7wq4

Galanin-bound galanin receptor 2 in complex with GqGalanin-bound galanin receptor 2 in complex with Gq

Structural highlights

7wq4 is a 6 chain structure with sequence from Bos taurus, Homo sapiens, Lama glama and Rattus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	Electron Microscopy, Resolution 2.6Å
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

GALR2_HUMAN Receptor for the hormone galanin and GALP. Receptor for the hormone spexin-1 (PubMed:24517231). The activity of this receptor is mediated by G proteins that activate the phospholipase C/protein kinase C pathway (via G(q)) and that inhibit adenylyl cyclase (via G(i)).^[1] ^[2] ^[3] ^[4] ^[5] ^[6]

References

↑ Kim DK, Yun S, Son GH, Hwang JI, Park CR, Kim JI, Kim K, Vaudry H, Seong JY. Coevolution of the spexin/galanin/kisspeptin family: Spexin activates galanin receptor type II and III. Endocrinology. 2014 May;155(5):1864-73. doi: 10.1210/en.2013-2106. Epub 2014 Feb , 11. PMID:24517231 doi:http://dx.doi.org/10.1210/en.2013-2106
↑ Guipponi M, Chentouf A, Webling KE, Freimann K, Crespel A, Nobile C, Lemke JR, Hansen J, Dorn T, Lesca G, Ryvlin P, Hirsch E, Rudolf G, Rosenberg DS, Weber Y, Becker F, Helbig I, Muhle H, Salzmann A, Chaouch M, Oubaiche ML, Ziglio S, Gehrig C, Santoni F, Pizzato M, Langel U, Antonarakis SE. Galanin pathogenic mutations in temporal lobe epilepsy. Hum Mol Genet. 2015 Jun 1;24(11):3082-91. doi: 10.1093/hmg/ddv060. Epub 2015 Feb , 17. PMID:25691535 doi:http://dx.doi.org/10.1093/hmg/ddv060
↑ Bloomquist BT, Beauchamp MR, Zhelnin L, Brown SE, Gore-Willse AR, Gregor P, Cornfield LJ. Cloning and expression of the human galanin receptor GalR2. Biochem Biophys Res Commun. 1998 Feb 13;243(2):474-9. PMID:9480833 doi:http://dx.doi.org/S0006-291X(98)98133-5
↑ Fathi Z, Battaglino PM, Iben LG, Li H, Baker E, Zhang D, McGovern R, Mahle CD, Sutherland GR, Iismaa TP, Dickinson KE, Zimanyi IA. Molecular characterization, pharmacological properties and chromosomal localization of the human GALR2 galanin receptor. Brain Res Mol Brain Res. 1998 Jul 15;58(1-2):156-69. PMID:9685625
↑ Kolakowski LF Jr, O'Neill GP, Howard AD, Broussard SR, Sullivan KA, Feighner SD, Sawzdargo M, Nguyen T, Kargman S, Shiao LL, Hreniuk DL, Tan CP, Evans J, Abramovitz M, Chateauneuf A, Coulombe N, Ng G, Johnson MP, Tharian A, Khoshbouei H, George SR, Smith RG, O'Dowd BF. Molecular characterization and expression of cloned human galanin receptors GALR2 and GALR3. J Neurochem. 1998 Dec;71(6):2239-51. doi: 10.1046/j.1471-4159.1998.71062239.x. PMID:9832121 doi:http://dx.doi.org/10.1046/j.1471-4159.1998.71062239.x
↑ Borowsky B, Walker MW, Huang LY, Jones KA, Smith KE, Bard J, Branchek TA, Gerald C. Cloning and characterization of the human galanin GALR2 receptor. Peptides. 1998;19(10):1771-81. doi: 10.1016/s0196-9781(98)00133-8. PMID:9880084 doi:http://dx.doi.org/10.1016/s0196-9781(98)00133-8

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OCA

[1] Kim DK, Yun S, Son GH, Hwang JI, Park CR, Kim JI, Kim K, Vaudry H, Seong JY. Coevolution of the spexin/galanin/kisspeptin family: Spexin activates galanin receptor type II and III. Endocrinology. 2014 May;155(5):1864-73. doi: 10.1210/en.2013-2106. Epub 2014 Feb , 11. PMID:24517231 doi:http://dx.doi.org/10.1210/en.2013-2106

[2] Guipponi M, Chentouf A, Webling KE, Freimann K, Crespel A, Nobile C, Lemke JR, Hansen J, Dorn T, Lesca G, Ryvlin P, Hirsch E, Rudolf G, Rosenberg DS, Weber Y, Becker F, Helbig I, Muhle H, Salzmann A, Chaouch M, Oubaiche ML, Ziglio S, Gehrig C, Santoni F, Pizzato M, Langel U, Antonarakis SE. Galanin pathogenic mutations in temporal lobe epilepsy. Hum Mol Genet. 2015 Jun 1;24(11):3082-91. doi: 10.1093/hmg/ddv060. Epub 2015 Feb , 17. PMID:25691535 doi:http://dx.doi.org/10.1093/hmg/ddv060

[3] Bloomquist BT, Beauchamp MR, Zhelnin L, Brown SE, Gore-Willse AR, Gregor P, Cornfield LJ. Cloning and expression of the human galanin receptor GalR2. Biochem Biophys Res Commun. 1998 Feb 13;243(2):474-9. PMID:9480833 doi:http://dx.doi.org/S0006-291X(98)98133-5

[4] Fathi Z, Battaglino PM, Iben LG, Li H, Baker E, Zhang D, McGovern R, Mahle CD, Sutherland GR, Iismaa TP, Dickinson KE, Zimanyi IA. Molecular characterization, pharmacological properties and chromosomal localization of the human GALR2 galanin receptor. Brain Res Mol Brain Res. 1998 Jul 15;58(1-2):156-69. PMID:9685625

[5] Kolakowski LF Jr, O'Neill GP, Howard AD, Broussard SR, Sullivan KA, Feighner SD, Sawzdargo M, Nguyen T, Kargman S, Shiao LL, Hreniuk DL, Tan CP, Evans J, Abramovitz M, Chateauneuf A, Coulombe N, Ng G, Johnson MP, Tharian A, Khoshbouei H, George SR, Smith RG, O'Dowd BF. Molecular characterization and expression of cloned human galanin receptors GALR2 and GALR3. J Neurochem. 1998 Dec;71(6):2239-51. doi: 10.1046/j.1471-4159.1998.71062239.x. PMID:9832121 doi:http://dx.doi.org/10.1046/j.1471-4159.1998.71062239.x

[6] Borowsky B, Walker MW, Huang LY, Jones KA, Smith KE, Bard J, Branchek TA, Gerald C. Cloning and characterization of the human galanin GALR2 receptor. Peptides. 1998;19(10):1771-81. doi: 10.1016/s0196-9781(98)00133-8. PMID:9880084 doi:http://dx.doi.org/10.1016/s0196-9781(98)00133-8

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