Print Email Facebook Twitter Interaction of reteplase with heparin. A comparison between reteplase and alteplase Title Interaction of reteplase with heparin. A comparison between reteplase and alteplase Author Rijken, D.C. Jie, A.F.H. Gaubius Laboratory TNO Preventie en Gezondheid Publication year 1996 Abstract Reteplase is a protein consisting of the kringle-2 and protease domains of tissue-type plasminogen activator (t-PA). Because intravenous heparin will be used as an adjunct to thrombolytic therapy with reteplase, we investigated the interactions in vitro between heparin and reteplase as well as between heparin and recombinant t-PA (alteplase) as a control. Reteplase and alteplase bound completely to a heparin-agarose column and eluted respectively at 0.39 M and 0.60 M in a NaCl gradient. Two-chain derivatives of reteplase and alteplase eluted at 0.31 M and 0.52 M NaCl, respectively. Plasminogen activation by the two-chain derivatives of reteplase and alteplase in a purified system at low ionic strength were stimulated by heparin up to 13- and 22-fold, respectively. However reteplase required five times more heparin for maximal stimulation than alteplase. In addition, the heparin stimulation of reteplase was more salt sensitive than that of alteplase. In conclusion, both heparin binding and heparin stimulation experiments showed that heparin interacts with reteplase, but the interaction is weaker than with alteplase. Chemicals/CAS: Amidohydrolases, EC 3.5.-; Anticoagulants; Fibrinolytic Agents; Heparin, 9005-49-6; heparin-sepharose; Peptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine Amidase, EC 220.127.116.11; Plasminogen Activators, EC 3.4.21.-; Plasminogen, 9001-91-6; Recombinant Proteins; reteplase, 133652-38-7; Sepharose, 9012-36-6; Tissue Plasminogen Activator, EC 18.104.22.168 Subject BiologyAlteplaseBM 06.022FibrinolysisHeparinPlasminogen activationReteplaseThrombolysisTissue-type plasminogen activatoralteplaseheparinreteplasearticleblood clot lysiscontrolled studydrug interactionfibrinolysisplasminogen activationpriority journalAmidohydrolasesAnticoagulantsDrug SynergismEnzyme ActivationFibrinolytic AgentsGlycosylationHeparinHumansPeptide-N4-(N-acetyl-beta-glucosaminyl) Asparagine AmidasePlasminogenPlasminogen ActivatorsProtein BindingRecombinant ProteinsSepharoseTissue Plasminogen Activator To reference this document use: http://resolver.tudelft.nl/uuid:27f6172d-5d1b-48a2-852d-12dbbb76e301 TNO identifier 233463 ISSN 0957-5235 Source Blood Coagulation and Fibrinolysis, 7 (5), 561-566 Document type article Files To receive the publication files, please send an e-mail request to TNO Library.