8fd7
From Proteopedia
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[8fd7]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8FD7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8FD7 FirstGlance]. <br> | <table><tr><td colspan='2'>[[8fd7]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Oryctolagus_cuniculus Oryctolagus cuniculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8FD7 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8FD7 FirstGlance]. <br> | ||
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=GBN:[1-(AMINOMETHYL)CYCLOHEXYL]ACETIC+ACID'>GBN</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=WO9:( | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">Electron Microscopy, [[Resolution|Resolution]] 3.1Å</td></tr> |
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=GBN:[1-(AMINOMETHYL)CYCLOHEXYL]ACETIC+ACID'>GBN</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=WO9:[(2~{R})-3-[2-azanylethoxy(oxidanyl)phosphoryl]oxy-2-dodecanoyloxy-propyl]+heptadecanoate'>WO9</scene>, <scene name='pdbligand=YSW:(2S)-3-{[(R)-(2-aminoethoxy)(hydroxy)phosphoryl]oxy}-2-(dodecanoyloxy)propyl+dodecanoate'>YSW</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=8fd7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8fd7 OCA], [https://pdbe.org/8fd7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8fd7 RCSB], [https://www.ebi.ac.uk/pdbsum/8fd7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8fd7 ProSAT]</span></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=8fd7 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8fd7 OCA], [https://pdbe.org/8fd7 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8fd7 RCSB], [https://www.ebi.ac.uk/pdbsum/8fd7 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8fd7 ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
[https://www.uniprot.org/uniprot/CA2D1_RABIT CA2D1_RABIT] The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. Plays an important role in excitation-contraction coupling. | [https://www.uniprot.org/uniprot/CA2D1_RABIT CA2D1_RABIT] The alpha-2/delta subunit of voltage-dependent calcium channels regulates calcium current density and activation/inactivation kinetics of the calcium channel. Plays an important role in excitation-contraction coupling. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Gabapentinoid drugs for pain and anxiety act on the Ca(V)alpha(2)delta-1 and Ca(V)alpha(2)delta-2 subunits of high-voltage-activated calcium channels (Ca(V)1s and Ca(V)2s). Here we present the cryo-EM structure of the gabapentin-bound brain and cardiac Ca(V)1.2/Ca(V)beta(3)/Ca(V)alpha(2)delta-1 channel. The data reveal a binding pocket in the Ca(V)alpha(2)delta-1 dCache1 domain that completely encapsulates gabapentin and define Ca(V)alpha(2)delta isoform sequence variations that explain the gabapentin binding selectivity of Ca(V)alpha(2)delta-1 and Ca(V)alpha(2)delta-2. | ||
| + | |||
| + | Structural basis for Ca(V)alpha(2)delta:gabapentin binding.,Chen Z, Mondal A, Minor DL Jr Nat Struct Mol Biol. 2023 Jun;30(6):735-739. doi: 10.1038/s41594-023-00951-7. , Epub 2023 Mar 27. PMID:36973510<ref>PMID:36973510</ref> | ||
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| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 8fd7" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[Ion channels 3D structures|Ion channels 3D structures]] | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
Current revision
Structure of the human L-type voltage-gated calcium channel Cav1.2 complexed with gabapentin
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