Structure-binding relation of philanthotoxins from nicotinic acetylcholine receptor binding assay
Autor: | Xuefei Huang, Seok-Ki Choi, Elizabeth J. Katz, Ying Liu, Koji Nakanishi, Kan Fang, Mohyee E. Eldefrawi, Danwen Huang, Hong Jiang |
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Rok vydání: | 1997 |
Předmět: |
Porphyrins
Stereochemistry Clinical Biochemistry Pharmaceutical Science Wasp Venoms Nicotinic Antagonists Receptors Nicotinic Photoaffinity Labels Torpedo Biochemistry Structure-Activity Relationship Ganglion type nicotinic receptor Drug Discovery Muscarinic acetylcholine receptor M5 Polyamines Animals Frozen Sections Amino Acids Nicotinic Antagonist Molecular Biology Chemistry Ligand binding assay Organic Chemistry Molecular Weight Nicotinic acetylcholine receptor Nicotinic agonist Molecular Medicine Alpha-4 beta-2 nicotinic receptor |
Zdroj: | Bioorganic & Medicinal Chemistry. 5:1969-1988 |
ISSN: | 0968-0896 |
Popis: | Philanthotoxins are noncompetitive inhibitors of the nicotinic acetylcholine receptor and the various glutamate receptors. Analogues carrying photoaffinity labels, fluorine atoms for solid-state NMR studies of ligand/receptor interaction, and large head groups such as porphyrins and planar bulky aromatic rings (BIG analogues) for clarifying mode of entry and orientation of analogues in receptors have been synthesized, assayed against the nicotinic acetylcholine receptor, and brief comments are given for the assay results. |
Databáze: | OpenAIRE |
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