Target intelligence / Profile preview

Adhesion G protein-coupled receptor F1 (GPR110) (ADGRF1)

Target
ADGRF1
Molecular classification
G protein-coupled receptor, Adhesion GPCR family, Receptor
01

Overview

Adhesion G protein-coupled receptor F1 (GPR110), also known as ADGRF1, is an orphan member of the adhesion GPCR family that has been identified as the functional receptor for synaptamide (N-docosahexaenoylethanolamine) (Lee et al., 2016, Nature Communications). Synaptamide is an endogenous metabolite derived from docosahexaenoic acid (DHA) that promotes essential neurodevelopmental processes, including neurogenesis, neurite outgrowth, and synaptogenesis (Kim et al., 2011, Journal of Biological Chemistry). Upon binding synaptamide, GPR110 activates the Gs-cAMP-PKA signaling pathway, which is crucial for brain development and cognitive function (Lee et al., 2016). This signaling axis is particularly important during the neonatal period, where it supports the expansion of the neuronal progenitor pool and the maturation of synaptic connections. Beyond its role in the central nervous system, GPR110 is frequently overexpressed in various cancers, such as lung and colon carcinomas, where it may contribute to tumor progression and metastasis (Lum et al., 2010, Molecular Cancer Research). Consequently, GPR110 represents a dual-interest target: its activation is sought for neuroprotection and repair, while its inhibition is explored for oncological applications.

Other names
Adhesion G protein-coupled receptor F1ADGRF1G-protein coupled receptor 110PGR19KPG_001hGPCR36
02

Mechanism of action

Synaptamide acts as an endogenous agonist for GPR110, triggering the activation of the Gs protein, which increases intracellular cAMP levels and subsequently activates the PKA/CREB pathway to promote neuronal development (Lee et al., 2016, Nature Communications).

03

Biological functions

Signal transductionNeurogenesisNeurite outgrowthSynaptogenesisCell adhesioncAMP signaling
04

Disease associations

CancerNeurodevelopmental disorderInflammation
05

Safety considerations

Potential for promoting tumor growth in certain cancers due to GPR110's role as an oncogene (Lum et al., 2010, Molecular Cancer Research)Blood-brain barrier permeability for synthetic analogs targeting the central nervous system
06

Interacting drugs

Synaptamide (N-docosahexaenoylethanolamine)
07

Biomarkers

GPR110 expression levels (mRNA/protein)Synaptamide levels in cerebrospinal fluid

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