Structure-activity relationship of linear peptide Bu-His6-DPhe7-Arg8-Trp9-Gly10-NH2 at the human melanocortin-1 and -4 receptors: DPhe7 and Trp9 substitution.
A series of pentapeptides, based on hMC4R pentapeptide agonist (Bu-His(6)-DPhe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2)), was prepared in which either DPhe(7) or Trp(9) residue was systematically substituted. A number of interesting DPhe surrogates (D-Thi, D-3-CF(3)Phe, D-2-Nal and D-3,4-diClPhe) as well as Trp surrogates (2-Nal and Bta) were identified in this study.
Danho
Waleed
W
Roche Research Center, Hoffmann-La Roche Inc., Nutley, NJ 07110, USA. waleed.danho@roche.com
Swistok
Joseph
J
Cheung
Adrian Wai-Hing
AW
Kurylko
Grazyna
G
Franco
Lucia
L
Chu
Xin-Jie
XJ
Chen
Li
L
Yagaloff
Keith
K
D019943:Amino Acid Substitution; D002460:Cell Line; D006801:Humans; D009765:Obesity / Q000188:drug therapy; D009842:Oligopeptides / Q000737:chemistry / Q000494:pharmacology*; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000235:genetics; D044101:Receptors, Melanocortin / Q000819:agonists* / Q000235:genetics; D013329:Structure-Activity Relationship; D014162:Transfection
C474662:Bu-His(6)-Phe(7)-Arg(8)-Trp(9)-Gly(10)-NH(2); D009842:Oligopeptides; D044105:Receptor, Melanocortin, Type 4; D044101:Receptors, Melanocortin