Reagents for reversible coupling of proteins to the active centres of trypsin-like serine proteinases. |
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Authors: | S B Kalindjian and R A Smith |
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Affiliation: | Beecham Pharmaceuticals Research Division, Biosciences Research Centre, Surrey, U.K. |
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Abstract: | In order to extend the scope for the application of acyl-enzymes as fibrinolytic agents, p-amidinophenyl ester enzyme substrates were prepared that gave stabilized acyl-enzymes capable of being coupled to other proteins. Coupling was achieved by reaction of protein thiol functions with a 2-pyridyldithio moiety within the acyl group. Acyl-enzymes derived from such substrates were stable enough to permit isolation of reversible conjugates between proteins and the active centres of plasminogen activators. Hydrolytic release of active enzyme from a conjugate of human immunoglobulin G and urokinase could be demonstrated. |
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