• Login
    View Item 
    •   Home
    • UA Faculty Research
    • UA Faculty Publications
    • View Item
    •   Home
    • UA Faculty Research
    • UA Faculty Publications
    • View Item
    JavaScript is disabled for your browser. Some features of this site may not work without it.

    Browse

    All of UA Campus RepositoryCommunitiesTitleAuthorsIssue DateSubmit DateSubjectsPublisherJournalThis CollectionTitleAuthorsIssue DateSubmit DateSubjectsPublisherJournal

    My Account

    LoginRegister

    About

    AboutUA Faculty PublicationsUA DissertationsUA Master's ThesesUA Honors ThesesUA PressUA YearbooksUA CatalogsUA Libraries

    Statistics

    Most Popular ItemsStatistics by CountryMost Popular Authors

    Cyclic Opioid Peptides.

    • CSV
    • RefMan
    • EndNote
    • BibTex
    • RefWorks
    Thumbnail
    Name:
    Lee YS text re-revision-final.pdf
    Size:
    625.7Kb
    Format:
    PDF
    Description:
    Final Accepted Manuscript
    Download
    Author
    Remesic, Michael
    Lee, Yeon Sun
    Hruby, Victor J
    Affiliation
    University of Arizona, Department of Chemistry and Biochemistry
    Issue Date
    2016
    Keywords
    review
    Opioid
    Cyclic peptides
    polycyclic
    opioid receptors
    analgesia
    central nervous system
    blood brain barrier penetration
    bioavailability
    
    Metadata
    Show full item record
    Publisher
    BENTHAM SCIENCE PUBL LTD
    Citation
    Cyclic Opioid Peptides. 2016, 23 (13):1288-303 Curr. Med. Chem.
    Journal
    Current medicinal chemistry
    Rights
    Copyright © 2016, Eureka Science Ltd.
    Collection Information
    This item from the UA Faculty Publications collection is made available by the University of Arizona with support from the University of Arizona Libraries. If you have questions, please contact us at repository@u.library.arizona.edu.
    Abstract
    For decades the opioid receptors have been an attractive therapeutic target for the treatment of pain. Since the first discovery of enkephalin, approximately a dozen endogenous opioid peptides have been known to produce opioid activity and analgesia, but their therapeutics have been limited mainly due to low blood brain barrier penetration and poor resistance to proteolytic degradation. One versatile approach to overcome these drawbacks is the cyclization of linear peptides to cyclic peptides with constrained topographical structure. Compared to their linear parents, cyclic analogs exhibit better metabolic stability, lower offtarget toxicity, and improved bioavailability. Extensive structure-activity relationship studies have uncovered promising compounds for the treatment of pain as well as further elucidate structural elements required for selective opioid receptor activity. The benefits that come with employing cyclization can be further enhanced through the generation of polycyclic derivatives. Opioid ligands generally have a short peptide chain and thus the realm of polycyclic peptides has yet to be explored. In this review, a brief history of designing ligands for the opioid receptors, including classic linear and cyclic ligands, is discussed along with recent approaches and successes of cyclic peptide ligands for the receptors. Various scaffolds and approaches to improve bioavailability are elaborated and concluded with a discourse towards polycyclic peptides.
    Note
    12 month embargo. Published 1 April 2016.
    ISSN
    1875-533X
    PubMed ID
    27117332
    DOI
    10.2174/0929867323666160427123005
    Version
    Final accepted manuscript
    ae974a485f413a2113503eed53cd6c53
    10.2174/0929867323666160427123005
    Scopus Count
    Collections
    UA Faculty Publications

    entitlement

    Related articles

    • Cyclization in opioid peptides.
    • Authors: Piekielna J, Perlikowska R, Gach K, Janecka A
    • Issue date: 2013 Jun
    • Development of opioid peptide analogs for pain relief.
    • Authors: Janecka A, Perlikowska R, Gach K, Wyrebska A, Fichna J
    • Issue date: 2010
    • Cyclic mu-opioid receptor ligands containing multiple N-methylated amino acid residues.
    • Authors: Adamska-Bartłomiejczyk A, Janecka A, Szabó MR, Cerlesi MC, Calo G, Kluczyk A, Tömböly C, Borics A
    • Issue date: 2017 Apr 15
    • New trends in the development of opioid peptide analogues as advanced remedies for pain relief.
    • Authors: Gentilucci L
    • Issue date: 2004
    • Nociceptin/orphanin FQ and the opioid receptor-like ORL1 receptor.
    • Authors: Meunier JC
    • Issue date: 1997 Dec 4
    The University of Arizona Libraries | 1510 E. University Blvd. | Tucson, AZ 85721-0055
    Tel 520-621-6442 | repository@u.library.arizona.edu
    DSpace software copyright © 2002-2017  DuraSpace
    Quick Guide | Contact Us | Send Feedback
    Open Repository is a service operated by 
    Atmire NV
     

    Export search results

    The export option will allow you to export the current search results of the entered query to a file. Different formats are available for download. To export the items, click on the button corresponding with the preferred download format.

    By default, clicking on the export buttons will result in a download of the allowed maximum amount of items.

    To select a subset of the search results, click "Selective Export" button and make a selection of the items you want to export. The amount of items that can be exported at once is similarly restricted as the full export.

    After making a selection, click one of the export format buttons. The amount of items that will be exported is indicated in the bubble next to export format.