Počet záznamů: 1  

Palmitoylation of Prolactin-Releasing Peptide Increased Affinity for and Activation of the GPR10, NPFF-R2 and NPFF-R1 Receptors: In Vitro Study

  1. 1.
    SYSNO ASEP0545497
    Druh ASEPJ - Článek v odborném periodiku
    Zařazení RIVJ - Článek v odborném periodiku
    Poddruh JČlánek ve WOS
    NázevPalmitoylation of Prolactin-Releasing Peptide Increased Affinity for and Activation of the GPR10, NPFF-R2 and NPFF-R1 Receptors: In Vitro Study
    Tvůrce(i) Karnošová, A. (CZ)
    Strnadová, V. (CZ)
    Holá, L. (CZ)
    Železná, B. (CZ)
    Kuneš, Jaroslav (FGU-C) RID, ORCID
    Maletínská, L. (CZ)
    Číslo článku8904
    Zdroj.dok.International Journal of Molecular Sciences. - : MDPI
    Roč. 22, č. 16 (2021)
    Poč.str.17 s.
    Jazyk dok.eng - angličtina
    Země vyd.CH - Švýcarsko
    Klíč. slovaprolactin-releasing peptide ; GPR10 ; neuropeptide FF ; NPFF-R2 ; NPFF-R1 ; binding properties ; signaling pathways
    Vědní obor RIVED - Fyziologie
    Obor OECDPhysiology (including cytology)
    CEPGA21-03691S GA ČR - Grantová agentura ČR
    Způsob publikováníOpen access
    Institucionální podporaFGU-C - RVO:67985823
    UT WOS000689129400001
    EID SCOPUS85112686217
    DOI10.3390/ijms22168904
    AnotaceThe anorexigenic neuropeptide prolactin-releasing peptide (PrRP) is involved in the regulation of food intake and energy expenditure. Lipidization of PrRP stabilizes the peptide, facilitates central effect after peripheral administration and increases its affinity for its receptor, GPR10, and for the neuropeptide FF (NPFF) receptor NPFF-R2. The two most potent palmitoylated analogs with anorectic effects in mice, palm(11)-PrRP31 and palm-PrRP31, were studied in vitro to determine their agonist/antagonist properties and mechanism of action on GPR10, NPFF-R2 and other potential off-target receptors related to energy homeostasis. Palmitoylation of both PrRP31 analogs increased the binding properties of PrRP31 to anorexigenic receptors GPR10 and NPFF-R2 and resulted in a high affinity for another NPFF receptor, NPFF-R1. Moreover, in CHO-K1 cells expressing GPR10, NPFF-R2 or NPFF-R1, palm(11)-PrRP and palm-PrRP significantly increased the phosphorylation of extracellular signal-regulated kinase (ERK), protein kinase B (Akt) and cAMP-responsive element-binding protein (CREB). Palm(11)-PrRP31, unlike palm-PrRP31, did not activate either c-Jun N-terminal kinase (JNK), p38, c-Jun, c-Fos or CREB pathways in cells expressing NPFF-1R. Palm-PrRP31 also has higher binding affinities for off-target receptors, namely, the ghrelin, opioid (KOR, MOR, DOR and OPR-L1) and neuropeptide Y (Y-1, Y-2 and Y-5) receptors. Palm(11)-PrRP31 exhibited fewer off-target activities, therefore, it has a higher potential to be used as an anti-obesity drug with anorectic effects.
    PracovištěFyziologický ústav
    KontaktLucie Trajhanová, lucie.trajhanova@fgu.cas.cz, Tel.: 241 062 400
    Rok sběru2022
    Elektronická adresahttps://www.mdpi.com/1422-0067/22/16/8904
Počet záznamů: 1  

  Tyto stránky využívají soubory cookies, které usnadňují jejich prohlížení. Další informace o tom jak používáme cookies.