TY - JOUR
T1 - Design and bioactivities of melanotropic peptide agonists and antagonists
T2 - Design based on a conformationally constrained somatostatin template
AU - Hruby, Victor J.
AU - Han, Guoxia
AU - Hadley, Mac E.
PY - 1998
Y1 - 1998
N2 - α-Melanotropin and ACTH, POMC peptides, initiate biological activity by interaction with the classical pigment cell (α-MSH receptor, MC1R) and adrenal gland (ACTH receptor, MC2R) melanocortin receptors, respectively. The recently discovered MC3R, MC4R and MC5R receptors provide new targets and new biological functions for POMC peptides. We have developed conformationally constrained α-melanotropin peptides that interact with all of these receptors as agonists and antagonists and are examining new approaches to obtain highly selective ligands for each of these melanocortin receptors. Previously, we had converted somatostatin-derived peptides into potent and highly selective analogues that act as antagonists at the μ opioid receptors. Using the reverse turn template that came out of these studies, we have designed, de novo, agonist and antagonist peptide analogues that interact with melanocortin receptors.
AB - α-Melanotropin and ACTH, POMC peptides, initiate biological activity by interaction with the classical pigment cell (α-MSH receptor, MC1R) and adrenal gland (ACTH receptor, MC2R) melanocortin receptors, respectively. The recently discovered MC3R, MC4R and MC5R receptors provide new targets and new biological functions for POMC peptides. We have developed conformationally constrained α-melanotropin peptides that interact with all of these receptors as agonists and antagonists and are examining new approaches to obtain highly selective ligands for each of these melanocortin receptors. Previously, we had converted somatostatin-derived peptides into potent and highly selective analogues that act as antagonists at the μ opioid receptors. Using the reverse turn template that came out of these studies, we have designed, de novo, agonist and antagonist peptide analogues that interact with melanocortin receptors.
KW - Agonists
KW - Antagonists
KW - De novo design
KW - Melanocortin receptors
KW - Melanotropins
KW - Opioids
KW - Somatostatin template
UR - http://www.scopus.com/inward/record.url?scp=0001659318&partnerID=8YFLogxK
U2 - 10.1007/BF02443451
DO - 10.1007/BF02443451
M3 - Article
AN - SCOPUS:0001659318
SN - 0929-5666
VL - 5
SP - 117
EP - 120
JO - Letters in Peptide Science
JF - Letters in Peptide Science
IS - 2-3
ER -