Structural and Dynamic View on Interactions of Low-Affmity Drugs with Neuronal Acetylcholine Recepto

来源 :2008中国深圳蛋白质和多肽科学大会 | 被引量 : 0次 | 上传用户:coosmic
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  The hetero-pentameric (α4)2(β2)3 and homo-pentameric (α7)5 neuronal acetylcholine receptors (nAChRs) are representative of two important subtype nAChRs that account for most of high-affinity binding sites in the central nervous system for nicotine and α-bungarotoxin,respectively.Despite their sequence homologous,(α4)2(β2)3 is supersensitive to inhibition by volatile anesthetics,whereas the (α7)5 is insensitive to these low-atfinity drugs.To understand how anesthetics modulate the receptor function,we studied the effects of halothane and isoflurane on full-length transmembrane (TM) domains of (α4)2(β2)3 and (α7)5 in a membrane mimetic environment.
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