Breaking barriers to novel analgesic drug development
Acute and chronic pain complaints, although common, are generally poorly served by
existing therapies. This unmet clinical need reflects a failure to develop novel classes of …
existing therapies. This unmet clinical need reflects a failure to develop novel classes of …
Regulating excitability of peripheral afferents: emerging ion channel targets
The transmission and processing of pain signals relies critically on the activities of ion
channels that are expressed in afferent pain fibers. This includes voltage-gated channels, as …
channels that are expressed in afferent pain fibers. This includes voltage-gated channels, as …
Parkinson's disease-risk protein TMEM175 is a proton-activated proton channel in lysosomes
Lysosomes require an acidic lumen between pH 4.5 and 5.0 for effective digestion of
macromolecules. This pH optimum is maintained by proton influx produced by the V-ATPase …
macromolecules. This pH optimum is maintained by proton influx produced by the V-ATPase …
High efficiency pure blue thermally activated delayed fluorescence molecules having 10 H-phenoxaborin and acridan units
Highly efficient blue thermally activated delayed fluorescence molecules having 10H-
phenoxaborin and acridan units were reported. Pure blue emission peaking at around 450 …
phenoxaborin and acridan units were reported. Pure blue emission peaking at around 450 …
K2P2. 1 (TREK-1)-activator complexes reveal a cryptic selectivity filter binding site
Monday, February 19, 2018 303a neuronal excitability, respond to lipids, temperature and
mechanical stretch, and influence pain, temperature perception and anaesthetic responses …
mechanical stretch, and influence pain, temperature perception and anaesthetic responses …
The family of K2P channels: salient structural and functional properties
S Feliciangeli, FC Chatelain, D Bichet… - The Journal of …, 2015 - Wiley Online Library
Potassium channels participate in many biological functions, from ion homeostasis to
generation and modulation of the electrical membrane potential. They are involved in a …
generation and modulation of the electrical membrane potential. They are involved in a …
Cardiac mechano-gated ion channels and arrhythmias
Mechanical forces will have been omnipresent since the origin of life, and living organisms
have evolved mechanisms to sense, interpret, and respond to mechanical stimuli. The …
have evolved mechanisms to sense, interpret, and respond to mechanical stimuli. The …
A pharmacological master key mechanism that unlocks the selectivity filter gate in K+ channels
Potassium (K+) channels have been evolutionarily tuned for activation by diverse biological
stimuli, and pharmacological activation is thought to target these specific gating …
stimuli, and pharmacological activation is thought to target these specific gating …
Potassium channel TASK-5 forms functional heterodimers with TASK-1 and TASK-3 to break its silence
S Rinné, F Schick, K Vowinkel, S Schütte… - Nature …, 2024 - nature.com
Abstract TASK-5 (KCNK15) belongs to the acid-sensitive subfamily of two-pore domain
potassium (K2P) channels, which includes TASK-1 and TASK-3. TASK-5 stands out as K2P …
potassium (K2P) channels, which includes TASK-1 and TASK-3. TASK-5 stands out as K2P …
Role of TREK-1 in health and disease, focus on the central nervous system
TREK-1 is the most studied background K2P channel. Its main role is to control cell
excitability and maintain the membrane potential below the threshold of depolarization …
excitability and maintain the membrane potential below the threshold of depolarization …