Department of Chemistry & Education, Seoul National University, Seoul 151-742, Republic of Korea.
Bioorg Med Chem Lett. 2011 Apr 15;21(8):2441-4. doi: 10.1016/j.bmcl.2011.02.062.
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.
我们构建了一个糖二肽缀合物文库，以寻找针对α-葡萄糖苷酶疏水性口袋的最佳互补物。从嗜热脂肪芽孢杆菌中提取的α-葡萄糖苷酶对最佳底物的 K(m) 值相对于对乙酰氨基苯-α-D-吡喃葡萄糖苷提高了 150 倍。利用互补信息，我们合成了 sp-WY 和β-Glc-sp-WY，它们对相应的酶具有选择性抑制作用。
