Structure-based design of inhibitors of coagulation factor XIa with novel P1 moieties
نویسندگان
چکیده
منابع مشابه
design and synthesis of novel oxindol derivatives with n-benzylpiperidine and n-benzylpiperazine moieties as cholinesterases inhibitors
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15 صفحه اولThe effect of platelets in the activation of human blood coagulation factor IX by factor XIa.
We report here the effect of activated human platelets on the activation of human factor IX by human factor XIa. Factor IXa formed during activation was determined via its ability to activate bovine factor X. To increase sensitivity, phospholipids and bovine factor VIIIa were present in the assay. The kinetic parameters of the factor IX activation were determined in the presence of 10 mmol/L Ca...
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Activated factor XI (FXIa) inhibitors are anticipated to combine anticoagulant and profibrinolytic effects with a low bleeding risk. This motivated a structure aided fragment based lead generation campaign to create novel FXIa inhibitor leads. A virtual screen, based on docking experiments, was performed to generate a FXIa targeted fragment library for an NMR screen that resulted in the identif...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2015
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2015.01.028