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Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide

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    SYSNO ASEP0364368
    Document TypeJ - Journal Article
    R&D Document TypeJournal Article
    Subsidiary JČlánek ve WOS
    TitleBiological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide
    Author(s) Maletínská, Lenka (UOCHB-X) RID
    Špolcová, Andrea (UOCHB-X) RID
    Maixnerová, Jana (UOCHB-X)
    Blechová, Miroslava (UOCHB-X)
    Železná, Blanka (UOCHB-X) RID
    Number of authors5
    Source TitlePeptides. - : Elsevier - ISSN 0196-9781
    Roč. 32, č. 9 (2011), s. 1887-1892
    Number of pages6 s.
    Languageeng - English
    CountryUS - United States
    Keywordspituitary cells ; PrRP analogs ; food intake
    Subject RIVCC - Organic Chemistry
    R&D ProjectsGAP303/10/1368 GA ČR - Czech Science Foundation (CSF)
    CEZAV0Z40550506 - UOCHB-X (2005-2011)
    UT WOS000295767400015
    DOI10.1016/j.peptides.2011.08.011
    AnnotationIn the present study, eight analogs of PrRP20 with C-terminal Phe amide modified with a bulky side chain or a halogenated aromatic ring revealed high binding potency, activation of mitogen-activated protein kinase/extracellular-regulated kinase (MAPK/ERK1/2) and cAMP response element-binding protein (CREB) and prolactin release in RC-4B/C cells. In particular, [PheNO231]PrRP20, [1-Nal31]PrRP20, [2-Nal31]PrRP20 and [Tyr31]PrRP20 showed not only in vitro effects comparable or higher than those of PrRP20, but also a very significant and long-lasting anorexigenic effect after central administration in fasted mice. The design of potent and long-lasting PrRP analogs with selective anorexigenic properties promise to contribute to the study of food intake disorders.
    WorkplaceInstitute of Organic Chemistry and Biochemistry
    ContactJana Procházková, janap@uochb.cas.cz, Tel.: 220 183 418 ; Viktorie Chládková, viktorie.chladkova@uochb.cas.cz, Tel.: 232 002 434
    Year of Publishing2012