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Self-Masked Aldehyde Inhibitors: A Novel Strategy for Inhibiting Cysteine Proteases.
Li L, Chenna BC, Yang KS, Cole TR, Goodall ZT, Giardini M, Moghadamchargari Z, Hernandez EA, Gomez J, Calvet CM, Bernatchez JA, Mellott DM, Zhu J, Rademacher A, Thomas D, Blankenship LR, Drelich A, Laganowsky A, Tseng CK, Liu WR, Wand AJ, Cruz-Reyes J, Siqueira-Neto JL, Meek TD. Li L, et al. Among authors: mellott dm. J Med Chem. 2021 Aug 12;64(15):11267-11287. doi: 10.1021/acs.jmedchem.1c00628. Epub 2021 Jul 21. J Med Chem. 2021. PMID: 34288674 Free PMC article.
Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity.
Chenna BC, Li L, Mellott DM, Zhai X, Siqueira-Neto JL, Calvet Alvarez C, Bernatchez JA, Desormeaux E, Alvarez Hernandez E, Gomez J, McKerrow JH, Cruz-Reyes J, Meek TD. Chenna BC, et al. Among authors: mellott dm. J Med Chem. 2020 Mar 26;63(6):3298-3316. doi: 10.1021/acs.jmedchem.9b02078. Epub 2020 Mar 17. J Med Chem. 2020. PMID: 32125159 Free PMC article.
A Clinical-Stage Cysteine Protease Inhibitor blocks SARS-CoV-2 Infection of Human and Monkey Cells.
Mellott DM, Tseng CT, Drelich A, Fajtová P, Chenna BC, Kostomiris DH, Hsu J, Zhu J, Taylor ZW, Kocurek KI, Tat V, Katzfuss A, Li L, Giardini MA, Skinner D, Hirata K, Yoon MC, Beck S, Carlin AF, Clark AE, Beretta L, Maneval D, Hook V, Frueh F, Hurst BL, Wang H, Raushel FM, O'Donoghue AJ, de Siqueira-Neto JL, Meek TD, McKerrow JH. Mellott DM, et al. ACS Chem Biol. 2021 Apr 16;16(4):642-650. doi: 10.1021/acschembio.0c00875. Epub 2021 Mar 31. ACS Chem Biol. 2021. PMID: 33787221
Bepridil is potent against SARS-CoV-2 in vitro.
Vatansever EC, Yang KS, Drelich AK, Kratch KC, Cho CC, Kempaiah KR, Hsu JC, Mellott DM, Xu S, Tseng CK, Liu WR. Vatansever EC, et al. Among authors: mellott dm. Proc Natl Acad Sci U S A. 2021 Mar 9;118(10):e2012201118. doi: 10.1073/pnas.2012201118. Proc Natl Acad Sci U S A. 2021. PMID: 33597253 Free PMC article.
Bepridil is potent against SARS-CoV-2 In Vitro.
Vatansever EC, Yang K, Kratch KC, Drelich A, Cho CC, Mellott DM, Xu S, Tseng CK, Liu WR. Vatansever EC, et al. Among authors: mellott dm. bioRxiv [Preprint]. 2020 Jul 27:2020.05.23.112235. doi: 10.1101/2020.05.23.112235. bioRxiv. 2020. PMID: 32511370 Free PMC article. Updated. Preprint.
A cysteine protease inhibitor blocks SARS-CoV-2 infection of human and monkey cells.
Mellott DM, Tseng CT, Drelich A, Fajtová P, Chenna BC, Kostomiris DH, Hsu J, Zhu J, Taylor ZW, Tat V, Katzfuss A, Li L, Giardini MA, Skinner D, Hirata K, Beck S, Carlin AF, Clark AE, Beretta L, Maneval D, Frueh F, Hurst BL, Wang H, Kocurek KI, Raushel FM, O'Donoghue AJ, de Siqueira-Neto JL, Meek TD, McKerrow JH. Mellott DM, et al. bioRxiv [Preprint]. 2020 Oct 30:2020.10.23.347534. doi: 10.1101/2020.10.23.347534. bioRxiv. 2020. PMID: 33140046 Free PMC article. Updated. Preprint.