid receptor antagonists for male contraception: current status†
Md Abdullah Al Noman1, Jillian L Kyzer1, Sanny S W Chung2
1Department of Medicinal Chemistry, College of Pharmacy, Institute for Therapeutics Discovery and Development, University of Minnesota, Minneapolis, MN, USA.
Abstract:
Retinoic acid receptor alpha (RARA), a nuclear receptor protein, has been validated as a target for male contraception by gene knockout studies and also pharmacologically using a pan-retinoic acid receptor antagonist. Retinoic acid receptor alpha activity is indispensable for the spermatogenic process, and therefore its antagonists have potential as male contraceptive agents. This review discusses the effects of systematic dosing regimen modifications of the orally bioavailable and reversible pan-antagonist BMS-189453 as well as studies with the alpha-selective antagonists BMS-189532 and BMS-189614 in a murine model. We also provide an overview of structure-activity studies of retinoic acid receptor alpha antagonists that provide insight for the design of novel alpha-selective ligands.
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