The pancreatic Kunitz inhibitor, also known as aprotinin, bovine basic pancreatic trypsin inhibitor (BPTI) and trypsin-kallikrein inhibitor, is one of the most extensively studies globular proteins. It has proved to be a particularly attractive and powerful tool for studying protein conformation as well as molecular basis of protein/protein interaction(s) and (macro)molecular recognition. BPTI has a relatively broad specificity, inhibiting trypsin- as well as chymotrypsin- and elastase-like serine (pro)enzymes endowed with very different primary specificity. BPTI reacts rapidly with serine proteases to form stable complexes, but the enzyme:inhibitor complex formation may involve several intermediates corresponding to discrete reaction steps. Moreover, BPTI inhibits the nitric oxide synthase type-I and -II action and impairs potassium ion transport by calcium-activated potassium channels. Clinically, the use of BPTI in selected surgical interventions, such as cardiopulmonary surgery and orthotopic liver transplantation, is advised as it significantly reduces hemorrhagic complications and thus blood-transfusion requirements. Here, the structural, inhibition and bio-medical aspects of BPTI are reported.
The bovine basic pancreatic trypsin inhibitor (Kunitz inhibitor): a milestone protein
SPALLAROSSA, ANDREA;
2003-01-01
Abstract
The pancreatic Kunitz inhibitor, also known as aprotinin, bovine basic pancreatic trypsin inhibitor (BPTI) and trypsin-kallikrein inhibitor, is one of the most extensively studies globular proteins. It has proved to be a particularly attractive and powerful tool for studying protein conformation as well as molecular basis of protein/protein interaction(s) and (macro)molecular recognition. BPTI has a relatively broad specificity, inhibiting trypsin- as well as chymotrypsin- and elastase-like serine (pro)enzymes endowed with very different primary specificity. BPTI reacts rapidly with serine proteases to form stable complexes, but the enzyme:inhibitor complex formation may involve several intermediates corresponding to discrete reaction steps. Moreover, BPTI inhibits the nitric oxide synthase type-I and -II action and impairs potassium ion transport by calcium-activated potassium channels. Clinically, the use of BPTI in selected surgical interventions, such as cardiopulmonary surgery and orthotopic liver transplantation, is advised as it significantly reduces hemorrhagic complications and thus blood-transfusion requirements. Here, the structural, inhibition and bio-medical aspects of BPTI are reported.
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