Design and pharmacology of peptoids and peptide-peptoid hybrids based on the melanocortin agonists core tetrapeptide sequence.
A series of N-substituted glycine oligomers (peptoids) and peptide-peptoid hybrids were synthesized based on the Ac-His-Phe-Arg-Trp-NH(2) tetrapeptide template. The compounds were pharmacologically characterized at the mouse melanocortin receptors (MC1R, MC3R-MC5R) for agonist activity.
Holder
Jerry Ryan
JR
Department of Medicinal Chemistry, University of Florida, PO Box 100485, Gainesville, FL 32610, USA.
Bauzo
Rayna M
RM
Xiang
Zhimin
Z
Scott
Joseph
J
Haskell-Luevano
Carrie
C
D000595:Amino Acid Sequence; D000818:Animals; D002460:Cell Line; D015195:Drug Design; D005998:Glycine / Q000031:analogs & derivatives; D006801:Humans; D007700:Kinetics; D008024:Ligands; D051379:Mice; D008958:Models, Molecular; D009842:Oligopeptides / Q000737:chemistry; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D034444:Peptoids / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D044104:Receptor, Melanocortin, Type 3 / Q000819:agonists* / Q000737:chemistry / Q000187:drug effects; D044105:Receptor, Melanocortin, Type 4 / Q000819:agonists* / Q000737:chemistry / Q000187:drug effects; D011994:Recombinant Proteins / Q000819:agonists / Q000737:chemistry / Q000187:drug effects; D013329:Structure-Activity Relationship; D014162:Transfection
D008024:Ligands; D009842:Oligopeptides; D010455:Peptides; D034444:Peptoids; D044104:Receptor, Melanocortin, Type 3; D044105:Receptor, Melanocortin, Type 4; D011994:Recombinant Proteins; D005998:Glycine