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- W3131446155 abstract "Significance There is no nonhormonal contraceptive pill for men, although hundreds of genes have been identified to play roles during spermatogenesis and fertilization in the male reproductive tract. To address the absence of contraceptive drugs for men, we established a DNA-encoded chemistry technology (DEC-Tec) platform. Our drug discovery campaign on BRDT, a validated spermatogenic-specific contraceptive target, yielded rapid discovery of potent and specific inhibitors of the second bromodomain of BRDT that have unique binding characteristics to BRDT-BD2 relative to BRDT-BD1. Our study emphasizes the robustness and validation of the DEC-Tec platform where the obtained structure–affinity relationship data would allow us to identify specific protein binders immediately without performing exhaustive medicinal chemistry optimization of compounds with potential as male contraceptives." @default.
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- W3131446155 date "2021-02-26" @default.
- W3131446155 modified "2023-10-03" @default.
- W3131446155 title "Discovery and characterization of bromodomain 2–specific inhibitors of BRDT" @default.
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- W3131446155 doi "https://doi.org/10.1073/pnas.2021102118" @default.
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