Mechanistic and kinetic studies of inhibition of enzymes

Cell Biochemistry and Biophysics
C G Whiteley

Abstract

A graphical method for analyzing enzyme data to obtain kinetic parameters, and to identify the types of inhibition and the enzyme mechanisms, is described. The method consists of plotting experimental data as nu/(V0 - nu) vs 1/(I) at different substrate concentrations. I is the inhibitor concentration; V0 and nu are the rates of enzyme reaction attained by the system in the presence of a fixed amount of substrate, and in the absence and presence of inhibitor, respectively. Complete inhibition gives straight lines that go through the origin; partial inhibition gives straight lines that converge on the 1-I axis, at a point away from the origin. For competitive inhibition, the slopes of the lines increase with increasing-substrate concentration; with noncompetitive inhibition, the slopes are independent of substrate concentration; with uncompetitive inhibition, the slopes of the lines decrease with increasing substrate concentrations. The kinetic parameters, Km, Ki, Ki', and beta (degree of partiality) can best be determined from respective secondary plots of slope and intercept vs substrate concentration, for competitive and noncompetitive inhibition mechanism or slope and intercept vs reciprocal substrate concentration for uncom...Continue Reading

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Citations

Jul 21, 2011·Journal of Biomedicine & Biotechnology·Satya PrakashArielle Cantor
Nov 17, 2009·Journal of Enzyme Inhibition and Medicinal Chemistry·Masataka Yoshino, Keiko Murakami
Jul 25, 2021·Biosensors & Bioelectronics·Amir M AshrafiVojtech Adam
Oct 1, 2021·International Journal of Oral Science·Qiong ZhangJing Zou

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