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Crystals of the urokinase type plasminogen activator variant beta(c)-uPAin complex with small molecule inhibitors open the way towards structure-based drug design.
Urokinase is a serine protease involved in cancer growth and metastasis. Here we present the first urokinase crystal structure in complex with reversible inhibitors at 2.1 and 2.6 A resolution. TheseExpand
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Secondary amides of sulfonylated 3-amidinophenylalanine. New potent and selective inhibitors of matriptase.
Matriptase is an epithelium-derived type II transmembrane serine protease and has been implicated in the activation of substrates such as pro-HGF/SF and pro-uPA, which are likely involved in tumorExpand
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Tick-borne Diseases (Borreliosis, Anaplasmosis, Babesiosis) in German and Austrian Dogs: Status quo and Review of Distribution, Transmission, Clinical Findings, Diagnostics and Prophylaxis
Tick-borne diseases (TBD) in dogs have gained in significance in German and Austrian veterinary practices. The widespread European tick species Ixodes ricinus represents an important vector forExpand
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Design of Novel and Selective Inhibitors of Urokinase-type Plasminogen Activator with Improved Pharmacokinetic Properties for Use as Antimetastatic Agents*[boxs]
The serine protease urokinase-type plasminogen activator (uPA) interacts with a specific receptor (uPAR) on the surface of various cell types, including tumor cells, and plays a crucial role inExpand
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Crystals of urokinase type plasminogen activator complexes reveal the binding mode of peptidomimetic inhibitors.
Urokinase type plasminogen activator (uPA), a trypsin-like serine proteinase, plays an important role in normal tissue re-modelling, cell adhesion, and cell motility. In addition, studies utilizingExpand
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In vitro inhibition of matriptase prevents invasive growth of cell lines of prostate and colon carcinoma.
Matriptase, also known as membrane-type-serine-protease 1 (MT-SP 1), is a type II transmembrane serine protease involved in the activation of the precursor form of hepatocyte growth factor/scatterExpand
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New substrate analogue inhibitors of factor Xa containing 4-amidinobenzylamide as P1 residue: part 1.
The trypsin-like serine protease factor Xa (fXa) is located at the convergence point of the intrinsic and extrinsic coagulation cascade, and therefore has emerged as an attractive target for theExpand
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Use of IHC and newly designed matriptase inhibitors to elucidate the role of matriptase in pancreatic ductal adenocarcinoma.
Matriptase, also known as MT-SP1, is a type II transmembrane serine protease strongly implicated in both the development and progression of a variety of epithelial cancers. Evidence comes fromExpand
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From selective substrate analogue factor Xa inhibitors to dual inhibitors of thrombin and factor Xa. Part 3.
Highly potent and selective substrate analogue factor Xa inhibitors were obtained by incorporation of non-basic or modestly basic P1 residues known from the development of thrombin inhibitors. TheExpand
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Increase of Anti-Metastatic Efficacy by Selectivity- But Not Affinity-Optimization of Synthetic Serine Protease Inhibitors
Abstract Although tumors frequently show elevated protease activities, the concept of anti-proteolytic cancer therapy has lost momentum after failure of clinical trials with broad-spectrum matrixExpand
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