title: Discovery of a beta-MSH-derived MC-4R selective agonist.
abstract: A series of novel, disulfide-constrained human beta-melanocyte stimulating hormone (beta-MSH)-derived peptides were optimized for in vitro melanocortin-4 receptor (MC-4R) binding affinity, agonist efficacy, and selectivity. The most promising of these, analogue 18, was further studied in vivo using chronic rat food intake and body weight models.
authors.affiliation: Lilly Research Laboratories, A Division of Eli Lilly and Co., Lilly Corporate Center, Indianapolis, Indiana 46285, USA. j.mayer@lilly.com
authors.forename: John P
authors.initials: JP
authors.lastname: Mayer
authors.forename: Hansen M
authors.initials: HM
authors.lastname: Hsiung
authors.forename: David B
authors.initials: DB
authors.lastname: Flora
authors.forename: Patrick
authors.initials: P
authors.lastname: Edwards
authors.forename: Dennis P
authors.initials: DP
authors.lastname: Smith
authors.forename: Xing-Yue
authors.initials: XY
authors.lastname: Zhang
authors.forename: Robert A
authors.initials: RA
authors.lastname: Gadski
authors.forename: Mark L
authors.initials: ML
authors.lastname: Heiman
authors.forename: Jeanne L
authors.initials: JL
authors.lastname: Hertel
authors.forename: Paul J
authors.initials: PJ
authors.lastname: Emmerson
authors.forename: Saba
authors.initials: S
authors.lastname: Husain
authors.forename: Thomas P
authors.initials: TP
authors.lastname: O'brien
authors.forename: Steven D
authors.initials: SD
authors.lastname: Kahl
authors.forename: David L
authors.initials: DL
authors.lastname: Smiley
authors.forename: Lianshan
authors.initials: L
authors.lastname: Zhang
authors.forename: Richard D
authors.initials: RD
authors.lastname: Dimarchi
authors.forename: Liang Zeng
authors.initials: LZ
authors.lastname: Yan
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001835:Body Weight / Q000187:drug effects; D002460:Cell Line; D004435:Eating / Q000187:drug effects; D006801:Humans; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011869:Radioligand Assay; D051381:Rats; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists*; D013329:Structure-Activity Relationship; D019824:beta-MSH / Q000737:chemistry*
chemical_list: D019440:Anti-Obesity Agents; D009842:Oligopeptides; D044105:Receptor, Melanocortin, Type 4; D019824:beta-MSH