The agouti-related protein decapeptide (Yc[CRFFNAFC]Y) possesses agonist activity at the murine melanocortin-1 receptor

Carrie Haskell-Luevano; Eileen K. Monck; Y. P. Wan; Anzeela M. Schentrup

doi:10.1016/S0196-9781(00)00194-7

The agouti-related protein decapeptide (Yc[CRFFNAFC]Y) possesses agonist activity at the murine melanocortin-1 receptor

Carrie Haskell-Luevano, Eileen K. Monck, Y. P. Wan, Anzeela M. Schentrup

Medicinal Chemistry

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

27 Scopus citations

Abstract

Agouti-related protein (AGRP) is a naturally occurring antagonist of the brain melanocortin receptors (MC3R and MC4R) and is physiologically implicated as participating in feeding behavior and energy homeostasis. The human AGRP decapeptide Yc[CRFFNAFC]Y has been previously reported as binding to the human MC3 and MC4 receptors and antagonizing the MC4 receptor. We have synthesized this decapeptide and pharmacologically characterized it at the murine melanocortin receptors and found it to possess MC4R antagonist activity (pA₂ = 6.8) and, unexpectedly, MC1R agonist activity (EC₅₀ = 2.89 μM). This study characterizes the first AGRP-based peptide agonist at the melanocortin receptors. Copyright (C) 2000 Elsevier Science Inc.

Original language	English (US)
Pages (from-to)	683-689
Number of pages	7
Journal	Peptides
Volume	21
Issue number	5
DOIs	https://doi.org/10.1016/S0196-9781(00)00194-7
State	Published - May 2000

Bibliographical note

Funding Information:
This work has been funded by the Howard Hughes Medical Institute Research Resources Program, University of Florida. C.H.-L. is a recipient of a Burroughs Wellcome fund Career Award in the Biomedical Sciences.

Keywords

Agouti-related protein
MC1R
MC4R
Melanocortin
Melanotropin
Obesity
α-Melanocyte stimulating hormone

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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title = "The agouti-related protein decapeptide (Yc[CRFFNAFC]Y) possesses agonist activity at the murine melanocortin-1 receptor",

abstract = "Agouti-related protein (AGRP) is a naturally occurring antagonist of the brain melanocortin receptors (MC3R and MC4R) and is physiologically implicated as participating in feeding behavior and energy homeostasis. The human AGRP decapeptide Yc[CRFFNAFC]Y has been previously reported as binding to the human MC3 and MC4 receptors and antagonizing the MC4 receptor. We have synthesized this decapeptide and pharmacologically characterized it at the murine melanocortin receptors and found it to possess MC4R antagonist activity (pA2 = 6.8) and, unexpectedly, MC1R agonist activity (EC50 = 2.89 μM). This study characterizes the first AGRP-based peptide agonist at the melanocortin receptors. Copyright (C) 2000 Elsevier Science Inc.",

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author = "Carrie Haskell-Luevano and Monck, {Eileen K.} and Wan, {Y. P.} and Schentrup, {Anzeela M.}",

note = "Funding Information: This work has been funded by the Howard Hughes Medical Institute Research Resources Program, University of Florida. C.H.-L. is a recipient of a Burroughs Wellcome fund Career Award in the Biomedical Sciences. ",

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AU - Haskell-Luevano, Carrie

AU - Monck, Eileen K.

AU - Wan, Y. P.

AU - Schentrup, Anzeela M.

N1 - Funding Information: This work has been funded by the Howard Hughes Medical Institute Research Resources Program, University of Florida. C.H.-L. is a recipient of a Burroughs Wellcome fund Career Award in the Biomedical Sciences.

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N2 - Agouti-related protein (AGRP) is a naturally occurring antagonist of the brain melanocortin receptors (MC3R and MC4R) and is physiologically implicated as participating in feeding behavior and energy homeostasis. The human AGRP decapeptide Yc[CRFFNAFC]Y has been previously reported as binding to the human MC3 and MC4 receptors and antagonizing the MC4 receptor. We have synthesized this decapeptide and pharmacologically characterized it at the murine melanocortin receptors and found it to possess MC4R antagonist activity (pA2 = 6.8) and, unexpectedly, MC1R agonist activity (EC50 = 2.89 μM). This study characterizes the first AGRP-based peptide agonist at the melanocortin receptors. Copyright (C) 2000 Elsevier Science Inc.

AB - Agouti-related protein (AGRP) is a naturally occurring antagonist of the brain melanocortin receptors (MC3R and MC4R) and is physiologically implicated as participating in feeding behavior and energy homeostasis. The human AGRP decapeptide Yc[CRFFNAFC]Y has been previously reported as binding to the human MC3 and MC4 receptors and antagonizing the MC4 receptor. We have synthesized this decapeptide and pharmacologically characterized it at the murine melanocortin receptors and found it to possess MC4R antagonist activity (pA2 = 6.8) and, unexpectedly, MC1R agonist activity (EC50 = 2.89 μM). This study characterizes the first AGRP-based peptide agonist at the melanocortin receptors. Copyright (C) 2000 Elsevier Science Inc.

KW - Agouti-related protein

KW - MC1R

KW - MC4R

KW - Melanocortin

KW - Melanotropin

KW - Obesity

KW - α-Melanocyte stimulating hormone

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ER -

The agouti-related protein decapeptide (Yc[CRFFNAFC]Y) possesses agonist activity at the murine melanocortin-1 receptor

Abstract

Bibliographical note

Keywords

UN SDGs

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