Allosteric Regulation and Toxicity

Paper Summary:

This paper examines how allosteric regulation can be defined as the regulation of an enzyme or protein by the binding of a substance (effector) at a site other than the protein's active site (allosteric site). It looks at how allosteric regulation plays an important role in many facets of toxicology, whether it activates or inhibits a metabolic pathway with a toxic result, creates synergistic and antagonistic effects among different toxins, or represents a promising methodology for physiological research and the development of novel drugs.

From the Paper:

"Two common forms of allosterically induced toxicity are due to allosteric inhibition or activation. A simple example of toxicity due to inhibitory interference with normal allosteric regulation is the well known alkaloid toxin strychnine. Strychnine inhibits the action of the neurotransmitter glycine, an inhibitory transmitter found in the human spinal cord and brain stem, by binding to the allosteric site on the glycine receptor and inducing a conformational change that lowers the affinity of glycine for the glycine receptor (Purves et al. 2008). By inhibiting the normal inhibitory function of glycine, sufficient doses of strychnine are able to produce muscular convulsions eventually resulting in death. "

Sample of Sources Used:

• Blasiak, J. "Allosteric inhibition of the (Na+/K+)-ATPase by parathion and methylparathion." Pesticide biochemistry and physiology 54.1 (1996): 40-47.
• Catterall, W. A. Pharmacol. Rev. 72 (suppl.), (1992): 15-48.
• Cestele, S., Sampieri F., H. Rochat, D. Gordon. "Tetrodotoxin reverses brevetoxin allosteric inhibition of scorpion alpha-toxin binding on rat brain sodium channels." J. Biol. Chem. (1996): 271: 18329-18332.
• Cestele S., Ben Khalifa R, Pelhate M, Rochat H, Gordon D (1995) -Scorpion toxins binding on rat brain and insect sodium channels reveal divergent allosteric modulations by brevetoxin and veratridine. J Biol Chem 270:15153-15161
• Le, Omelchenko, Hryshko, Uliyanova, Condrescu, and Reeves. Allosteric activation of sodium-calcium exchange by picomolar concentrations of cadmium. J Physiol. 2005 February 15.

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