IUBMB Enzyme Nomenclature


Accepted name: tissue kallikrein

Reaction: Preferential cleavage of Arg bonds in small molecule substrates. Highly selective action to release kallidin (lysyl-bradykinin) from kininogen involves hydrolysis of Met or Leu. The rat enzyme is unusual in liberating bradykinin directly from autologous kininogens by cleavage at two Arg bonds [5]

Other names: glandular kallikrein; pancreatic kallikrein; submandibular kallikrein; submaxillary kallikrein; kidney kallikrein; urinary kallikrein; kallikrein; salivary kallikrein; kininogenin; kininogenase; callicrein; glumorin; padreatin; padutin; kallidinogenase; bradykininogenase; depot-padutin; urokallikrein; dilminal D; onokrein P

Comments: Formed from tissue prokallikrein by activation with trypsin. In peptidase family S1 (trypsin family). Formerly EC and included in EC A large number of tissue kallikrein-related sequences have been reported for rats [16] and mice [7], though fewer seem to exist in other mammals. The few that have been isolated and tested on substrates include mouse γ-renin (EC, submandibular proteinase A (formerly EC [2,15], epidermal growth-factor-binding protein, nerve growth factor γ-subunit, rat tonin [3,4,9], submaxillary proteinases A and B [10], T-kininogenase [18], kallikreins k7 and k8 [17] and human prostate-specific antigen (γ-seminoprotein, [6])

Links to other databases: BRENDA, EXPASY, KEGG, MEROPS, Metacyc, PDB, CAS registry number: 389069-73-2


1. Fiedler, F., Fink, E., Tschesche, H. and Fritz, H. Porcine glandular kallikreins. Methods Enzymol. 80 (1981) 493-532. [PMID: 7043199]

2. Anundi, H., Ronne, H., Peterson, P.A. and Rask, L. Partial amino-acid sequence of the epidermal growth-factor-binding protein. Eur. J. Biochem. 129 (1982) 365-371. [PMID: 6295764]

3. Pesquero, J.L., Boschcov, P., Oliveira, M.C.F. and Paiva, A.C.M. Effect of substrate size on tonin activity. Biochem. Biophys. Res. Commun. 108 (1982) 1441-1446. [PMID: 6295383]

4. Gutkowska, J., Corvol, P., Figueiredo, A.F.S., Inagami, T., Bouhnik, J. and Genest, J. Kinetic studies of rat renin and tonin on purified rat angiotensinogen. Can. J. Biochem. Cell Biol. 62 (1984) 136-142. [PMID: 6043136]

5. Kato, H., Enjyoji, K., Miyata, T., Hayashi, I., Oh-Ishi, S. and Iwanaga, S. Demonstration of arginyl-bradykinin moiety in rat HMW kininogen: direct evidence for liberation of bradykinin by rat glandular kallikreins. Biochem. Biophys. Res. Commun. 127 (1985) 289-295. [PMID: 3844939]

6. Akiyama, K., Nakamura, T., Iwanaga, S. and Hara, M. The chymotrypsin-like activity of human prostate-specific antigen, γ-seminoprotein. FEBS Lett. 225 (1987) 168-172. [PMID: 3691800]

7. Evans, B.A., Drinkwater, C.C. and Richards, R.I. Mouse glandular kallikrein genes. Structure and partial sequence analysis of the kallikrein gene locus. J. Biol. Chem. 262 (1987) 8027-8034. [PMID: 3036794]

8. Fiedler, F. Effects of secondary interactions on the kinetics of peptide and peptide ester hydrolysis by tissue kallikrein and trypsin. Eur. J. Biochem. 163 (1987) 303-312. [PMID: 7043199]

9. Fujinaga, M. and James, M.N.G. Rat submaxillary gland serine protease, tonin. Structure solution and refinement at 1.8 Å resolution. J. Mol. Biol. 195 (1987) 373-396. [PMID: 2821276]

10. Kato, H., Nakanishi, E., Enjyoji, K., Hayashi, I., Oh-ishi, S. and Iwanaga, S. Characterization of serine proteinases isolated from rat submaxillary gland: with special reference to the degradation of rat kininogens by these enzymes. J. Biochem. (Tokyo) 102 (1987) 1389-1404. [PMID: 3844939]

11. Bailey, G.S. Rat pancreas kallikrein. Methods Enzymol. 163 (1989) 115-128. [PMID: 3237072]

12. Blaber, M., Isackson, P.J., Marsters, J.C., Jr, Burnier, J.P. and Bradshaw, R.A. Substrate specificities of growth factor associated kallikreins of the mouse submandibular gland. Biochemistry 28 (1988) 7813-7819. [PMID: 2611215]

13. Chao, J. and Chao, L. Rat urinary kallikrein. Methods Enzymol. 163 (1988) 128-143. [PMID: 3070295]

14. Geiger, R. and Miska, W. Human tissue kallikrein. Methods Enzymol. 163 (1988) 102-115. [PMID: 2975076]

15. Bertrand, R., Derancourt, J. and Kassab, R. Selective cleavage at lysine of the 50 kDa-20 kDa connector loop segment of skeletal myosin S-1 by endoproteinase Arg-C. FEBS Lett. 246 (1989) 171-176. [PMID: 2523317]

16. Wines, D.R., Brady, J.M., Pritchett, D.B., Roberts, J.L. and MacDonald, R.J. Organization and expression of the rat kallikrein gene family. J. Biol. Chem. 264 (1989) 7653-7662. [PMID: 2708383]

17. Elmoujahed, A., Gutman, N., Brillard, M. and Gauthier, F. Substrate specificity of two kallikrein family gene products isolated from the rat submaxillary gland. FEBS Lett. 265 (1990) 137-140. [PMID: 2194829]

18. Xiong, W., Chen, L.-M. and Chao, J. Purification and characterization of a kallikrein-like T-kininogenase. J. Biol. Chem. 265 (1990) 2822-2827. [PMID: 2303430]

[EC created 1965 as EC, transferred 1972 to EC, part transferred 1981 to EC]

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