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A Second-Generation Oral SARS-CoV-2 Main Protease Inhibitor Clinical Candidate for the Treatment of COVID-19.
Allerton CMN, Arcari JT, Aschenbrenner LM, Avery M, Bechle BM, Behzadi MA, Boras B, Buzon LM, Cardin RD, Catlin NR, Carlo AA, Coffman KJ, Dantonio A, Di L, Eng H, Farley KA, Ferre RA, Gernhardt SS, Gibson SA, Greasley SE, Greenfield SR, Hurst BL, Kalgutkar AS, Kimoto E, Lanyon LF, Lovett GH, Lian Y, Liu W, Martínez Alsina LA, Noell S, Obach RS, Owen DR, Patel NC, Rai DK, Reese MR, Rothan HA, Sakata S, Sammons MF, Sathish JG, Sharma R, Steppan CM, Tuttle JB, Verhoest PR, Wei L, Yang Q, Yurgelonis I, Zhu Y. Allerton CMN, et al. Among authors: reese mr. J Med Chem. 2024 Apr 30. doi: 10.1021/acs.jmedchem.3c02469. Online ahead of print. J Med Chem. 2024. PMID: 38687966
Small molecule branched-chain ketoacid dehydrogenase kinase (BDK) inhibitors with opposing effects on BDK protein levels.
Roth Flach RJ, Bollinger E, Reyes AR, Laforest B, Kormos BL, Liu S, Reese MR, Martinez Alsina LA, Buzon L, Zhang Y, Bechle B, Rosado A, Sahasrabudhe PV, Knafels J, Bhattacharya SK, Omoto K, Stansfield JC, Hurley LD, Song L, Luo L, Breitkopf SB, Monetti M, Cunio T, Tierney B, Geoly FJ, Delmore J, Siddall CP, Xue L, Yip KN, Kalgutkar AS, Miller RA, Zhang BB, Filipski KJ. Roth Flach RJ, et al. Among authors: reese mr. Nat Commun. 2023 Aug 9;14(1):4812. doi: 10.1038/s41467-023-40536-y. Nat Commun. 2023. PMID: 37558654 Free PMC article.
Discovery of the Potent and Selective MC4R Antagonist PF-07258669 for the Potential Treatment of Appetite Loss.
Garnsey MR, Smith AC, Polivkova J, Arons AL, Bai G, Blakemore C, Boehm M, Buzon LM, Campion SN, Cerny M, Chang SC, Coffman K, Farley KA, Fonseca KR, Ford KK, Garren J, Kong JX, Koos MRM, Kung DW, Lian Y, Li MM, Li Q, Martinez-Alsina LA, O'Connor R, Ogilvie K, Omoto K, Raymer B, Reese MR, Ryder T, Samp L, Stevens KA, Widlicka DW, Yang Q, Zhu K, Fortin JP, Sammons MF. Garnsey MR, et al. Among authors: reese mr. J Med Chem. 2023 Mar 9;66(5):3195-3211. doi: 10.1021/acs.jmedchem.2c02012. Epub 2023 Feb 19. J Med Chem. 2023. PMID: 36802610
Structural studies identify angiotensin II receptor blocker-like compounds as branched-chain ketoacid dehydrogenase kinase inhibitors.
Liu S, Kormos BL, Knafels JD, Sahasrabudhe PV, Rosado A, Sommese RF, Reyes AR, Ward J, Roth Flach RJ, Wang X, Buzon LM, Reese MR, Bhattacharya SK, Omoto K, Filipski KJ. Liu S, et al. Among authors: reese mr. J Biol Chem. 2023 Mar;299(3):102959. doi: 10.1016/j.jbc.2023.102959. Epub 2023 Jan 28. J Biol Chem. 2023. PMID: 36717078 Free PMC article.
An oral SARS-CoV-2 Mpro inhibitor clinical candidate for the treatment of COVID-19.
Owen DR, Allerton CMN, Anderson AS, Aschenbrenner L, Avery M, Berritt S, Boras B, Cardin RD, Carlo A, Coffman KJ, Dantonio A, Di L, Eng H, Ferre R, Gajiwala KS, Gibson SA, Greasley SE, Hurst BL, Kadar EP, Kalgutkar AS, Lee JC, Lee J, Liu W, Mason SW, Noell S, Novak JJ, Obach RS, Ogilvie K, Patel NC, Pettersson M, Rai DK, Reese MR, Sammons MF, Sathish JG, Singh RSP, Steppan CM, Stewart AE, Tuttle JB, Updyke L, Verhoest PR, Wei L, Yang Q, Zhu Y. Owen DR, et al. Among authors: reese mr. Science. 2021 Dec 24;374(6575):1586-1593. doi: 10.1126/science.abl4784. Epub 2021 Nov 2. Science. 2021. PMID: 34726479 Free article.
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: reese mr. Nat Commun. 2021 Oct 18;12(1):6055. doi: 10.1038/s41467-021-26239-2. Nat Commun. 2021. PMID: 34663813 Free PMC article.
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: reese mr. 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.
5-Aryltetrazoles from Direct C-H Arylation with Aryl Bromides.
Zhang Y, Lee JCH, Reese MR, Boscoe BP, Humphrey JM, Helal CJ. Zhang Y, et al. Among authors: reese mr. J Org Chem. 2020 Apr 17;85(8):5718-5723. doi: 10.1021/acs.joc.0c00085. Epub 2020 Mar 31. J Org Chem. 2020. PMID: 32208719
High-Throughput Ligand Screening Enables the Enantioselective Conjugate Borylation of Cyclobutenones to Access Synthetically Versatile Tertiary Cyclobutylboronates.
Clement HA, Boghi M, McDonald RM, Bernier L, Coe JW, Farrell W, Helal CJ, Reese MR, Sach NW, Lee JC, Hall DG. Clement HA, et al. Among authors: reese mr. Angew Chem Int Ed Engl. 2019 Dec 16;58(51):18405-18409. doi: 10.1002/anie.201909308. Epub 2019 Oct 31. Angew Chem Int Ed Engl. 2019. PMID: 31591755
Sulfonamide Synthesis via Calcium Triflimide Activation of Sulfonyl Fluorides.
Mukherjee P, Woroch CP, Cleary L, Rusznak M, Franzese RW, Reese MR, Tucker JW, Humphrey JM, Etuk SM, Kwan SC, Am Ende CW, Ball ND. Mukherjee P, et al. Among authors: reese mr. Org Lett. 2018 Jul 6;20(13):3943-3947. doi: 10.1021/acs.orglett.8b01520. Epub 2018 Jun 11. Org Lett. 2018. PMID: 29888600 Free PMC article.
25 results