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Diversity oriented clicking delivers β-substituted alkenyl sulfonyl fluorides as covalent human neutrophil elastase inhibitors.
Cheng Y, Li G, Smedley CJ, Giel MC, Kitamura S, Woehl JL, Bianco G, Forli S, Homer JA, Cappiello JR, Wolan DW, Moses JE, Sharpless KB. Cheng Y, et al. Among authors: wolan dw. Proc Natl Acad Sci U S A. 2022 Sep 13;119(37):e2208540119. doi: 10.1073/pnas.2208540119. Epub 2022 Sep 7. Proc Natl Acad Sci U S A. 2022. PMID: 36070343 Free PMC article.
Proteome-wide covalent ligand discovery in native biological systems.
Backus KM, Correia BE, Lum KM, Forli S, Horning BD, González-Páez GE, Chatterjee S, Lanning BR, Teijaro JR, Olson AJ, Wolan DW, Cravatt BF. Backus KM, et al. Among authors: wolan dw. Nature. 2016 Jun 23;534(7608):570-4. doi: 10.1038/nature18002. Epub 2016 Jun 15. Nature. 2016. PMID: 27309814 Free PMC article.
SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase.
Zheng Q, Woehl JL, Kitamura S, Santos-Martins D, Smedley CJ, Li G, Forli S, Moses JE, Wolan DW, Sharpless KB. Zheng Q, et al. Among authors: wolan dw. Proc Natl Acad Sci U S A. 2019 Sep 17;116(38):18808-18814. doi: 10.1073/pnas.1909972116. Epub 2019 Sep 4. Proc Natl Acad Sci U S A. 2019. PMID: 31484779 Free PMC article.
Diversity Oriented Clicking (DOC): Divergent Synthesis of SuFExable Pharmacophores from 2-Substituted-Alkynyl-1-Sulfonyl Fluoride (SASF) Hubs.
Smedley CJ, Li G, Barrow AS, Gialelis TL, Giel MC, Ottonello A, Cheng Y, Kitamura S, Wolan DW, Sharpless KB, Moses JE. Smedley CJ, et al. Among authors: wolan dw. Angew Chem Int Ed Engl. 2020 Jul 20;59(30):12460-12469. doi: 10.1002/anie.202003219. Epub 2020 Jun 4. Angew Chem Int Ed Engl. 2020. PMID: 32301265 Free PMC article.
Sulfur(VI) Fluoride Exchange (SuFEx)-Enabled High-Throughput Medicinal Chemistry.
Kitamura S, Zheng Q, Woehl JL, Solania A, Chen E, Dillon N, Hull MV, Kotaniguchi M, Cappiello JR, Kitamura S, Nizet V, Sharpless KB, Wolan DW. Kitamura S, et al. Among authors: wolan dw. J Am Chem Soc. 2020 Jun 24;142(25):10899-10904. doi: 10.1021/jacs.9b13652. Epub 2020 Jun 10. J Am Chem Soc. 2020. PMID: 32479075 Free PMC article.
Discovery of small-molecule enzyme activators by activity-based protein profiling.
Kok BP, Ghimire S, Kim W, Chatterjee S, Johns T, Kitamura S, Eberhardt J, Ogasawara D, Xu J, Sukiasyan A, Kim SM, Godio C, Bittencourt JM, Cameron M, Galmozzi A, Forli S, Wolan DW, Cravatt BF, Boger DL, Saez E. Kok BP, et al. Among authors: wolan dw. Nat Chem Biol. 2020 Sep;16(9):997-1005. doi: 10.1038/s41589-020-0555-4. Epub 2020 Jun 8. Nat Chem Biol. 2020. PMID: 32514184 Free PMC article.
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