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- W4281622422 abstract "Significance BET bromodomain inhibition is therapeutic in multiple diseases; however, pan-BET inhibitors have induced significant myelosuppression and gastrointestinal toxicity, perhaps due to inhibition of both tandem bromodomains (BD) of all BET family members. However, selective inhibition of just the first BD (BD1) phenocopies pan-BET inhibitor activity in preclinical models of cancer, other diseases, and, for BRDT, in the testes for a contraceptive effect. Here, we leveraged our multibillion-molecule collection of DNA-encoded chemical libraries (DECLs) to identify BET BD1-selective inhibitors of specific chirality with high potency, stability, and good cellular activity. Our findings highlight the robustness and efficiency of the DECL platform to identify specific, potent protein binders that have promise as potential anticancer and anti-inflammatory agents and as male contraceptives." @default.
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- W4281622422 date "2022-05-27" @default.
- W4281622422 modified "2023-10-18" @default.
- W4281622422 title "Discovery of potent BET bromodomain 1 stereoselective inhibitors using DNA-encoded chemical library selections" @default.
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- W4281622422 doi "https://doi.org/10.1073/pnas.2122506119" @default.
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