- Home
- Targets
- G protein-coupled receptors
- Adhesion Class GPCRs
Adhesion Class GPCRs C
Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Overview
Show »« Hide
More detailed introduction 
Adhesion GPCRs are structurally identified on the basis of a large extracellular region, similar to the Class B GPCR, but which is linked to the 7TM region by a GPCR autoproteolysis-inducing (GAIN) domain [3] containing a GPCR proteolysis site (GPS). The N-terminal extracellular region often shares structural homology with adhesive domains (e.g. cadherins, immunolobulin, lectins) facilitating inter- and matricellular interactions and leading to the term adhesion GPCR [29,116]. Several receptors have been suggested to function as mechanosensors [12,71,87,110]. Cryo-EM structures of the 7-transmembrane domain of several adhesion GPCRs have been determined recently [5,53,73-74,80-81,112,120]. The nomenclature of these receptors was revised in 2015 as recommended by NC-IUPHAR and the Adhesion GPCR Consortium [33].
Receptors
Targets of relevance to immunopharmacology are highlighted in blue
|
ADGRA1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRA2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRA3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRB1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRB2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRB3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
CELSR1 / ADGRC1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
CELSR2 / ADGRC2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
CELSR3 / ADGRC3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRD1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRD2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRE1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRE2
C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRE3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRE4P C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRE5
C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRF1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRF2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRF3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRF4 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRF5 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRG1
C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRG2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRG3
C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRG4 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRG5 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRG6 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRG7 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRL1 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRL2 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRL3 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRL4 C
Show summary »« Hide summary
More detailed page
|
|||||||||||||||||||
|
ADGRV1 C
Show summary »« Hide summary
More detailed page
|
Further reading
* Key recommended reading is highlighted with an asterisk
* Bassilana F, Nash M, Ludwig MG. (2019) Adhesion G protein-coupled receptors: opportunities for drug discovery. Nat Rev Drug Discov, 18 (11): 869-884. [PMID:31462748]
* Hamann J, Aust G, Araç D, Engel FB, Formstone C, Fredriksson R, Hall RA, Harty BL, Kirchhoff C, Knapp B et al.. (2015) International Union of Basic and Clinical Pharmacology. XCIV. Adhesion G protein-coupled receptors. Pharmacol Rev, 67 (2): 338-67. [PMID:25713288]
* Langenhan T, Aust G, Hamann J. (2013) Sticky signaling--adhesion class G protein-coupled receptors take the stage. Sci Signal, 6 (276): re3. [PMID:23695165]
* Liebscher I, Schöneberg T. (2016) Tethered Agonism: A Common Activation Mechanism of Adhesion GPCRs. Handb Exp Pharmacol, 234: 111-125. [PMID:27832486]
* Monk KR, Hamann J, Langenhan T, Nijmeijer S, Schöneberg T, Liebscher I. (2015) Adhesion G Protein-Coupled Receptors: From In Vitro Pharmacology to In Vivo Mechanisms. Mol Pharmacol, 88 (3): 617-23. [PMID:25956432]
* Purcell RH, Hall RA. (2018) Adhesion G Protein-Coupled Receptors as Drug Targets. Annu Rev Pharmacol Toxicol, 58: 429-449. [PMID:28968187]
Wang N, Qian Y, Xia R, Zhu X, Xiong Y, Zhang A, Guo C, He Y. (2023) Structural basis of CD97 activation and G-protein coupling. Cell Chem Biol, 30 (11): 1343-1353.e5. [PMID:37673067]
Yona S, Lin HH, Siu WO, Gordon S, Stacey M. (2008) Adhesion-GPCRs: emerging roles for novel receptors. Trends Biochem Sci, 33 (10): 491-500. [PMID:18789697]
References
1. Ackerman SD, Luo R, Poitelon Y, Mogha A, Harty BL, D'Rozario M, Sanchez NE, Lakkaraju AKK, Gamble P, Li J et al.. (2018) GPR56/ADGRG1 regulates development and maintenance of peripheral myelin. J Exp Med, 215 (3): 941-961. [PMID:29367382]
2. An W, Lin H, Ma L, Zhang C, Zheng Y, Cheng Q, Ma C, Wu X, Zhang Z, Zhong Y et al.. (2022) Progesterone activates GPR126 to promote breast cancer development via the Gi pathway. Proc Natl Acad Sci U S A, 119 (15): e2117004119. [PMID:35394864]
3. Araç D, Boucard AA, Bolliger MF, Nguyen J, Soltis SM, Südhof TC, Brunger AT. (2012) A novel evolutionarily conserved domain of cell-adhesion GPCRs mediates autoproteolysis. EMBO J, 31 (6): 1364-78. [PMID:22333914]
4. Arcos-Burgos M, Jain M, Acosta MT, Shively S, Stanescu H, Wallis D, Domené S, Vélez JI, Karkera JD, Balog J et al.. (2010) A common variant of the latrophilin 3 gene, LPHN3, confers susceptibility to ADHD and predicts effectiveness of stimulant medication. Mol Psychiatry, 15 (11): 1053-66. [PMID:20157310]
5. Barros-Álvarez X, Nwokonko RM, Vizurraga A, Matzov D, He F, Papasergi-Scott MM, Robertson MJ, Panova O, Yardeni EH, Seven AB et al.. (2022) The tethered peptide activation mechanism of adhesion GPCRs. Nature, 604 (7907): 757-762. [PMID:35418682]
6. Bayin NS, Frenster JD, Kane JR, Rubenstein J, Modrek AS, Baitalmal R, Dolgalev I, Rudzenski K, Scarabottolo L, Crespi D et al.. (2016) GPR133 (ADGRD1), an adhesion G-protein-coupled receptor, is necessary for glioblastoma growth. Oncogenesis, 5 (10): e263. [PMID:27775701]
7. Bhudia N, Desai S, King N, Ancellin N, Grillot D, Barnes AA, Dowell SJ. (2020) Author Correction: G Protein-Coupling of Adhesion GPCRs ADGRE2/EMR2 and ADGRE5/CD97, and Activation of G Protein Signalling by an Anti-EMR2 Antibody. Sci Rep, 10 (1): 5097. [PMID:32184438]
8. Bianchi E, Sun Y, Almansa-Ordonez A, Woods M, Goulding D, Martinez-Martin N, Wright GJ. (2021) Control of oviductal fluid flow by the G-protein coupled receptor Adgrd1 is essential for murine embryo transit. Nat Commun, 12 (1): 1251. [PMID:33623007]
9. Bohnekamp J, Schöneberg T. (2011) Cell adhesion receptor GPR133 couples to Gs protein. J Biol Chem, 286 (49): 41912-6. [PMID:22025619]
10. Bolliger MF, Martinelli DC, Südhof TC. (2011) The cell-adhesion G protein-coupled receptor BAI3 is a high-affinity receptor for C1q-like proteins. Proc Natl Acad Sci USA, 108 (6): 2534-9. [PMID:21262840]
11. Boucard AA, Ko J, Südhof TC. (2012) High affinity neurexin binding to cell adhesion G-protein-coupled receptor CIRL1/latrophilin-1 produces an intercellular adhesion complex. J Biol Chem, 287 (12): 9399-413. [PMID:22262843]
12. Boyden SE, Desai A, Cruse G, Young ML, Bolan HC, Scott LM, Eisch AR, Long RD, Lee CC, Satorius CL et al.. (2016) Vibratory Urticaria Associated with a Missense Variant in ADGRE2. N Engl J Med, 374 (7): 656-63. [PMID:26841242]
13. Bradley EC, Cunningham RL, Wilde C, Morgan RK, Klug EA, Letcher SM, Schöneberg T, Monk KR, Liebscher I, Petersen SC. (2019) In vivo identification of small molecules mediating Gpr126/Adgrg6 signaling during Schwann cell development. Ann N Y Acad Sci, 1456 (1): 44-63. [PMID:31529518]
14. Bridges JP, Ludwig MG, Mueller M, Kinzel B, Sato A, Xu Y, Whitsett JA, Ikegami M. (2013) Orphan G protein-coupled receptor GPR116 regulates pulmonary surfactant pool size. Am J Respir Cell Mol Biol, 49 (3): 348-57. [PMID:23590306]
15. Brown K, Filuta A, Ludwig MG, Seuwen K, Jaros J, Vidal S, Arora K, Naren AP, Kandasamy K, Parthasarathi K et al.. (2017) Epithelial Gpr116 regulates pulmonary alveolar homeostasis via Gq/11 signaling. JCI Insight, 2 (11). [PMID:28570277]
16. Carr JC, Boese EA, Spanheimer PM, Dahdaleh FS, Martin M, Calva D, Schafer B, Thole DM, Braun T, O'Dorisio TM et al.. (2012) Differentiation of small bowel and pancreatic neuroendocrine tumors by gene-expression profiling. Surgery, 152 (6): 998-1007. [PMID:23158174]
17. Chang GW, Hsiao CC, Peng YM, Vieira Braga FA, Kragten NA, Remmerswaal EB, van de Garde MD, Straussberg R, König GM, Kostenis E et al.. (2016) The Adhesion G Protein-Coupled Receptor GPR56/ADGRG1 Is an Inhibitory Receptor on Human NK Cells. Cell Rep, 15 (8): 1757-70. [PMID:27184850]
18. Chang J, Mancuso MR, Maier C, Liang X, Yuki K, Yang L, Kwong JW, Wang J, Rao V, Vallon M et al.. (2017) Gpr124 is essential for blood-brain barrier integrity in central nervous system disease. Nat Med, 23 (4): 450-460. [PMID:28288111]
19. Chiang NY, Chang GW, Huang YS, Peng YM, Hsiao CC, Kuo ML, Lin HH. (2016) Heparin interacts with the adhesion GPCR GPR56, reduces receptor shedding, and promotes cell adhesion and motility. J Cell Sci, 129 (11): 2156-69. [PMID:27068534]
20. Chiba Y, Yoshizaki K, Saito K, Ikeuchi T, Iwamoto T, Rhodes C, Nakamura T, de Vega S, Morell RJ, Boger ET et al.. (2020) G protein-coupled receptor Gpr115 (Adgrf4) is required for enamel mineralization mediated by ameloblasts. J Biol Chem, 295 (45): 15328-15341. [PMID:32868297]
21. Cho C, Smallwood PM, Nathans J. (2017) Reck and Gpr124 Are Essential Receptor Cofactors for Wnt7a/Wnt7b-Specific Signaling in Mammalian CNS Angiogenesis and Blood-Brain Barrier Regulation. Neuron, 95 (5): 1056-1073.e5. [PMID:28803732]
22. Chong ZS, Ohnishi S, Yusa K, Wright GJ. (2018) Pooled extracellular receptor-ligand interaction screening using CRISPR activation. Genome Biol, 19 (1): 205. [PMID:30477585]
23. Das S, Owen KA, Ly KT, Park D, Black SG, Wilson JM, Sifri CD, Ravichandran KS, Ernst PB, Casanova JE. (2011) Brain angiogenesis inhibitor 1 (BAI1) is a pattern recognition receptor that mediates macrophage binding and engulfment of Gram-negative bacteria. Proc Natl Acad Sci USA, 108 (5): 2136-41. [PMID:21245295]
24. Demberg LM, Rothemund S, Schöneberg T, Liebscher I. (2015) Identification of the tethered peptide agonist of the adhesion G protein-coupled receptor GPR64/ADGRG2. Biochem Biophys Res Commun, 464 (3): 743-7. [PMID:26188515]
25. 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]
26. Devenport D, Oristian D, Heller E, Fuchs E. (2011) Mitotic internalization of planar cell polarity proteins preserves tissue polarity. Nat Cell Biol, 13 (8): 893-902. [PMID:21743464]
27. Duman JG, Mulherkar S, Tu YK, Erikson KC, Tzeng CP, Mavratsas VC, Ho TS, Tolias KF. (2019) The adhesion-GPCR BAI1 shapes dendritic arbors via Bcr-mediated RhoA activation causing late growth arrest. Elife, 8. [PMID:31461398]
28. Eubelen M, Bostaille N, Cabochette P, Gauquier A, Tebabi P, Dumitru AC, Koehler M, Gut P, Alsteens D, Stainier DYR et al.. (2018) A molecular mechanism for Wnt ligand-specific signaling. Science, 361 (6403). [PMID:30026314]
29. Fredriksson R, Lagerström MC, Lundin LG, Schiöth HB. (2003) The G-protein-coupled receptors in the human genome form five main families. Phylogenetic analysis, paralogon groups, and fingerprints. Mol Pharmacol, 63 (6): 1256-72. [PMID:12761335]
30. Fukuzawa T, Ishida J, Kato A, Ichinose T, Ariestanti DM, Takahashi T, Ito K, Abe J, Suzuki T, Wakana S et al.. (2013) Lung surfactant levels are regulated by Ig-Hepta/GPR116 by monitoring surfactant protein D. PLoS ONE, 8 (7): e69451. [PMID:23922714]
31. Giera S, Deng Y, Luo R, Ackerman SD, Mogha A, Monk KR, Ying Y, Jeong SJ, Makinodan M, Bialas AR et al.. (2015) The adhesion G protein-coupled receptor GPR56 is a cell-autonomous regulator of oligodendrocyte development. Nat Commun, 6: 6121. [PMID:25607655]
32. Gupte J, Swaminath G, Danao J, Tian H, Li Y, Wu X. (2012) Signaling property study of adhesion G-protein-coupled receptors. FEBS Lett, 586 (8): 1214-9. [PMID:22575658]
33. Hamann J, Aust G, Araç D, Engel FB, Formstone C, Fredriksson R, Hall RA, Harty BL, Kirchhoff C, Knapp B et al.. (2015) International Union of Basic and Clinical Pharmacology. XCIV. Adhesion G protein-coupled receptors. Pharmacol Rev, 67 (2): 338-67. [PMID:25713288]
34. Hamann J, Vogel B, van Schijndel GM, van Lier RA. (1996) The seven-span transmembrane receptor CD97 has a cellular ligand (CD55, DAF). J Exp Med, 184 (3): 1185-9. [PMID:9064337]
35. Hamoud N, Tran V, Croteau LP, Kania A, Côté JF. (2014) G-protein coupled receptor BAI3 promotes myoblast fusion in vertebrates. Proc Natl Acad Sci USA, 111 (10): 3745-50. [PMID:24567399]
36. Hsiao CC, Chu TY, Wu CJ, van den Biggelaar M, Pabst C, Hébert J, Kuijpers TW, Scicluna BP, I KY, Chen TC et al.. (2018) The Adhesion G Protein-Coupled Receptor GPR97/ADGRG3 Is Expressed in Human Granulocytes and Triggers Antimicrobial Effector Functions. Front Immunol, 9: 2830. [PMID:30559745]
37. Hsiao CC, van der Poel M, van Ham TJ, Hamann J. (2019) Macrophages Do Not Express the Phagocytic Receptor BAI1/ADGRB1. Front Immunol, 10: 962. [PMID:31130954]
38. Irmscher S, Brix SR, Zipfel SLH, Halder LD, Mutlutürk S, Wulf S, Girdauskas E, Reichenspurner H, Stahl RAK, Jungnickel B et al.. (2019) Serum FHR1 binding to necrotic-type cells activates monocytic inflammasome and marks necrotic sites in vasculopathies. Nat Commun, 10 (1): 2961. [PMID:31273197]
39. Jackson VA, Mehmood S, Chavent M, Roversi P, Carrasquero M, Del Toro D, Seyit-Bremer G, Ranaivoson FM, Comoletti D, Sansom MS et al.. (2016) Super-complexes of adhesion GPCRs and neural guidance receptors. Nat Commun, 7: 11184. [PMID:27091502]
40. Jacobson SG, Cideciyan AV, Aleman TS, Sumaroka A, Roman AJ, Gardner LM, Prosser HM, Mishra M, Bech-Hansen NT, Herrera W, Schwartz SB, Liu XZ, Kimberling WJ, Steel KP, Williams DS. (2008) Usher syndromes due to MYO7A, PCDH15, USH2A or GPR98 mutations share retinal disease mechanism. Hum Mol Genet, 17 (15): 2405-15. [PMID:18463160]
41. Karpus ON, Veninga H, Hoek RM, Flierman D, van Buul JD, Vandenakker CC, vanBavel E, Medof ME, van Lier RA, Reedquist KA et al.. (2013) Shear stress-dependent downregulation of the adhesion-G protein-coupled receptor CD97 on circulating leukocytes upon contact with its ligand CD55. J Immunol, 190 (7): 3740-8. [PMID:23447688]
42. Kim JJ, Park YM, Baik KH, Choi HY, Yang GS, Koh I, Hwang JA, Lee J, Lee YS, Rhee H et al.. (2012) Exome sequencing and subsequent association studies identify five amino acid-altering variants influencing human height. Hum Genet, 131 (3): 471-8. [PMID:21959382]
43. Kim YK, Moon S, Hwang MY, Kim DJ, Oh JH, Kim YJ, Han BG, Lee JY, Kim BJ. (2013) Gene-based copy number variation study reveals a microdeletion at 12q24 that influences height in the Korean population. Genomics, 101 (2): 134-8. [PMID:23147675]
44. Knierim AB, Röthe J, Çakir MV, Lede V, Wilde C, Liebscher I, Thor D, Schöneberg T. (2019) Genetic basis of functional variability in adhesion G protein-coupled receptors. Sci Rep, 9 (1): 11036. [PMID:31363148]
45. Kreienkamp HJ, Zitzer H, Gundelfinger ED, Richter D, Bockers TM. (2000) The calcium-independent receptor for alpha-latrotoxin from human and rodent brains interacts with members of the ProSAP/SSTRIP/Shank family of multidomain proteins. J Biol Chem, 275 (42): 32387-90. [PMID:10964907]
46. 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]
47. Lei Y, Zhu H, Yang W, Ross ME, Shaw GM, Finnell RH. (2014) Identification of novel CELSR1 mutations in spina bifida. PLoS ONE, 9 (3): e92207. [PMID:24632739]
48. Leja J, Essaghir A, Essand M, Wester K, Oberg K, Tötterman TH, Lloyd R, Vasmatzis G, Demoulin JB, Giandomenico V. (2009) Novel markers for enterochromaffin cells and gastrointestinal neuroendocrine carcinomas. Mod Pathol, 22 (2): 261-72. [PMID:18953328]
49. Lelianova VG, Davletov BA, Sterling A, Rahman MA, Grishin EV, Totty NF, Ushkaryov YA. (1997) Alpha-latrotoxin receptor, latrophilin, is a novel member of the secretin family of G protein-coupled receptors. J Biol Chem, 272 (34): 21504-8. [PMID:9261169]
50. Li X, Roszko I, Sepich DS, Ni M, Hamm HE, Marlow FL, Solnica-Krezel L. (2013) Gpr125 modulates Dishevelled distribution and planar cell polarity signaling. Development, 140 (14): 3028-39. [PMID:23821037]
51. Liebscher I, Schön J, Petersen SC, Fischer L, Auerbach N, Demberg LM, Mogha A, Cöster M, Simon KU, Rothemund S et al.. (2014) A tethered agonist within the ectodomain activates the adhesion G protein-coupled receptors GPR126 and GPR133. Cell Rep, 9 (6): 2018-26. [PMID:25533341]
52. Liebscher I, Schöneberg T, Prömel S. (2013) Progress in demystification of adhesion G protein-coupled receptors. Biol Chem, 394 (8): 937-50. [PMID:23518449]
53. Lin H, Xiao P, Bu RQ, Guo S, Yang Z, Yuan D, Zhu ZL, Zhang CX, He QT, Zhang C et al.. (2022) Structures of the ADGRG2-Gs complex in apo and ligand-bound forms. Nat Chem Biol, 18 (11): 1196-1203. [PMID:35982227]
54. Lindenmaier LB, Parmentier N, Guo C, Tissir F, Wright KM. (2019) Dystroglycan is a scaffold for extracellular axon guidance decisions. Elife, 8. [PMID:30758284]
55. Liu D, Duan L, Rodda LB, Lu E, Xu Y, An J, Qiu L, Liu F, Looney MR, Yang Z et al.. (2022) CD97 promotes spleen dendritic cell homeostasis through the mechanosensing of red blood cells. Science, 375 (6581): eabi5965. [PMID:35143305]
56. Liu Z, Easson GWD, Zhao J, Makki N, Ahituv N, Hilton MJ, Tang SY, Gray RS. (2019) Dysregulation of STAT3 signaling is associated with endplate-oriented herniations of the intervertebral disc in Adgrg6 mutant mice. PLoS Genet, 15 (10): e1008096. [PMID:31652254]
57. Luo R, Jeong SJ, Jin Z, Strokes N, Li S, Piao X. (2011) G protein-coupled receptor 56 and collagen III, a receptor-ligand pair, regulates cortical development and lamination. Proc Natl Acad Sci USA, 108 (31): 12925-30. [PMID:21768377]
58. Martin M, Vermeiren S, Bostaille N, Eubelen M, Spitzer D, Vermeersch M, Profaci CP, Pozuelo E, Toussay X, Raman-Nair J et al.. (2022) Engineered Wnt ligands enable blood-brain barrier repair in neurological disorders. Science, 375 (6582): eabm4459. [PMID:35175798]
59. Mathiasen S, Palmisano T, Perry NA, Stoveken HM, Vizurraga A, McEwen DP, Okashah N, Langenhan T, Inoue A, Lambert NA et al.. (2020) G12/13 is activated by acute tethered agonist exposure in the adhesion GPCR ADGRL3. Nat Chem Biol, 16 (12): 1343-1350. [PMID:32778842]
60. Mogha A, Benesh AE, Patra C, Engel FB, Schöneberg T, Liebscher I, Monk KR. (2013) Gpr126 functions in Schwann cells to control differentiation and myelination via G-protein activation. J Neurosci, 33 (46): 17976-85. [PMID:24227709]
61. Monk KR, Naylor SG, Glenn TD, Mercurio S, Perlin JR, Dominguez C, Moens CB, Talbot WS. (2009) A G protein-coupled receptor is essential for Schwann cells to initiate myelination. Science, 325 (5946): 1402-5. [PMID:19745155]
62. Monk KR, Oshima K, Jörs S, Heller S, Talbot WS. (2011) Gpr126 is essential for peripheral nerve development and myelination in mammals. Development, 138 (13): 2673-80. [PMID:21613327]
63. Müller A, Winkler J, Fiedler F, Sastradihardja T, Binder C, Schnabel R, Kungel J, Rothemund S, Hennig C, Schöneberg T et al.. (2015) Oriented Cell Division in the C. elegans Embryo Is Coordinated by G-Protein Signaling Dependent on the Adhesion GPCR LAT-1. PLoS Genet, 11 (10): e1005624. [PMID:26505631]
64. Ni YY, Chen Y, Lu SY, Sun BY, Wang F, Wu XL, Dang SY, Zhang GH, Zhang HX, Kuang Y et al.. (2014) Deletion of Gpr128 results in weight loss and increased intestinal contraction frequency. World J Gastroenterol, 20 (2): 498-508. [PMID:24574718]
65. Nishimura T, Honda H, Takeichi M. (2012) Planar cell polarity links axes of spatial dynamics in neural-tube closure. Cell, 149 (5): 1084-97. [PMID:22632972]
66. Nybo ML, Kvam JM, Nielsen JE, Frederiksen H, Spiess K, Jensen KHR, Gadgaard S, Walser ALS, Thomsen JS, Cowin P et al.. (2023) Loss of Adgra3 causes obstructive azoospermia with high penetrance in male mice. FASEB J, 37 (2): e22781. [PMID:36688818]
67. O'Sullivan ML, de Wit J, Savas JN, Comoletti D, Otto-Hitt S, Yates 3rd JR, Ghosh A. (2012) FLRT proteins are endogenous latrophilin ligands and regulate excitatory synapse development. Neuron, 73 (5): 903-10. [PMID:22405201]
68. Park D, Tosello-Trampont AC, Elliott MR, Lu M, Haney LB, Ma Z, Klibanov AL, Mandell JW, Ravichandran KS. (2007) BAI1 is an engulfment receptor for apoptotic cells upstream of the ELMO/Dock180/Rac module. Nature, 450 (7168): 430-4. [PMID:17960134]
69. Patat O, Pagin A, Siegfried A, Mitchell V, Chassaing N, Faguer S, Monteil L, Gaston V, Bujan L, Courtade-Saïdi M et al.. (2016) Truncating Mutations in the Adhesion G Protein-Coupled Receptor G2 Gene ADGRG2 Cause an X-Linked Congenital Bilateral Absence of Vas Deferens. Am J Hum Genet, 99 (2): 437-42. [PMID:27476656]
70. Patra C, van Amerongen MJ, Ghosh S, Ricciardi F, Sajjad A, Novoyatleva T, Mogha A, Monk KR, Mühlfeld C, Engel FB. (2013) Organ-specific function of adhesion G protein-coupled receptor GPR126 is domain-dependent. Proc Natl Acad Sci USA, 110 (42): 16898-903. [PMID:24082093]
71. Petersen SC, Luo R, Liebscher I, Giera S, Jeong SJ, Mogha A, Ghidinelli M, Feltri ML, Schöneberg T, Piao X et al.. (2015) The adhesion GPCR GPR126 has distinct, domain-dependent functions in Schwann cell development mediated by interaction with laminin-211. Neuron, 85 (4): 755-69. [PMID:25695270]
72. Piao X, Hill RS, Bodell A, Chang BS, Basel-Vanagaite L, Straussberg R, Dobyns WB, Qasrawi B, Winter RM, Innes AM et al.. (2004) G protein-coupled receptor-dependent development of human frontal cortex. Science, 303 (5666): 2033-6. [PMID:15044805]
73. Ping YQ, Mao C, Xiao P, Zhao RJ, Jiang Y, Yang Z, An WT, Shen DD, Yang F, Zhang H et al.. (2021) Structures of the glucocorticoid-bound adhesion receptor GPR97-Go complex. Nature, 589 (7843): 620-626. [PMID:33408414]
74. Ping YQ, Xiao P, Yang F, Zhao RJ, Guo SC, Yan X, Wu X, Zhang C, Lu Y, Zhao F et al.. (2022) Structural basis for the tethered peptide activation of adhesion GPCRs. Nature, 604 (7907): 763-770. [PMID:35418678]
75. Popova NV, Plotnikov A, Deev IE, Petrenko AG. (2007) Interaction of calcium-independent latrotoxin receptor with intracellular adapter protein TRIP8b. Dokl Biochem Biophys, 414: 149-51. [PMID:17695324]
76. Popova NV, Plotnikov AN, Ziganshin RKh, Deyev IE, Petrenko AG. (2008) Analysis of proteins interacting with TRIP8b adapter. Biochemistry Mosc, 73 (6): 644-51. [PMID:18620529]
77. Posokhova E, Shukla A, Seaman S, Volate S, Hilton MB, Wu B, Morris H, Swing DA, Zhou M, Zudaire E et al.. (2015) GPR124 functions as a WNT7-specific coactivator of canonical β-catenin signaling. Cell Rep, 10 (2): 123-30. [PMID:25558062]
78. 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]
79. Purcell RH, Toro C, Gahl WA, Hall RA. (2017) A disease-associated mutation in the adhesion GPCR BAI2 (ADGRB2) increases receptor signaling activity. Hum Mutat, 38 (12): 1751-1760. [PMID:28891236]
80. Qian Y, Ma Z, Liu C, Li X, Zhu X, Wang N, Xu Z, Xia R, Liang J, Duan Y et al.. (2022) Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling. Mol Cell, 82 (22): 4340-4352.e6. [PMID:36309016]
81. Qu X, Qiu N, Wang M, Zhang B, Du J, Zhong Z, Xu W, Chu X, Ma L, Yi C et al.. (2022) Structural basis of tethered agonism of the adhesion GPCRs ADGRD1 and ADGRF1. Nature, 604 (7907): 779-785. [PMID:35418679]
82. Rahman MA, Ashton AC, Meunier FA, Davletov BA, Dolly JO, Ushkaryov YA. (1999) Norepinephrine exocytosis stimulated by alpha-latrotoxin requires both external and stored Ca2+ and is mediated by latrophilin, G proteins and phospholipase C. Philos Trans R Soc Lond, B, Biol Sci, 354 (1381): 379-86. [PMID:10212487]
83. Ravenscroft G, Nolent F, Rajagopalan S, Meireles AM, Paavola KJ, Gaillard D, Alanio E, Buckland M, Arbuckle S, Krivanek M et al.. (2015) Mutations of GPR126 are responsible for severe arthrogryposis multiplex congenita. Am J Hum Genet, 96 (6): 955-61. [PMID:26004201]
84. Reiners J, van Wijk E, Märker T, Zimmermann U, Jürgens K, te Brinke H, Overlack N, Roepman R, Knipper M, Kremer H et al.. (2005) Scaffold protein harmonin (USH1C) provides molecular links between Usher syndrome type 1 and type 2. Hum Mol Genet, 14 (24): 3933-43. [PMID:16301216]
85. Sabik OL, Calabrese GM, Taleghani E, Ackert-Bicknell CL, Farber CR. (2020) Identification of a Core Module for Bone Mineral Density through the Integration of a Co-expression Network and GWAS Data. Cell Rep, 32 (11): 108145. [PMID:32937138]
86. Salašová A, Yokota C, Potěšil D, Zdráhal Z, Bryja V, Arenas E. (2017) A proteomic analysis of LRRK2 binding partners reveals interactions with multiple signaling components of the WNT/PCP pathway. Mol Neurodegener, 12 (1): 54. [PMID:28697798]
87. Scholz N, Gehring J, Guan C, Ljaschenko D, Fischer R, Lakshmanan V, Kittel RJ, Langenhan T. (2015) The adhesion GPCR latrophilin/CIRL shapes mechanosensation. Cell Rep, 11 (6): 866-874. [PMID:25937282]
88. Seandel M, James D, Shmelkov SV, Falciatori I, Kim J, Chavala S, Scherr DS, Zhang F, Torres R, Gale NW et al.. (2007) Generation of functional multipotent adult stem cells from GPR125+ germline progenitors. Nature, 449 (7160): 346-50. [PMID:17882221]
89. Shima Y, Kawaguchi SY, Kosaka K, Nakayama M, Hoshino M, Nabeshima Y, Hirano T, Uemura T. (2007) Opposing roles in neurite growth control by two seven-pass transmembrane cadherins. Nat Neurosci, 10 (8): 963-9. [PMID:17618280]
90. Silva JP, Lelianova VG, Ermolyuk YS, Vysokov N, Hitchen PG, Berninghausen O, Rahman MA, Zangrandi A, Fidalgo S, Tonevitsky AG et al.. (2011) Latrophilin 1 and its endogenous ligand Lasso/teneurin-2 form a high-affinity transsynaptic receptor pair with signaling capabilities. Proc Natl Acad Sci USA, 108 (29): 12113-8. [PMID:21724987]
91. Stacey M, Chang GW, Davies JQ, Kwakkenbos MJ, Sanderson RD, Hamann J, Gordon S, Lin HH. (2003) The epidermal growth factor-like domains of the human EMR2 receptor mediate cell attachment through chondroitin sulfate glycosaminoglycans. Blood, 102 (8): 2916-24. [PMID:12829604]
92. Stoveken HM, Bahr LL, Anders MW, Wojtovich AP, Smrcka AV, Tall GG. (2016) Dihydromunduletone Is a Small-Molecule Selective Adhesion G Protein-Coupled Receptor Antagonist. Mol Pharmacol, 90 (3): 214-24. [PMID:27338081]
93. 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]
94. Stoveken HM, Larsen SD, Smrcka AV, Tall GG. (2018) Gedunin- and Khivorin-Derivatives Are Small-Molecule Partial Agonists for Adhesion G Protein-Coupled Receptors GPR56/ADGRG1 and GPR114/ADGRG5. Mol Pharmacol, 93 (5): 477-488. [PMID:29476042]
95. Sun P, He L, Jia K, Yue Z, Li S, Jin Y, Li Z, Siwko S, Xue F, Su J et al.. (2020) Regulation of body length and bone mass by Gpr126/Adgrg6. Sci Adv, 6 (12): eaaz0368. [PMID:32219165]
96. Tang X, Jin R, Qu G, Wang X, Li Z, Yuan Z, Zhao C, Siwko S, Shi T, Wang P et al.. (2013) GPR116, an adhesion G-protein-coupled receptor, promotes breast cancer metastasis via the Gαq-p63RhoGEF-Rho GTPase pathway. Cancer Res, 73 (20): 6206-18. [PMID:24008316]
97. Thakar S, Wang L, Yu T, Ye M, Onishi K, Scott J, Qi J, Fernandes C, Han X, Yates 3rd JR et al.. (2017) Evidence for opposing roles of Celsr3 and Vangl2 in glutamatergic synapse formation. Proc Natl Acad Sci USA, 114 (4): E610-E618. [PMID:28057866]
98. Torregrosa-Carrión R, Piñeiro-Sabarís R, Siguero-Álvarez M, Grego-Bessa J, Luna-Zurita L, Fernandes VS, MacGrogan D, Stainier DYR, de la Pompa JL. (2021) Adhesion G protein-coupled receptor Gpr126/Adgrg6 is essential for placental development. Sci Adv, 7 (46): eabj5445. [PMID:34767447]
99. Tönjes A, Koriath M, Schleinitz D, Dietrich K, Böttcher Y, Rayner NW, Almgren P, Enigk B, Richter O, Rohm S, Fischer-Rosinsky A, Pfeiffer A, Hoffmann K, Krohn K, Aust G, Spranger J, Groop L, Blüher M, Kovacs P, Stumvoll M. (2009) Genetic variation in GPR133 is associated with height: genome wide association study in the self-contained population of Sorbs. Hum Mol Genet, 18 (23): 4662-8. [PMID:19729412]
100. Vallon M, Essler M. (2006) Proteolytically processed soluble tumor endothelial marker (TEM) 5 mediates endothelial cell survival during angiogenesis by linking integrin alpha(v)beta3 to glycosaminoglycans. J Biol Chem, 281 (45): 34179-88. [PMID:16982628]
101. Vallon M, Yuki K, Nguyen TD, Chang J, Yuan J, Siepe D, Miao Y, Essler M, Noda M, Garcia KC et al.. (2018) A RECK-WNT7 Receptor-Ligand Interaction Enables Isoform-Specific Regulation of Wnt Bioavailability. Cell Rep, 25 (2): 339-349.e9. [PMID:30304675]
102. van Wijk E, van der Zwaag B, Peters T, Zimmermann U, Te Brinke H, Kersten FF, Märker T, Aller E, Hoefsloot LH, Cremers CW et al.. (2006) The DFNB31 gene product whirlin connects to the Usher protein network in the cochlea and retina by direct association with USH2A and VLGR1. Hum Mol Genet, 15 (5): 751-65. [PMID:16434480]
103. Vanhollebeke B, Stone OA, Bostaille N, Cho C, Zhou Y, Maquet E, Gauquier A, Cabochette P, Fukuhara S, Mochizuki N et al.. (2015) Tip cell-specific requirement for an atypical Gpr124- and Reck-dependent Wnt/β-catenin pathway during brain angiogenesis. Elife, 4. [PMID:26051822]
104. Vilboux T, Malicdan MC, Roney JC, Cullinane AR, Stephen J, Yildirimli D, Bryant J, Fischer R, Vemulapalli M, Mullikin JC et al.. (2017) CELSR2, encoding a planar cell polarity protein, is a putative gene in Joubert syndrome with cortical heterotopia, microophthalmia, and growth hormone deficiency. Am J Med Genet A, 173 (3): 661-666. [PMID:28052552]
105. Waller-Evans H, Prömel S, Langenhan T, Dixon J, Zahn D, Colledge WH, Doran J, Carlton MB, Davies B, Aparicio SA et al.. (2010) The orphan adhesion-GPCR GPR126 is required for embryonic development in the mouse. PLoS ONE, 5 (11): e14047. [PMID:21124978]
106. Wandel E, Saalbach A, Sittig D, Gebhardt C, Aust G. (2012) Thy-1 (CD90) is an interacting partner for CD97 on activated endothelial cells. J Immunol, 188 (3): 1442-50. [PMID:22210915]
107. Wang F, Wang Y, Qiu W, Zhang Q, Yang H, Song G. (2023) Crystal Structure of the Extracellular Domains of GPR110. J Mol Biol, 435 (6): 167979. [PMID:36716818]
108. Wang S, Mandell JD, Kumar Y, Sun N, Morris MT, Arbelaez J, Nasello C, Dong S, Duhn C, Zhao X et al.. (2018) De Novo Sequence and Copy Number Variants Are Strongly Associated with Tourette Disorder and Implicate Cell Polarity in Pathogenesis. Cell Rep, 24 (13): 3441-3454.e12. [PMID:30257206]
109. Wang T, Ward Y, Tian L, Lake R, Guedez L, Stetler-Stevenson WG, Kelly K. (2005) CD97, an adhesion receptor on inflammatory cells, stimulates angiogenesis through binding integrin counterreceptors on endothelial cells. Blood, 105 (7): 2836-44. [PMID:15576472]
110. Wilde C, Fischer L, Lede V, Kirchberger J, Rothemund S, Schöneberg T, Liebscher I. (2016) The constitutive activity of the adhesion GPCR GPR114/ADGRG5 is mediated by its tethered agonist. FASEB J, 30 (2): 666-73. [PMID:26499266]
111. Willsey AJ, Fernandez TV, Yu D, King RA, Dietrich A, Xing J, Sanders SJ, Mandell JD, Huang AY, Richer P et al.. (2017) De Novo Coding Variants Are Strongly Associated with Tourette Disorder. Neuron, 94 (3): 486-499.e9. [PMID:28472652]
112. Xiao P, Guo S, Wen X, He QT, Lin H, Huang SM, Gou L, Zhang C, Yang Z, Zhong YN et al.. (2022) Tethered peptide activation mechanism of the adhesion GPCRs ADGRG2 and ADGRG4. Nature, 604 (7907): 771-778. [PMID:35418677]
113. Xu L, Begum S, Hearn JD, Hynes RO. (2006) GPR56, an atypical G protein-coupled receptor, binds tissue transglutaminase, TG2, and inhibits melanoma tumor growth and metastasis. Proc Natl Acad Sci USA, 103 (24): 9023-8. [PMID:16757564]
114. Yang MY, Hilton MB, Seaman S, Haines DC, Nagashima K, Burks CM, Tessarollo L, Ivanova PT, Brown HA, Umstead TM et al.. (2013) Essential regulation of lung surfactant homeostasis by the orphan G protein-coupled receptor GPR116. Cell Rep, 3 (5): 1457-64. [PMID:23684610]
115. Yeung J, Adili R, Stringham EN, Luo R, Vizurraga A, Rosselli-Murai LK, Stoveken HM, Yu M, Piao X, Holinstat M et al.. (2020) GPR56/ADGRG1 is a platelet collagen-responsive GPCR and hemostatic sensor of shear force. Proc Natl Acad Sci U S A, 117 (45): 28275-28286. [PMID:33097663]
116. Yona S, Lin HH, Siu WO, Gordon S, Stacey M. (2008) Adhesion-GPCRs: emerging roles for novel receptors. Trends Biochem Sci, 33 (10): 491-500. [PMID:18789697]
117. Zhang DL, Sun YJ, Ma ML, Wang YJ, Lin H, Li RR, Liang ZL, Gao Y, Yang Z, He DF et al.. (2018) Gq activity- and β-arrestin-1 scaffolding-mediated ADGRG2/CFTR coupling are required for male fertility. Elife, 7. [PMID:29393851]
118. Zhou Y, Nathans J. (2014) Gpr124 controls CNS angiogenesis and blood-brain barrier integrity by promoting ligand-specific canonical wnt signaling. Dev Cell, 31 (2): 248-56. [PMID:25373781]
119. Zhu D, Osuka S, Zhang Z, Reichert ZR, Yang L, Kanemura Y, Jiang Y, You S, Zhang H, Devi NS et al.. (2018) BAI1 Suppresses Medulloblastoma Formation by Protecting p53 from Mdm2-Mediated Degradation. Cancer Cell, 33 (6): 1004-1016.e5. [PMID:29894688]
120. Zhu X, Qian Y, Li X, Xu Z, Xia R, Wang N, Liang J, Yin H, Zhang A, Guo C et al.. (2022) Structural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling. Nat Commun, 13 (1): 5513. [PMID:36127364]
121. Zuko A, Oguro-Ando A, Post H, Taggenbrock RL, van Dijk RE, Altelaar AF, Heck AJ, Petrenko AG, van der Zwaag B, Shimoda Y et al.. (2016) Association of Cell Adhesion Molecules Contactin-6 and Latrophilin-1 Regulates Neuronal Apoptosis. Front Mol Neurosci, 9: 143. [PMID:28018171]
NC-IUPHAR subcommittee and family contributors
|
Demet Arac-Ozkan
Gabriela Aust
Tom I. Bonner
Heike Cappallo-Obermann
Caroline Formstone
Jörg Hamann
Breanne Harty
Henrike Heyne
Christiane Kirchhoff
Barbara Knapp
Arunkumar Krishnan
Tobias Langenhan
Diana Le Duc
Hsi-Hsien Lin
David C. Martinelli
Kelly Monk
Xianhua Piao
Simone Prömel
Helgi Schiöth
Torsten Schöneberg
Kathleen Singer
Martin Stacey
Yuri Ushkaryov
Uwe Wolfrum
Lei Xu |
How to cite this family page
Database page citation (select format):
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Christopoulos A, Davenport AP, Kelly E, Mathie AA, Peters JA, Veale EL, Armstrong JF, Faccenda E, Harding SD, Davies JA et al. (2023) The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors. Br J Pharmacol. 180 Suppl 2:S23-S144.
This work is licensed under a Creative Commons Attribution-ShareAlike 4.0 International License