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Lipstatin, an inhibitor of pancreatic lipase, produced by Streptomyces toxytricini. I. Producing organism, fermentation, isolation and biological activity.
Lipstatin, a new and very potent inhibitor of pancreatic lipase (the key enzyme of intestinal fat digestion) was isolated from Streptomyces toxytricini. Lipstatin contains a beta-lactone structureExpand
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Inhibition of gastrointestinal lipolysis by Orlistat during digestion of test meals in healthy volunteers.
The inhibition of digestive lipases by the antiobesity drug Orlistat along with lipolysis levels and fecal fat excretion were measured in healthy humans. Orlistat was found to be a powerful gastricExpand
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Inhibition of pancreatic lipase in vitro by the covalent inhibitor tetrahydrolipstatin.
Tetrahydrolipstatin inhibits pancreatic lipase from several species, including man, with comparable potency. The lipase is progressively inactivated through the formation of a long-lived covalentExpand
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Low molecular weight, non-peptide fibrinogen receptor antagonists.
The tetrapeptide H-Arg-Gly-Asp-Ser-OH (1) (RGDS), representing a recognition sequence of fibrinogen for its platelet receptor GP IIb-IIIa (integrin alpha IIb beta 3), served as lead compound for theExpand
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Crystallographic analysis at 3.0-A resolution of the binding to human thrombin of four active site-directed inhibitors.
The mode of binding of four active-site directed inhibitors to human thrombin has been determined by x-ray crystallographic analysis. The inhibitors studied are benzamidine, PPACK, NAPAP, and MD-805,Expand
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The lipase inhibitor tetrahydrolipstatin binds covalently to the putative active site serine of pancreatic lipase.
Tetrahydrolipstatin (THL) is a selective inhibitor of fat absorption. In animal models, it has anti-obesity and anti-hypercholesterolemic activity and is presently in clinical trials for theseExpand
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Endothelial cells stimulated with tumor necrosis factor-alpha express varying amounts of tissue factor resulting in inhomogenous fibrin deposition in a native blood flow system. Effects of thrombin
TNF-alpha induces changes in endothelial cell functions, such as upregulation of tissue factor, resulting in endothelial procoagulant activity which may play a role in disseminated intravascularExpand
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Orally active fibrinogen receptor antagonists. 2. Amidoximes as prodrugs of amidines.
The potent and selective GP IIb-IIIa antagonist lamifiban (1, Ro 44-9883) is currently in clinical development as an injectable antithrombotic agent for treating and preventing acute coronaryExpand
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Identification of the active‐site serine in human pancreatic lipase by chemical modification with tetrahydrolipstatin
A chemical modification approach was used in this study to identify the active site serine residue of human pancreatic lipase. Purified human pancreatic lipase was covalently modified by incubationExpand
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Surface behaviour of bile salts and tetrahydrolipstatin at air/water and oil/water interfaces.
The surface behaviour of two bile salts, sodium deoxycholate (NaDC) and sodium taurodeoxycholate (NaTDC), as well as that of tetrahydrolipstatin (THL), a potent gastrointestinal lipase inhibitor, wasExpand
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