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Structural basis for the activation of flaviviral NS3 proteases from dengue and West Nile virus
The replication of flaviviruses requires the correct processing of their polyprotein by the viral NS3 protease (NS3pro). Essential for the activation of NS3pro is a 47-residue region of NS2B. Here weExpand
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Structural Mapping of the Active Site Specificity Determinants of Human Tissue-type Plasminogen Activator
The recent structure determination of the catalytic domain of tissue-type plasminogen activator (tPA) suggested residue Arg174 could play a role in P3/P4 substrate specificity. Six syntheticExpand
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Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase.
The trypsin-like serine proteinase superfamily contains a number of potential therapeutic targets, many of which are unsuitable for routine X-ray crystallographic studies. We have cocrystallized aExpand
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Lysine 156 promotes the anomalous proenzyme activity of tPA: X‐ray crystal structure of single‐chain human tPA
Tissue type plasminogen activator (tPA) is the physiological initiator of fibrinolysis, activating plasminogen via highly specific proteolysis; plasmin then degrades fibrin with relatively broadExpand
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Tissue-type plasminogen activator: variants and crystal/solution structures demarcate structural determinants of function.
  • W. Bode, M. Renatus
  • Biology, Medicine
  • Current opinion in structural biology
  • 1 December 1997
NMR and crystal structure of many components of tissue-type plasminogen activator (t-PA) are now available: the finger-EGF pair and the kringle-2 domain structures have been solved, as have theExpand
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Catalytic domain structure of vampire bat plasminogen activator: a molecular paradigm for proteolysis without activation cleavage.
The saliva of the blood-eating vampire bat Desmodus rotundus contains plasminogen activators (PAs) that maintain the fluidity of the prey's blood by activating plasminogen and dissolving developingExpand
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Design and evaluation of novel bivalent thrombin inhibitors based on amidinophenylalanines.
Two bivalent thrombin inhibitors were synthesized, which consist of a benzamidine-based active-site-blocking segment, a fibrinogen recognition exosite inhibitor and a peptidic linker connecting theseExpand
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3-Amidinophenylalanine-based inhibitors of urokinase.
Synthesis and anti-uPA activity of a series of Nalpha-triisopropyl-phenylsulfonyl-protected 3-amidinophenylalanine amides are described. We have explored SAR around the C-terminal amide part forExpand
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An active zymogen: unravelling the mystery of tissue-type plasminogen activator.
In contrast to almost all other proteinases, human tissue-type plasminogen activator (tPA) is also proteolytically active in its zymogen or single-chain form. The closely related plasminogenExpand
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