Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Eugene N. Bush"'
Autor:
Jiahong Wang, DeAnne Stolarik, Hovis M. Imade, Victoria Knourek-Segel, Phong Nguyen, Denise Wilcox, Peer B. Jacobson, Michael E. Brune, William Chiou, Steven Fung, Robin Shapiro, Vince Yeh, J.T. Link, Ravi Kurukulasuriya, Katina Monzon, Eugene N. Bush
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:5555-5560
A series of metabolically stable butyrolactam 11beta-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::16d60418fa06ac90a6a4054cde3829be
https://doi.org/10.1016/j.bmcl.2006.08.034
https://doi.org/10.1016/j.bmcl.2006.08.034
Autor:
Gilbert Diaz, Lee C. Preusser, Ann Mikhail, Christopher A. Ogiela, Lynch John K, Philip R. Kym, Lisa M. Hernández, Dariusz Wodka, Gang Zhao, Doug H. Falls, Eugene N. Bush, James S. Polakowski, Andrew S. Judd, Robin Shapiro, Hing L. Sham, James J. Napier, Christine A. Collins, Kennan C. Marsh, Victoria Knourek-Segel, Glenn A. Reinhart, Thomas J Campbell, Sevan Brodjian, Michael E. Brune, Brian A. Droz, Mathew M. Mulhern, Kathryn Houseman, Regina M. Reilly, Brian D. Dayton, Ryan M. Fryer, James T. Limberis, Rajesh R. Iyengar, Freeman Jennifer C
Publikováno v:
Journal of Medicinal Chemistry. 49:6569-6584
Evaluation of multiple structurally distinct series of melanin concentrating hormone receptor 1 antagonists in an anesthetized rat cardiovascualar assay led to the identification of a chromone-2-carboxamide series as having excellent safety against t
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b667ab564d57ac2f27112dd9382a72ab
https://doi.org/10.1021/jm060683e
https://doi.org/10.1021/jm060683e
Autor:
Verlyn G. Schaefer, Michael D. Serby, Bo Liu, Christine A. Collins, H. Douglas Falls, Hongyu Zhao, Eugene N. Bush, Victoria Knourek-Segel, Theresa M Turner, Michael E. Brune, Gang Liu, Thomas A. Fey, Wiweka Kaszubska, Brian A. Droz, Christi Kosogof, Zhili Xin, David W A Beno, Robin Shapiro, Peer B. Jacobson, Bruce G. Szczepankiewicz, Mei Liu, Nelson Lissa T, Hing L. Sham
Publikováno v:
Journal of Medicinal Chemistry. 49:2568-2578
Ghrelin, a gut-derived orexigenic hormone, is an endogenous ligand of the growth hormone secretagogue receptor (GHS-R). Centrally administered ghrelin has been shown to cause hunger and increase food intake in rodents. Inhibition of ghrelin actions w
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b0d352477e306be3be634175471489d0
https://doi.org/10.1021/jm0510934
https://doi.org/10.1021/jm0510934
Autor:
Emily Lin, Robin Shapiro, Victoria Knourek-Segel, Michael E. Brune, Brian A. Droz, Thomas A. Fey, Peer B. Jacobson, Eugene N. Bush
Publikováno v:
Endocrine. 29:375-382
Dexfenfluramine (DEX) and sibutramine (SIB) are effective antiobesity agents. Their effects on weight control and hormone profile have not been previously studied in diet-switched diet-induced obese (DIO) mice, in which treatment is initiated upon ce
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::67bc4a9ba15f316e481d8d35260eebfd
https://doi.org/10.1385/endo:29:2:375
https://doi.org/10.1385/endo:29:2:375
Autor:
Christine A. Collins, Victoria Knourek-Segel, Philip R. Kym, Dariusz Wodka, Hing L. Sham, Brad J. Geddes, Rajesh R. Iyengar, Anil Vasudevan, Ju Gao, Su Jen Lai, Elizabeth K. Govek, Thomas A. Fey, Freeman Jennifer C, Gang Zhao, Dennis G Fry, Michael E. Brune, Jennifer Lee Che, Brian D. Dayton, Doug H. Falls, Kennan C. Marsh, Andrew J. Souers, James Brown, Jon Roses, Michael A. Patane, Matthew J. LaMarche, Cathleen Mcdowell, Lee C. Preusser, Lisa E. Hernandez, Mathew M. Mulhern, Courtney Cullis, Tom Marsilje, Sevan Brodjian, Lynch John K, Eugene N. Bush, Sells Todd B, Robin Shapiro, Christopher Blackburn, Andrew S. Judd, Glenn A. Reinhart
Publikováno v:
Journal of Medicinal Chemistry. 48:5888-5891
4-(1-Benzo[1,3]dioxol-5-ylmethylpiperidine-4-ylmethyl)-6-chlorochromen-2-one (7) is a potent, orally bioavailable melanin concentrating hormone receptor 1 (MCHr1) antagonist that causes dose-dependent weight loss in diet-induced obese mice. Further e
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b385adec4f57fc115bc33dad4a4acdf7
https://doi.org/10.1021/jm050598r
https://doi.org/10.1021/jm050598r
Autor:
Christine A. Collins, Brian D. Dayton, Eugene N. Bush, Mathew M. Mulhern, Andrew J. Souers, Kennan C. Marsh, Anil Vasudevan, Dariusz Wodka, Hing L. Sham, Lisa E. Hernandez, Ju Gao, Robin Shapiro, Sevan Brodjian, Andrew S. Judd, Philip R. Kym, Michael E. Brune
Publikováno v:
Journal of Medicinal Chemistry. 48:1318-1321
Optimization of a high-throughput screening hit against melanin-concentrating hormone receptor 1 (MCHr1) led to the discovery of 2-(4-benzyloxy-phenyl)-N-[1-(2-pyrrolidin-1-yl-ethyl)-1H-indazol-6-yl]acetamide (7a). This compound was found to be a hig
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1a3b327a29055590c8bf6c4061cc9a7c
https://doi.org/10.1021/jm0490890
https://doi.org/10.1021/jm0490890
Autor:
Arthur A. Hancock, Thomas R. Miller, Kathleen M. Krueger, Gopala Krishna, Peer B. Jacobson, Marilyn S. Diehl, Ramin Faghih, Wilcox, Eugene N. Bush, John K. Pratt, Timothy A. Esbenshade, Marlon D. Cowart, Phong Nguyen
Publikováno v:
Pharmacology and Toxicology. 95:144-152
A-331440 {4′-[3-(3(R)-(dimethylamino)-pyrrolidin-1-yl)-propoxy]-biphenyl-4-carbonitrile}, a potent and selective antagonist of histamine H3 receptors, yielded positive results in an in vitro micronucleus assay, predictive of genotoxicity in vivo. B
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::e10c85daf5d315d66c3726c015eca909
https://doi.org/10.1111/j.1742-7843.2004.950307.x
https://doi.org/10.1111/j.1742-7843.2004.950307.x
Autor:
Jo Ann Janovick, Mark T. Goulet, Jonathan Greer, P. Michael Conn, Eugene N. Bush, David G. Wettlaufer
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 305:608-614
We expressed a test system of wild-type (WT) rat (r) and human (h) gonadotropin-releasing hormone (GnRH) receptors (GnRHRs), including naturally occurring (13) and manufactured (five) "loss-of-function" mutants of the GnRHR. These were used to assess
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a15af25a4430c2ece6c0c99c8468c0ac
https://doi.org/10.1124/jpet.102.048454
https://doi.org/10.1124/jpet.102.048454
Autor:
Ruojing Yang, Sevan Brodjian, Martin J. Voorbach, Terry K. Surowy, Katherine T. Landschulz, Christine A. Collins, Stella Doktor, Denise Wilcox, Cristina M. Rondinone, James M. Trevillyan, Peer B. Jacobson, Eugene N. Bush, Emily Lin, Phong Nguyen, Deanna L. Haasch, Paul M. Jung
Publikováno v:
The Journal of biological chemistry. 282(31)
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 JNK2, improves insulin sensitivity in diet-induced obese (DIO) mice. We applied RNA interfer
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::17cf1a3363dfafb5f884e93c5c4288b6
https://pubmed.ncbi.nlm.nih.gov/17550900
https://pubmed.ncbi.nlm.nih.gov/17550900
Autor:
Ann Mikhail, Sandra Leitza, Gilbert Diaz, Brian D. Dayton, Lynch John K, Robin Shapiro, Kathryn Houseman, Freeman Jennifer C, Philip R. Kym, Dariusz Wodka, Sevan Brodjian, Eugene N. Bush, Ju Gao, Regina M. Reilly, Gary Gintant, Kennan C. Marsh, Mathew M. Mulhern, Andrew S. Judd, Christine A. Collins, Victoria Knourek-Segel, Andrew J. Souers, Lisa E. Hernandez, H. Douglas Falls, James T. Limberis, Rajesh R. Iyengar, Gang Zhao, Hing L. Sham
Publikováno v:
Bioorganicmedicinal chemistry letters. 17(8)
A series of potent 2-carboxychromone-based melanin-concentrating hormone receptor 1 (MCHr1) antagonists were synthesized and evaluated for hERG (human Ether-a-go-go Related Gene) channel affinity and functional blockade. Basic dialkylamine-terminated
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7b5abf393ce4ce2e27f9d18993ae6cf1
https://pubmed.ncbi.nlm.nih.gov/17350253
https://pubmed.ncbi.nlm.nih.gov/17350253