Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor

Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor

In an effort to develop potent and selective agonists and antagonists for the human melanocortin-3 receptor, several new peptide design approaches were employed. This includes peptides featuring a chimeric fusion of the alpha-MSH and AgRP critical pharmacophores, as well as a variety of cyclic ligan...

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Main Author: Soto, Robert Joseph
Language:en
Published: The University of Arizona. 2012
Online Access:http://hdl.handle.net/10150/244784
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spelling ndltd-arizona.edu-oai-arizona.openrepository.com-10150-2447842015-10-23T04:57:18Z Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor Soto, Robert Joseph In an effort to develop potent and selective agonists and antagonists for the human melanocortin-3 receptor, several new peptide design approaches were employed. This includes peptides featuring a chimeric fusion of the alpha-MSH and AgRP critical pharmacophores, as well as a variety of cyclic ligands which incorporated a variety of amino acid substitutions and dicarboxylic acid linkers for the construction of lactam bridges. Not only were potent and selective hMC3R superagonists obtained through this study (SRJ-(17-18)S), but several hMC1R (SRJ-(20-31)S) and hMC5R (SRJ-(02-03)L) selective peptides were also found. The active peptides identified in this study not only provide a basis for the rational design of melanocortin receptor ligands in the future, but show promise in therapeutic applications. 2012-05 text Electronic Thesis http://hdl.handle.net/10150/244784 en Copyright © is held by the author. Digital access to this material is made possible by the University Libraries, University of Arizona. Further transmission, reproduction or presentation (such as public display or performance) of protected items is prohibited except with permission of the author. The University of Arizona.
collection NDLTD
language en
sources NDLTD
description In an effort to develop potent and selective agonists and antagonists for the human melanocortin-3 receptor, several new peptide design approaches were employed. This includes peptides featuring a chimeric fusion of the alpha-MSH and AgRP critical pharmacophores, as well as a variety of cyclic ligands which incorporated a variety of amino acid substitutions and dicarboxylic acid linkers for the construction of lactam bridges. Not only were potent and selective hMC3R superagonists obtained through this study (SRJ-(17-18)S), but several hMC1R (SRJ-(20-31)S) and hMC5R (SRJ-(02-03)L) selective peptides were also found. The active peptides identified in this study not only provide a basis for the rational design of melanocortin receptor ligands in the future, but show promise in therapeutic applications.
author Soto, Robert Joseph
spellingShingle Soto, Robert Joseph
Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor
author_facet Soto, Robert Joseph
author_sort Soto, Robert Joseph
title Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor
title_short Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor
title_full Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor
title_fullStr Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor
title_full_unstemmed Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor
title_sort design, synthesis, and biological evaluation of novel chimeric and cyclic peptide ligands targeting the human melanocortin-3 receptor
publisher The University of Arizona.
publishDate 2012
url http://hdl.handle.net/10150/244784
work_keys_str_mv AT sotorobertjoseph designsynthesisandbiologicalevaluationofnovelchimericandcyclicpeptideligandstargetingthehumanmelanocortin3receptor
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