Structure of the Nicotinic Receptor Acetylcholine-binding Site
نویسندگان
چکیده
منابع مشابه
Structure-activity relationship and site of binding of polyamine derivatives at the nicotinic acetylcholine receptor.
Several wasp venoms contain philanthotoxins (PhTXs), natural polyamine amides, which act as noncompetitive inhibitors (NCIs) on the nicotinic acetylcholine receptor (nAChR). Effects of varying the structure of PhTXs and poly(methylene tetramine)s on the binding affinity have been investigated. Using the fluorescent NCI ethidium in a displacement assay Kapp values of these compounds have been de...
متن کاملLocation of the polyamine binding site in the vestibule of the nicotinic acetylcholine receptor ion channel.
To map the structure of a ligand-gated ion channel, we used the photolabile polyamine-containing toxin MR44 as photoaffinity label. MR44 binds with high affinity to the nicotinic acetylcholine receptor in its closed channel conformation. The binding stoichiometry was two molecules of MR44 per receptor monomer. Upon UV irradiation of the receptor-ligand complex, (125)I-MR44 was incorporated into...
متن کاملAn allosteric binding site of the α7 nicotinic acetylcholine receptor revealed in a humanized acetylcholine-binding protein
Nicotinic acetylcholine receptors (nAChRs) belong to the family of pentameric ligand-gated ion channels and mediate fast excitatory transmission in the central and peripheral nervous systems. Among the different existing receptor subtypes, the homomeric α7 nAChR has attracted considerable attention because of its possible implication in several neurological and psychiatric disorders, including ...
متن کاملCharacterization of the dizocilpine binding site on the nicotinic acetylcholine receptor.
Although the dissociative anesthetic dizocilpine [(+)-MK-801] inhibits nicotinic acetylcholine receptor (AChR) function in a noncompetitive manner, the location of the dizocilpine binding site(s) has yet to be clearly established. Thus, to characterize the binding site for dizocilpine on the AChR we examined 1) the dissociation constant (K(d)) and stoichiometry of [(3)H]dizocilpine binding; 2) ...
متن کاملLocalization of the quinacrine binding site on the nicotinic acetylcholine receptor
The high-affinity uptake of phosphate in the yeast Saccharomyces cerevisiae is mediated via the Pho84p which catalyzes a phosphate uptake in symport with H+ at acidic conditions or by Pho89p which is Na+-coupled and active at more alkaline conditions. These proteins are synthesized and active when the cell meets limitations in available external phosphate [I]. Based on a similar phenotype of a ...
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ژورنال
عنوان ژورنال: Journal of Biological Chemistry
سال: 1995
ISSN: 0021-9258
DOI: 10.1074/jbc.270.7.3160