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Page 1 (in Ch.7) Page 2 Tertiary Structure; Substrates Page 3 Active Site
Page 4 Diagrams Page 5 Reaction Mechanism Page 6 Crystal Structures

An example of an active site: the serine proteases

References

• Bachovchin, W.W. (1985) Confirmation of the assignment of the low-field proton resonance of serine proteases by using specifically nitrogen-15 labelled enzyme Proc. Natl. Acad. Sci. USA 82, 7948-7951
• Carter, P. and Wells, J.A. (1988) Dissecting the catalytic triad of a serine protease Nature 332, 564-568
• Craik, C.S.Roczniak, S., Largman, C. and Rutter, W.J. (1987) The catalytic role of the active site aspartic acid in serine proteases Science 237, 909-913
• Fersht, A.R. (1985) Enzyme Structure and Mechanism, W.H. Freeman and Co., New York
  • Summary, pp. 405-413
  • Specificity, pp. 17-21
  • Enzyme-substrate complex, enzyme-product complex, pp. 27-30
  • Reaction pathway/kinetics, pp. 195-208
  • pH-dependence of catalysis and state of ionization of active site, pp. 167-171
  • Utilisation of binding energy to increase catalytic constant, pp. 317-319
  • Transition state stabilisation pp. 338-341
  • stereoelectronic effects pp. 245-246
• Graf, L., Hegyi, G., Liko, I., Hepp, J., Medzihradszky, K., Craik, C.S. and Rutter, W.J. (1988) Structural and functional integrity of specificity and catalytic sites of trypsin Intl. J. Peptide and Protein Research 32, 512-518
• Graf, L., Jancso, A. Szilagyi, L. Hegyi, G., Pinter, K., Narayszabo, G. Hepp, J., Medzihradszky, K. and Rutter, W.J. (1988) Electrostatic complementarity within the substrate-binding pocket of trypsin Proc. Natl. Acad. Sci. USA 85, 4961-4965
• Huber, R. and Bode, W. (1978) Structural basis of the activation and action of trypsin Acc. Chem. Res. 11, 114-122
• Kossiakoff, A.A. and Spencer, S.A. (1981) Direct determination of aspartic acid-102 and histidine-57 in the tetrahedral intermediate of the serine proteases: neutron structure of trypsin Biochemistry 20, 6462-6474
• Kraut, J. (1977) Serine proteases: structure and mechanism of catalysis Ann. Rev. Biochem. 46, 331-358
• Polgar, L. (1989) Mechanisms of Protease Action, CRC Press, Florida Chapters 3-6
• Polgar, L. (1990) Common feature of the four types of protease mechanism Biol. Chem. Hoppe-Seyler 371 Suppl. 327-331
• Steitz, T.A. and Shulman, R.G. (1982) Crystallographic and NMR studies of the serine proteases Ann. Rev. Biophys. Bioeng. 11, 419-444
• Stroud, R.M., Kossiakoff, A.A. and Chambers, J.L. (1977) Mechanism of zymogen activation Ann. Rev. Biophys. Bioeng. 6, 177-193
• Tsukada, H. and Blow, D.M. (1985) Structure of alpha-chymotrypsin refined at 1.68Å resolution J. Mol. Biol. 184, 703-711
• Warshel, A., Narayszabo, G., Sussman, F. and Hwang, J.K. (1989) How do serine proteases really work? Biochemistry 28, 3188-3197

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J. Walshaw