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7xbd

From Proteopedia

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Current revision

Cryo-EM structure of human galanin receptor 2

Structural highlights

7xbd is a 6 chain structure with sequence from Homo sapiens and Mus musculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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]

Publication Abstract from PubMed

Galanin is a neuropeptide expressed in the central and peripheral nervous systems, where it regulates various processes including neuroendocrine release, cognition, and nerve regeneration. Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts to treat diseases including Alzheimer's disease, anxiety, and addiction. To understand the basis of the ligand preferences of the receptors and to assist structure-based drug design, we used cryo-electron microscopy (cryo-EM) to solve the molecular structure of GALR2 bound to galanin and a cognate heterotrimeric G-protein, providing a molecular view of the neuropeptide binding site. Mutant proteins were assayed to help reveal the basis of ligand specificity, and structural comparison between the activated GALR2 and inactive hbeta2AR was used to relate galanin binding to the movements of transmembrane (TM) helices and the G-protein interface.

Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand specificity and how binding affects the G-protein interface.,Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY PLoS Biol. 2022 Aug 1;20(8):e3001714. doi: 10.1371/journal.pbio.3001714., eCollection 2022 Aug. PMID:35913979^[7]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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
↑ Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY. Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand specificity and how binding affects the G-protein interface. PLoS Biol. 2022 Aug 1;20(8):e3001714. doi: 10.1371/journal.pbio.3001714., eCollection 2022 Aug. PMID:35913979 doi:http://dx.doi.org/10.1371/journal.pbio.3001714

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/7xbd"

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
-The entry 7xbd is ON HOLD
+==Cryo-EM structure of human galanin receptor 2==
+<StructureSection load='7xbd' size='340' side='right'caption='[[7xbd]], [[Resolution|resolution]] 3.11&Aring;' scene=''>
+== Structural highlights ==
+<table><tr><td colspan='2'>[[7xbd]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7XBD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7XBD FirstGlance]. <br>
+</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7xbd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7xbd OCA], [https://pdbe.org/7xbd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7xbd RCSB], [https://www.ebi.ac.uk/pdbsum/7xbd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7xbd ProSAT]</span></td></tr>
+</table>
+== Function ==
+[[https://www.uniprot.org/uniprot/GALR2_HUMAN 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)).<ref>PMID:24517231</ref> <ref>PMID:25691535</ref> <ref>PMID:9480833</ref> <ref>PMID:9685625</ref> <ref>PMID:9832121</ref> <ref>PMID:9880084</ref>
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+Galanin is a neuropeptide expressed in the central and peripheral nervous systems, where it regulates various processes including neuroendocrine release, cognition, and nerve regeneration. Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts to treat diseases including Alzheimer's disease, anxiety, and addiction. To understand the basis of the ligand preferences of the receptors and to assist structure-based drug design, we used cryo-electron microscopy (cryo-EM) to solve the molecular structure of GALR2 bound to galanin and a cognate heterotrimeric G-protein, providing a molecular view of the neuropeptide binding site. Mutant proteins were assayed to help reveal the basis of ligand specificity, and structural comparison between the activated GALR2 and inactive hbeta2AR was used to relate galanin binding to the movements of transmembrane (TM) helices and the G-protein interface.
-Authors:
+Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of ligand specificity and how binding affects the G-protein interface.,Heo Y, Ishimoto N, Jeon YE, Yun JH, Ohki M, Anraku Y, Sasaki M, Kita S, Fukuhara H, Ikuta T, Kawakami K, Inoue A, Maenaka K, Tame JRH, Lee W, Park SY PLoS Biol. 2022 Aug 1;20(8):e3001714. doi: 10.1371/journal.pbio.3001714., eCollection 2022 Aug. PMID:35913979<ref>PMID:35913979</ref>
-Description:
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-[[Category: Unreleased Structures]]
+</div>
+<div class="pdbe-citations 7xbd" style="background-color:#fffaf0;"></div>
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Homo sapiens]]
+[[Category: Large Structures]]
+[[Category: Mus musculus]]
+[[Category: Ishimoto N]]
+[[Category: Kita S]]
+[[Category: Park SY]]

7xbd

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Current revision

Cryo-EM structure of human galanin receptor 2

Structural highlights

Function

Publication Abstract from PubMed

References

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