About: Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide     Goto   Sponge   NotDistinct   Permalink

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  • 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.
  • 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. (en)
Title
  • Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide
  • Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide (en)
skos:prefLabel
  • Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide
  • Biological properties of prolactin-releasing peptide analogs with a modified aromatic ring of a C-terminal phenylalanine amide (en)
skos:notation
  • RIV/61388963:_____/11:00364368!RIV12-AV0-61388963
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • P(GAP303/10/1368), Z(AV0Z40550506)
http://linked.open...iv/cisloPeriodika
  • 9
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 188324
http://linked.open...ai/riv/idVysledku
  • RIV/61388963:_____/11:00364368
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • pituitary cells; PrRP analogs; food intake (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • US - Spojené státy americké
http://linked.open...ontrolniKodProRIV
  • [367B6D80B735]
http://linked.open...i/riv/nazevZdroje
  • Peptides
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...vavai/riv/projekt
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 32
http://linked.open...iv/tvurceVysledku
  • Blechová, Miroslava
  • Maixnerová, Jana
  • Maletínská, Lenka
  • Špolcová, Andrea
  • Železná, Blanka
http://linked.open...ain/vavai/riv/wos
  • 000295767400015
http://linked.open...n/vavai/riv/zamer
issn
  • 0196-9781
number of pages
http://bibframe.org/vocab/doi
  • 10.1016/j.peptides.2011.08.011
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