Palmitoylation of Prolactin-Releasing Peptide Increased Affinity for and Activation of the GPR10, NPFF-R2 and NPFF-R1 Receptors: In Vitro Study
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F67985823%3A_____%2F21%3A00545497" target="_blank" >RIV/67985823:_____/21:00545497 - isvavai.cz</a>
Alternative codes found
RIV/61388963:_____/21:00544980 RIV/00216208:11110/21:10430340
Result on the web
<a href="https://www.mdpi.com/1422-0067/22/16/8904" target="_blank" >https://www.mdpi.com/1422-0067/22/16/8904</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.3390/ijms22168904" target="_blank" >10.3390/ijms22168904</a>
Alternative languages
Result language
angličtina
Original language name
Palmitoylation of Prolactin-Releasing Peptide Increased Affinity for and Activation of the GPR10, NPFF-R2 and NPFF-R1 Receptors: In Vitro Study
Original language description
The 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.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30105 - Physiology (including cytology)
Result continuities
Project
<a href="/en/project/GA21-03691S" target="_blank" >GA21-03691S: Neuropeptide FF-2 receptor as a potential anti-obesity target: Impact of new analogs of RF-amide peptides</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2021
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
International Journal of Molecular Sciences
ISSN
1422-0067
e-ISSN
1422-0067
Volume of the periodical
22
Issue of the periodical within the volume
16
Country of publishing house
CH - SWITZERLAND
Number of pages
17
Pages from-to
8904
UT code for WoS article
000689129400001
EID of the result in the Scopus database
2-s2.0-85112686217