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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. 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
More than an Amide Bioisostere: Discovery of 1,2,4-Triazole-containing Pyrazolo[1,5-a]pyrimidine Host CSNK2 Inhibitors for Combatting β-Coronavirus Replication.
Ong HW, Yang X, Smith JL, Dickmander RJ, Brown JW, Havener TM, Taft-Benz S, Howell S, Sanders MK, Capener JL, Couñago RM, Chang E, Krämer A, Moorman NJ, Heise M, Axtman AD, Drewry DH, Willson TM. Ong HW, et al. J Med Chem. 2024 Jul 25;67(14):12261-12313. doi: 10.1021/acs.jmedchem.4c00962. Epub 2024 Jul 3. J Med Chem. 2024. PMID: 38959455 Free PMC article.
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. 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. 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. 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.