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Page 1
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.
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
O'Neill BT, Beck EM, Butler CR, Nolan CE, Gonzales C, Zhang L, Doran SD, Lapham K, Buzon LM, Dutra JK, Barreiro G, Hou X, Martinez-Alsina LA, Rogers BN, Villalobos A, Murray JC, Ogilvie K, LaChapelle EA, Chang C, Lanyon LF, Steppan CM, Robshaw A, Hales K, Boucher GG, Pandher K, Houle C, Ambroise CW, Karanian D, Riddell D, Bales KR, Brodney MA. O'Neill BT, et al. Among authors: steppan cm. J Med Chem. 2018 May 24;61(10):4476-4504. doi: 10.1021/acs.jmedchem.8b00246. Epub 2018 Apr 17. J Med Chem. 2018. PMID: 29613789
Design, Optimization, and Study of Small Molecules That Target Tau Pre-mRNA and Affect Splicing.
Chen JL, Zhang P, Abe M, Aikawa H, Zhang L, Frank AJ, Zembryski T, Hubbs C, Park H, Withka J, Steppan C, Rogers L, Cabral S, Pettersson M, Wager TT, Fountain MA, Rumbaugh G, Childs-Disney JL, Disney MD. Chen JL, et al. J Am Chem Soc. 2020 May 13;142(19):8706-8727. doi: 10.1021/jacs.0c00768. Epub 2020 May 4. J Am Chem Soc. 2020. PMID: 32364710 Free PMC article.
Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors.
Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Préville C, Samas B, She L, Sobol Z, Steppan CM, Stevens BD, Thuma BA, Tugnait M, Zeng D, Zhu T. Mascitti V, et al. Among authors: steppan cm. J Med Chem. 2011 Apr 28;54(8):2952-60. doi: 10.1021/jm200049r. Epub 2011 Mar 30. J Med Chem. 2011. PMID: 21449606
Photoaffinity Labeling and Quantitative Chemical Proteomics Identify LXRβ as the Functional Target of Enhancers of Astrocytic apoE.
Seneviratne U, Huang Z, Am Ende CW, Butler TW, Cleary L, Dresselhaus E, Evrard E, Fisher EL, Green ME, Helal CJ, Humphrey JM, Lanyon LF, Marconi M, Mukherjee P, Sciabola S, Steppan CM, Sylvain EK, Tuttle JB, Verhoest PR, Wager TT, Xie L, Ramaswamy G, Johnson DS, Pettersson M. Seneviratne U, et al. Among authors: steppan cm. Cell Chem Biol. 2021 Feb 18;28(2):148-157.e7. doi: 10.1016/j.chembiol.2020.09.002. Epub 2020 Sep 29. Cell Chem Biol. 2021. PMID: 32997975 Free article.
Discovery of Ketone-Based Covalent Inhibitors of Coronavirus 3CL Proteases for the Potential Therapeutic Treatment of COVID-19.
Hoffman RL, Kania RS, Brothers MA, Davies JF, Ferre RA, Gajiwala KS, He M, Hogan RJ, Kozminski K, Li LY, Lockner JW, Lou J, Marra MT, Mitchell LJ Jr, Murray BW, Nieman JA, Noell S, Planken SP, Rowe T, Ryan K, Smith GJ 3rd, Solowiej JE, Steppan CM, Taggart B. Hoffman RL, et al. Among authors: steppan cm. J Med Chem. 2020 Nov 12;63(21):12725-12747. doi: 10.1021/acs.jmedchem.0c01063. Epub 2020 Oct 15. J Med Chem. 2020. PMID: 33054210
C-Aryl glycoside inhibitors of SGLT2: Exploration of sugar modifications including C-5 spirocyclization.
Robinson RP, Mascitti V, Boustany-Kari CM, Carr CL, Foley PM, Kimoto E, Leininger MT, Lowe A, Klenotic MK, Macdonald JI, Maguire RJ, Masterson VM, Maurer TS, Miao Z, Patel JD, Préville C, Reese MR, She L, Steppan CM, Thuma BA, Zhu T. Robinson RP, et al. Among authors: steppan cm. Bioorg Med Chem Lett. 2010 Mar 1;20(5):1569-72. doi: 10.1016/j.bmcl.2010.01.075. Epub 2010 Jan 21. Bioorg Med Chem Lett. 2010. PMID: 20149653
N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors.
Atkinson KA, Beretta EE, Brown JA, Castrodad M, Chen Y, Cosgrove JM, Du P, Litchfield J, Makowski M, Martin K, McLellan TJ, Neagu C, Perry DA, Piotrowski DW, Steppan CM, Trilles R. Atkinson KA, et al. Among authors: steppan cm. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5. doi: 10.1016/j.bmcl.2011.01.113. Epub 2011 Jan 31. Bioorg Med Chem Lett. 2011. PMID: 21324691
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.
47 results