New highly specific agonistic peptides for human melanocortin MC1 receptor

Michael Szardenings; Ruta Muceniece; Ilze Mutule; Felikss Mutulis; Jarl E.S. Wikberg

doi:10.1016/S0196-9781(99)00207-7

New highly specific agonistic peptides for human melanocortin MC₁ receptor

Michael Szardenings
, Ruta Muceniece
, Ilze Mutule
, Felikss Mutulis
, Jarl E.S. Wikberg^*

^*Corresponding author for this work

Uppsala University
Melacure Therapeutics AB

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

45 Citations (Scopus)

Abstract

A peptide with very high specificity for the human melanocortin MC₁ receptor identified by phage display was used as a lead for the design of new peptides. Two new peptides, MS05 and MS09, were synthesized and found to bind with sub-nanomolar affinities to the MC₁ receptor. Both these peptides showed strong agonistic activity at the MC₁ receptor. The MS05 was the most MC₁ receptor selective as it showed virtually no binding affinity for the MC₄ and MC₅ receptors and only micromolar affinity for the MC₃ receptor. The selectivity and potency of the new peptides make them potent tools for studies of MC₁ receptors, as well as novel potential candidate drugs for the treatment of inflammatory conditions. Copyright (C) 2000 Elsevier Science Inc.

Original language	English
Pages (from-to)	239-243
Number of pages	5
Journal	Peptides
Volume	21
Issue number	2
DOIs	https://doi.org/10.1016/S0196-9781(99)00207-7
Publication status	Published - Feb 2000
Externally published	Yes

UN SDGs

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

SDG 3 Good Health and Well-being

Keywords

Melanocortin receptors
Melanocyte stimulating hormone
Receptor selective peptides

Access to Document

10.1016/S0196-9781(99)00207-7

Cite this

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title = "New highly specific agonistic peptides for human melanocortin MC1 receptor",

abstract = "A peptide with very high specificity for the human melanocortin MC1 receptor identified by phage display was used as a lead for the design of new peptides. Two new peptides, MS05 and MS09, were synthesized and found to bind with sub-nanomolar affinities to the MC1 receptor. Both these peptides showed strong agonistic activity at the MC1 receptor. The MS05 was the most MC1 receptor selective as it showed virtually no binding affinity for the MC4 and MC5 receptors and only micromolar affinity for the MC3 receptor. The selectivity and potency of the new peptides make them potent tools for studies of MC1 receptors, as well as novel potential candidate drugs for the treatment of inflammatory conditions. Copyright (C) 2000 Elsevier Science Inc.",

keywords = "Melanocortin receptors, Melanocyte stimulating hormone, Receptor selective peptides",

author = "Michael Szardenings and Ruta Muceniece and Ilze Mutule and Felikss Mutulis and Wikberg, \{Jarl E.S.\}",

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language = "English",

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T1 - New highly specific agonistic peptides for human melanocortin MC1 receptor

AU - Szardenings, Michael

AU - Muceniece, Ruta

AU - Mutule, Ilze

AU - Mutulis, Felikss

AU - Wikberg, Jarl E.S.

PY - 2000/2

Y1 - 2000/2

N2 - A peptide with very high specificity for the human melanocortin MC1 receptor identified by phage display was used as a lead for the design of new peptides. Two new peptides, MS05 and MS09, were synthesized and found to bind with sub-nanomolar affinities to the MC1 receptor. Both these peptides showed strong agonistic activity at the MC1 receptor. The MS05 was the most MC1 receptor selective as it showed virtually no binding affinity for the MC4 and MC5 receptors and only micromolar affinity for the MC3 receptor. The selectivity and potency of the new peptides make them potent tools for studies of MC1 receptors, as well as novel potential candidate drugs for the treatment of inflammatory conditions. Copyright (C) 2000 Elsevier Science Inc.

AB - A peptide with very high specificity for the human melanocortin MC1 receptor identified by phage display was used as a lead for the design of new peptides. Two new peptides, MS05 and MS09, were synthesized and found to bind with sub-nanomolar affinities to the MC1 receptor. Both these peptides showed strong agonistic activity at the MC1 receptor. The MS05 was the most MC1 receptor selective as it showed virtually no binding affinity for the MC4 and MC5 receptors and only micromolar affinity for the MC3 receptor. The selectivity and potency of the new peptides make them potent tools for studies of MC1 receptors, as well as novel potential candidate drugs for the treatment of inflammatory conditions. Copyright (C) 2000 Elsevier Science Inc.

KW - Melanocortin receptors

KW - Melanocyte stimulating hormone

KW - Receptor selective peptides

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DO - 10.1016/S0196-9781(99)00207-7

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