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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. Among authors: mckerrow jh. 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
Potent Anti-SARS-CoV-2 Activity by the Natural Product Gallinamide A and Analogues via Inhibition of Cathepsin L.
Ashhurst AS, Tang AH, Fajtová P, Yoon MC, Aggarwal A, Bedding MJ, Stoye A, Beretta L, Pwee D, Drelich A, Skinner D, Li L, Meek TD, McKerrow JH, Hook V, Tseng CT, Larance M, Turville S, Gerwick WH, O'Donoghue AJ, Payne RJ. Ashhurst AS, et al. Among authors: mckerrow jh. J Med Chem. 2022 Feb 24;65(4):2956-2970. doi: 10.1021/acs.jmedchem.1c01494. Epub 2021 Nov 3. J Med Chem. 2022. PMID: 34730959 Free PMC article.
Structure-Based Identification of Naphthoquinones and Derivatives as Novel Inhibitors of Main Protease Mpro and Papain-like Protease PLpro of SARS-CoV-2.
Santos LH, Kronenberger T, Almeida RG, Silva EB, Rocha REO, Oliveira JC, Barreto LV, Skinner D, Fajtová P, Giardini MA, Woodworth B, Bardine C, Lourenço AL, Craik CS, Poso A, Podust LM, McKerrow JH, Siqueira-Neto JL, O'Donoghue AJ, da Silva Júnior EN, Ferreira RS. Santos LH, et al. Among authors: mckerrow jh. J Chem Inf Model. 2022 Dec 26;62(24):6553-6573. doi: 10.1021/acs.jcim.2c00693. Epub 2022 Aug 12. J Chem Inf Model. 2022. PMID: 35960688
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: mckerrow jh. 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 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. Among authors: mckerrow jh. 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.
Discovery of Triple Inhibitors of Both SARS-CoV-2 Proteases and Human Cathepsin L.
Meewan I, Kattoula J, Kattoula JY, Skinner D, Fajtová P, Giardini MA, Woodworth B, McKerrow JH, Lage de Siqueira-Neto J, O'Donoghue AJ, Abagyan R. Meewan I, et al. Among authors: mckerrow jh. Pharmaceuticals (Basel). 2022 Jun 13;15(6):744. doi: 10.3390/ph15060744. Pharmaceuticals (Basel). 2022. PMID: 35745663 Free PMC article.
Small-Molecule Thioesters as SARS-CoV-2 Main Protease Inhibitors: Enzyme Inhibition, Structure-Activity Relationships, Antiviral Activity, and X-ray Structure Determination.
Pillaiyar T, Flury P, Krüger N, Su H, Schäkel L, Barbosa Da Silva E, Eppler O, Kronenberger T, Nie T, Luedtke S, Rocha C, Sylvester K, Petry MRI, McKerrow JH, Poso A, Pöhlmann S, Gütschow M, O'Donoghue AJ, Xu Y, Müller CE, Laufer SA. Pillaiyar T, et al. Among authors: mckerrow jh. J Med Chem. 2022 Jul 14;65(13):9376-9395. doi: 10.1021/acs.jmedchem.2c00636. Epub 2022 Jun 16. J Med Chem. 2022. PMID: 35709506
Potent in vitro anti-SARS-CoV-2 activity by gallinamide A and analogues via inhibition of cathepsin L.
Ashhurst AS, Tang AH, Fajtová P, Yoon M, Aggarwal A, Stoye A, Larance M, Beretta L, Drelich A, Skinner D, Li L, Meek TD, McKerrow JH, Hook V, Tseng CK, Turville S, Gerwick WH, O'Donoghue AJ, Payne RJ. Ashhurst AS, et al. Among authors: mckerrow jh. bioRxiv [Preprint]. 2020 Dec 24:2020.12.23.424111. doi: 10.1101/2020.12.23.424111. bioRxiv. 2020. PMID: 33398273 Free PMC article. Updated. Preprint.
351 results