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Can I read Structure–activity Relationship and Site of Binding of Polyamine Derivatives at the Nicotinic Acetylcholine Receptor on EtoBox?
Structure–activity Relationship and Site of Binding of Polyamine Derivatives at the Nicotinic Acetylcholine Receptor by M. Gabriele Bixel; Michael Krauss; Ying Liu; Maria L. Bolognesi; Michela Rosini; Ian S. Mellor; Peter N. R. Usherwood; Carlo Melchiorre; Koji Nakanishi; Ferdinand Hucho is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Structure–activity Relationship and Site of Binding of Polyamine Derivatives at the Nicotinic Acetylcholine Receptor about?
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 __K__~app~ values of these compounds have been determined. We found that an increase in size of the PhTX's hydrophobic head group significantly increased the binding affinity, while inserting positive charge almost completely destroyed it. Elongating the PhTX polyamine chain by introducing an additional aminomethylene group decreased the binding affinity, whereas a terminal lysine improved it. In general, poly(methylene tetramine)s showed higher binding affinities than PhTX analogues. The stoichiometry of PhTX binding was determined to be two PhTX molecules per receptor monomer. PhTXs appeared to bind to a single class of nonallosterically interacting binding sites and bound PhTX was found to be completely displaced by well‐characterized luminal NCIs. To elucidate the site of PhTX binding, a photolabile, radioactive PhTX derivative wa
Who reads Structure–activity Relationship and Site of Binding of Polyamine Derivatives at the Nicotinic Acetylcholine Receptor?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- M. Gabriele Bixel; Michael Krauss; Ying Liu; Maria L. Bolognesi; Michela Rosini; Ian S. Mellor; Peter N. R. Usherwood; Carlo Melchiorre; Koji Nakanishi; Ferdinand Hucho
- Publisher
- John Wiley and Sons; Springer; Wiley (Blackwell Publishing); Springer-Verlag; Blackwell Publishing Inc.; Springer Verlag; Wiley; Springer Science and Business Media LLC (ISSN 1432-1327)
- Published
- 2000
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Physical Sciences)