Search Results - "Bush, Eugene N."

Liver-specific Knockdown of JNK1 Up-regulates Proliferator-activated Receptor γ Coactivator 1β and Increases Plasma Triglyceride despite Reduced Glucose and Insulin Levels in Diet-induced Obese Mice by Yang, Ruojing, Wilcox, Denise M., Haasch, Deanna L., Jung, Paul M., Nguyen, Phong T., Voorbach, Martin J., Doktor, Stella, Brodjian, Sevan, Bush, Eugene N., Lin, Emily, Jacobson, Peer B., Collins, Christine A., Landschulz, Katherine T., Trevillyan, James M., Rondinone, Cristina M., Surowy, Terry K.

“…The c-Jun N-terminal kinases (JNKs) have been implicated in the development of insulin resistance, diabetes, and obesity. Genetic disruption of JNK1, but not…”
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Antiobesity effects of A-331440, a novel non-imidazole histamine H3 receptor antagonist by HANCOCK, Arthur A, BENNANI, Youssef L, JIA BAO PAN, SHAPIRO, Robin, WITTE, David G, YAO, Betty B, BUSH, Eugene N, ESBENSHADE, Timothy A, FAGHIH, Ramin, FOX, Gerard B, JACOBSON, Peer, KNOUREK-SEGEL, Victoria, KRUEGER, Kathleen M, NUSS, Merrill E

“…Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H(3)…”
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Effect of N-methyl substitution of the peptide bonds in luteinizing hormone-releasing hormone agonists by Haviv, Fortuna, Fitzpatrick, Timothy D, Swenson, Rolf E, Nichols, Charles J, Mort, Nicholas A, Bush, Eugene N, Diaz, Gilbert, Bammert, Gary, Nguyen, A

“…Each peptide bond in leuprolide (1), deslorelin (13), and nafarelin (24) was separately substituted with N-methyl. The synthesized compounds were tested for in…”
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Discovery and Pharmacological Evaluation of Growth Hormone Secretagogue Receptor Antagonists by Xin, Zhili, Serby, Michael D, Zhao, Hongyu, Kosogof, Christi, Szczepankiewicz, Bruce G, Liu, Mei, Hutchins, Charles W, Sarris, Kathy A, Hoff, Ethan D, Falls, H. Douglas, Lin, Chun W, Ogiela, Christopher A, Collins, Christine A, Brune, Michael E, Bush, Eugene N, Droz, Brian A, Fey, Thomas A, Knourek-Segel, Victoria E, Shapiro, Robin, Jacobson, Peer B, Beno, David W. A, Turner, Teresa M, Sham, Hing L, Liu, Gang

“…The discovery and pharmacological evaluation of potent, selective, and orally bioavailable growth hormone secretagogue receptor (GHS-R) antagonists are…”
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2,4-Diaminopyrimidine Derivatives as Potent Growth Hormone Secretagogue Receptor Antagonists by Serby, Michael D., Zhao, Hongyu, Szczepankiewicz, Bruce G., Kosogof, Christi, Xin, Zhili, Liu, Bo, Liu, Mei, Nelson, Lissa T. J., Kaszubska, Wiweka, Falls, H. Douglas, Schaefer, Verlyn, Bush, Eugene N., Shapiro, Robin, Droz, Brian A., Knourek-Segel, Victoria E., Fey, Thomas A., Brune, Michael E., Beno, David W. A., Turner, Theresa M., Collins, Christine A., Jacobson, Peer B., Sham, Hing L., Liu, Gang

“…Ghrelin, a gut-derived orexigenic hormone, is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R). Centrally administered ghrelin has been…”
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Synthesis and evaluation of urea-based indazoles as melanin-concentrating hormone receptor 1 antagonists for the treatment of obesity by Souers, Andrew J., Gao, Ju, Wodka, Dariusz, Judd, Andrew S., Mulhern, Mathew M., Napier, James J., Brune, Michael E., Bush, Eugene N., Brodjian, Sevan J., Dayton, Brian D., Shapiro, Robin, Hernandez, Lisa E., Marsh, Kennan C., Sham, Hing L., Collins, Christine A., Kym, Philip R.

“…A series of urea-based N-1-(2-aminoethyl)-indazoles was synthesized and evaluated for melanin-concentrating hormone receptor 1 (MCHr1) antagonism. Several…”
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Nonpeptide Luteinizing Hormone-Releasing Hormone Antagonists Derived from Erythromycin A:  Design, Synthesis, and Biological Activity of Cladinose Replacement Analogues by Randolph, John T, Waid, Philip, Nichols, Charles, Sauer, Daryl, Haviv, Fortuna, Diaz, Gilbert, Bammert, Gary, Besecke, Leslie M, Segreti, Jason A, Mohning, Kurt M, Bush, Eugene N, Wegner, Craig D, Greer, Jonathan

“…The design and synthesis of a series of 11,12-cyclic carbamate derivatives of 6-O-methylerythromycin A that are novel, nonpeptide LHRH antagonists, is…”
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Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity by Judd, Andrew S., Souers, Andrew J., Wodka, Dariusz, Zhao, Gang, Mulhern, Mathew M., Iyengar, Rajesh R., Gao, Ju, Lynch, John K., Freeman, Jennifer C., Falls, H. Douglas, Brodjian, Sevan, Dayton, Brian D., Reilly, Regina M., Gintant, Gary, Limberis, James T., Mikhail, Ann, Leitza, Sandra T., Houseman, Kathryn A., Diaz, Gilbert, Bush, Eugene N., Shapiro, Robin, Knourek-Segel, Victoria, Hernandez, Lisa E., Marsh, Kennan C., Sham, Hing L., Collins, Christine A., Kym, Philip R.

“…A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human…”
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In vitro Optimization of Structure Activity Relationships of Analogues of A‐331440 Combining Radioligand Receptor Binding Assays and Micronucleus Assays of Potential Antiobesity Histamine H3 Receptor Antagonists by Hancock, Arthur A., Diehl, Marilyn S., Faghih, Ramin, Bush, Eugene N., Krueger, Kathleen M., Krishna, Gopala, Miller, Thomas R., Wilcox, Nguyen, Phong, Pratt, John K., Cowart, Marlon D., Esbenshade, Timothy A., Jacobson, Peer B.

“…: A‐331440 {4′‐[3‐(3(R)‐(dimethylamino)‐pyrrolidin‐1‐yl)‐propoxy]‐biphenyl‐4‐carbonitrile}, a potent and selective antagonist of histamine H3 receptors,…”
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Chronic treatment with either dexfenfluramine or sibutramine in diet-switched diet-induced obese mice by Bush, Eugene N, Shapiro, Robin, Brune, Michael E, Knourek-Segel, Victoria E, Droz, Brian A, Fey, Thomas, Lin, Emily, Jacobson, Peer B

“…Dexfenfluramine (DEX) and sibutramine (SIB) are effective antiobesity agents. Their effects on weight control and hormone profile have not been previously…”
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Constrained 7-fluorocarboxychromone-4-aminopiperidine based Melanin-concentrating hormone receptor 1 antagonists: The effects of chirality on substituted indan-1-ylamines by Souers, Andrew J., Iyengar, Rajesh R., Judd, Andrew S., Beno, David W.A., Gao, Ju, Zhao, Gang, Brune, Michael E., Napier, James J., Mulhern, Mathew M., Lynch, John K., Freeman, Jennifer C., Wodka, Dariusz, Chen, Chong J., Falls, H. Doug, Brodjian, Sevan, Dayton, Brian D., Diaz, Gilbert J., Bush, Eugene N., Shapiro, Robin, Droz, Brian A., Knourek-Segel, Victoria, Hernandez, Lisa E., Marsh, Kennan C., Reilly, Regina M., Sham, Hing L., Collins, Christine A., Kym, Philip R.

“…The incorporation of constrained tertiary amines into an existing class of N-benzyl-4-aminopiperidinyl chromone-based MCHr1 antagonists led to the…”
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In vitro and in vivo Activities of Reduced-Size Antagonists of Luteinizing Hormone-Releasing Hormone by Haviv, Fortuna, Fitzpatrick, Timothy D, Nichols, Charles J, Bush, Eugene N, Diaz, Gilbert, Bammert, Gary, Nguyen, A. T, Johnson, Edwin S, Knittle, Judith, Greer, Jonathan

“…A novel series of octapeptide LHRH antagonists was designed on the basis of the structure of the (2-9) fragment of a LHRH agonist. By adopting a systematic SAR…”
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Pharmacological and endocrine characterization of A-198401, an orally active GnRH antagonist, in intact and castrate male rat models by Besecke, Leslie M., Diaz, Gilbert J., Segreti, Jason A., Mohning, Kurt M., Cybulski, Van A., Rao, Mira, Bush, Eugene N., Randolph, John T., Waid, Philip L., Haviv, Fortuna, Wegner, Craig D., Greer, Jonathan

“…Gonadotropin‐releasing hormone (GnRH) stimulates the synthesis and secretion of the gonadotropins that maintain the reproductive axis in mammals. Efforts have…”
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Obesity by Bush, Eugene N

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Obesity by Bush, Eugene N

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Divergence of ANF analogs in smooth muscle cell cGMP response and aorta vasorelaxation: evidence for receptor subtypes by Budzik, G P, Firestone, S L, Bush, E N, Connolly, P J, Rockway, T W, Sarin, V K, Holleman, W H

“…ANF analog potencies in stimulating smooth muscle cell cGMP were compared with the ability to relax histamine-constricted rabbit aorta in vitro. ANF[1-28],…”
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Stabilization of the N-terminal residues of luteinizing hormone-releasing hormone agonists and the effect on pharmacokinetics by Haviv, Fortuna, Fitzpatrick, Timothy D, Nichols, Charles J, Swenson, Rolf E, Bush, Eugene N, Diaz, Gilbert, Nguyen, A, Nellans, Hugh N, Hoffman, Daniel J

“…To stabilize leuprolide (1) against chymotrypsin and intestinal degradation several agonists of LHRH (2-12), modified at position 1, 2, or 3 and/or containing…”
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Antiobesity effects of A-331440, a novel non-imidazole histamine H 3 receptor antagonist by Hancock, Arthur A., Bennani, Youssef L., Bush, Eugene N., Esbenshade, Timothy A., Faghih, Ramin, Fox, Gerard B., Jacobson, Peer, Knourek-Segel, Victoria, Krueger, Kathleen M., Nuss, Merrill E., Pan, Jia Bao, Shapiro, Robin, Witte, David G., Yao, Betty B.

“…Histamine affects homeostatic mechanisms, including food and water consumption, by acting on central nervous system (CNS) receptors. Presynaptic histamine H 3…”
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Active reduced-size hexapeptide analogs of luteinizing hormone-releasing hormone by Haviv, Fortuna, Palabrica, Christopher A, Bush, Eugene N, Diaz, Gilbert, Johnson, Edwin S, Love, Stephen, Greer, Jonathan

“…A series of reduced-size hexapeptide analogues of LH-RH were synthesized that contain the residues corresponding to amino acid positions 4-9 and are linked to…”
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Small atrial natriuretic peptide analogs: design, synthesis, and structural requirements for guanylate cyclase activation by Von Geldern, Thomas W, Rockway, Todd W, Davidsen, Steven K, Budzik, Gerald P, Bush, Eugene N, Chu-Moyer, Margaret Y, Devine, Edward M, Holleman, William H, Johnson, Marty C

“…Structure/activity studies on atrial natriuretic peptide ANP (1-28) have highlighted three portions of the native molecule as necessary for its biological…”
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