Top ▲

GtoPdb is requesting financial support from commercial users. Please see our sustainability page for more information.

ADGRF1

Click here for help

Target id: 190

Nomenclature: ADGRF1

Family: Adhesion Class GPCRs

Contents:

Gene and Protein Information Click here for help
Adhesion G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 910 6p12.3 ADGRF1 adhesion G protein-coupled receptor F1 3
Mouse 7 908 17 B3 Adgrf1 adhesion G protein-coupled receptor F1
Rat 7 909 9q12 Adgrf1 adhesion G protein-coupled receptor F1
Previous and Unofficial Names Click here for help
GPR110 (G protein-coupled receptor 110) | PGR19
Database Links Click here for help
Specialist databases
GPCRdb agrf1_human (Hs), agrf1_mouse (Mm)
Other databases
Alphafold Q5T601 (Hs), Q8VEC3 (Mm)
CATH/Gene3D 3.30.70.960
ChEMBL Target CHEMBL4523872 (Hs)
Ensembl Gene ENSG00000153292 (Hs), ENSMUSG00000041293 (Mm), ENSRNOG00000062544 (Rn)
Entrez Gene 266977 (Hs), 77596 (Mm), 301266 (Rn)
Human Protein Atlas ENSG00000153292 (Hs)
KEGG Gene hsa:266977 (Hs), mmu:77596 (Mm), rno:301266 (Rn)
Pharos Q5T601 (Hs)
RefSeq Nucleotide NM_153840 (Hs), NM_133776 (Mm)
RefSeq Protein NP_722582 (Hs), NP_598537 (Mm)
UniProtKB Q5T601 (Hs), Q8VEC3 (Mm)
Wikipedia ADGRF1 (Hs)
Endogenous agonists
Peptides derived from the Stachel sequence TSFSILMSPFVPSTIFPVVKWIT  [1,9]

Download all structure-activity data for this target as a CSV file go icon to follow link

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
synaptamide Small molecule or natural product Ligand is endogenous in the given species Hs Agonist - - 5
⤷ [5]
Agonist Comments
N-docosahexaenoylethanolamine (synaptamide) is an ADGRF1 agonist [6], as are peptides derived from the Stachel sequence TSFSILMSPFVPSTIFPVVKWIT [1,9].
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family
References:  1,6
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family
References:  1,9
Tissue Distribution Click here for help
Unigene expression profile: high frequency in trachea, mouth, kidney, lung, prostate.
Species:  Human
Technique: 
References: 
Kidney and prostate, overexpressed in lung and prostate tumors, present in lung cancer cell lines (A549, H460, H23) and the prostate cell line PC-3
Species:  Human
Technique:  RT-PCR and immunohistochemistry
References:  7
Peripheral blood cells/bone marrow of pediatric B-precursor acute lymphoblastic leukemia patients
Species:  Human
Technique:  Microarray analysis
References:  4
Spleen, T lymphomas
Species:  Mouse
Technique:  RT-PCR
References:  7
Liver, kidney (renal pelvis), adrenal gland
Species:  Mouse
Technique:  RT-PCR and LacZ insertion
References:  8
Unigene expression profile: high frequency in the eye.
Species:  Rat
Technique: 
References: 
Expression Datasets Click here for help

Show »

Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays Click here for help
ADGRF1 couples to Gs proteins in COS-7 cells and neural stem cells, as determined by Alpha screen assay, cAMP measurement and GTPγS binding.
Species:  None
Tissue:  COS-7 cells, neural stem cells.
Response measured: 
References:  1,6
ADGRF1 couples to Gq proteins as determined by GTPγS binding assay and IP1 assay.
Species:  None
Tissue: 
Response measured: 
References:  1,9
General Comments
ADGRF1 (formerly GPR110) is an orphan receptor that belongs to Family VI Adhesion-GPCRs together with ADGRF2-5 (formerly GPR111, GPR113, GPR115 and GPR116 respectively) [2]. The genes of Family VI Adhesion-GPCRs except ADGRF3 are syntenically clustered on human chromosome 6 and mouse chromosome 17 suggesting the evolution from an ancestral gene through gene duplication and exon shuffling [8]. The N terminus of ADGRF1 contains a GPCR proteolysis site (GPS) and a SEA (Sperm protein, Enterokinase and Agrin) domain. ADGRF1 is a receptor for N-docosahexaenoylethanolamine (synaptamide), an endogenous metabolite of docosahexaenoic acid, that potently promotes neurogenesis, neuritogenesis and synaptogenesis. ADGRF1 knockout mice show significant deficits in object recognition and spatial memory [6].

References

Show »

1. Demberg LM, Winkler J, Wilde C, Simon KU, Schön J, Rothemund S, Schöneberg T, Prömel S, Liebscher I. (2017) Activation of Adhesion G Protein-coupled Receptors: AGONIST SPECIFICITY OF STACHEL SEQUENCE-DERIVED PEPTIDES. J Biol Chem, 292 (11): 4383-4394. [PMID:28154189]

2. Fredriksson R, Gloriam DE, Höglund PJ, Lagerström MC, Schiöth HB. (2003) There exist at least 30 human G-protein-coupled receptors with long Ser/Thr-rich N-termini. Biochem Biophys Res Commun, 301 (3): 725-34. [PMID:12565841]

3. Fredriksson R, Lagerström MC, Höglund PJ, Schiöth HB. (2002) Novel human G protein-coupled receptors with long N-terminals containing GPS domains and Ser/Thr-rich regions. FEBS Lett, 531 (3): 407-14. [PMID:12435584]

4. Harvey RC, Mullighan CG, Wang X, Dobbin KK, Davidson GS, Bedrick EJ, Chen IM, Atlas SR, Kang H, Ar K et al.. (2010) Identification of novel cluster groups in pediatric high-risk B-precursor acute lymphoblastic leukemia with gene expression profiling: correlation with genome-wide DNA copy number alterations, clinical characteristics, and outcome. Blood, 116 (23): 4874-84. [PMID:20699438]

5. Kwon HS, Kevala K, Qian H, Abu-Asab M, Patnaik S, Marugan J, Kim HY. (2023) Ligand-Induced Activation of GPR110 (ADGRF1) to Improve Visual Function Impaired by Optic Nerve Injury. Int J Mol Sci, 24 (6). [PMID:36982411]

6. Lee JW, Huang BX, Kwon H, Rashid MA, Kharebava G, Desai A, Patnaik S, Marugan J, Kim HY. (2016) Orphan GPR110 (ADGRF1) targeted by N-docosahexaenoylethanolamine in development of neurons and cognitive function. Nat Commun, 7: 13123. [PMID:27759003]

7. Lum AM, Wang BB, Beck-Engeser GB, Li L, Channa N, Wabl M. (2010) Orphan receptor GPR110, an oncogene overexpressed in lung and prostate cancer. BMC Cancer, 10: 40. [PMID:20149256]

8. Prömel S, Waller-Evans H, Dixon J, Zahn D, Colledge WH, Doran J, Carlton MB, Grosse J, Schöneberg T, Russ AP et al.. (2012) Characterization and functional study of a cluster of four highly conserved orphan adhesion-GPCR in mouse. Dev Dyn, 241 (10): 1591-602. [PMID:22837050]

9. Stoveken HM, Hajduczok AG, Xu L, Tall GG. (2015) Adhesion G protein-coupled receptors are activated by exposure of a cryptic tethered agonist. Proc Natl Acad Sci USA, 112 (19): 6194-9. [PMID:25918380]

Contributors

Show »

How to cite this page