8fd7

From Proteopedia

Structure of the human L-type voltage-gated calcium channel Cav1.2 complexed with gabapentin

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.
Method:	Electron Microscopy, Resolution 3.1Å
Ligands:	CA, CLR, GBN, NA, NAG, WO9, YSW
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.

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Citations

3 reviews cite this structure

Peptide and Peptidomimetic Inhibitors Targeting the Interaction of Collapsin Response Mediator Protein 2 with the N-Type Calcium Channel for Pain Relief.

Perez-Miller et al. (2024)

2 more

6 other articles

No citations found

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

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

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PDB ID 8fd7

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8fd7

From Proteopedia

Structure of the human L-type voltage-gated calcium channel Cav1.2 complexed with gabapentin

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

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