Bioorganic & Medicinal Chemistry Letters 2011-04-15

Selective α-glucosidase substrates and inhibitors containing short aromatic peptidyl moieties.

Sangeun Park, Soonsil Hyun, Su-il Do, Jaehoon Yu

Index: Bioorg. Med. Chem. Lett. 21 , 2441-4, (2011)

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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.Copyright © 2011 Elsevier Ltd. All rights reserved.