TY - JOUR
T1 - Design of novel melanocortin receptor ligands
T2 - Multiple receptors, complex pharmacology, the challenge
AU - Hruby, Victor J.
AU - Cai, Minying
AU - Cain, James
AU - Nyberg, Joel
AU - Trivedi, Dev
N1 - Funding Information:
We are particularly grateful to the many outstanding collaborators and colleagues who have made this research possible. Their names appear in the publications referenced here and in many other critical publications. The research was supported in part by grants from the U.S. Public Health Service . We thank Margie Colie for her help with the manuscript.
PY - 2011/6/11
Y1 - 2011/6/11
N2 - The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.
AB - The major pharmacophore for the melanocortin 1, 3, 4 and 5 receptors is the sequence -His-Phe-Arg-Trp-. There is a need for potent, biologically stable, receptor selective ligands, both agonists and antagonists, for these receptors. In this report we briefly examine the structural and biophysical approaches we have taken to develop selective agonist and antagonist ligands that can cross (or not) the blood brain barrier. Remaining questions and unmet needs are also discussed.
KW - Agonists and antagonists for MCR
KW - Melanocortin receptor ligand SAR
KW - Melanocortin receptor selective ligand
KW - Orthosteric and allosteric ligand
KW - Selective ligand for MCR
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U2 - 10.1016/j.ejphar.2010.10.109
DO - 10.1016/j.ejphar.2010.10.109
M3 - Review article
C2 - 21208601
AN - SCOPUS:79955941240
SN - 0014-2999
VL - 660
SP - 88
EP - 93
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
IS - 1
ER -