PCR method was used to introduce the code sequence of Factor Xa cleavage site to the 5′ end of cecropin CMIV mutant gene X,then the gene was cloned into the expression vector pGEX KG,and was highly expressed in E.col...PCR method was used to introduce the code sequence of Factor Xa cleavage site to the 5′ end of cecropin CMIV mutant gene X,then the gene was cloned into the expression vector pGEX KG,and was highly expressed in E.coli BL21 by IPTG induction.The fusion protein was purified by affinity chromatography and was cleaved by Factor Xa.Cecropin X with antibacterial activity was obtained after purified by ion exchange chromatography.展开更多
Coagulation Factor Xa(FXa)is the crucial enzyme at the convergent point of the intrinsic and extrinsic coagulation pathways.The inhibition of FXa is an effective approach against thrombotic diseases.In the present stu...Coagulation Factor Xa(FXa)is the crucial enzyme at the convergent point of the intrinsic and extrinsic coagulation pathways.The inhibition of FXa is an effective approach against thrombotic diseases.In the present study,a specific strategy is reported to discover 10 novel FXa inhibitors based on ligand-based(pharmacophore)virtual screening and molecular docking analysis from a dataset of specs(containing 220000 molecules).The binding modes analysis provide insights into the contribution of particular structural moieties of the compounds towards their activity against FXa,and 10 novel structural compounds were discovered as potent candidate molecules.This work could be helpful in further design and development of FXa inhibitors.展开更多
文摘PCR method was used to introduce the code sequence of Factor Xa cleavage site to the 5′ end of cecropin CMIV mutant gene X,then the gene was cloned into the expression vector pGEX KG,and was highly expressed in E.coli BL21 by IPTG induction.The fusion protein was purified by affinity chromatography and was cleaved by Factor Xa.Cecropin X with antibacterial activity was obtained after purified by ion exchange chromatography.
基金the Science and Technology Innovation Talent Project of Sichuanprovince (Grant number 2016073).
文摘Coagulation Factor Xa(FXa)is the crucial enzyme at the convergent point of the intrinsic and extrinsic coagulation pathways.The inhibition of FXa is an effective approach against thrombotic diseases.In the present study,a specific strategy is reported to discover 10 novel FXa inhibitors based on ligand-based(pharmacophore)virtual screening and molecular docking analysis from a dataset of specs(containing 220000 molecules).The binding modes analysis provide insights into the contribution of particular structural moieties of the compounds towards their activity against FXa,and 10 novel structural compounds were discovered as potent candidate molecules.This work could be helpful in further design and development of FXa inhibitors.
