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_0805 | Potassium channel subfamily K member 1 | Bos taurus (Bovine) | Q0P5A0 | KCNK1 |
| ICDB_Pro_1007 | Potassium channel subfamily K member 1 | Pongo abelii (Sumatran orangutan) (Pongo pygmaeus abelii) | Q5RD07 | KCNK1 |
| ICDB_Pro_1016 | Potassium channel subfamily K member 1 | Oryctolagus cuniculus (Rabbit) | Q5UE96 | KCNK1 |
| ICDB_Pro_0167 | Potassium channel subfamily K member 1 | Homo sapiens (Human) | O00180 | KCNK1; HOHO1; KCNO1; TWIK1 |
| ICDB_Pro_0176 | Potassium channel subfamily K member 1 | Mus musculus (Mouse) | O08581 | Kcnk1 |
| ICDB_Pro_1300 | Potassium channel subfamily K member 1 | Cavia porcellus (Guinea pig) | Q8R454 | KCNK1 |
| ICDB_Pro_1734 | Potassium channel subfamily K member 1 | Rattus norvegicus (Rat) | Q9Z2T2 | Kcnk1 |
| ICDB_Pro_0639 | Potassium channel subfamily K member 10 | Homo sapiens (Human) | P57789 | KCNK10; TREK2 |
| ICDB_Pro_1527 | Potassium channel subfamily K member 10 | Rattus norvegicus (Rat) | Q9JIS4 | Kcnk10; Trek2 |
| ICDB_Pro_1483 | Potassium channel subfamily K member 12 | Rattus norvegicus (Rat) | Q9ERS1 | Kcnk12 |