Metalloprotease inhibitor
Encyclopedia
There are three classes of commonly used inhibitors
for metalloproteinase
s.
Enzyme inhibitor
An enzyme inhibitor is a molecule that binds to enzymes and decreases their activity. Since blocking an enzyme's activity can kill a pathogen or correct a metabolic imbalance, many drugs are enzyme inhibitors. They are also used as herbicides and pesticides...
for metalloproteinase
Metalloproteinase
Metalloproteinases constitute a family of enzymes from the group of proteases, classified by the nature of the most prominent functional group in their active site. These are proteolytic enzymes whose catalytic mechanism involves a metal. Most metalloproteases are zinc-dependent, but some use...
s.
- In vitro, EDTAEDTAEthylenediaminetetraacetic acid, widely abbreviated as EDTA , is a polyamino carboxylic acid and a colourless, water-soluble solid. Its conjugate base is named ethylenediaminetetraacetate. It is widely used to dissolve limescale. Its usefulness arises because of its role as a hexadentate ligand...
, 1,10-phenanthroline and other chelating compounds lower the concentration of metal to the point where the metal is removed from the enzymeEnzymeEnzymes are proteins that catalyze chemical reactions. In enzymatic reactions, the molecules at the beginning of the process, called substrates, are converted into different molecules, called products. Almost all chemical reactions in a biological cell need enzymes in order to occur at rates...
active siteActive siteIn biology the active site is part of an enzyme where substrates bind and undergo a chemical reaction. The majority of enzymes are proteins but RNA enzymes called ribozymes also exist. The active site of an enzyme is usually found in a cleft or pocket that is lined by amino acid residues that...
.
- Classical lock and key inhibitors such as phosphoramidonPhosphoramidonPhosphoramidon is a chemical compound derived from cultures of Streptomyces tanashiensis. It is an inhibitor of the enzyme thermolysin, a membrane metallo-endopeptidase inhibitor, and an endothelin converting enzyme inhibitor...
and bestatin bind tightly by approximating the transition stateTransition stateThe transition state of a chemical reaction is a particular configuration along the reaction coordinate. It is defined as the state corresponding to the highest energy along this reaction coordinate. At this point, assuming a perfectly irreversible reaction, colliding reactant molecules will always...
of the hydrolysis of the peptide, preventing it from acting on other substrates.
- Protein inhibitors such as α2-macroglobulinMacroglobulinA macroglobulin is a plasma globulin of high molecular weight. Elevated levels of macroglobulins may cause manifestations of excess blood viscosity and/or precipitate within blood vessels when temperature drops .Other macroglobulins include alpha-2 macroglobulin, which is...
are known to work with metalloproteinases.