Kinetic studies of the inhibitory effects of propeptides subtilisin BPN' and Carlsberg to bacterial serine proteases. 1997

H W Huang, and W C Chen, and C Y Wu, and H C Yu, and W Y Lin, and S T Chen, and K T Wang
Institute of Biological Chemistry, Academia Sinica, National Taiwan University, Republic of China.

The propeptides of bacterial subtilisin BPN' and Carlsberg were synthesized to investigate their inhibitory function on the enzymes. Kinetically, pro-BPN' inhibits the proteolytic activities of subtilisin BPN' and Carlsberg separately in a slow binding mode. Pro-Carlsberg behaves as a typical rapid equilibrium competitive inhibitor for these two proteases. Functionally, pro-Carlsberg inhibits the subtilisins with moderate selectivity. The inhibition constant Ki of pro-BPN' to subtilisin BPN' is 5.0 nM, and 6.1 nM to subtilisin Carlsberg. The on-rate of pro-BPN' to subtilisin BPN' is 5.8 x 10(5) M(-1)s(-1), and the off-rate 2.9 x 10(-3) s(-1). Similarly, the on-rate of pro-BPN' to subtilisin Carlsberg is 2.2 x 10(5) M(-1)s(-1), and the off-rate 1.3 x 10(-3) s(-1). On the other hand, the Ki of pro-Carlsberg to subtilisin BPN' gives 1.3 x 10(2) nM, and 88 nM to subtilisin Carlsberg. Based on the key features of the interactions between pro-BPN' and subtilisin from X-ray crystallographic results (Gallagher et al., 1995), the correlation between the sequence of subtilisin propeptides and their inhibition abilities on the proteases are compared and discussed.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008969 Molecular Sequence Data Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories. Sequence Data, Molecular,Molecular Sequencing Data,Data, Molecular Sequence,Data, Molecular Sequencing,Sequencing Data, Molecular
D009842 Oligopeptides Peptides composed of between two and twelve amino acids. Oligopeptide
D009994 Osmolar Concentration The concentration of osmotically active particles in solution expressed in terms of osmoles of solute per liter of solution. Osmolality is expressed in terms of osmoles of solute per kilogram of solvent. Ionic Strength,Osmolality,Osmolarity,Concentration, Osmolar,Concentrations, Osmolar,Ionic Strengths,Osmolalities,Osmolar Concentrations,Osmolarities,Strength, Ionic,Strengths, Ionic
D011498 Protein Precursors Precursors, Protein
D002942 Circular Dichroism A change from planar to elliptic polarization when an initially plane-polarized light wave traverses an optically active medium. (McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed) Circular Dichroism, Vibrational,Dichroism, Circular,Vibrational Circular Dichroism
D004591 Electrophoresis, Polyacrylamide Gel Electrophoresis in which a polyacrylamide gel is used as the diffusion medium. Polyacrylamide Gel Electrophoresis,SDS-PAGE,Sodium Dodecyl Sulfate-PAGE,Gel Electrophoresis, Polyacrylamide,SDS PAGE,Sodium Dodecyl Sulfate PAGE,Sodium Dodecyl Sulfate-PAGEs
D000595 Amino Acid Sequence The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION. Protein Structure, Primary,Amino Acid Sequences,Sequence, Amino Acid,Sequences, Amino Acid,Primary Protein Structure,Primary Protein Structures,Protein Structures, Primary,Structure, Primary Protein,Structures, Primary Protein
D000596 Amino Acids Organic compounds that generally contain an amino (-NH2) and a carboxyl (-COOH) group. Twenty alpha-amino acids are the subunits which are polymerized to form proteins. Amino Acid,Acid, Amino,Acids, Amino
D001426 Bacterial Proteins Proteins found in any species of bacterium. Bacterial Gene Products,Bacterial Gene Proteins,Gene Products, Bacterial,Bacterial Gene Product,Bacterial Gene Protein,Bacterial Protein,Gene Product, Bacterial,Gene Protein, Bacterial,Gene Proteins, Bacterial,Protein, Bacterial,Proteins, Bacterial

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