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

0364368 - ÚOCHB 2012 RIV US eng J - Journal Article
Maletínská, Lenka - Špolcová, Andrea - Maixnerová, Jana - Blechová, Miroslava - Železná, Blanka
Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide.
Peptides. Roč. 32, č. 9 (2011), s. 1887-1892. ISSN 0196-9781. E-ISSN 1873-5169
R&D Projects: GA ČR GAP303/10/1368
Institutional research plan: CEZ:AV0Z40550506
Keywords : pituitary cells * PrRP analogs * food intake
Subject RIV: CC - Organic Chemistry
Impact factor: 2.434, year: 2011

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.
Permanent Link: http://hdl.handle.net/11104/0199867