Bisubstrate inhibition: Theory and application to N-acetyltransferases

Michael Yu, Maria L B Magalhães, Paul F. Cook, John S. Blanchard

Research output: Contribution to journalArticle

43 Citations (Scopus)

Abstract

Bisubstrate inhibitors represent a potentially powerful group of compounds that have found significant therapeutic utility. Although these compounds have been synthesized and tested against a number of enzymes that catalyze sequential bireactant reactions, the detailed theory for predicting the expected patterns of inhibition against the two substrates for various bireactant kinetic mechanisms has, heretofore, not been presented. We have derived the rate equations for all likely sequential bireactant mechanisms and provide two examples in which bisubstrate inhibitors allow the kinetic mechanism to be determined. Bisubstrate inhibitor kinetics is a powerful diagnostic for the determination of kinetic mechanisms.

Original languageEnglish (US)
Pages (from-to)14788-14794
Number of pages7
JournalBiochemistry
Volume45
Issue number49
DOIs
StatePublished - Dec 12 2006

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Acetyltransferases
Kinetics
Substrates
Enzymes
Therapeutics

ASJC Scopus subject areas

  • Biochemistry

Cite this

Bisubstrate inhibition : Theory and application to N-acetyltransferases. / Yu, Michael; Magalhães, Maria L B; Cook, Paul F.; Blanchard, John S.

In: Biochemistry, Vol. 45, No. 49, 12.12.2006, p. 14788-14794.

Research output: Contribution to journalArticle

Yu, Michael ; Magalhães, Maria L B ; Cook, Paul F. ; Blanchard, John S. / Bisubstrate inhibition : Theory and application to N-acetyltransferases. In: Biochemistry. 2006 ; Vol. 45, No. 49. pp. 14788-14794.
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