Structure–activity relationship of cyclic peptide penta-c[Asp-His6-DPhe7-Arg8-Trp9-Lys]-NH2 at the human melanocortin-1 and -4 receptors: His6 substitution

Autor: Keith A. Yagaloff, Xin-Jie Chu, Lucia Franco, Mitch Yeon, Grazyna Kurylko, Lida Qi, Li Chen, Adrian Wai-Hing Cheung, Karen Rowan, Joseph Swistok, Waleed Danho

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 13:1307-1311

A series of MT-II related cyclic peptides, based on potent but non-selective hMC4R agonist (Penta-c[Asp-His(6)-DPhe(7)-Arg(8)-Trp(9)-Lys]-NH(2)) was prepared in which His(6) residue was systematically substituted. Two of the most interesting peptides

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::47749aaf28fdcb9a19bda21a311182db
https://doi.org/10.1016/s0960-894x(03)00114-8

Response of melanocortin–4 receptor–deficient mice to anorectic and orexigenic peptides

Autor: Dennis Huszar, Donald J. Marsh, Gunther Hollopeter, Ralph Laufer, Richard D. Palmiter, Keith A. Yagaloff, Paul Burn, Stewart L. Fisher

Publikováno v: Nature Genetics. 21:119-122

Mutations reducing the functional activity of leptin, the leptin receptor, alpha-melanocyte stimulating hormones (alpha-MSH) and the melanocortin-4 receptor (Mc4r) all lead to obesity in mammals. Moreover, mutant mice that ectopically express either

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6f087649002b3ee37f521451db9f560
https://doi.org/10.1038/5070

Central infusion of melanocortin agonist MTII in rats: assessment of c-Fos expression and taste aversion

Autor: Gertjan van Dijk, Randy J. Seeley, Todd E. Thiele, Keith A. Yagaloff, Stewart L. Fisher, Paul Burn, Michael W. Schwartz

Publikováno v: American Journal of Physiology-Regulatory, Integrative and Comparative Physiology, 274(1), R248-R254. AMER PHYSIOLOGICAL SOC
Europe PubMed Central

Like leptin (OB protein), central infusion of the nonspecific melanocortin agonist MTII reduces food intake for relatively long periods of time (i.e., 12 h; W. Fan, B. A. Boston, R. A. Kesterson, V. J. Hruby, and R. D. Cone, Nature: 385: 165–168, 1

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f577fd112681eccaf38ac85363fd7088
https://doi.org/10.1152/ajpregu.1998.274.1.r248

Section Review: Recent progress in the development of leukotriene B4antagonists

Autor: Keith A. Yagaloff, Noal Cohen

Publikováno v: Expert Opinion on Investigational Drugs. 3:13-22

Leukotriene B4 (LTB4) is a potent proinflammatory lipid mediator derived from arachidonic acid via the 5-lipoxygenase pathway. It is a powerful chemoattractant and activator of neutrophils and exhibits effects on other cell types as well. This eicosa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::226b629ae8c3975ad3552bcad490842f
https://doi.org/10.1517/13543784.3.1.13

Discovery of 1-amino-4-phenylcyclohexane-1-carboxylic acid and its influence on agonist selectivity between human melanocortin-4 and -1 receptors in linear pentapeptides

Autor: Lucia Franco, Joseph Swistok, Karen Rowan, David Joseph Bartkovitz, Li Chen, Adrian Wai-Hing Cheung, Lida Qi, Xin-Jie Chu, Mitch Yeon, Keith A. Yagaloff, Grazyna Kurylko, Waleed Danho

Publikováno v: Bioorganicmedicinal chemistry letters. 15(22)

Linear pentapeptides (Penta-cis-Apc-DPhe-Arg-Trp-Gly-NH2) containing 1-amino-4-phenylcyclohexane-1-carboxylic acid (cis-Apc) and substituted Apc are potent hMC4R agonists and they are inactive or weakly active in hMC1R, hMC3R, and hMC5R agonist assay

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::90f6161601842ff762bf0f2bc6180ba0
https://pubmed.ncbi.nlm.nih.gov/16169218