Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors

Minying Cai; Alexander V. Mayorov; Jinfa Ying; Magda Stankova; Dev Trivedi; Chris Cabello; Victor J. Hruby

doi:10.1016/j.peptides.2005.03.020

Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors

Minying Cai, Alexander V. Mayorov, Jinfa Ying, Magda Stankova, Dev Trivedi, Chris Cabello, Victor J. Hruby

Research output: Contribution to journal › Article › peer-review

32 Scopus citations

Abstract

α-MSH and γ-MSH are the natural endogenous hormones for the human melanocortin-1, 3, 4 and 5 receptors (hMC1R, hMC3R, hMC4R and hMC5R). These and more potent, stable and prolonged acting analogues such as NDP-α-MSH, MT-II and SHU-9119 are not very receptor selective. To develop potent and selective agonist and antagonist ligands for the melanocortin receptors we have used state-of-the-art biophysical studies, computational chemistry, and design of conformational and topographical constraints with novel templates.

Original language	English (US)
Pages (from-to)	1481-1485
Number of pages	5
Journal	Peptides
Volume	26
Issue number	8
DOIs	https://doi.org/10.1016/j.peptides.2005.03.020
State	Published - Aug 2005

Keywords

Conformation constraints
Cyclic melanotropins
Melanocortin receptor pharmacophores
Melanocortin receptors
Melanotropins
Receptor selective melanotropin agonists
Receptor selective melanotropin antagonists
Structure-biological activity relationships

ASJC Scopus subject areas

Biochemistry
Physiology
Endocrinology
Cellular and Molecular Neuroscience

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10.1016/j.peptides.2005.03.020

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@article{a8aeeadf5c104c92b252d69d25a7950c,

title = "Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors",

abstract = "α-MSH and γ-MSH are the natural endogenous hormones for the human melanocortin-1, 3, 4 and 5 receptors (hMC1R, hMC3R, hMC4R and hMC5R). These and more potent, stable and prolonged acting analogues such as NDP-α-MSH, MT-II and SHU-9119 are not very receptor selective. To develop potent and selective agonist and antagonist ligands for the melanocortin receptors we have used state-of-the-art biophysical studies, computational chemistry, and design of conformational and topographical constraints with novel templates.",

keywords = "Conformation constraints, Cyclic melanotropins, Melanocortin receptor pharmacophores, Melanocortin receptors, Melanotropins, Receptor selective melanotropin agonists, Receptor selective melanotropin antagonists, Structure-biological activity relationships",

author = "Minying Cai and Mayorov, {Alexander V.} and Jinfa Ying and Magda Stankova and Dev Trivedi and Chris Cabello and Hruby, {Victor J.}",

note = "Funding Information: We gratefully acknowledge the support of the U.S. Public Health Service, Grant Numbers DK 17420, DA 06284 and DA 13449 which made this work possible.",

year = "2005",

month = aug,

doi = "10.1016/j.peptides.2005.03.020",

language = "English (US)",

volume = "26",

pages = "1481--1485",

journal = "Peptides",

issn = "0196-9781",

publisher = "Elsevier Inc.",

number = "8",

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TY - JOUR

T1 - Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors

AU - Cai, Minying

AU - Mayorov, Alexander V.

AU - Ying, Jinfa

AU - Stankova, Magda

AU - Trivedi, Dev

AU - Cabello, Chris

AU - Hruby, Victor J.

N1 - Funding Information: We gratefully acknowledge the support of the U.S. Public Health Service, Grant Numbers DK 17420, DA 06284 and DA 13449 which made this work possible.

PY - 2005/8

Y1 - 2005/8

N2 - α-MSH and γ-MSH are the natural endogenous hormones for the human melanocortin-1, 3, 4 and 5 receptors (hMC1R, hMC3R, hMC4R and hMC5R). These and more potent, stable and prolonged acting analogues such as NDP-α-MSH, MT-II and SHU-9119 are not very receptor selective. To develop potent and selective agonist and antagonist ligands for the melanocortin receptors we have used state-of-the-art biophysical studies, computational chemistry, and design of conformational and topographical constraints with novel templates.

AB - α-MSH and γ-MSH are the natural endogenous hormones for the human melanocortin-1, 3, 4 and 5 receptors (hMC1R, hMC3R, hMC4R and hMC5R). These and more potent, stable and prolonged acting analogues such as NDP-α-MSH, MT-II and SHU-9119 are not very receptor selective. To develop potent and selective agonist and antagonist ligands for the melanocortin receptors we have used state-of-the-art biophysical studies, computational chemistry, and design of conformational and topographical constraints with novel templates.

KW - Conformation constraints

KW - Cyclic melanotropins

KW - Melanocortin receptor pharmacophores

KW - Melanocortin receptors

KW - Melanotropins

KW - Receptor selective melanotropin agonists

KW - Receptor selective melanotropin antagonists

KW - Structure-biological activity relationships

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U2 - 10.1016/j.peptides.2005.03.020

DO - 10.1016/j.peptides.2005.03.020

M3 - Article

C2 - 15876475

AN - SCOPUS:22544465245

SN - 0196-9781

VL - 26

SP - 1481

EP - 1485

JO - Peptides

JF - Peptides

IS - 8

ER -

Design of novel melanotropin agonists and antagonists with high potency and selectivity for human melanocortin receptors

Abstract

Keywords

ASJC Scopus subject areas

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