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      Prodrugs of Thyrotropin-Releasing Hormone and Related Peptides as Central Nervous System Agents

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          Abstract

          Prodrug design for brain delivery of small- and medium-sized neuropeptides was reviewed, focusing on thyrotropin-releasing hormone and structurally related peptides as examples. We have summarized our most important advances in methodology, as well as assessed the benefits and limitations of bioreversible chemical manipulation techniques to achieve targeting of the parent molecules into the central nervous system. The value of prodrug-amenable analogues as potential drug-like central nervous systems agents was highlighted.

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          Most cited references61

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          Depression: a new animal model sensitive to antidepressant treatments.

          R. PORSOLT, M. LE PICHON, M Jalfre (1977)
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            Dipeptidyl-peptidase IV from bench to bedside: an update on structural properties, functions, and clinical aspects of the enzyme DPP IV.

            Anne-Marie Lambeir, Christine Durinx, Simon Scharpé … (2003)
            Dipeptidyl-peptidase IV/CD26 (DPP IV) is a cell-surface protease belonging to the prolyloligopeptidase family. It selectively removes the N-terminal dipeptide from peptides with proline or alanine in the second position. Apart from its catalytic activity, it interacts with several proteins, for instance, adenosine deaminase, the HIV gp120 protein, fibronectin, collagen, the chemokine receptor CXCR4, and the tyrosine phosphatase CD45. DPP IV is expressed on a specific set of T lymphocytes, where it is up-regulated after activation. It is also expressed in a variety of tissues, primarily on endothelial and epithelial cells. A soluble form is present in plasma and other body fluids. DPP IV has been proposed as a diagnostic or prognostic marker for various tumors, hematological malignancies, immunological, inflammatory, psychoneuroendocrine disorders, and viral infections. DPP IV truncates many bioactive peptides of medical importance. It plays a role in glucose homeostasis through proteolytic inactivation of the incretins. DPP IV inhibitors improve glucose tolerance and pancreatic islet cell function in animal models of type 2 diabetes and in diabetic patients. The role of DPP IV/ CD26 within the immune system is a combination of its exopeptidase activity and its interactions with different molecules. This enables DPP IV/CD26 to serve as a co-stimulatory molecule to influence T cell activity and to modulate chemotaxis. DPP IV is also implicated in HIV-1 entry, malignant transformation, and tumor invasion.
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              Relationship of octanol/water partition coefficient and molecular weight to rat brain capillary permeability.

              Victor Levin (1980)
              The rat brain capillary permeability coefficient was determined for 27 compounds. The relationship of permeability to octanol/water partition coefficient and molecular weight was found to be predictable for drugs with molecular weights less than 400.
              Article 0 comments Cited 103 times – based on 0 reviews     Review now
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                Author and article information

                Journal
                Journal ID (nlm-ta): Molecules
                Journal ID (iso-abbrev): Molecules
                Journal ID (publisher-id): molecules
                Title: Molecules
                Publisher: Molecular Diversity Preservation International
                ISSN (Electronic): 1420-3049
                Publication date (Electronic): 06 February 2009
                Publication date Collection: February 2009
                Volume: 14
                Issue: 2
                Pages: 633-654
                Affiliations
                [1 ]Department of Pharmacology & Neuroscience, University of North Texas Health Science Center, Fort Worth, TX, USA
                [2 ]Department of Molecular Biology & Immunology, University of North Texas Health Science Center, Fort Worth, TX, USA; E-mail: lprokai@ 123456hsc.unt.edu (L.P.)
                Author notes
                [* ]Author to whom correspondence should be addressed; E-mail: kprokai@ 123456hsc.unt.edu ; Tel.: +1-817-735-0617; Fax: +1-817-735-2118.
                Article
                Publisher ID: molecules-14-00633
                DOI: 10.3390/molecules14020633
                PMC ID: 6253886
                PubMed ID: 19214153
                SO-VID: 6f97440d-6b69-490e-ba35-4774eef77133
                Copyright © © 2009 by the authors;
                License:

                licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license ( http://creativecommons.org/licenses/by/3.0/).

                History
                Date received : 01 January 2009
                Date revision received : 21 January 2009
                Date accepted : 05 February 2009
                Categories
                Subject: Review

                Keywords: neuropeptide,cns-delivery,trh,analogue,prodrug,prodrug-amenable analogue.
                Data availability:
                Keywords: neuropeptide, cns-delivery, trh, analogue, prodrug, prodrug-amenable analogue.

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