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",

}

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

UR - https://www.scopus.com/pages/publications/22544465245

UR - https://www.scopus.com/pages/publications/22544465245#tab=citedBy

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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