PMID: 8589074Jan 1, 1995Paper

Structure activity studies of the substrate binding site in monoamine oxidase B

Biochimie
D E Edmondson

Abstract

The influence of para and meta substitution of benzylamine analogues on their interaction with bovine liver monoamine oxidase B has been investigated to provide insights into the nature of the substrate binding site. Binding data with para-substituted benzylamine analogues show the area of the binding site about the para position to be hydrophobic and exhibiting some steric constraints. Alkylation of the benzylamine nitrogen with methyl groups results in a dominance of steric constraints about the para-position as an influence on binding. meta-Substitution of the benzylamine ring results in a decreased binding affinity which exhibits a dependence on the van der Waals volume of the substituent indicating steric constraints also occur about this area of the bound substrate. The independence of the rate of enzyme reduction with the nature of the meta-substituent suggests these benzylamine analogues are bound in the substrate site in a manner which optimizes overlap of the pro-R benzyl C-H bond with the lone pair orbital on the nitrogen. In contrast, the observed rates of enzyme reduction by para-substituted benzylamine analogues exhibit a dominant steric dependence which suggests the mode of binding of this class of analogues does...Continue Reading

References

May 7, 1991·Biochemistry·R R Ramsay
Feb 1, 1991·Biochemical Society Transactions·R B Silverman
Dec 31, 1990·Biochemical and Biophysical Research Communications·W WeylerJ I Salach
Jan 1, 1990·Pharmacology & Therapeutics·W WeylerX O Breakefield
Jul 1, 1988·Proceedings of the National Academy of Sciences of the United States of America·A W BachJ C Shih
Feb 1, 1984·The Journal of Pharmacy and Pharmacology·C J Fowler, K F Tipton
Nov 1, 1981·Archives of Biochemistry and Biophysics·J I Salach, W Weyler
Jul 1, 1995·Xenobiotica; the Fate of Foreign Compounds in Biological Systems·D E Edmondson
Dec 13, 1994·Biochemistry·T JonssonJ P Klinman

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Citations

Jun 20, 2015·Journal of Chemical Information and Modeling·Gerald Zapata-TorresCristian Celis-Barros

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