The Polysite Pharmacology of TREK K_2P Channels.

ABSTRACT: K_2P (KCNK) potassium channels form "background" or "leak" currents that have critical roles in cell excitability control in the brain, cardiovascular system, and somatosensory neurons. Similar to many ion channel families, studies of K_2Ps have been limited by poor pharmacology. Of six K_2P subfamilies, the thermo- and mechanosensitive TREK subfamily comprising K_2P2.1 (TREK-1), K_2P4.1 (TRAAK), and K_2P10.1 (TREK-2) are the first to have structures determined for each subfamily member. These structural studies have revealed key architectural features that underlie K_2P function and have uncovered sites residing at every level of the channel structure with respect to the membrane where small molecules or lipids can cont

SUBMITTER: Pope L 

PROVIDER: S-EPMC8887811 | biostudies-literature | 2021

REPOSITORIES: biostudies-literature