Department of Pharmaceutical & Biological Chemistry, The School of Pharmacy, University of London, 29/39 Brunswick Square, London, WC1N 1AX, UK.
Chem Commun (Camb). 2011 Oct 14;47(38):10569-71. doi: 10.1039/c1cc13552j. Epub 2011 Aug 24.
Glycosylated analogues of novobiocin, discovered using a broad library of enzymes, have 100-fold improved activity against breast, brain, pancreatic, lung and ovarian cancers and ablated associated off-target activity leading to an up to 2.7 × 10(4) fold increase in selectivity.
使用广泛的酶文库发现的新生霉素糖基类似物对乳腺癌、脑癌、胰腺癌、肺癌和卵巢癌的活性提高了 100 倍,并消除了相关的脱靶活性,从而使选择性提高了 2.7×10(4)倍。