Spatial Relationships between Drug Binding Sites on the Surface of the Acetylcholine Receptor
Abstract
This report describes the preparation and/or characterization of several fluorescent probes of the muscle-type nicotinic acetylcholine receptor for Torpedo californica. These probes include the following: (1) four fluorescein isothiocyante Naja naja siamensis alpha-toxin 3 derivatives labeled at either lys-23, lys35, lys-49, or lys-69. (2) a tetramethylrhodamine alpha- toxin derivative labeled at lys-23. (3) ethidium bromide, and (4) decidium. With these probes and 6-(5-dimethylaminonaphthalene-1-sulfonamido)hexanoic acid beta(N-trimethylammonium)ester (dansyl-C6-choline) and bis(choline)-N-(4- nitrobenzo-2-oxa 1,3-diazol-7-yl)-iminodiproprionate (BCNI), we estimated the distance between the acetylcholine binding sites and the high-affinity noncompetitive inhibitor site by using fluorescence energy transfer techniques. We, also, estimated the orientation of the snake venom alpha-toxin bound to the acetylcholine receptor with respect to the central ion channel and the plane of the membrane. (js)
Document Details
- Document Type
- Technical Report
- Publication Date
- Feb 13, 1989
- Accession Number
- ADA228229
Entities
People
- David A. Johnson
Organizations
- University of California, Riverside