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==Crystal structure of a mutant binding protein (5HTBP-AChBP) in complex with serotonin (5-hydroxytryptamine)== | ==Crystal structure of a mutant binding protein (5HTBP-AChBP) in complex with serotonin (5-hydroxytryptamine)== | ||
<StructureSection load='2ymd' size='340' side='right' caption='[[2ymd]], [[Resolution|resolution]] 1.96Å' scene=''> | <StructureSection load='2ymd' size='340' side='right'caption='[[2ymd]], [[Resolution|resolution]] 1.96Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[2ymd]] is a 10 chain structure with sequence from [ | <table><tr><td colspan='2'>[[2ymd]] is a 10 chain structure with sequence from [https://en.wikipedia.org/wiki/Aplysia_californica Aplysia californica]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2YMD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2YMD FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=SRO:SEROTONIN'>SRO</scene> | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.96Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=SRO:SEROTONIN'>SRO</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=2ymd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ymd OCA], [https://pdbe.org/2ymd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2ymd RCSB], [https://www.ebi.ac.uk/pdbsum/2ymd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2ymd ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | |||
[https://www.uniprot.org/uniprot/Q8WSF8_APLCA Q8WSF8_APLCA] | |||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
| Line 17: | Line 19: | ||
</div> | </div> | ||
<div class="pdbe-citations 2ymd" style="background-color:#fffaf0;"></div> | <div class="pdbe-citations 2ymd" style="background-color:#fffaf0;"></div> | ||
==See Also== | |||
*[[Acetylcholine binding protein 3D structures|Acetylcholine binding protein 3D structures]] | |||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: | [[Category: Aplysia californica]] | ||
[[Category: Brams | [[Category: Large Structures]] | ||
[[Category: Danielson | [[Category: Brams M]] | ||
[[Category: Elk | [[Category: Danielson UH]] | ||
[[Category: Geitmann | [[Category: Elk Rv]] | ||
[[Category: Guskov | [[Category: Geitmann M]] | ||
[[Category: Kesters | [[Category: Guskov A]] | ||
[[Category: Lummis | [[Category: Kesters D]] | ||
[[Category: Smit | [[Category: Lummis SCR]] | ||
[[Category: Spurny | [[Category: Smit AB]] | ||
[[Category: Thompson | [[Category: Spurny R]] | ||
[[Category: Ulens | [[Category: Thompson AJ]] | ||
[[Category: Villalgordo | [[Category: Ulens C]] | ||
[[Category: Villalgordo JM]] | |||
Latest revision as of 13:55, 20 December 2023
Crystal structure of a mutant binding protein (5HTBP-AChBP) in complex with serotonin (5-hydroxytryptamine)Crystal structure of a mutant binding protein (5HTBP-AChBP) in complex with serotonin (5-hydroxytryptamine)
Structural highlights
FunctionPublication Abstract from PubMedThe 5-HT3 receptor is a pentameric serotonin-gated ion channel, which mediates rapid excitatory neurotransmission and is the target of a therapeutically important class of anti-emetic drugs, such as granisetron. We report crystal structures of a binding protein engineered to recognize the agonist serotonin and the antagonist granisetron with affinities comparable to the 5-HT3 receptor. In the serotonin-bound structure, we observe hydrophilic interactions with loop E-binding site residues, which might enable transitions to channel opening. In the granisetron-bound structure, we observe a critical cation-pi interaction between the indazole moiety of the ligand and a cationic centre in loop D, which is uniquely present in the 5-HT3 receptor. We use a series of chemically tuned granisetron analogues to demonstrate the energetic contribution of this electrostatic interaction to high-affinity ligand binding in the human 5-HT3 receptor. Our study offers the first structural perspective on recognition of serotonin and antagonism by anti-emetics in the 5-HT3 receptor. Structural basis of ligand recognition in 5-HT3 receptors.,Kesters D, Thompson AJ, Brams M, van Elk R, Spurny R, Geitmann M, Villalgordo JM, Guskov A, Helena Danielson U, Lummis SC, Smit AB, Ulens C EMBO Rep. 2012 Nov 30. doi: 10.1038/embor.2012.189. PMID:23196367[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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