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Structure-based discovery of thiosemicarbazones as SARS-CoV-2 main protease inhibitors.
Maltarollo VG, da Silva EB, Kronenberger T, Sena Andrade MM, de Lima Marques GV, Cândido Oliveira NJ, Santos LH, Oliveira Rezende Júnior C, Cassiano Martinho AC, Skinner D, Fajtová P, M Fernandes TH, Silveira Dos Santos ED, Rodrigues Gazolla PA, Martins de Souza AP, da Silva ML, Dos Santos FS, Lavorato SN, Oliveira Bretas AC, Carvalho DT, Franco LL, Luedtke S, Giardini MA, Poso A, Dias LC, Podust LM, Alves RJ, McKerrow J, Andrade SF, Teixeira RR, Siqueira-Neto JL, O'Donoghue A, de Oliveira RB, Ferreira RS. Maltarollo VG, et al. Future Med Chem. 2023 Jun;15(11):959-985. doi: 10.4155/fmc-2023-0034. Epub 2023 Jul 12. Future Med Chem. 2023. PMID: 37435731
Development of a Potent Inhibitor of the Plasmodium Proteasome with Reduced Mammalian Toxicity.
LaMonte GM, Almaliti J, Bibo-Verdugo B, Keller L, Zou BY, Yang J, Antonova-Koch Y, Orjuela-Sanchez P, Boyle CA, Vigil E, Wang L, Goldgof GM, Gerwick L, O'Donoghue AJ, Winzeler EA, Gerwick WH, Ottilie S. LaMonte GM, et al. J Med Chem. 2017 Aug 10;60(15):6721-6732. doi: 10.1021/acs.jmedchem.7b00671. Epub 2017 Jul 25. J Med Chem. 2017. PMID: 28696697 Free PMC article.
SmSP2: A serine protease secreted by the blood fluke pathogen Schistosoma mansoni with anti-hemostatic properties.
Leontovyč A, Ulrychová L, O'Donoghue AJ, Vondrášek J, Marešová L, Hubálek M, Fajtová P, Chanová M, Jiang Z, Craik CS, Caffrey CR, Mareš M, Dvořák J, Horn M. Leontovyč A, et al. PLoS Negl Trop Dis. 2018 Apr 20;12(4):e0006446. doi: 10.1371/journal.pntd.0006446. eCollection 2018 Apr. PLoS Negl Trop Dis. 2018. PMID: 29677188 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. bioRxiv [Preprint]. 2020 Oct 30:2020.10.23.347534. doi: 10.1101/2020.10.23.347534. bioRxiv. 2020. Update in: ACS Chem Biol. 2021 Apr 16;16(4):642-650. doi: 10.1021/acschembio.0c00875 PMID: 33140046 Free PMC article. Updated. Preprint.
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. bioRxiv [Preprint]. 2020 Dec 24:2020.12.23.424111. doi: 10.1101/2020.12.23.424111. bioRxiv. 2020. Update in: J Med Chem. 2022 Feb 24;65(4):2956-2970. doi: 10.1021/acs.jmedchem.1c01494 PMID: 33398273 Free PMC article. Updated. Preprint.
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
263 results