- Selective α-glucosidase substrates and inhibitors containing short aromatic peptidyl moieties.
Selective α-glucosidase substrates and inhibitors containing short aromatic peptidyl moieties.
Bioorganic & medicinal chemistry letters (2011-03-15)
Sangeun Park, Soonsil Hyun, Su-il Do, Jaehoon Yu
PMID21397496
ABSTRACT
We constructed a library of sugar-dipeptide conjugate to find out the best complementary against hydrophobic pocket of α-glucosidase. The best substrate showed 150-fold improved K(m) value relative p-acetaminophenyl-α-D-glucopyranoside for α-glucosidase from Bacillus stearothermophillus. Using information from the complementary, we synthesized sp-WY and β-Glc-sp-WY, which selectivity inhibited the cognate enzyme.
MATERIALS