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Page 1
Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors.
Burdick DJ, Wang S, Heise C, Pan B, Drummond J, Yin J, Goeser L, Magnuson S, Blaney J, Moffat J, Wang W, Chen H. Burdick DJ, et al. Among authors: heise c. Bioorg Med Chem Lett. 2015 Nov 1;25(21):4728-4732. doi: 10.1016/j.bmcl.2015.08.048. Epub 2015 Aug 22. Bioorg Med Chem Lett. 2015. PMID: 26338362
Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors.
Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H, DiPasquale AG, Friedman LS, Heise C, Koeppen H, Kotey A, Mintzer R, Oh A, Roberts DA, Rouge L, Rudolph J, Tam C, Wang W, Xiao Y, Young A, Zhang Y, Hoeflich KP. Staben ST, et al. Among authors: heise c. J Med Chem. 2014 Feb 13;57(3):1033-45. doi: 10.1021/jm401768t. Epub 2014 Feb 4. J Med Chem. 2014. PMID: 24432870
Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.
Crawford JJ, Lee W, Aliagas I, Mathieu S, Hoeflich KP, Zhou W, Wang W, Rouge L, Murray L, La H, Liu N, Fan PW, Cheong J, Heise CE, Ramaswamy S, Mintzer R, Liu Y, Chao Q, Rudolph J. Crawford JJ, et al. J Med Chem. 2015 Jun 25;58(12):5121-36. doi: 10.1021/acs.jmedchem.5b00572. Epub 2015 Jun 12. J Med Chem. 2015. PMID: 26030457
Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.
Rudolph J, Aliagas I, Crawford JJ, Mathieu S, Lee W, Chao Q, Dong P, Rouge L, Wang W, Heise C, Murray LJ, La H, Liu Y, Manning G, Diederich F, Hoeflich KP. Rudolph J, et al. Among authors: heise c. ACS Med Chem Lett. 2015 May 20;6(6):711-5. doi: 10.1021/acsmedchemlett.5b00151. eCollection 2015 Jun 11. ACS Med Chem Lett. 2015. PMID: 26101579 Free PMC article.
Synthesis and structure-activity relationships of retro bis-aminopyrrolidine urea (rAPU) derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Part 1.
Rowbottom MW, Vickers TD, Dyck B, Grey J, Tamiya J, Zhang M, Kiankarimi M, Wu D, Dwight W, Wade WS, Schwarz D, Heise CE, Madan A, Fisher A, Petroski R, Goodfellow VS. Rowbottom MW, et al. Bioorg Med Chem Lett. 2006 Sep 1;16(17):4450-7. doi: 10.1016/j.bmcl.2006.06.045. Epub 2006 Jun 30. Bioorg Med Chem Lett. 2006. PMID: 16814542
Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window.
Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood E, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, Zhang H, Heise CE, Oh A, Ong CC, La H, Chakravarty P, Chan C, Jakubiak D, Epler J, Ramaswamy S, Vega R, Cain G, Diaz D, Zhong Y. Rudolph J, et al. Among authors: heise ce. J Med Chem. 2016 Jun 9;59(11):5520-41. doi: 10.1021/acs.jmedchem.6b00638. Epub 2016 May 24. J Med Chem. 2016. PMID: 27167326
Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1).
Rowbottom MW, Vickers TD, Tamiya J, Zhang M, Dyck B, Grey J, Schwarz D, Heise CE, Hedrick M, Wen J, Tang H, Wang H, Fisher A, Aparicio A, Saunders J, Goodfellow VS. Rowbottom MW, et al. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2171-8. doi: 10.1016/j.bmcl.2007.01.104. Epub 2007 Feb 4. Bioorg Med Chem Lett. 2007. PMID: 17350839
334 results