Publication

Rational Design of an Organometallic Glutathione Transferase Inhibitor

Paul Joseph Dyson, Wee Han Ang
2009
Journal Articles

Abstract

Double trouble: A hybrid org.-inorg. (organometallic) inhibitor was designed to target glutathione transferases. The metal center is used to direct protein binding, while the org. moiety acts as the active-site inhibitor (see picture). The mechanism of inhibition was studied using a range of biophys. and biochem. methods.

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https://infoscience.epfl.ch/entities/publication/f21230ae-e3b3-4128-a932-0979784d7a8e

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Paul Joseph Dyson, Wee Han Ang
2009
Journal Articles

Abstract

Official source

https://infoscience.epfl.ch/entities/publication/f21230ae-e3b3-4128-a932-0979784d7a8e

About this result

Related concepts (11)

Enzyme inhibitor

An enzyme inhibitor is a molecule that binds to an enzyme and blocks its activity. Enzymes are proteins that speed up chemical reactions necessary for life, in which substrate molecules are converted into products. An enzyme facilitates a specific chemical reaction by binding the substrate to its active site, a specialized area on the enzyme that accelerates the most difficult step of the reaction.

Renin inhibitor

Renin inhibitors are pharmaceutical drugs inhibiting the activity of renin that is responsible for hydrolyzing angiotensinogen to angiotensin I, which in turn reduces the formation of angiotensin II that facilitates blood pressure. Renin inhibitor is often preceded by direct, called direct renin inhibitor in order to distinguish its mechanism from other renin–angiotensin–aldosterone system-interfering drugs such as angiotensin converting enzyme inhibitors (ACEIs), angiotensin receptor blockers (ARBs) and aldosterone receptor antagonists.

Active site

In biology and biochemistry, the active site is the region of an enzyme where substrate molecules bind and undergo a chemical reaction. The active site consists of amino acid residues that form temporary bonds with the substrate, the binding site, and residues that catalyse a reaction of that substrate, the catalytic site. Although the active site occupies only ~10–20% of the volume of an enzyme, it is the most important part as it directly catalyzes the chemical reaction.

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