Zobrazeno 1 - 10
of 14
pro vyhledávání: '"Russell James Sheldon"'
Autor:
Julie A. Farmer, Adrian Gregory Switzer, Martin E. Dowty, Timothy B. Field, Adam W. Mazur, Xinrong Tian, Russell James Sheldon, Beth B. Pinney, Steve Berberich, Lalith R. Jayasinghe, Frank H. Ebetino, Doreen Crossdoersen, John August Wos, Cindy Obringer
Publikováno v:
Journal of Medicinal Chemistry. 49:4745-4761
The design, synthesis, and structure-activity relationships (SAR) of a series of novel proline and pyrrolidine based melanocortin receptor (MCR) agonists are described. To validate a conformationally constrained Arg-Nal dipeptide analogue strategy, w
Autor:
Beth B. Pinney, Jeffery C. Hayes, Xinrong Tian, Russell James Sheldon, Mark Gregory Solinsky, Adrian Gregory Switzer, Frank H. Ebetino, Doreen Crossdoersen, John August Wos, Julie A. Farmer, Xuemei Chen, Lixian Gan
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 16:1721-1725
The first synthesis of Tic-D-Phe Psi[CH(2)-CH(2)] isostere is described, which features diastereoselective alkylation of the tricyclic lactam 14. The use of this novel dipeptide isostere in the development of melanocortin agonists has been demonstrat
Autor:
Russell James Sheldon, Frank H. Ebetino, Doreen Crossdoersen, Beth B. Pinney, Timothy B. Field, John August Wos, Adam W. Mazur, Xinrong Tian
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:2819-2823
A series of proline based melanocortin ligands has been developed on the basis of initial piperazine leads by using a more conformationally rigid scaffold. A number of these novel ligands showed significant binding affinity for MC3 and MC4 receptors.
Autor:
Jana S. Lange, Richard T. Hinkle, Elizabeth Donnelly, Eric Tobar, Russell James Sheldon, Sarah C. Coste, Steven Samuelsson, Robert J. Isfort, Mark A. Tarnopolsky, Mary Beth Bauer, David B. Cody, Mary P. Stenzel-Poore
Publikováno v:
American Journal of Physiology-Endocrinology and Metabolism. 285:E889-E898
Two receptors activated by the corticotropin-releasing factor (CRF) family of peptides have been identified, the CRF 1 receptor (CRF1R) and the CRF 2 receptor (CRF2R). Of these, the CRF2R is expressed in skeletal muscle. To understand the role of the
Autor:
Randy J. Seeley, Patrick Messerschmidt, Stephen C. Woods, Dawn M.M Eckstein, Karen M.B. Hodge, Charles C. McOsker, Kihmberly A. Wilmer, Russell James Sheldon, Melissa B. Jones, Stephen C. Benoit, Ellen L. Air
Publikováno v:
Physiology & Behavior. 79:761-766
The conditioned taste aversion (CTA) is routinely used to assess the aversive consequences of anorexic agents, including potential pharmacological therapies for obesity. In a typical CTA paradigm, rats briefly sampling a novel tastant (e.g., sacchari
Autor:
Karen M.B. Hodge, Kihmberly A. Wilmer, Stephen C. Woods, Randy J. Seeley, Charles C. McOsker, P Messerschmidt, Ellen L. Air, Stephen C. Benoit, Melissa B. Jones, Russell James Sheldon, D M M Eckstein
Publikováno v:
International Journal of Obesity. 27:550-556
BACKGROUND: The synthetic melanocortin (MC) agonist, melanotan-II (MTII), reduces food intake and body weight for hours to days after administration. One early report on the effect of MTII suggested that part of its anorexic action may be mediated by
Autor:
Melissa B. Jones, Russell James Sheldon, N. Leigh Anderson, Thomas Keough, Richard T. Hinkle, Feng Wang, Robert J. Isfort, Yiping Sun, Kenneth D. Greis
Publikováno v:
Electrophoresis. 21:2228-2234
A proteomic analysis was performed comparing normal rat soleus muscle to denervated soleus muscle at 0.5, 1, 2, 4, 6, 8 and 10 days post denervation. Muscle mass measurements demonstrated that the times of major mass changes occurred between 2 and 4
Autor:
Frank H. Ebetino, Doreen Crossdoersen, Lily Dong, Mark E. Webster, Beth B. Pinney, Russell James Sheldon, Adrian Gregory Switzer, Cindy Obringer, Mumin Rashid Naeem, Lalith R. Jayasinghe, Anny-Odile Colson, Rajesh K. Mishra, Charles A. Cruze, John August Wos, Steve A. Derose, Mark Gregory Solinsky, Martin E. Dowty, Paula M. Suchanek, Xinrong Tian, Julie A. Farmer, Melissa L. Burklow, Mary Kay Dirr
Publikováno v:
Journal of medicinal chemistry. 51(19)
A study that was designed to identify plausible replacements for highly basic guanidine moiety contained in potent MC4R agonists, as exemplified by 1, led to the discovery of initial nonguanidine lead 5. Propyl analog 23 was subsequently found to be
Autor:
Adam W. Mazur, Russell James Sheldon, Nick K. Kim, Julie A. Farmer, Xinrong Tian, John August Wos, Frank H. Ebetino, Doreen Crossdoersen, X. Eric Hu, Adrian Gregory Switzer, Rajesh K. Mishra, Beth B. Pinney
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(17)
The design and synthesis of a series of potent 1,3,4-trisubstituted-2-oxopiperazine based MC4 agonists are described. The tripeptidomimetic analogs (12a,b and 23) and the dipeptidomimetic 27 displayed single-nanomolar binding affinity and agonist pot
Autor:
Ofer Reizes, Russell James Sheldon, Melissa L. Burklow, Randy J. Seeley, Maria Claudia Gross, Darren Paul Trokhan, Colette C. Matthews, Kihmberly A. Wilmer, Charles C. McOsker
Publikováno v:
Endocrinology. 146(9)
A wide range of experimental evidence implicates a critical role for melanocortin signaling in the control of food intake and body adiposity. Melanocortin receptor agonists such as MT-II potently reduce food intake and body weight, making such agonis