The Melanocortin System: Structure Activity Relationships of Alpha-N-Methylated MT-II Analogues and Mutation Studies of Human Melanocortin Receptor Subtypes 1 and 4

Persistent Link:
http://hdl.handle.net/10150/193306
Title:
The Melanocortin System: Structure Activity Relationships of Alpha-N-Methylated MT-II Analogues and Mutation Studies of Human Melanocortin Receptor Subtypes 1 and 4
Author:
Dedek, Matthew Milan
Issue Date:
2007
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:
The melanocortin system regulates various physiological processes including feeding behavior, sexual function, skin pigmentation and photoprotection via five G-protein coupled receptors and several endogenous ligands. There is a need for selective and potent ligands to the human melanocortin receptors (hMCRs) that can chemically resolve these various functions. This thesis presents three studies aimed at refining the understanding of the structural differences between binding pockets of the hMCR subtypes. In the first study α-N-methylated analogues of the non-selective agonist, MT-II, are evaluated for their in vitro function. This study produced the most potent hMC1R selective agonist to date. The following two studies examine the effects of mutations on the biological activity of melanocortin receptor subtypes 1 and 4. Much of the mutation study data is preliminary and requires a demonstration of reproducibility.
Type:
text; Electronic Thesis
Keywords:
structure activity relationship; melanocortin 1 receptor; melanocortin; MT-II; mutagenesis; melanocortin 4 receptor
Degree Name:
MS
Degree Level:
masters
Degree Program:
Medical Pharmacology; Graduate College
Degree Grantor:
University of Arizona
Advisor:
Hruby, Victor J.
Committee Chair:
Hruby, Victor J.

Full metadata record

DC FieldValue Language
dc.language.isoENen_US
dc.titleThe Melanocortin System: Structure Activity Relationships of Alpha-N-Methylated MT-II Analogues and Mutation Studies of Human Melanocortin Receptor Subtypes 1 and 4en_US
dc.creatorDedek, Matthew Milanen_US
dc.contributor.authorDedek, Matthew Milanen_US
dc.date.issued2007en_US
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.abstractThe melanocortin system regulates various physiological processes including feeding behavior, sexual function, skin pigmentation and photoprotection via five G-protein coupled receptors and several endogenous ligands. There is a need for selective and potent ligands to the human melanocortin receptors (hMCRs) that can chemically resolve these various functions. This thesis presents three studies aimed at refining the understanding of the structural differences between binding pockets of the hMCR subtypes. In the first study α-N-methylated analogues of the non-selective agonist, MT-II, are evaluated for their in vitro function. This study produced the most potent hMC1R selective agonist to date. The following two studies examine the effects of mutations on the biological activity of melanocortin receptor subtypes 1 and 4. Much of the mutation study data is preliminary and requires a demonstration of reproducibility.en_US
dc.typetexten_US
dc.typeElectronic Thesisen_US
dc.subjectstructure activity relationshipen_US
dc.subjectmelanocortin 1 receptoren_US
dc.subjectmelanocortinen_US
dc.subjectMT-IIen_US
dc.subjectmutagenesisen_US
dc.subjectmelanocortin 4 receptoren_US
thesis.degree.nameMSen_US
thesis.degree.levelmastersen_US
thesis.degree.disciplineMedical Pharmacologyen_US
thesis.degree.disciplineGraduate Collegeen_US
thesis.degree.grantorUniversity of Arizonaen_US
dc.contributor.advisorHruby, Victor J.en_US
dc.contributor.chairHruby, Victor J.en_US
dc.contributor.committeememberChen, Qinen_US
dc.contributor.committeememberLai, Josephineen_US
dc.identifier.proquest2533en_US
dc.identifier.oclc659748470en_US
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