Retinoic acid receptor antagonists for male contraception: current status.
Biol Reprod
; 103(2): 390-399, 2020 08 04.
Article
em En
| MEDLINE
| ID: mdl-32671394
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.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Espermatogênese
/
Receptores do Ácido Retinoico
/
Anticoncepção
Limite:
Animals
/
Humans
Idioma:
En
Revista:
Biol Reprod
Ano de publicação:
2020
Tipo de documento:
Article
País de afiliação:
Estados Unidos