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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
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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 [30,117]. Several receptors have been suggested to function as mechanosensors [13,72,88,111]. Cryo-EM structures of the 7-transmembrane domain of several adhesion GPCRs have been determined recently [6,54,74-75,81-82,113,121]. The nomenclature of these receptors was revised in 2015 as recommended by NC-IUPHAR and the Adhesion GPCR Consortium [34].
Receptors
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ADGRA1
C
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ADGRA2
C
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ADGRA3
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ADGRB1
C
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ADGRB2
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ADGRB3
C
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CELSR1 / ADGRC1
C
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CELSR2 / ADGRC2
C
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CELSR3 / ADGRC3
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ADGRD1
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ADGRD2
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ADGRE1
C
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ADGRE2
C
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ADGRE3
C
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ADGRE4P
C
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ADGRE5
C
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ADGRF1
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ADGRF2
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ADGRF3
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ADGRF4
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ADGRF5
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ADGRG1
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ADGRG2
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ADGRG3
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ADGRG4
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ADGRG5
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ADGRG6
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ADGRG7
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ADGRL1
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ADGRL2
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ADGRL3
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ADGRL4
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ADGRV1
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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]
Dates AN, Jones DTD, Smith JS, Skiba MA, Rich MF, Burruss MM, Kruse AC, Blacklow SC. (2024) Heterogeneity of tethered agonist signaling in adhesion G protein-coupled receptors. Cell Chem Biol, 31 (8): 1542-1553.e4. [PMID:38608683]
* 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
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65. 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]
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67. 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]
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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.
