Journal ArticleDOI
Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.
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The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.About:
This article is published in Biochemical Pharmacology.The article was published on 1973-12-01. It has received 12583 citations till now. The article focuses on the topics: Uncompetitive inhibitor & Non-competitive inhibition.read more
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Ligand: a versatile computerized approach for characterization of ligand-binding systems.
Peter J. Munson,David Rodbard +1 more
TL;DR: This approach provides two major advantages compared with other available methods: it uses an exact mathematical model of the ligand-binding system, thereby avoiding the possible biases introduced by several commonly used approximations and it uses a statistically valid, appropriately weighted least-squares curve-fitting algorithm with objective measurement of goodness of fit.
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Theoretical Basis, Experimental Design, and Computerized Simulation of Synergism and Antagonism in Drug Combination Studies
TL;DR: The median-effect principle and its mass-action law based computer software are gaining increased applications in biomedical sciences, from how to effectively evaluate a single compound or entity to how to beneficially use multiple drugs or modalities in combination therapies.
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g_mmpbsa--a GROMACS tool for high-throughput MM-PBSA calculations.
TL;DR: A new tool, g_mmpbsa, which implements the MM-PBSA approach using subroutines written in-house or sourced from the GROMACS and APBS packages is described, and the calculated interaction energy of 37 structurally diverse HIV-1 protease inhibitor complexes is compared.
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The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist.
Erik H. F. Wong,John A. Kemp,Tony Priestley,Antony R. Knight,Geoffrey Neil Woodruff,L. L. Iversen +5 more
TL;DR: Neurophysiological studies in vitro, using a rat cortical-slice preparation, demonstrated a potent, selective, and noncompetitive antagonistic action of MK-801 on depolarizing responses to N-Me-D-Asp but not to kainate or quisqualate, providing an explanation for the mechanism of action ofMK-801 as an anticonvulsant.
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Auto-inhibition of brain histamine release mediated by a novel class (H3) of histamine receptor.
TL;DR: It is shown here that histamine inhibits its own release from depolarized slices of rat cerebral cortex, an action apparently mediated by a class of receptor (H3) pharmacologically distinct from those previously characterized, that is, the H1 and H2 receptors.
References
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Journal ArticleDOI
The kinetics of enzyme-catalyzed reactions with two or more substrates or products. I. Nomenclature and rate equations
TL;DR: A nomenclature to facilitate discussion of possible mechanisms for enzyme-catalyzed reactions with more than one substrate or product is proposed and examples are given to illustrate the types of information about reaction mechanisms that can be obtained.
Journal ArticleDOI
The kinetics of enzyme-catalyzed reactions with two or more substrates or products. II. Inhibition: nomenclature and theory.
TL;DR: A nomenclature is proposed to describe different types of inhibitions of enzyme-catalyzed reactions, particularly for reactions with more than one substrate and product, and the rate equations for such inhibitions are discussed.