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

Persistent Link:
http://hdl.handle.net/10150/244784
Title:
Design, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptor
Author:
Soto, Robert Joseph
Issue Date:
May-2012
Publisher:
The University of Arizona.
Rights:
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.
Abstract:
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.
Type:
text; Electronic Thesis
Degree Name:
B.S.
Degree Level:
bachelors
Degree Program:
Honors College; Chemistry
Degree Grantor:
University of Arizona

Full metadata record

DC FieldValue Language
dc.language.isoenen_US
dc.titleDesign, Synthesis, and Biological Evaluation of Novel Chimeric and Cyclic Peptide Ligands Targeting the Human Melanocortin-3 Receptoren_US
dc.creatorSoto, Robert Josephen_US
dc.contributor.authorSoto, Robert Josephen_US
dc.date.issued2012-05-
dc.publisherThe University of Arizona.en_US
dc.rightsCopyright © 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.en_US
dc.description.abstractIn 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.en_US
dc.typetexten_US
dc.typeElectronic Thesisen_US
thesis.degree.nameB.S.en_US
thesis.degree.levelbachelorsen_US
thesis.degree.disciplineHonors Collegeen_US
thesis.degree.disciplineChemistryen_US
thesis.degree.grantorUniversity of Arizonaen_US
All Items in UA Campus Repository are protected by copyright, with all rights reserved, unless otherwise indicated.