【摘 要】
:
Aminocoumarin antibiotics,such as novobiocin and clorobiocin,represent a weak but unique class of Hsp90 inhibitors that bind to the ATP-binding site located within the C-terminal domain of the protein
【机 构】
:
Institute of Materia Medica,Peking Union Medical College & Chinese Academy of Medical Sciences,No.1
【出 处】
:
第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会
论文部分内容阅读
Aminocoumarin antibiotics,such as novobiocin and clorobiocin,represent a weak but unique class of Hsp90 inhibitors that bind to the ATP-binding site located within the C-terminal domain of the protein.Previous studies unveiled that simplified analogues of these natural products exhibited significantly improved protein binding affinities,but not antiproliferative activities in cancer cells.We report herein that replacement of the 3-OH in the noviose moiety with an amino group would provide a useful solution to this problem.
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