Nonstandard abbreviations: GABA: γ-aminobutyric acid TM: transmembrane domain Amil: amiloride ASIC: acid-sensing ion channel GMQ: 2-guanidine-4-methylquinazoline EGTA: ethylene glycol-bis(2-aminoethylether)-N,N,N′,N′-tetraacetic acid HEPES: 2-[4-(2-hydroxyethyl)piperazin-1-yl]ethanesulfonic acid TEA-Cl: tetraethylammonium chloride DMSO: dimethylsulfoxide GLIC: Gloeobacter violaceus pentameric ligand-gated ion channel PAM: positive allosteric modulation
نویسندگان
چکیده
Amil: amiloride ASIC: acid-sensing ion channel GMQ: 2-guanidine-4-methylquinazoline EGTA: ethylene
منابع مشابه
Amiloride and GMQ Allosteric Modulation of the GABA-A r1 Receptor: Influences of the Intersubunit Site s
Amiloride, a diuretic used in the treatment of hypertension and congestive heart failure, and 2-guanidine-4-methylquinazoline (GMQ) are guanidine compounds that modulate acid-sensing ion channels. Both compounds have demonstrated affinity for a variety of membrane proteins, including members of the Cysloop family of ligand-gated ion channels, such as the heteromeric GABA-A abg receptors. The ac...
متن کاملAmiloride and GMQ Allosteric Modulation of the GABA-A r1 Receptor: Influences of the Intersubunit Site
Amiloride, a diuretic used in the treatment of hypertension and congestive heart failure, and 2-guanidine-4-methylquinazoline (GMQ) are guanidine compounds that modulate acid-sensing ion channels. Both compounds have demonstrated affinity for a variety of membrane proteins, including members of the Cysloop family of ligand-gated ion channels, such as the heteromeric GABA-A abg receptors. The ac...
متن کاملAmiloride and GMQ Allosteric Modulation of the GABA-A ρ1 Receptor: Influences of the Intersubunit Site.
Amiloride, a diuretic used in the treatment of hypertension and congestive heart failure, and 2-guanidine-4-methylquinazoline (GMQ) are guanidine compounds that modulate acid-sensing ion channels. Both compounds have demonstrated affinity for a variety of membrane proteins, including members of the Cys-loop family of ligand-gated ion channels, such as the heteromeric GABA-A αβγ receptors. The a...
متن کاملA Nonproton Ligand Sensor in the Acid-Sensing Ion Channel
Acid-sensing ion channels (ASICs) have long been considered as extracellular proton (H(+))-gated cation channels, and peripheral ASIC3 channels seem to be a natural sensor of acidic pain. Here, we report the identification of a nonproton sensor on ASIC3. We show first that 2-guanidine-4-methylquinazoline (GMQ) causes persistent ASIC3 channel activation at the normal pH. Using GMQ as a probe and...
متن کاملA gating mechanism of pentameric ligand-gated ion channels.
Pentameric ligand-gated ion channels (pLGICs) play a central role in intercellular communication in the nervous system and are involved in fundamental processes such as attention, learning, and memory. They are oligomeric protein assemblies that convert a chemical signal into an ion flux through the postsynaptic membrane, but the molecular mechanism of gating ions has remained elusive. Here, we...
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