6KZP

calcium channel-ligand

Summary for 6KZP

• Entry DOI: 10.2210/pdb6kzp/pdb
• EMDB information: 0792
• Descriptor: Voltage-dependent T-type calcium channel subunit alpha-1G,Voltage-dependent T-type calcium channel subunit alpha-1G, CALCIUM ION, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... (6 entities in total)
• Functional Keywords: channel, blocker, membrane protein
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 1
• Total formula weight: 247668.56

Authors

Yan, N. (deposition date: 2019-09-25, release date: 2019-12-18, Last modification date: 2024-11-06)

Primary citation

Zhao, Y.,Huang, G.,Wu, Q.,Wu, K.,Li, R.,Lei, J.,Pan, X.,Yan, N.
Cryo-EM structures of apo and antagonist-bound human Cav3.1.
Nature, 576:492-497, 2019

PubMed Abstract: Among the ten subtypes of mammalian voltage-gated calcium (Ca) channels, Ca3.1-Ca3.3 constitute the T-type, or the low-voltage-activated, subfamily, the abnormal activities of which are associated with epilepsy, psychiatric disorders and pain. Here we report the cryo-electron microscopy structures of human Ca3.1 alone and in complex with a highly Ca3-selective blocker, Z944, at resolutions of 3.3 Å and 3.1 Å, respectively. The arch-shaped Z944 molecule reclines in the central cavity of the pore domain, with the wide end inserting into the fenestration on the interface between repeats II and III, and the narrow end hanging above the intracellular gate like a plug. The structures provide the framework for comparative investigation of the distinct channel properties of different Ca subfamilies.

PubMed: 31766050
DOI: 10.1038/s41586-019-1801-3

Experimental method

ELECTRON MICROSCOPY (3.1 Å)