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Page 1
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. Among authors: giardini ma. 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
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: giardini ma. 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
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: giardini ma. Pharmaceuticals (Basel). 2022 Jun 13;15(6):744. doi: 10.3390/ph15060744. Pharmaceuticals (Basel). 2022. PMID: 35745663 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. Among authors: giardini ma. 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
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. 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.
Discovery of pyrazolopyrrolidinones as potent, broad-spectrum inhibitors of Leishmania infection.
Kavouris JA, McCall LI, Giardini MA, De Muylder G, Thomas D, Garcia-Pérez A, Cantizani J, Cotillo I, Fiandor JM, McKerrow JH, De Oliveira CI, Siqueira-Neto JL, González S, Brown LE, Schaus SE. Kavouris JA, et al. Among authors: giardini ma. Front Trop Dis. 2023;3:1011124. doi: 10.3389/fitd.2022.1011124. Epub 2023 Jan 23. Front Trop Dis. 2023. PMID: 36818551 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: giardini ma. 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.
A Broad Spectrum Antiparasitic Activity of Organotin (IV) Derivatives and Its Untargeted Proteomic Profiling Using Leishmania donovani.
Hayat O, Ullah N, Sirajuddin M, Giardini MA, Nguyen JV, Francisco KR, Liu LJ, Sun YU, Maurya S, McGrosso D, Gonzalez DJ, Caffrey CR, Debnath A, Siqueira-Neto JL. Hayat O, et al. Among authors: giardini ma. Pathogens. 2022 Nov 26;11(12):1424. doi: 10.3390/pathogens11121424. Pathogens. 2022. PMID: 36558759 Free PMC article.
20 results