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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 ASEP 0364368 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide Author(s) Maletínská, Lenka (UOCHB-X) RID, ORCID
Špolcová, Andrea (UOCHB-X) RID, ORCID
Maixnerová, Jana (UOCHB-X)
Blechová, Miroslava (UOCHB-X)
Železná, Blanka (UOCHB-X) RID, ORCIDNumber of authors 5 Source Title Peptides. - : Elsevier - ISSN 0196-9781
Roč. 32, č. 9 (2011), s. 1887-1892Number of pages 6 s. Language eng - English Country US - United States Keywords pituitary cells ; PrRP analogs ; food intake Subject RIV CC - Organic Chemistry R&D Projects GAP303/10/1368 GA ČR - Czech Science Foundation (CSF) CEZ AV0Z40550506 - UOCHB-X (2005-2011) UT WOS 000295767400015 DOI 10.1016/j.peptides.2011.08.011 Annotation In 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. Workplace Institute of Organic Chemistry and Biochemistry Contact asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434 Year of Publishing 2012
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