Crystal structures of factor Xa specific inhibitors in complex with trypsin: structural grounds for inhibition of factor Xa and selectivity against thrombin
نویسندگان
چکیده
منابع مشابه
Oral direct factor Xa inhibitors.
Vitamin K antagonists, such as warfarin, have been the mainstay of oral anticoagulation for many decades. Although effective, warfarin has numerous limitations, including a variable dose requirement from patient to patient because of differences in dietary vitamin K intake, common genetic polymorphisms, and multiple drug interactions that affect its pharmacodynamics and metabolism. Consequently...
متن کاملOral direct thrombin inhibitors or oral factor Xa inhibitors for the treatment of deep vein thrombosis.
BACKGROUND Deep vein thrombosis (DVT) is a condition in which a clot forms in the deep veins, most commonly of the leg. It occurs in approximately 1 in 1,000 people. If left untreated, the clot can travel up to the lungs and cause a potentially life-threatening pulmonary embolism (PE). Previously, a DVT was treated with the anticoagulants heparin and vitamin K antagonists. However, two forms of...
متن کاملNovel factor Xa inhibitors: a patent review.
IMPORTANCE OF THE FIELD New oral anticoagulants with favorable safety profiles and fixed doses are required for the management of thromboembolism and stroke prevention in patients with atrial fibrillation. Among them, fXa inhibitors (the so-called xabans) are attractive options that can overcome limitations (e.g., bleeding) of the current oral antithrombotic therapy. The rational design of smal...
متن کاملThe Relative Importance of Thrombin Inhibition and Factor Xa Inhibition to the Antithrombotic Effects of Heparin
The relative importance of antithrombin and anti-factor Xa activities of heparin fractions required to achieve optimal antithrombotic effects is unknown. To study this. we measured the effects of standard heparin. an octasaccharide heparin fraction (anti-factor Xa activity only). and dermatan sulfate (antithrombin activity only) on the prevention of thrombosis and related this to their anticoag...
متن کاملThe relative importance of thrombin inhibition and factor Xa inhibition to the antithrombotic effects of heparin.
The relative importance of antithrombin and anti-factor Xa activities of heparin fractions required to achieve optimal antithrombotic effects is unknown. To study this, we measured the effects of standard heparin, an octasaccharide heparin fraction (anti-factor Xa activity only), and dermatan sulfate (antithrombin activity only) on the prevention of thrombosis and related this to their anticoag...
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ژورنال
عنوان ژورنال: FEBS Letters
سال: 1995
ISSN: 0014-5793
DOI: 10.1016/0014-5793(95)01190-p