Structural highlights
8fd7 is a 3 chain structure with sequence from Homo sapiens and Oryctolagus cuniculus. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
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| Method: | Electron Microscopy, Resolution 3.1Å |
| Ligands: | , , , , , , |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
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.
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[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
See Also
References
- ↑ Chen Z, Mondal A, Minor DL Jr. Structural basis for Ca(V)α(2)δ:gabapentin binding. Nat Struct Mol Biol. 2023 Jun;30(6):735-739. PMID:36973510 doi:10.1038/s41594-023-00951-7
