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_0295 | Potassium channel subfamily K member 5 | Homo sapiens (Human) | O95279 | KCNK5; TASK2 |
| ICDB_Pro_1713 | Potassium channel subfamily K member 6 | Homo sapiens (Human) | Q9Y257 | KCNK6; TOSS; TWIK2 |
| ICDB_Pro_1714 | Potassium channel subfamily K member 7 | Homo sapiens (Human) | Q9Y2U2 | KCNK7 |
| ICDB_Pro_1733 | Potassium channel subfamily K member 7 | Mus musculus (Mouse) | Q9Z2T1 | Kcnk7; Dpkch3; Kcnk6; Kcnk8; Knot1 |
| ICDB_Pro_1059 | Potassium channel subfamily K member 9 | Xenopus laevis (African clawed frog) | Q63ZI0 | kcnk9 |
| ICDB_Pro_0929 | Potassium channel subfamily K member 9 | Mus musculus (Mouse) | Q3LS21 | Kcnk9; Task3 |
| ICDB_Pro_1485 | Potassium channel subfamily K member 9 | Rattus norvegicus (Rat) | Q9ES08 | Kcnk9; Task3 |
| ICDB_Pro_1544 | Potassium channel subfamily K member 9 | Cavia porcellus (Guinea pig) | Q9JL58 | KCNK9; TASK3 |
| ICDB_Pro_1579 | Potassium channel subfamily K member 9 | Homo sapiens (Human) | Q9NPC2 | KCNK9; TASK3 |
| ICDB_Pro_0856 | TWiK family of potassium channels protein 12 | Caenorhabditis elegans | Q19907 | twk-12;F29F11.4 |