TY - JOUR
T1 - Melanocortin Ligands
T2 - 30 Years of Structure-Activity Relationship (SAR) Studies
AU - Holder, Jerry Ryan
AU - Haskell-Luevano, Carrie
N1 - Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.
PY - 2004/5
Y1 - 2004/5
N2 - The challenge of peptide and peptidomimetic research is the development of methods and techniques to improve the biological properties of native peptides and to convert peptide ligands into non-peptide compounds. Improved biological properties of peptides includes enhancement of stability, potency, and receptor selectivity, for both in vivo and in vitro applications. The design of a ligand with specific activity and desired biological properties is a complex task, and, to accomplish this objective, knowledge about putative interactions between a ligand and the corresponding receptor will be valuable. This includes interactions for both the binding and signal transduction processes. Structure-activity relationship (SAR) studies involve systematic modification of a lead peptide and are designed to provide insight into potential interactions involved in the formation of the ligand-receptor complex. It is desirable to have knowledge about both favorable and unfavorable processes that may occur in putative ligand-receptor interactions that result in either receptor stimulation or inhibition. Herein, we discuss various SAR studies that have involved melanocortin peptides over three decades and the information these studies have provided to the melanocortin field.
AB - The challenge of peptide and peptidomimetic research is the development of methods and techniques to improve the biological properties of native peptides and to convert peptide ligands into non-peptide compounds. Improved biological properties of peptides includes enhancement of stability, potency, and receptor selectivity, for both in vivo and in vitro applications. The design of a ligand with specific activity and desired biological properties is a complex task, and, to accomplish this objective, knowledge about putative interactions between a ligand and the corresponding receptor will be valuable. This includes interactions for both the binding and signal transduction processes. Structure-activity relationship (SAR) studies involve systematic modification of a lead peptide and are designed to provide insight into potential interactions involved in the formation of the ligand-receptor complex. It is desirable to have knowledge about both favorable and unfavorable processes that may occur in putative ligand-receptor interactions that result in either receptor stimulation or inhibition. Herein, we discuss various SAR studies that have involved melanocortin peptides over three decades and the information these studies have provided to the melanocortin field.
KW - G-protein coupled receptors
KW - Melanocortin receptors
KW - Melanotropin
KW - Obesity
KW - Peptidomimetic
KW - Structure-activity relationship
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U2 - 10.1002/med.10064
DO - 10.1002/med.10064
M3 - Review article
C2 - 14994367
AN - SCOPUS:1842841995
SN - 0198-6325
VL - 24
SP - 325
EP - 356
JO - Medicinal Research Reviews
JF - Medicinal Research Reviews
IS - 3
ER -