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In search of negative allosteric modulators of biological targets

Duncan R Groebe1

  • 1Abbott Laboratories, R4PN/J35, 200 Abbott Park Road, Abbott Park, IL 60064, USA. duke.groebe@abbott.com

Drug Discovery Today
|November 1, 2008
PubMed

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Allosteric Regulation01:08

Allosteric Regulation

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Negative Regulator Molecules

Positive regulators allow a cell to advance through cell cycle checkpoints. Negative regulators have an equally important role as they terminate a cell’s progression through the cell cycle—or pause it—until the cell meets specific criteria.
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Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
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Allosteric Proteins-ATCase

Binding sites linkages can regulate a protein's function.  For example, enzyme activity is often regulated through a feedback mechanism where the end product of the biochemical process serves as an inhibitor.
Aspartate transcarbamoylase (ATCase) is a cytosolic enzyme that catalyzes the condensation of L-aspartate and carbamoyl phosphate to  N-carbamoyl-L-aspartate. This reaction is the first step in pyrimidine biosynthesis. UTP and CTP, the end products of the pyrimidine synthesis pathway,...
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Cooperative Allosteric Transitions

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