5g53: Difference between revisions

Latest revision as of 13:39, 26 July 2023

Structure of the adenosine A2A receptor bound to an engineered G protein

Structural highlights

5g53 is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 3.4Å
Ligands:	GDP, NEC, SOG
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

AA2AR_HUMAN Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.

Publication Abstract from PubMed

G-protein-coupled receptors (GPCRs) are essential components of the signalling network throughout the body. To understand the molecular mechanism of G-protein-mediated signalling, solved structures of receptors in inactive conformations and in the active conformation coupled to a G protein are necessary. Here we present the structure of the adenosine A(2A) receptor (A(2A)R) bound to an engineered G protein, mini-Gs, at 3.4 A resolution. Mini-Gs binds to A(2A)R through an extensive interface (1,048 A2) that is similar, but not identical, to the interface between Gs and the beta2-adrenergic receptor. The transition of the receptor from an agonist-bound active-intermediate state to an active G-protein-bound state is characterized by a 14 A shift of the cytoplasmic end of transmembrane helix 6 (H6) away from the receptor core, slight changes in the positions of the cytoplasmic ends of H5 and H7 and rotamer changes of the amino acid side chains Arg3.50, Tyr5.58 and Tyr7.53. There are no substantial differences in the extracellular half of the receptor around the ligand binding pocket. The A(2A)R-mini-Gs structure highlights both the diversity and similarity in G-protein coupling to GPCRs and hints at the potential complexity of the molecular basis for G-protein specificity.

Structure of the adenosine A(2A) receptor bound to an engineered G protein.,Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG Nature. 2016 Aug 4;536(7614):104-7. PMID:27462812^[1]

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

References

↑ Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG. Structure of the adenosine A(2A) receptor bound to an engineered G protein. Nature. 2016 Aug 4;536(7614):104-7. PMID:27462812 doi:https://dx.doi.org/10.1038/nature18966

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OCA

[1] Carpenter B, Nehme R, Warne T, Leslie AG, Tate CG. Structure of the adenosine A(2A) receptor bound to an engineered G protein. Nature. 2016 Aug 4;536(7614):104-7. PMID:27462812 doi:https://dx.doi.org/10.1038/nature18966

[1]

@@ Line 3: / Line 3: @@
 <StructureSection load='5g53' size='340' side='right'caption='[[5g53]], [[Resolution|resolution]] 3.40&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[5g53]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5G53 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5G53 FirstGlance]. <br>
+<table><tr><td colspan='2'>[[5g53]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5G53 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5G53 FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=NEC:N-ETHYL-5-CARBOXAMIDO+ADENOSINE'>NEC</scene>, <scene name='pdbligand=SOG:2-HYDROXYMETHYL-6-OCTYLSULFANYL-TETRAHYDRO-PYRAN-3,4,5-TRIOL'>SOG</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 3.4&#8491;</td></tr>
-<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5g53 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5g53 OCA], [http://pdbe.org/5g53 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5g53 RCSB], [http://www.ebi.ac.uk/pdbsum/5g53 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5g53 ProSAT]</span></td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=NEC:N-ETHYL-5-CARBOXAMIDO+ADENOSINE'>NEC</scene>, <scene name='pdbligand=SOG:2-HYDROXYMETHYL-6-OCTYLSULFANYL-TETRAHYDRO-PYRAN-3,4,5-TRIOL'>SOG</scene></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=5g53 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5g53 OCA], [https://pdbe.org/5g53 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5g53 RCSB], [https://www.ebi.ac.uk/pdbsum/5g53 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5g53 ProSAT]</span></td></tr>
 </table>
-== Disease ==
-[[http://www.uniprot.org/uniprot/GNAS2_HUMAN GNAS2_HUMAN]] Pseudopseudohypoparathyroidism;Pseudohypoparathyroidism type 1A;Progressive osseous heteroplasia;Polyostotic fibrous dysplasia;Monostotic fibrous dysplasia;Pseudohypoparathyroidism type 1C;Pseudohypoparathyroidism type 1B;McCune-Albright syndrome. The disease is caused by mutations affecting the gene represented in this entry.  The disease is caused by mutations affecting the gene represented in this entry.  The disease is caused by mutations affecting the gene represented in this entry.  The disease is caused by mutations affecting the gene represented in this entry.  The disease is caused by mutations affecting the gene represented in this entry.  The disease is caused by mutations affecting the gene represented in this entry.  The disease is caused by mutations affecting the gene represented in this entry. Most affected individuals have defects in methylation of the gene. In some cases microdeletions involving the STX16 appear to cause loss of methylation at exon A/B of GNAS, resulting in PHP1B. Paternal uniparental isodisomy have also been observed.  The disease is caused by mutations affecting the gene represented in this entry.  The disease is caused by mutations affecting the gene represented in this entry.
 == Function ==
-[[http://www.uniprot.org/uniprot/AA2AR_HUMAN AA2AR_HUMAN]] Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase. [[http://www.uniprot.org/uniprot/GNAS2_HUMAN GNAS2_HUMAN]] Guanine nucleotide-binding proteins (G proteins) function as transducers in numerous signaling pathways controlled by G protein-coupled receptors (GPCRs) (PubMed:17110384). Signaling involves the activation of adenylyl cyclases, resulting in increased levels of the signaling molecule cAMP (PubMed:26206488, PubMed:8702665). GNAS functions downstream of several GPCRs, including beta-adrenergic receptors (PubMed:21488135). Stimulates the Ras signaling pathway via RAPGEF2 (PubMed:12391161).<ref>PMID:12391161</ref> <ref>PMID:17110384</ref> <ref>PMID:21488135</ref> <ref>PMID:26206488</ref> <ref>PMID:8702665</ref>
+[https://www.uniprot.org/uniprot/AA2AR_HUMAN AA2AR_HUMAN] Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==
@@ Line 27: / Line 26: @@
 __TOC__
 </StructureSection>
-[[Category: Human]]
+[[Category: Homo sapiens]]
 [[Category: Large Structures]]
-[[Category: Carpenter, B]]
+[[Category: Carpenter B]]
-[[Category: Leslie, A G.W]]
+[[Category: Leslie AGW]]
-[[Category: Nehme, R]]
+[[Category: Nehme R]]
-[[Category: Tate, C G]]
+[[Category: Tate CG]]
-[[Category: Warne, T]]
+[[Category: Warne T]]
-[[Category: Adenosine receptor]]
-[[Category: Engineered g protein]]
-[[Category: G protein coupled receptor]]
-[[Category: Gpcr]]
-[[Category: Gpcr-g protein complex]]
-[[Category: Integral membrane protein]]
-[[Category: Mini-g]]
-[[Category: Seven-helix receptor]]
-[[Category: Signaling protein]]

5g53: Difference between revisions

Latest revision as of 13:39, 26 July 2023

Structure of the adenosine A2A receptor bound to an engineered G protein

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

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