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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: steppan cm. J Med Chem. 2024 Aug 22;67(16):13550-13571. doi: 10.1021/acs.jmedchem.3c02469. Epub 2024 Apr 30. J Med Chem. 2024. PMID: 38687966 Free PMC article.
Structural basis of the acyl-transfer mechanism of human GPAT1.
Johnson ZL, Ammirati M, Wasilko DJ, Chang JS, Noell S, Foley TL, Yoon H, Smith K, Asano S, Hales K, Wan M, Yang Q, Piotrowski MA, Farley KA, Gilbert T, Aschenbrenner LM, Fennell KF, Dutra JK, Xu M, Guo C, Varghese AE, Bellenger J, Quinn A, Am Ende CW, West GM, Griffor MC, Bennett D, Calabrese M, Steppan CM, Han S, Wu H. Johnson ZL, et al. Among authors: steppan cm. Nat Struct Mol Biol. 2023 Jan;30(1):22-30. doi: 10.1038/s41594-022-00884-7. Epub 2022 Dec 15. Nat Struct Mol Biol. 2023. PMID: 36522428
Design and Synthesis of Clinical Candidate PF-06852231 (CVL-231): A Brain Penetrant, Selective, Positive Allosteric Modulator of the M4 Muscarinic Acetylcholine Receptor.
Butler CR, Popiolek M, McAllister LA, LaChapelle EA, Kramer M, Beck EM, Mente S, Brodney MA, Brown M, Gilbert A, Helal C, Ogilvie K, Starr J, Uccello D, Grimwood S, Edgerton J, Garst-Orozco J, Kozak R, Lotarski S, Rossi A, Smith D, O'Connor R, Lazzaro J, Steppan C, Steyn SJ. Butler CR, et al. J Med Chem. 2024 Jul 11;67(13):10831-10847. doi: 10.1021/acs.jmedchem.4c00293. Epub 2024 Jun 18. J Med Chem. 2024. PMID: 38888621
In vitro selection and analysis of SARS-CoV-2 nirmatrelvir resistance mutations contributing to clinical virus resistance surveillance.
Zhu Y, Yurgelonis I, Noell S, Yang Q, Guan S, Li Z, Hao L, Rothan H, Rai DK, McMonagle P, Baniecki ML, Greasley SE, Plotnikova O, Lee J, Nicki JA, Ferre R, Byrnes LJ, Liu W, Craig TK, Steppan CM, Liberator P, Soares HD, Allerton CMN, Anderson AS, Cardin RD. Zhu Y, et al. Among authors: steppan cm. Sci Adv. 2024 Jul 26;10(30):eadl4013. doi: 10.1126/sciadv.adl4013. Epub 2024 Jul 24. Sci Adv. 2024. PMID: 39047088 Free PMC article.
Accelerating SLC Transporter Research: Streamlining Knowledge and Validated Tools.
Wiedmer T, Ingles-Prieto A, Goldmann U, Steppan CM, Superti-Furga G; RESOLUTE, REsolution consortia. Wiedmer T, et al. Among authors: steppan cm. Clin Pharmacol Ther. 2022 Sep;112(3):439-442. doi: 10.1002/cpt.2639. Epub 2022 Aug 8. Clin Pharmacol Ther. 2022. PMID: 35938294 Free PMC article. No abstract available.
Discovery of Small-Molecule CD33 Pre-mRNA Splicing Modulators.
Chappie TA, Abdelmessih M, Ambroise CW, Boehm M, Cai M, Green M, Guilmette E, Steppan CM, Stevens LM, Wei L, Xi S, Hasson SA. Chappie TA, et al. Among authors: steppan cm. ACS Med Chem Lett. 2022 Jan 4;13(1):55-62. doi: 10.1021/acsmedchemlett.1c00396. eCollection 2022 Jan 13. ACS Med Chem Lett. 2022. PMID: 35059124 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: steppan cm. Science. 2021 Dec 24;374(6575):1586-1593. doi: 10.1126/science.abl4784. Epub 2021 Nov 2. Science. 2021. PMID: 34726479 Free article.
An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters.
Dvorak V, Wiedmer T, Ingles-Prieto A, Altermatt P, Batoulis H, Bärenz F, Bender E, Digles D, Dürrenberger F, Heitman LH, IJzerman AP, Kell DB, Kickinger S, Körzö D, Leippe P, Licher T, Manolova V, Rizzetto R, Sassone F, Scarabottolo L, Schlessinger A, Schneider V, Sijben HJ, Steck AL, Sundström H, Tremolada S, Wilhelm M, Wright Muelas M, Zindel D, Steppan CM, Superti-Furga G. Dvorak V, et al. Among authors: steppan cm. Front Pharmacol. 2021 Aug 10;12:722889. doi: 10.3389/fphar.2021.722889. eCollection 2021. Front Pharmacol. 2021. PMID: 34447313 Free PMC article. Review.
41 results