WIKINDX
WIKINDX Resources
Al Noman, Md Abdullah, et al. "Retinoic acid receptor antagonists for male contraception: current status." Biology of reproduction 103.2 (2020): 390-99.
DOI: 10.1093/biolre/ioaa122
ID no. (ISBN etc.): 0006-3363
BibTeX citation key: AlNoman2020
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Categories:
Keywords: Birth control, Cell receptors, Dehydrogenases, DNA, Gene expression, Male contraception, Metabolism, Sperm, Spermatogenesis, Vitamin A
Creators: Al Noman, Chung, Georg, Kyzer, Wolgemuth
Collection: Biology of reproduction
Keywords: Birth control, Cell receptors, Dehydrogenases, DNA, Gene expression, Male contraception, Metabolism, Sperm, Spermatogenesis, Vitamin A
Creators: Al Noman, Chung, Georg, Kyzer, Wolgemuth
Collection: Biology of reproduction
Attachments
oxford-ioaa122.pdf 
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 structureâ??activity studies of retinoic acid receptor alpha antagonists that provide insight for the design of novel alpha-selective ligands. Summary sentence Fertility studies with retinoic acid receptor antagonists in male mice and the current state of RARA-selective antagonist development are reviewed.