Organic & Biomolecular Chemistry · 2012 · 32 citations · 63 references
Life SciencesBiochemistryMedicinal ChemistryDrug DiscoveryEnzymologyStructural BiologyEnzyme DiscoveryEnzyme InhibitionEnzyme StructureEnzyme-substrate RecognitionStructural EnzymologyEnzyme Inhibitor DiscoveryExoglycosidase ActivityGlycan HydrolasesGlycan LyasesGlycosidase InhibitionGlycosidase InhibitorsGlycosidasesX-ray Diffraction Analysis
One useful methodology that has been used to give insight into how chemically synthesized inhibitors bind to enzymes and the reasons underlying their potency is crystallographic studies of inhibitor-enzyme complexes. Presented here is the X-ray structural analysis of a representative family 20 exo-β-N-acetylhexosaminidase in complex with various known classes of inhibitor of these types of enzymes, which highlights how different inhibitor classes can inhibit the same enzyme. This study will aid in the future development of inhibitors of not only exo-β-N-acetylhexosaminidases but also other types of glycoside hydrolases.
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The determination of enzyme inhibitor constants
Martin Dixon · Biochemical Journal · 1953 · 4.1K citations · Full text