Synthesis of Novel Biologically Active Peptide Analogues that are Agonists at Opioid Receptors and Antagonists at Cholecystokinin Receptors

Persistent Link:
http://hdl.handle.net/10150/193314
Title:
Synthesis of Novel Biologically Active Peptide Analogues that are Agonists at Opioid Receptors and Antagonists at Cholecystokinin Receptors
Author:
Wooden, Ekaphol
Issue Date:
2005
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:
We know that many disease states lead to changes in expressed proteins. Therefore, drug design and discovery based on normal states and single targets often is inadequate. The "system changes" that occurs must be considered in any treatment for the disease, clearly evident in neuropathic pain where opioids can actually heighten pain. To effectively treat diseases involving "systems changes" a new paradigm was recently introduced. In this new approach single peptide molecules are designed to interact with multiple receptor targets. For the treatment of pain, a series of linear and cyclic peptides were designed based on the overlapping pharmacophores of opioid and CCK ligands. The opioid/CCK analogues were synthesized and evaluated for their biological activities. Several analogues were found to simultaneously interact with opioid receptors as agonists and CCK receptors as antagonists. This study further modifies the RSA analogues to improve on the bioassays of the previous peptides.
Type:
text; Electronic Thesis
Keywords:
Chemistry
Degree Name:
MS
Degree Level:
masters
Degree Program:
Chemistry; Graduate College
Degree Grantor:
University of Arizona
Committee Chair:
Hruby, Victor J.

Full metadata record

DC FieldValue Language
dc.language.isoENen_US
dc.titleSynthesis of Novel Biologically Active Peptide Analogues that are Agonists at Opioid Receptors and Antagonists at Cholecystokinin Receptorsen_US
dc.creatorWooden, Ekapholen_US
dc.contributor.authorWooden, Ekapholen_US
dc.date.issued2005en_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.abstractWe know that many disease states lead to changes in expressed proteins. Therefore, drug design and discovery based on normal states and single targets often is inadequate. The "system changes" that occurs must be considered in any treatment for the disease, clearly evident in neuropathic pain where opioids can actually heighten pain. To effectively treat diseases involving "systems changes" a new paradigm was recently introduced. In this new approach single peptide molecules are designed to interact with multiple receptor targets. For the treatment of pain, a series of linear and cyclic peptides were designed based on the overlapping pharmacophores of opioid and CCK ligands. The opioid/CCK analogues were synthesized and evaluated for their biological activities. Several analogues were found to simultaneously interact with opioid receptors as agonists and CCK receptors as antagonists. This study further modifies the RSA analogues to improve on the bioassays of the previous peptides.en_US
dc.typetexten_US
dc.typeElectronic Thesisen_US
dc.subjectChemistryen_US
thesis.degree.nameMSen_US
thesis.degree.levelmastersen_US
thesis.degree.disciplineChemistryen_US
thesis.degree.disciplineGraduate Collegeen_US
thesis.degree.grantorUniversity of Arizonaen_US
dc.contributor.chairHruby, Victor J.en_US
dc.identifier.proquest1282en_US
dc.identifier.oclc137354798en_US
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