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Discovery of a Novel Inhibitor of Coronavirus 3CL Protease for the Potential Treatment of COVID-19.
Boras B, Jones RM, Anson BJ, Arenson D, Aschenbrenner L, Bakowski MA, Beutler N, Binder J, Chen E, Eng H, Hammond H, Hammond J, Haupt RE, Hoffman R, Kadar EP, Kania R, Kimoto E, Kirkpatrick MG, Lanyon L, Lendy EK, Lillis JR, Logue J, Luthra SA, Ma C, Mason SW, McGrath ME, Noell S, Obach RS, O'Brien MN, O'Connor R, Ogilvie K, Owen D, Pettersson M, Reese MR, Rogers TF, Rossulek MI, Sathish JG, Shirai N, Steppan C, Ticehurst M, Updyke LW, Weston S, Zhu Y, Wang J, Chatterjee AK, Mesecar AD, Frieman MB, Anderson AS, Allerton C. Boras B, et al. Among authors: mesecar ad. bioRxiv [Preprint]. 2021 Feb 12:2020.09.12.293498. doi: 10.1101/2020.09.12.293498. bioRxiv. 2021. PMID: 32935104 Free PMC article. Updated. Preprint.
Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19.
Boras B, Jones RM, Anson BJ, Arenson D, Aschenbrenner L, Bakowski MA, Beutler N, Binder J, Chen E, Eng H, Hammond H, Hammond J, Haupt RE, Hoffman R, Kadar EP, Kania R, Kimoto E, Kirkpatrick MG, Lanyon L, Lendy EK, Lillis JR, Logue J, Luthra SA, Ma C, Mason SW, McGrath ME, Noell S, Obach RS, O' Brien MN, O'Connor R, Ogilvie K, Owen D, Pettersson M, Reese MR, Rogers TF, Rosales R, Rossulek MI, Sathish JG, Shirai N, Steppan C, Ticehurst M, Updyke LW, Weston S, Zhu Y, White KM, García-Sastre A, Wang J, Chatterjee AK, Mesecar AD, Frieman MB, Anderson AS, Allerton C. Boras B, et al. Among authors: mesecar ad. Nat Commun. 2021 Oct 18;12(1):6055. doi: 10.1038/s41467-021-26239-2. Nat Commun. 2021. PMID: 34663813 Free PMC article.
Indole Chloropyridinyl Ester-Derived SARS-CoV-2 3CLpro Inhibitors: Enzyme Inhibition, Antiviral Efficacy, Structure-Activity Relationship, and X-ray Structural Studies.
Ghosh AK, Raghavaiah J, Shahabi D, Yadav M, Anson BJ, Lendy EK, Hattori SI, Higashi-Kuwata N, Mitsuya H, Mesecar AD. Ghosh AK, et al. Among authors: mesecar ad. J Med Chem. 2021 Oct 14;64(19):14702-14714. doi: 10.1021/acs.jmedchem.1c01214. Epub 2021 Sep 16. J Med Chem. 2021. PMID: 34528437 Free PMC article.
A small molecule compound with an indole moiety inhibits the main protease of SARS-CoV-2 and blocks virus replication.
Hattori SI, Higashi-Kuwata N, Hayashi H, Allu SR, Raghavaiah J, Bulut H, Das D, Anson BJ, Lendy EK, Takamatsu Y, Takamune N, Kishimoto N, Murayama K, Hasegawa K, Li M, Davis DA, Kodama EN, Yarchoan R, Wlodawer A, Misumi S, Mesecar AD, Ghosh AK, Mitsuya H. Hattori SI, et al. Among authors: mesecar ad. Nat Commun. 2021 Jan 28;12(1):668. doi: 10.1038/s41467-021-20900-6. Nat Commun. 2021. PMID: 33510133 Free PMC article.
Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing.
Riva L, Yuan S, Yin X, Martin-Sancho L, Matsunaga N, Pache L, Burgstaller-Muehlbacher S, De Jesus PD, Teriete P, Hull MV, Chang MW, Chan JF, Cao J, Poon VK, Herbert KM, Cheng K, Nguyen TH, Rubanov A, Pu Y, Nguyen C, Choi A, Rathnasinghe R, Schotsaert M, Miorin L, Dejosez M, Zwaka TP, Sit KY, Martinez-Sobrido L, Liu WC, White KM, Chapman ME, Lendy EK, Glynne RJ, Albrecht R, Ruppin E, Mesecar AD, Johnson JR, Benner C, Sun R, Schultz PG, Su AI, García-Sastre A, Chatterjee AK, Yuen KY, Chanda SK. Riva L, et al. Among authors: mesecar ad. Nature. 2020 Oct;586(7827):113-119. doi: 10.1038/s41586-020-2577-1. Epub 2020 Jul 24. Nature. 2020. PMID: 32707573 Free PMC article.
Highly Selective and Potent Human β-Secretase 2 (BACE2) Inhibitors against Type 2 Diabetes: Design, Synthesis, X-ray Structure and Structure-Activity Relationship Studies.
Ghosh AK, Brindisi M, Yen YC, Lendy EK, Kovela S, Cárdenas EL, Reddy BS, Rao KV, Downs D, Huang X, Tang J, Mesecar AD. Ghosh AK, et al. Among authors: mesecar ad. ChemMedChem. 2019 Mar 5;14(5):545-560. doi: 10.1002/cmdc.201800725. Epub 2019 Feb 5. ChemMedChem. 2019. PMID: 30637955 Free PMC article.
152 results