畜牧兽医学报2024，Vol.55Issue(5)：2273-2280,8.DOI:10.11843/j.issn.0366-6964.2024.05.045
七种蛋白酶抑制剂对多房棘球蚴DNA损伤诱导样1蛋白活性的影响
The Effect of Seven Protease Inhibitors on Activity of DNA Damage Inducible 1 Protein in Echinococcus multilocularis
摘要
Abstract
As no effective treatment for alveolar echinococcosis(AE)is currently available,the therapeutic drugs are needed urgently.Early stage studies have shown that the protease inhibitors of HIV could also be anticancer and anti-parasitic.The purpose of this paper is to study the effect of the inhibitors(HIV PIs)on the activity of DNA damage inducible 1 protein of Echinococcus multilocularis(EmuDdi1).The recombinant vector pFastBac1-EmuDdi1 was constructed and expressed in Sf9 cell,and the soluble protein was successfully purified in P2 generations.Then the enzyme activity of Ddi1 protein was detected with the specific fluorescent substrates,and the inhibition rate of seven HIV PIs including saquinavir(SQV),ritonavir(RTV),amprenavir(APV),atazanavir(ATV),lopinavir(LPV),fosamprenavir(Fos),tipranavir(TPV)and darunavir(DRV)on Ddi1 protein activity was further examined.The results showed that EmuDdi1had high affinity and activity,and saquinavir showed the highest inhibition rate at 67％to inhibit protease activity of EmuDdi1 with a IC50 at 34.These results suggested that saquinavir is effcetive to inhibit the activity of Ddi1,and could be used to develop a potential targeting drug for AE.关键词
蛋白酶抑制剂/多房棘球蚴/DNA损伤诱导样蛋白/酶活性/抑制率Key words
protease inhibitors/Echinococcus multilocularis/DNA damage inducible 1 protein/enzyme activity/inhibition rate分类
农业科技引用本文复制引用
张生英,刘仲藜,郭爱疆,王帅..七种蛋白酶抑制剂对多房棘球蚴DNA损伤诱导样1蛋白活性的影响[J].畜牧兽医学报,2024,55(5):2273-2280,8.基金项目
国家重点研发计划项目(2022YFD1800205) （2022YFD1800205）
甘肃省杰出青年基金(21JR7RA027) （21JR7RA027）
