Changing the selectivity profile – from substrate analog inhibitors of thrombin and factor Xa to potent matriptase inhibitors
نویسندگان
چکیده
منابع مشابه
Oral 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 کاملOral 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 کاملDesign and synthesis of potent, selective inhibitors of matriptase.
Matriptase is a member of the type II transmembrane serine protease family. Several studies have reported deregulated matriptase expression in several types of epithelial cancers, suggesting that matriptase constitutes a potential target for cancer therapy. We report herein a new series of slow, tight-binding inhibitors of matriptase, which mimic the P1-P4 substrate recognition sequence of the ...
متن کاملNatural peptides and proteins: potent tyrosinase inhibitors
Background and objectives: Tyrosinase is a copper containing oxidase which is crucial for controlling the production of melanin in creatures such as bacteria, fungi, plants and mammals. It is involved in the first two steps of melanin biosynthesis and leads to pigmentation and different types of cancer such as melanoma. Also, it is responsible for browning of fruits and vegetab...
متن کاملGuidance on the emergent reversal of oral thrombin and factor Xa inhibitors.
The new oral anticoagulants dabigatran, rivaroxaban and apixaban have advantages over warfarin which include no need for laboratory monitoring, less drug-drug interactions and less food-drug interactions. However, there is no established antidote for patients who are bleeding or require emergent surgery and there is a paucity of evidence to guide the clinical care during these situations. Membe...
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ژورنال
عنوان ژورنال: Journal of Enzyme Inhibition and Medicinal Chemistry
سال: 2016
ISSN: 1475-6366,1475-6374
DOI: 10.3109/14756366.2016.1172574