rivaroxaban has been researched along with nafamostat* in 2 studies
2 other study(ies) available for rivaroxaban and nafamostat
| Article | Year |
|---|---|
Structure-based discovery of small molecule hepsin and HGFA protease inhibitors: Evaluation of potency and selectivity derived from distinct binding pockets.
Hepatocyte growth factor activator (HGFA), matriptase and hepsin are all S1 trypsin-like serine endopeptidases. HGFA is a plasma protease while hepsin and matriptase are type II transmembrane proteases (TTSPs). Upregulated expression and activity of all three proteases is associated with aberrant cancer cell signaling through c-MET and RON tyrosine kinase cell-signaling pathways in cancer. We modeled known benzamidine protease inhibitor scaffolds into the active sites of matriptase, hepsin and HGFA to design new non-peptide inhibitors of hepsin and HGFA. First, we used a docking model of the irreversible inhibitor, Nafamostat, bound to the active site of HGFA in order to explore structure activity relationships (SAR). Compounds were screened for inhibition of HGFA activity in a kinetic enzyme assay using a chromogenic substrate. Next, we designed matched pair compound libraries of 3-amidino and 4-amidino phenylalanine (benzamidine) arginine peptidomimetics based on the structure of matriptase inhibitor, CJ-672. Compounds were screened for inhibition of HGFA, matriptase, and hepsin enzyme activity using fluorogenic substrates. Using this strategy we have discovered the first reported non-peptide small molecule inhibitors of both HGFA and hepsin. These inhibitors have differential potency and selectivity towards all three proteases. A subset of piperazinyl ureas highlighted by 25a, have excellent potency and selectivity for hepsin over matriptase and HGFA. Topics: Amidines; Antineoplastic Agents; Arginine; Benzamidines; Catalytic Domain; Drug Design; Enzyme Assays; Guanidines; High-Throughput Screening Assays; Humans; Kinetics; Molecular Docking Simulation; Neoplasm Proteins; Peptidomimetics; Phenylalanine; Piperazines; Protease Inhibitors; Recombinant Proteins; Serine Endopeptidases; Structure-Activity Relationship; Urea | 2015 |
Use of rivaroxaban for the effective management of disseminated intravascular coagulation associated with abdominal aortic aneurysm.
A 67-year-old man with non-valvular atrial fibrillation (AF) and previous myocardial and cerebral infarctions had uncontrollable bleeding after undergoing dental extraction because of an exacerbation of chronic disseminated intravascular coagulation (DIC) due to an abdominal aortic aneurysm. After successful treatment of the bleeding with the transfusion of fresh frozen plasma and platelets, nafamostat mesilate was used to treat the chronic DIC. Finally, rivaroxaban (an oral direct Factor Xa inhibitor) was prescribed for chronic DIC, as well as non-valvular AF. Following the initiation of rivaroxaban, the chronic DIC gradually improved, and the patient was discharged. Topics: Aged; Anticoagulants; Aortic Aneurysm, Abdominal; Benzamidines; Blood Platelets; Blood Transfusion; Disseminated Intravascular Coagulation; Guanidines; Humans; Male; Rivaroxaban; Tooth Extraction | 2015 |