BET proteins: Investigating BRDT as a potential target for male contraception.
Bromodomain and extra terminal (BET) family proteins
Bromodomains
Contraception
Contraceptives
Journal
Bioorganic & medicinal chemistry letters
ISSN: 1464-3405
Titre abrégé: Bioorg Med Chem Lett
Pays: England
ID NLM: 9107377
Informations de publication
Date de publication:
15 03 2020
15 03 2020
Historique:
received:
15
10
2019
revised:
01
01
2020
accepted:
02
01
2020
pubmed:
6
2
2020
medline:
21
4
2021
entrez:
6
2
2020
Statut:
ppublish
Résumé
While many contraception options are available for women, birth control methods for men are limited to condoms and vasectomy. Past research into male contraceptives has focused on hormonal options but the associated side effects have thus far precluded this method from reaching the market. Non-hormonal male contraceptives and vas occlusion have also been explored, but to date no method has progressed past clinical testing. Recent interest in epigenetic research has unveiled a new potential non-hormonal male contraceptive target: the testis-specific bromodomain BRDT. Potent inhibitors for bromodomain-containing proteins are described in the literature, but a BRDT-specific compound has yet to be designed, prepared and tested. The high similarity between bromodomain proteins of the BET family makes development of selective and specific inhibitors both difficult and necessary. Selective inhibition of BRDT by a small molecule is an exciting new target in the search for a new non-hormonal male contraceptive.
Identifiants
pubmed: 32019712
pii: S0960-894X(20)30011-1
doi: 10.1016/j.bmcl.2020.126958
pmc: PMC7023680
mid: NIHMS1555481
pii:
doi:
Substances chimiques
BRDT protein, human
0
Contraceptive Agents, Male
0
Nuclear Proteins
0
Organic Chemicals
0
Proteins
0
bromodomain and extra-terminal domain protein, human
0
Types de publication
Journal Article
Research Support, N.I.H., Extramural
Review
Langues
eng
Sous-ensembles de citation
IM
Pagination
126958Subventions
Organisme : NICHD NIH HHS
ID : P50 HD093540
Pays : United States
Organisme : NICHD NIH HHS
ID : U54 HD093540
Pays : United States
Organisme : NICHD NIH HHS
ID : HHSN275201300017C
Pays : United States
Informations de copyright
Copyright © 2020 Elsevier Ltd. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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