Ligand binding: proteinase-protein inhibitor interactions

Abstract Until recently, the substrate-like, canonical inhibition of ‘small’ serine proteinase inhibitors and the product-like inhibition of the carboxypeptidase inhibitor from potato provided the only models for protein inhibitor-proteinase interactions. Recently published structures of cystatin/stefin-papain complexes and hirudin-thrombin complexes reveal novel modes of interaction that are only partially substrate-like in character. Despite considerable progress in understanding the native-to-cleaved transition of the serpins, the mechanism of their interaction with their cognate serine proteinases is still a matter of conjecture.

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