The Polysite Pharmacology of TREK K2P Channels.
Sign Up to like & getrecommendations! Published in 2021 at "Advances in experimental medicine and biology"
DOI: 10.1007/978-981-16-4254-8_4
Abstract: K2P (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 K2Ps have… read more here.
Keywords: channel; function; trek; polysite pharmacology ... See more keywords
Discovery of ONO-TR-772 (VU6018042): A Highly Selective and CNS Penetrant TREK Inhibitor in Vivo Tool Compound
Sign Up to like & getrecommendations! Published in 2025 at "ACS Medicinal Chemistry Letters"
DOI: 10.1021/acsmedchemlett.5c00215
Abstract: Herein we describe our continuing work on the K2P family of potassium ion channels with the chemical optimization of a selective and CNS penetrant series of TREK inhibitors, culminating in the discovery of ONO-TR-772 (VU6018042).… read more here.
Keywords: selective cns; ono 772; trek; cns penetrant ... See more keywords
Tension activation of mechanosensitive two-pore domain K+ channels TRAAK, TREK-1, and TREK-2
Sign Up to like & getrecommendations! Published in 2024 at "Nature Communications"
DOI: 10.1038/s41467-024-47208-5
Abstract: TRAAK, TREK-1, and TREK-2 are mechanosensitive two-pore domain K+ (K2P) channels that contribute to action potential propagation, sensory transduction, and muscle contraction. While structural and functional studies have led to models that explain their mechanosensitivity,… read more here.
Keywords: traak trek; two pore; trek; trek trek ... See more keywords
Atomistic mechanism of coupling between cytosolic sensor domain and selectivity filter in TREK K2P channels
Sign Up to like & getrecommendations! Published in 2024 at "Nature Communications"
DOI: 10.1038/s41467-024-48823-y
Abstract: The two-pore domain potassium (K2P) channels TREK-1 and TREK-2 link neuronal excitability to a variety of stimuli including mechanical force, lipids, temperature and phosphorylation. This regulation involves the C-terminus as a polymodal stimulus sensor and… read more here.
Keywords: filter; trek; selectivity filter; mechanism ... See more keywords
Interaction of cochlin and mechanosensitive channel TREK-1 in trabecular meshwork cells influences the regulation of intraocular pressure
Sign Up to like & getrecommendations! Published in 2017 at "Scientific Reports"
DOI: 10.1038/s41598-017-00430-2
Abstract: In the eye, intraocular pressure (IOP) is tightly regulated and its persistent increase leads to ocular hypertension and glaucoma. We have previously shown that trabecular meshwork (TM) cells might detect aqueous humor fluid shear stress… read more here.
Keywords: intraocular pressure; trabecular meshwork; meshwork cells; trek ... See more keywords
TREK-1 and TREK-2 knockout mice are not resistant to halothane or isoflurane.
Sign Up to like & getrecommendations! Published in 2023 at "Anesthesiology"
DOI: 10.1097/aln.0000000000004577
Abstract: Background: A variety of molecular targets for volatile anesthetics have been suggested, including the anesthetic-sensitive potassium leak channel, TREK-1. Knockout of TREK-1 is reported to render mice resistant to volatile anesthetics, making TREK-1 channels compelling… read more here.
Keywords: minimum alveolar; isoflurane; halothane; trek trek ... See more keywords
Deficiency of TREK‐1 potassium channel exacerbates secondary injury following spinal cord injury in mice
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Neurochemistry"
DOI: 10.1111/jnc.13980
Abstract: Spinal cord injury (SCI) involves complex pathological process which can be complicated by secondary injury. TREK‐1 is a member of the two‐pore domain potassium (K2P) channel family, which can be modulated by a number of… read more here.
Keywords: mice; trek; injury; deficiency ... See more keywords
The two-pore domain potassium channel TREK-1 mediates cardiac fibrosis and diastolic dysfunction
Sign Up to like & getrecommendations! Published in 2018 at "Journal of Clinical Investigation"
DOI: 10.1172/jci95945
Abstract: Cardiac two-pore domain potassium channels (K2P) exist in organisms from Drosophila to humans; however, their role in cardiac function is not known. We identified a K2P gene, CG8713 (sandman), in a Drosophila genetic screen and… read more here.
Keywords: dysfunction; two pore; pore domain; domain potassium ... See more keywords
Esketamine reduces postoperative depression in breast cancer through TREK-1 channel inhibition and neurotransmitter modulation
Sign Up to like & getrecommendations! Published in 2025 at "Cancer Cell International"
DOI: 10.1186/s12935-025-03664-7
Abstract: Postoperative depression significantly affects the quality of life of breast cancer patients. This study explores the potential therapeutic effects of esketamine on postoperative depression through modulation of the TREK-1 two-pore domain potassium channel. We analyzed… read more here.
Keywords: cancer; postoperative depression; breast cancer; trek ... See more keywords
Deficiency of TREK-1 potassium channel exacerbates blood-brain barrier damage and neuroinflammation after intracerebral hemorrhage in mice
Sign Up to like & getrecommendations! Published in 2019 at "Journal of Neuroinflammation"
DOI: 10.1186/s12974-019-1485-5
Abstract: BackgroundIntracerebral hemorrhage (ICH) is a devastating medical emergency with high mortality and severe neurological deficit. ICH-related poor outcomes are due to a combination of pathological processes that could be complicated by secondary insults. TWIK-related K+… read more here.
Keywords: blood brain; intracerebral hemorrhage; hemorrhage; trek ... See more keywords
Sodium permeable and “hypersensitive” TREK‐1 channels cause ventricular tachycardia
Sign Up to like & getrecommendations! Published in 2017 at "EMBO Molecular Medicine"
DOI: 10.15252/emmm.201606690
Abstract: In a patient with right ventricular outflow tract (RVOT) tachycardia, we identified a heterozygous point mutation in the selectivity filter of the stretch‐activated K2P potassium channel TREK‐1 (KCNK2 or K2P2.1). This mutation introduces abnormal sodium… read more here.
Keywords: stretch; sodium permeable; tachycardia; trek ... See more keywords