【摘 要】
：
Tasiamide B contains the characteristic statine-type(γ-amino-β-hydroxy acid) unit that confers the affinity to the active site of certain aspartic proteases.A series of new tasiamide B derivatives wer
【机 构】
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School of Pharmacy,Fudan University,Shanghai 201203,China
【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
Tasiamide B contains the characteristic statine-type(γ-amino-β-hydroxy acid) unit that confers the affinity to the active site of certain aspartic proteases.A series of new tasiamide B derivatives were designed,synthesized and tested for their inhibition against BACE-1,cathepsins D and E.The inhibitors show high potency against BACE-1,cathepsin D and E where the most potent inhibitor displays IC50<50nM.The crystal structure of Tasiamide B in complex with BACE-1 has also been found.
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