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Frontiers in Medical Science Research, 2019, 1(1); doi: 10.25236/FMSR.20190106.

Research Advanced in Small Molecular Inhibitors of Human BRDT which for male contraceptives development

Author(s)

Juan Zhang, Hui Li

Corresponding Author:
Juan Zhang
Affiliation(s)

Reproductive Medicine Center of Zhuzhou Central Hospital, Zhuzhou, China

Abstract

Testis specific Bromodomain proteins (BRDT) belong to the BET protein (Bromodomain and extra-terminal),which only expressed in testis . Recent studies have found that broad-spectrum BET protein inhibitor JQ1 can affect the binding between the BD1 domain of BRDT and acetylated histone H4, thus inhibiting sperm formation. Therefore, it has become a star molecule in male reproductive mechanism research and contraceptive drug development. At present, several research on BRDT inhibitors has started by using JQ1-based virtual screening and  in vitro binding assay to screen out a variety of small molecular compounds that can effectively reduce the activity of BRDT. In this paper, the progress in this field in recent years is reviewed, and the screening direction of this kind of small molecule compounds in the later stage is analyzed and discussed.

Keywords

Testicular specific bromine domain protein; Male antifertility; Spermatogenesis; Virtual screening

Cite This Paper

Juan Zhang, Hui Li, Research Advanced in Small Molecular Inhibitors of Human BRDT which for male contraceptives development. Frontiers in Medical Science Research (2019) Vol. 1 Issue 1: 61-67. https://doi.org/10.25236/FMSR.20190106.

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