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Structural studies on vertebrate and invertebrate acetylcholinesterases and their complexes with functional ligands
Author(s) -
Greenblatt Harry M.,
Silman Israel,
Sussman Joel L.
Publication year - 2000
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/1098-2299(200007/08)50:3/4<573::aid-ddr41>3.0.co;2-7
Subject(s) - acetylcholinesterase , aché , drosophila melanogaster , vertebrate , torpedo , chemistry , melanogaster , stereochemistry , structure–activity relationship , enzyme , invertebrate , biochemistry , pharmacology , biology , ecology , acetylcholine receptor , receptor , in vitro , gene
The structure of Torpedo californica acetylcholinesterase (AChE) was examined in complex with several inhibitors which are either in use or under development for treatment of Alzheimer's disease. The inhibitors vary greatly in their structures, offering differing starting points for future drug design. The structure of T. californica AChE is also compared to the recently solved structure of Drosophila melanogaster AChE, the first invertebrate enzyme to have its structure determined. The structure of D. melanogaster AChE complexed with a potential insecticide is described. Drug Dev. Res. 50:573–583, 2000. © 2000 Wiley‐Liss, Inc.