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Page 1
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).
Fotsch C, Smith DM, Adams JA, Cheetham J, Croghan M, Doherty EM, Hale C, Jarosinski MA, Kelly MG, Norman MH, Tamayo NA, Xi N, Baumgartner JW. Fotsch C, et al. Among authors: croghan m. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2337-40. doi: 10.1016/s0960-894x(03)00412-8. Bioorg Med Chem Lett. 2003. PMID: 12824029
Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N → S (nN → σ*S-X) Interaction for Conformational Constraint.
Pennington LD, Bartberger MD, Croghan MD, Andrews KL, Ashton KS, Bourbeau MP, Chen J, Chmait S, Cupples R, Fotsch C, Helmering J, Hong FT, Hungate RW, Jordan SR, Kong K, Liu L, Michelsen K, Moyer C, Nishimura N, Norman MH, Reichelt A, Siegmund AC, Sivits G, Tadesse S, Tegley CM, Van G, Yang KC, Yao G, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Pennington LD, et al. Among authors: croghan md. J Med Chem. 2015 Dec 24;58(24):9663-79. doi: 10.1021/acs.jmedchem.5b01367. Epub 2015 Dec 1. J Med Chem. 2015. PMID: 26551034 Free article.
Quinolinone-based agonists of S1P₁: use of a N-scan SAR strategy to optimize in vitro and in vivo activity.
Pennington LD, Croghan MD, Sham KK, Pickrell AJ, Harrington PE, Frohn MJ, Lanman BA, Reed AB, Lee MR, Xu H, McElvain M, Xu Y, Zhang X, Fiorino M, Horner M, Morrison HG, Arnett HA, Fotsch C, Tasker AS, Wong M, Cee VJ. Pennington LD, et al. Among authors: croghan md. Bioorg Med Chem Lett. 2012 Jan 1;22(1):527-31. doi: 10.1016/j.bmcl.2011.10.085. Epub 2011 Nov 4. Bioorg Med Chem Lett. 2012. PMID: 22104144
The discovery of an orally efficacious positive allosteric modulator of the calcium sensing receptor containing a dibenzylamine core.
Harrington PE, St Jean DJ Jr, Clarine J, Coulter TS, Croghan M, Davenport A, Davis J, Ghiron C, Hutchinson J, Kelly MG, Lott F, Lu JY, Martin D, Morony S, Poon SF, Portero-Larragueta E, Reagan JD, Regal KA, Tasker A, Wang M, Yang Y, Yao G, Zeng Q, Henley C 3rd, Fotsch C. Harrington PE, et al. Among authors: croghan m. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5544-7. doi: 10.1016/j.bmcl.2010.07.060. Epub 2010 Aug 12. Bioorg Med Chem Lett. 2010. PMID: 20708930
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 1. Discovery of a novel tool compound for in vivo proof-of-concept.
Ashton KS, Andrews KL, Bryan MC, Chen J, Chen K, Chen M, Chmait S, Croghan M, Cupples R, Fotsch C, Helmering J, Jordan SR, Kurzeja RJ, Michelsen K, Pennington LD, Poon SF, Sivits G, Van G, Vonderfecht SL, Wahl RC, Zhang J, Lloyd DJ, Hale C, St Jean DJ Jr. Ashton KS, et al. Among authors: croghan m. J Med Chem. 2014 Jan 23;57(2):309-24. doi: 10.1021/jm4016735. Epub 2014 Jan 9. J Med Chem. 2014. PMID: 24405172
4-Methoxy-N-[2-(trifluoromethyl)biphenyl-4-ylcarbamoyl]nicotinamide: A Potent and Selective Agonist of S1P1.
Pennington LD, Sham KK, Pickrell AJ, Harrington PE, Frohn MJ, Lanman BA, Reed AB, Croghan MD, Lee MR, Xu H, McElvain M, Xu Y, Zhang X, Fiorino M, Horner M, Morrison HG, Arnett HA, Fotsch C, Wong M, Cee VJ. Pennington LD, et al. Among authors: croghan md. ACS Med Chem Lett. 2011 Jul 29;2(10):752-7. doi: 10.1021/ml2001399. eCollection 2011 Oct 13. ACS Med Chem Lett. 2011. PMID: 24900263 Free PMC article.
Optimization of a Potent, Orally Active S1P1 Agonist Containing a Quinolinone Core.
Harrington PE, Croghan MD, Fotsch C, Frohn M, Lanman BA, Pennington LD, Pickrell AJ, Reed AB, Sham KK, Tasker A, Arnett HA, Fiorino M, Lee MR, McElvain M, Morrison HG, Xu H, Xu Y, Zhang X, Wong M, Cee VJ. Harrington PE, et al. Among authors: croghan md. ACS Med Chem Lett. 2011 Nov 23;3(1):74-8. doi: 10.1021/ml200252b. eCollection 2012 Jan 12. ACS Med Chem Lett. 2011. PMID: 24900374 Free PMC article.
Design and synthesis of potent, orally efficacious hydroxyethylamine derived β-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Dineen TA, Weiss MM, Williamson T, Acton P, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dunn RT 2nd, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, San Miguel T, Sickmier EA, Vargas HM, Wahl RC, Wen PH, Whittington DA, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Dineen TA, et al. Among authors: croghan md. J Med Chem. 2012 Nov 8;55(21):9025-44. doi: 10.1021/jm300118s. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468684
Design and preparation of a potent series of hydroxyethylamine containing β-secretase inhibitors that demonstrate robust reduction of central β-amyloid.
Weiss MM, Williamson T, Babu-Khan S, Bartberger MD, Brown J, Chen K, Cheng Y, Citron M, Croghan MD, Dineen TA, Esmay J, Graceffa RF, Harried SS, Hickman D, Hitchcock SA, Horne DB, Huang H, Imbeah-Ampiah R, Judd T, Kaller MR, Kreiman CR, La DS, Li V, Lopez P, Louie S, Monenschein H, Nguyen TT, Pennington LD, Rattan C, San Miguel T, Sickmier EA, Wahl RC, Wen PH, Wood S, Xue Q, Yang BH, Patel VF, Zhong W. Weiss MM, et al. Among authors: croghan md. J Med Chem. 2012 Nov 8;55(21):9009-24. doi: 10.1021/jm300119p. Epub 2012 Apr 18. J Med Chem. 2012. PMID: 22468639
A Potent and Orally Efficacious, Hydroxyethylamine-Based Inhibitor of β-Secretase.
Kaller MR, Harried SS, Albrecht B, Amarante P, Babu-Khan S, Bartberger MD, Brown J, Brown R, Chen K, Cheng Y, Citron M, Croghan MD, Graceffa R, Hickman D, Judd T, Kriemen C, La D, Li V, Lopez P, Luo Y, Masse C, Monenschein H, Nguyen T, Pennington LD, Miguel TS, Sickmier EA, Wahl RC, Weiss MM, Wen PH, Williamson T, Wood S, Xue M, Yang B, Zhang J, Patel V, Zhong W, Hitchcock S. Kaller MR, et al. Among authors: croghan md. ACS Med Chem Lett. 2012 Mar 29;3(11):886-91. doi: 10.1021/ml3000148. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900403 Free PMC article.
20 results