Journal
CHEMBIOCHEM
Volume 9, Issue 18, Pages 2920-2928Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.200800528
Keywords
allosteric regulation; drug discovery; enzymes; proteases; small molecules
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Allostery is a basic principle of control of enzymatic activities based on the interaction of a protein or small molecule at a site distinct from an enzyme's active center. Allosteric modulators represent an alternative approach to the design and synthesis of small-molecule activators or inhibitors of proteases and are therefore of wide interest for medicinal chemistry. The structural bases of some proteinaceous and small-molecule allosteric protease regulators have already been elucidated, indicating a general mechanism that might be exploitable for future rational design of small-molecule effectors.
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