Zobrazeno 1 - 10
of 27
pro vyhledávání: '"Alan D. Adams"'
Autor:
Zhihua Li, Joel P. Berger, Raynald Bergeron, Alan D. Adams, Thomas W. Doebber, Jun Yao, John Woods, Bei B. Zhang, Emanuel Zycband, David E. Moller, Cherrie Liu
Publikováno v:
Endocrinology. 147:4252-4262
Peroxisome proliferator-activated receptor (PPAR)-gamma agonists are insulin sensitizers, whereas PPAR alpha agonists are lipid-lowering agents in humans. Chronic treatment with PPAR gamma agonists has been shown to prevent the onset of diabetes in y
Autor:
Denise P. Milot, Jacqueline C. Lopez, Laurence B. Peterson, Alan D. Adams, Samuel D. Wright, Jayne Chin, Lyndon J. Mitnaul, Sandra E. Rex-Rabe, Erik G. Lund, Carl P. Sparrow, John G. Menke, Jenny Tian, My-Hanh Lam, Melanie Latham, Ray Rosa, Shaei Huang, Qiu Guo, Charlotte Burton
Publikováno v:
Biochemical Pharmacology. 71:453-463
Liver X receptor (LXR) alpha and LXRbeta are closely related nuclear receptors that respond to elevated levels of intracellular cholesterol by enhancing transcription of genes that control cholesterol efflux and fatty acid biosynthesis. The consequen
Autor:
John G. Menke, Lyndon J. Mitnaul, Alan D. Adams, Carl P. Sparrow, Raul Lacson, Paul A. Fischer, Aileen Bouffard, Ahren I. Green, Jayne Chin, Todd Smith
Publikováno v:
ASSAY and Drug Development Technologies. 1:777-787
Activation of liver X receptors (LXRs) induces reverse cholesterol transport and increases high-density lipoprotein cholesterol in vivo. Here, we describe novel, functional, homogeneous cell-based fluorescence resonance energy transfer assays for ide
Autor:
Michael J. Forrest, Zao Hu, Roger Meurer, Alan D. Adams, Alex Elbrecht, Thomas W. Doebber, Joel P. Berger, Derek Von Langen, Adonis Dadiz, A. Brian Jones, David E. Moller, Karen L. MacNaul, Gaochao Zhou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:3185-3190
A new class of O-arylmandelic acid PPAR agonists show excellent anti-hyperglycemic efficacy in a db/db mouse model of DM2. These PPARα-weighted agonists do not show the typical PPARγ associated side effects of BAT proliferation and cardiac hypertro
Autor:
John Ventre, Mona Parikh, Thomas W. Doebber, Bruce A. Johnson, Ann Petro, Gaochao Zhou, Joel Berger, Bei B. Zhang, Linda J. Kelly, Neelam Sharma, Michael R. Tanen, Alan D. Adams, Chhabi Biswas, Ralph T. Mosley, Richard S. Surwit, Alex Elbrecht, G. Marie Thompson, David E. Moller, Karen L. MacNaul, Karen Richards
Publikováno v:
Molecular Endocrinology. 17:662-676
Antidiabetic thiazolidinediones (TZDs) and non-TZD compounds have been shown to serve as agonists of the peroxisome proliferator-activated receptor gamma (PPARgamma). Here, we report the identification and characterization of a novel non-TZD selectiv
Autor:
Conrad Santini, Zao Hu, Alan D. Adams, Winston Yuen, Joel P. Berger, A. Brian Jones, David E. Moller, Karen L. MacNaul, Thomas W. Doebber
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:931-935
A series of amphipathic 3-phenylbenzisoxazoles were found to be potent agonists of human PPARalpha, gamma and delta. The optimization of acid proximal structure for in vitro and in vivo potency is described. Results of po dosed efficacy studies in th
Autor:
Jane-L. Lo, Alan D. Adams, Samuel D. Wright, Edward Metzger, Jinghua Yu, Li Huang, Jisong Cui, Peter T. Meinke, Annie Zhao
Publikováno v:
Journal of Biological Chemistry. 277:31441-31447
Bile salt export pump (BSEP) is a major bile acid transporter in the liver. Mutations in BSEP result in progressive intrahepatic cholestasis, a severe liver disease that impairs bile flow and causes irreversible liver damage. BSEP is a target for inh
Autor:
Alan D. Adams, Richard A. Blevins, Yuli Chen, David Gerhold, Jian Xu, Alex Elbrecht, Joel P. Berger
Publikováno v:
Journal of the Association for Laboratory Automation. 6:71-75
Ligands for peroxisome proliferator activated receptors (PPARs) are used as hypolipidemic agents and for the treatment of type II diabetes, PPARa and PPARg, respectively. PPARs are members of the nuclear receptor family of ligand activated transcript
Autor:
Alan D. Adams, Yuli Chen, Alex Elbrecht, Joel Berger, Patrick R. Griffin, Roy G. Smith, Gaochao Zhou, David E. Moller, Bei Zhang, Tracey Klatt, John G. Menke
Publikováno v:
Journal of Biological Chemistry. 274:7913-7922
Insulin-sensitizing thiazolidinedione (TZD) compounds are high affinity ligands for a member of the nuclear receptor family, peroxisome proliferator-activated receptor (PPAR) γ. A scintillation proximity assay for measurement of3H-radiolabeled TZD b
Autor:
Andrew D. Howard, Peter T. Meinke, Elizabeth Murphy, Meng Yang, Ralph Mosely, Cai Li, Rachel G. Samuel, Alan D. Adams, Gary G. Chicchi, John J. Acton, Yong Zhang, Harold B. Wood, Kake Zhao, Stanley Freeman, Jason W. Szewczyk, Yong Huang, Conrad Santini
Publikováno v:
Bioorganicmedicinal chemistry letters. 21(9)
Screening of the Merck sample collection identified compound 1 as a weakly potent GPR119 agonist (hEC(50)=3600 nM). Dual termini optimization of 1 led to compound 36 having improved potency, selectivity, and formulation profile, however, modest physi