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A Covalent Chemical Probe for Chikungunya nsP2 Cysteine Protease with Antialphaviral Activity and Proteome-wide Selectivity.
Ghoshal A, Tse EG, Hossain MA, Asressu KH, Merten EM, Sears JD, Howell S, Perveen S, Burdick J, Morales NL, Martinez SA, Law I, Davenport BJ, Morrison TE, Streblow ZJ, Streblow DN, Mordant AL, Webb TS, Cabrera A, Herring LE, Arrowsmith CH, Pearce KH, Moorman NJ, Heise MT, Couñago RM, Brown PJ, Willson TM. Ghoshal A, et al. Among authors: brown pj. Res Sq [Preprint]. 2024 Nov 12:rs.3.rs-5363451. doi: 10.21203/rs.3.rs-5363451/v1. Res Sq. 2024. PMID: 39606462 Free PMC article. Preprint.
Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of Chikungunya nsP2 Cysteine Protease with Anti-alphavirus Activity.
Ghoshal A, Asressu KH, Hossain MA, Brown PJ, Merten EM, Sears JD, Perveen S, Pearce KH, Popov KI, Moorman NJ, Heise MT, Willson TM. Ghoshal A, et al. Among authors: brown pj. bioRxiv [Preprint]. 2024 Jun 13:2024.06.12.598722. doi: 10.1101/2024.06.12.598722. bioRxiv. 2024. Update in: J Med Chem. 2024 Sep 26;67(18):16505-16532. doi: 10.1021/acs.jmedchem.4c01346 PMID: 38915519 Free PMC article. Updated. Preprint.
Structure Activity of β-Amidomethyl Vinyl Sulfones as Covalent Inhibitors of Chikungunya nsP2 Cysteine Protease with Antialphavirus Activity.
Ghoshal A, Asressu KH, Hossain MA, Brown PJ, Nandakumar M, Vala A, Merten EM, Sears JD, Law I, Burdick JE, Morales NL, Perveen S, Pearce KH, Popov KI, Moorman NJ, Heise MT, Willson TM. Ghoshal A, et al. Among authors: brown pj. J Med Chem. 2024 Sep 26;67(18):16505-16532. doi: 10.1021/acs.jmedchem.4c01346. Epub 2024 Sep 5. J Med Chem. 2024. PMID: 39235978 Free PMC article.
Identification of a cell-active chikungunya virus nsP2 protease inhibitor using a covalent fragment-based screening approach.
Merten EM, Sears JD, Leisner TM, Hardy PB, Ghoshal A, Hossain MA, Asressu KH, Brown PJ, Tse EG, Stashko MA, Li K, Norris-Drouin JL, Herring LE, Mordant AL, Webb TS, Mills CA, Barker NK, Streblow ZJ, Perveen S, Arrowsmith CH, Couñago RM, Arnold JJ, Cameron CE, Streblow DN, Moorman NJ, Heise MT, Willson TM, Popov KI, Pearce KH. Merten EM, et al. Among authors: brown pj. Proc Natl Acad Sci U S A. 2024 Oct 15;121(42):e2409166121. doi: 10.1073/pnas.2409166121. Epub 2024 Oct 10. Proc Natl Acad Sci U S A. 2024. PMID: 39388272
Identification of Inhibitors of Chikungunya virus nsP2 ATPase.
Navarro H, Scott JE, Smith GR, Ghiabi P, Gibson E, Loppnau P, Harding RJ, Hossain MA, Bose MR, Pearce KH, Merten EM, Willson TM, Brown PJ. Navarro H, et al. Among authors: brown pj. bioRxiv [Preprint]. 2024 Dec 6:2024.12.02.625520. doi: 10.1101/2024.12.02.625520. bioRxiv. 2024. PMID: 39677726 Free PMC article. Preprint.
Discovery of a chemical probe for PRDM9.
Allali-Hassani A, Szewczyk MM, Ivanochko D, Organ SL, Bok J, Ho JSY, Gay FPH, Li F, Blazer L, Eram MS, Halabelian L, Dilworth D, Luciani GM, Lima-Fernandes E, Wu Q, Loppnau P, Palmer N, Talib SZA, Brown PJ, Schapira M, Kaldis P, O'Hagan RC, Guccione E, Barsyte-Lovejoy D, Arrowsmith CH, Sanders JM, Kattar SD, Bennett DJ, Nicholson B, Vedadi M. Allali-Hassani A, et al. Among authors: brown pj. Nat Commun. 2019 Dec 17;10(1):5759. doi: 10.1038/s41467-019-13652-x. Nat Commun. 2019. PMID: 31848333 Free PMC article.
Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2.
Hanley RP, Nie DY, Tabor JR, Li F, Sobh A, Xu C, Barker NK, Dilworth D, Hajian T, Gibson E, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Herring LE, Wang GG, Licht JD, Vedadi M, Arrowsmith CH, James LI. Hanley RP, et al. Among authors: brown pj. J Am Chem Soc. 2023 Apr 12;145(14):8176-8188. doi: 10.1021/jacs.3c01421. Epub 2023 Mar 28. J Am Chem Soc. 2023. PMID: 36976643 Free PMC article.
682 results