Article
Specificity and orientation of trigonal carboxyl esters and tetrahedral alkylphosphonyl esters in cholinesterases.
Biochemistry - 12 Sept 1995
Hosea N A, Berman H A, Taylor P
Abstract excerpt
We have examined the specificity of planar carboxyl and tetrahedral phosphonyl esters for mouse cholinesterases and have delineated the orientation of these ligands in the enzyme active center. The approach involved altering acyl pocket dimensions by site-specific mutagenesis of two phenylalanines and varying ligand size and enantiomer presentation. Substrate catalysis rates by wild type acetylcholinesterase...
Topics
- Acetylcholinesterase
- Acylation
- Animals
- Butyrylcholinesterase
- Cell Line
- Cholinesterase Inhibitors
- Esters
- Humans
- Kinetics
- Mice
- Mutation
- Organophosphorus Compounds