Christopher E. Heise, Ph.D. - Publications

Affiliations: 
2002 University of Virginia, Charlottesville, VA 
Area:
receptor pharmacology

34 high-probability publications. We are testing a new system for linking publications to authors. You can help! If you notice any inaccuracies, please sign in and mark papers as correct or incorrect matches. If you identify any major omissions or other inaccuracies in the publication list, please let us know.

Year Citation  Score
2016 Lee W, Crawford JJ, Aliagas I, Murray LJ, Tay S, Wang W, Heise CE, Hoeflich KP, La H, Mathieu S, Mintzer R, Ramaswamy S, Rouge L, Rudolph J. Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 27346791 DOI: 10.1016/J.Bmcl.2016.06.031  0.36
2016 Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood EM, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, ... ... Heise CE, et al. Chemically diverse Group I p21-activated kinase (PAK) inhibitors impart acute cardiovascular toxicity with a narrow therapeutic window. Journal of Medicinal Chemistry. PMID 27167326 DOI: 10.1021/Acs.Jmedchem.6B00638  0.36
2015 Burdick DJ, Wang S, Heise C, Pan B, Drummond J, Yin J, Goeser L, Magnuson S, Blaney J, Moffat J, Wang W, Chen H. Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 26338362 DOI: 10.1016/J.Bmcl.2015.08.048  0.36
2015 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, et al. Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series. Acs Medicinal Chemistry Letters. 6: 711-5. PMID 26101579 DOI: 10.1021/Acsmedchemlett.5B00151  0.36
2015 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, et al. Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors. Journal of Medicinal Chemistry. 58: 5121-36. PMID 26030457 DOI: 10.1021/Acs.Jmedchem.5B00572  0.36
2015 Ndubaku CO, Crawford JJ, Drobnick J, Aliagas I, Campbell D, Dong P, Dornan LM, Duron S, Epler J, Gazzard L, Heise CE, Hoeflich KP, Jakubiak D, La H, Lee W, et al. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pKa Polar Moiety Acs Medicinal Chemistry Letters. 6: 1241-1246. DOI: 10.1021/acsmedchemlett.5b00398  0.36
2014 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, et al. Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. Journal of Medicinal Chemistry. 57: 1033-45. PMID 24432870 DOI: 10.1021/Jm401768T  0.36
2013 Lauffer BE, Mintzer R, Fong R, Mukund S, Tam C, Zilberleyb I, Flicke B, Ritscher A, Fedorowicz G, Vallero R, Ortwine DF, Gunzner J, Modrusan Z, Neumann L, Koth CM, ... ... Heise CE, et al. Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability. The Journal of Biological Chemistry. 288: 26926-43. PMID 23897821 DOI: 10.1074/Jbc.M113.490706  0.36
2012 Heise CE, Murray J, Augustyn KE, Bravo B, Chugha P, Cohen F, Giannetti AM, Gibbons P, Hannoush RN, Hearn BR, Jaishankar P, Ly CQ, Shah K, Stanger K, Steffek M, et al. Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6. Plos One. 7: e50864. PMID 23227217 DOI: 10.1371/Journal.Pone.0050864  0.36
2012 Mintzer R, Ramaswamy S, Shah K, Hannoush RN, Pozniak CD, Cohen F, Zhao X, Plise E, Lewcock JW, Heise CE. A whole cell assay to measure caspase-6 activity by detecting cleavage of lamin A/C. Plos One. 7: e30376. PMID 22253931 DOI: 10.1371/Journal.Pone.0030376  0.36
2012 Liu Y, Beresini MH, Johnson A, Mintzer R, Shah K, Clark K, Schmidt S, Lewis C, Liimatta M, Elliott LO, Gustafson A, Heise CE. Case studies of minimizing nonspecific inhibitors in HTS campaigns that use assay-ready plates. Journal of Biomolecular Screening. 17: 225-36. PMID 21940710 DOI: 10.1177/1087057111421525  0.36
2011 Atwal JK, Chen Y, Chiu C, Mortensen DL, Meilandt WJ, Liu Y, Heise CE, Hoyte K, Luk W, Lu Y, Peng K, Wu P, Rouge L, Zhang Y, Lazarus RA, et al. A therapeutic antibody targeting BACE1 inhibits amyloid-β production in vivo. Science Translational Medicine. 3: 84ra43. PMID 21613622 DOI: 10.1126/Scitranslmed.3002254  0.36
2010 Ramaswamy S, Yen I, Sideris S, Malek S, Heise CE. A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade. Assay and Drug Development Technologies. 8: 497-503. PMID 20482377 DOI: 10.1089/Adt.2009.0259  0.36
2007 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, et al. Synthesis and structure-activity relationships of spirohydantoin-derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Bioorganic & Medicinal Chemistry Letters. 17: 2171-8. PMID 17350839 DOI: 10.1016/J.Bmcl.2007.01.104  0.36
2007 Zhang M, Tamiya J, Nguyen L, Rowbottom MW, Dyck B, Vickers TD, Grey J, Schwarz DA, Heise CE, Haelewyn J, Mistry MS, Goodfellow VS. Thienopyrimidinone bis-aminopyrrolidine ureas as potent melanin-concentrating hormone receptor-1 (MCH-R1) antagonists. Bioorganic & Medicinal Chemistry Letters. 17: 2535-9. PMID 17329101 DOI: 10.1016/J.Bmcl.2007.02.012  0.36
2007 Heise CE, Sullivan SK, Crowe PD. Scintillation proximity assay as a high-throughput method to identify slowly dissociating nonpeptide ligand binding to the GnRH receptor. Journal of Biomolecular Screening. 12: 235-9. PMID 17208923 DOI: 10.1177/1087057106297362  0.36
2007 Mesleh MF, Shirley WA, Heise CE, Ling N, Maki RA, Laura RP. NMR structural characterization of a minimal peptide antagonist bound to the extracellular domain of the corticotropin-releasing factor1 receptor. The Journal of Biological Chemistry. 282: 6338-46. PMID 17192263 DOI: 10.1074/Jbc.M609816200  0.36
2006 Schwarz DA, Allen MM, Petroski RE, Pomeroy JE, Heise CE, Mistry MS, Selkirk JV, Nottebaum LM, Grey J, Zhang M, Goodfellow VS, Maki RA. Manipulation of small-molecule inhibitory kinetics modulates MCH-R1 function. Molecular and Cellular Endocrinology. 259: 1-9. PMID 16987592 DOI: 10.1016/J.Mce.2006.07.003  0.36
2006 Sullivan SK, Hoare SR, Fleck BA, Zhu YF, Heise CE, Struthers RS, Crowe PD. Kinetics of nonpeptide antagonist binding to the human gonadotropin-releasing hormone receptor: Implications for structure-activity relationships and insurmountable antagonism. Biochemical Pharmacology. 72: 838-49. PMID 16930559 DOI: 10.1016/j.bcp.2006.07.011  0.36
2006 Hudson S, Kiankarimi M, Rowbottom MW, Vickers TD, Wu D, Pontillo J, Ching B, Dwight W, Goodfellow VS, Schwarz D, Heise CE, Madan A, Wen J, Ban W, Wang H, et al. 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 2. Bioorganic & Medicinal Chemistry Letters. 16: 4922-30. PMID 16824755 DOI: 10.1016/j.bmcl.2006.06.049  0.36
2006 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, et al. 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. Bioorganic & Medicinal Chemistry Letters. 16: 4450-7. PMID 16814542 DOI: 10.1016/J.Bmcl.2006.06.045  0.36
2006 Dyck B, Markison S, Zhao L, Tamiya J, Grey J, Rowbottom MW, Zhang M, Vickers T, Sorensen K, Norton C, Wen J, Heise CE, Saunders J, Conlon P, Madan A, et al. A thienopyridazinone-based melanin-concentrating hormone receptor 1 antagonist with potent in vivo anorectic properties. Journal of Medicinal Chemistry. 49: 3753-6. PMID 16789729 DOI: 10.1021/Jm051263C  0.36
2006 Dyck B, Zhao L, Tamiya J, Pontillo J, Hudson S, Ching B, Heise CE, Wen J, Norton C, Madan A, Schwarz D, Wade W, Goodfellow VS. Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists. Bioorganic & Medicinal Chemistry Letters. 16: 4237-42. PMID 16762549 DOI: 10.1016/J.Bmcl.2006.05.075  0.36
2005 Huang CQ, Baker T, Schwarz D, Fan J, Heise CE, Zhang M, Goodfellow VS, Markison S, Gogas KR, Chen T, Wang XC, Zhu YF. 1-(4-Amino-phenyl)-pyrrolidin-3-yl-amine and 6-(3-amino-pyrrolidin-1-yl)-pyridin-3-yl-amine derivatives as melanin-concentrating hormone receptor-1 antagonists. Bioorganic & Medicinal Chemistry Letters. 15: 3701-6. PMID 16005225 DOI: 10.1016/j.bmcl.2005.05.130  0.36
2005 Rowbottom MW, Vickers TD, Dyck B, Tamiya J, Zhang M, Zhao L, Grey J, Provencal D, Schwarz D, Heise CE, Mistry M, Fisher A, Dong T, Hu T, Saunders J, et al. Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Bioorganic & Medicinal Chemistry Letters. 15: 3439-45. PMID 15950467 DOI: 10.1016/J.Bmcl.2005.05.015  0.36
2005 Heise CE, Pahuja A, Hudson SC, Mistry MS, Putnam AL, Gross MM, Gottlieb PA, Wade WS, Kiankarimi M, Schwarz D, Crowe P, Zlotnik A, Alleva DG. Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. The Journal of Pharmacology and Experimental Therapeutics. 313: 1263-71. PMID 15761110 DOI: 10.1124/Jpet.105.083683  0.36
2005 Grey J, Dyck B, Rowbottom MW, Tamiya J, Vickers TD, Zhang M, Zhao L, Heise CE, Schwarz D, Saunders J, Goodfellow VS. Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 15: 999-1004. PMID 15686900 DOI: 10.1016/J.Bmcl.2004.12.036  0.36
2002 Brinkmann V, Davis MD, Heise CE, Albert R, Cottens S, Hof R, Bruns C, Prieschl E, Baumruker T, Hiestand P, Foster CA, Zollinger M, Lynch KR. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. The Journal of Biological Chemistry. 277: 21453-7. PMID 11967257 DOI: 10.1074/Jbc.C200176200  0.36
2001 Heise CE, Santos WL, Schreihofer AM, Heasley BH, Mukhin YV, Macdonald TL, Lynch KR. Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist. Molecular Pharmacology. 60: 1173-80. PMID 11723223 DOI: 10.1124/Mol.60.6.1173  0.36
2001 Im DS, Heise CE, Nguyen T, O'Dowd BF, Lynch KR. Identification of a molecular target of psychosine and its role in globoid cell formation. The Journal of Cell Biology. 153: 429-34. PMID 11309421 DOI: 10.1083/Jcb.153.2.429  0.36
2001 Hooks SB, Santos WL, Im DS, Heise CE, Macdonald TL, Lynch KR. Lysophosphatidic acid-induced mitogenesis is regulated by lipid phosphate phosphatases and is Edg-receptor independent. The Journal of Biological Chemistry. 276: 4611-21. PMID 11042183 DOI: 10.1074/Jbc.M007782200  0.36
2000 Heise CE, O'Dowd BF, Figueroa DJ, Sawyer N, Nguyen T, Im DS, Stocco R, Bellefeuille JN, Abramovitz M, Cheng R, Williams DL, Zeng Z, Liu Q, Ma L, Clements MK, et al. Characterization of the human cysteinyl leukotriene 2 receptor. The Journal of Biological Chemistry. 275: 30531-6. PMID 10851239 DOI: 10.1074/Jbc.M003490200  0.36
2000 Im DS, Heise CE, Ancellin N, O'Dowd BF, Shei GJ, Heavens RP, Rigby MR, Hla T, Mandala S, McAllister G, George SR, Lynch KR. Characterization of a novel sphingosine 1-phosphate receptor, Edg-8. The Journal of Biological Chemistry. 275: 14281-6. PMID 10799507 DOI: 10.1074/Jbc.275.19.14281  0.36
2000 Im DS, Heise CE, Harding MA, George SR, O'Dowd BF, Theodorescu D, Lynch KR. Molecular cloning and characterization of a lysophosphatidic acid receptor, Edg-7, expressed in prostate. Molecular Pharmacology. 57: 753-9. PMID 10727522 DOI: 10.1124/Mol.57.4.753  0.36
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