The Primary Information of Tandem Pore Domain Potassium Channel (K2P)

1. Summary

The two-pore-domain or tandem pore domain potassium channels (K2P) are a family of 15 members (K2p1.1, K2p2.1, K2p3.1, K2p4.1, K2p5.1, K2p6.1, K2p7.1, K2p9.1, K2p10.1, K2p12.1, K2p13.1, K2p15.1, K2p16.1, K2p17.1, K2p18.1) that form what is known as leak channels which possess Goldman-Hodgkin-Katz (open) rectification [1].

2. Binding Sites

Ruthenium red binds to the residues (D135 (red sphere) in TREK-2 [2] and E70 (yellow sphere) in TASK-3 [3]) lining the wall of the extracellular ion pathway to inhibit TREK-2 and TASK-3. Mutations of the residues A35, E38 and V42 (black sphere) within the binding site in the extracellular cap of TRAAK significantly increased the TKDC-induced inhibition, indicating that the proposed site was involved in modulating channels. [4] Central cartoon shows the locations of structurally defined K2P small molecule binding sites including the Keystone inhibitor site (white sphere) [5], K2P modulator pocket (grey)[6], Fenestration site (green sphere) [7], Modulatory lipid site (Orange sphere) [8], and Vestibule site (blue) [9].

3. Target List

ICDB_Pro ID Protein Name Organism Uniport Accession Number Gene Name
ICDB_Pro_0854TWiK family of potassium channels protein 18Caenorhabditis elegansQ18120twk-18;C24A3.6
ICDB_Pro_0487TWiK family of potassium channels protein 7Caenorhabditis elegansP34410twk-7;twk-8;F22B7.7
ICDB_Pro_0868TWiK family of potassium channels protein 9Caenorhabditis elegansQ23435twk-9;ZK1251.8
ICDB_Pro_0072TWIK1 (K2P1.1; KCNK1)Caenorhabditis briggsaeA8X8I4twk-12;CBG09670