蒙布雷汀A类似物的合成产生了对人胰腺α淀粉酶有效的竞争性抑制剂。
Synthesis of montbretin A analogues yields potent competitive inhibitors of human pancreatic α-amylase.
作者信息
Tysoe Christina R, Caner Sami, Calvert Matthew B, Win-Mason Anna, Brayer Gary D, Withers Stephen G
机构信息
Department of Chemistry , University of British Columbia , 2036 Main Mall , Vancouver BC , Canada V6T 1Z1 . Email:
Department of Biochemistry and Molecular Biology , University of British Columbia , 2350 Health Sciences Mall , Vancouver BC , Canada V6T 1Z3.
出版信息
Chem Sci. 2019 Oct 18;10(48):11073-11077. doi: 10.1039/c9sc02610j. eCollection 2019 Dec 28.
Simplified analogues of the potent human amylase inhibitor montbretin A were synthesised and shown to bind tightly, = 60 and 70 nM, with improved specificity over medically relevant glycosidases, making them promising candidates for controlling blood glucose. Crystallographic analysis confirmed similar binding modes and identified new active site interactions.
合成了强效人淀粉酶抑制剂蒙布菌素A的简化类似物，结果表明它们能紧密结合，解离常数分别为60和70 nM，对医学上相关的糖苷酶具有更高的特异性，使其成为控制血糖的有潜力的候选物。晶体学分析证实了类似的结合模式，并确定了新的活性位点相互作用。
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