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Page 1
Small Molecule Disruptors of the Glucokinase-Glucokinase Regulatory Protein Interaction: 5. A Novel Aryl Sulfone Series, Optimization Through Conformational Analysis.
Tamayo NA, Norman MH, Bartberger MD, Hong FT, Bo Y, Liu L, Nishimura N, Yang KC, Tadesse S, Fotsch C, Chen J, Chmait S, Cupples R, Hale C, Jordan SR, Lloyd DJ, Sivits G, Van G, St Jean DJ Jr. Tamayo NA, et al. Among authors: norman mh. J Med Chem. 2015 Jun 11;58(11):4462-82. doi: 10.1021/jm5018175. Epub 2015 Jun 1. J Med Chem. 2015. PMID: 25914941
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N, Xi N, Xu S, Bannon AW, Baumgartner JW. Fotsch C, et al. Among authors: norman mh. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7. doi: 10.1016/j.bmcl.2005.01.060. Bioorg Med Chem Lett. 2005. PMID: 15745810
Phospshoinositide 3-kinase (PI3K)/mammalian target of rapamycin (mTOR) dual inhibitors: discovery and structure-activity relationships of a series of quinoline and quinoxaline derivatives.
Nishimura N, Siegmund A, Liu L, Yang K, Bryan MC, Andrews KL, Bo Y, Booker SK, Caenepeel S, Freeman D, Liao H, McCarter J, Mullady EL, San Miguel T, Subramanian R, Tamayo N, Wang L, Whittington DA, Zalameda L, Zhang N, Hughes PE, Norman MH. Nishimura N, et al. Among authors: norman mh. J Med Chem. 2011 Jul 14;54(13):4735-51. doi: 10.1021/jm200386s. Epub 2011 Jun 20. J Med Chem. 2011. PMID: 21612232
Structure-based design of a novel series of potent, selective inhibitors of the class I phosphatidylinositol 3-kinases.
Smith AL, D'Angelo ND, Bo YY, Booker SK, Cee VJ, Herberich B, Hong FT, Jackson CL, Lanman BA, Liu L, Nishimura N, Pettus LH, Reed AB, Tadesse S, Tamayo NA, Wurz RP, Yang K, Andrews KL, Whittington DA, McCarter JD, Miguel TS, Zalameda L, Jiang J, Subramanian R, Mullady EL, Caenepeel S, Freeman DJ, Wang L, Zhang N, Wu T, Hughes PE, Norman MH. Smith AL, et al. Among authors: norman mh. J Med Chem. 2012 Jun 14;55(11):5188-219. doi: 10.1021/jm300184s. Epub 2012 May 23. J Med Chem. 2012. PMID: 22548365
Selective class I phosphoinositide 3-kinase inhibitors: optimization of a series of pyridyltriazines leading to the identification of a clinical candidate, AMG 511.
Norman MH, Andrews KL, Bo YY, Booker SK, Caenepeel S, Cee VJ, D'Angelo ND, Freeman DJ, Herberich BJ, Hong FT, Jackson CL, Jiang J, Lanman BA, Liu L, McCarter JD, Mullady EL, Nishimura N, Pettus LH, Reed AB, Miguel TS, Smith AL, Stec MM, Tadesse S, Tasker A, Aidasani D, Zhu X, Subramanian R, Tamayo NA, Wang L, Whittington DA, Wu B, Wu T, Wurz RP, Yang K, Zalameda L, Zhang N, Hughes PE. Norman MH, et al. J Med Chem. 2012 Sep 13;55(17):7796-816. doi: 10.1021/jm300846z. Epub 2012 Aug 30. J Med Chem. 2012. PMID: 22897589
Antidiabetic effects of glucokinase regulatory protein small-molecule disruptors.
Lloyd DJ, St Jean DJ Jr, Kurzeja RJ, Wahl RC, Michelsen K, Cupples R, Chen M, Wu J, Sivits G, Helmering J, Komorowski R, Ashton KS, Pennington LD, Fotsch C, Vazir M, Chen K, Chmait S, Zhang J, Liu L, Norman MH, Andrews KL, Bartberger MD, Van G, Galbreath EJ, Vonderfecht SL, Wang M, Jordan SR, Véniant MM, Hale C. Lloyd DJ, et al. Among authors: norman mh. Nature. 2013 Dec 19;504(7480):437-40. doi: 10.1038/nature12724. Epub 2013 Nov 13. Nature. 2013. PMID: 24226772
Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.
St Jean DJ Jr, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C. St Jean DJ Jr, et al. Among authors: norman mh. J Med Chem. 2014 Jan 23;57(2):325-38. doi: 10.1021/jm4016747. Epub 2014 Jan 9. J Med Chem. 2014. PMID: 24405213
Optimization of potency and pharmacokinetic properties of tetrahydroisoquinoline transient receptor potential melastatin 8 (TRPM8) antagonists.
Horne DB, Tamayo NA, Bartberger MD, Bo Y, Clarine J, Davis CD, Gore VK, Kaller MR, Lehto SG, Ma VV, Nishimura N, Nguyen TT, Tang P, Wang W, Youngblood BD, Zhang M, Gavva NR, Monenschein H, Norman MH. Horne DB, et al. Among authors: norman mh. J Med Chem. 2014 Apr 10;57(7):2989-3004. doi: 10.1021/jm401955h. Epub 2014 Mar 19. J Med Chem. 2014. PMID: 24597733
71 results