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Example sentences for: nachr
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A disulfide bridge (the so-called cys-loop), present only in the alpha subunits of nAChR, is known to be part of the agonist binding site of the receptor [ 7 ] . This was a clear indication that, in order to build a dimer interface that includes the ligand binding pocket, alpha subunits had to be aligned onto the template monomer presenting a disulfide bridge at the interface (subunit 1).
In recent years, it has become clear that the neuronal nAChR is a valid target against a variety of diseases, including cognitive and attention deficits, Parkinson's disease, anxiety, and pain management [ 3 4 ] ; the addiction liability and other undesirable side-effects of nicotine prohibit the use of this natural product for therapeutic applications, but the active development of nAChR agonists presenting adequate receptor subtype specificity should result in improved pharmacology and potency [ 4 ] . As for most membrane proteins, information on the 3 dimensional structure of the nAChR is limited, and the best experimental structure consists of 4.6 A data from electron microscopy [ 5 ] , a resolution that does not allow for structure-based design approaches.
PKC has been suggested to play a role in synapse stability and signal transduction at the NMJ [ 24 ] . When calcium influx through the nAChR occurs, acetylcholine appears to activate PKC phosphorylation of this receptor [reviewed by [ 31 ] ]. Phorbol ester activation of PKC causes loss of synapses and nAChR [ 49 ] . Because the presynaptic PKCβ fluorescence band parallels the nAChR band (see fig.
Alternatively, immunoreactivity of nAChR was labeled with a N,N'-biscarboxypentyl-5,5'-disulfonatoindodicarbocyanine (Cy5) coupled fluorescent secondary antibody.
Based on data obtained from affinity labeling and site directed mutagenesis studies, several regions of the nicotinic acetylcholine receptor have been implicated in ligand binding [ 10 ] . Six essential loops appear to contribute to the binding site with the position of each loop differing slightly depending on whether the receptor is heteromeric or homomeric [ 4 ] . For homomeric receptors such as the α7 nAChR, the loops are identified as A, B, C, D, E and F [ 4 11 ] . The amino acids that interact with ligands presumably extend into the binding site from these loops.
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