Mutations in Arg143 and Lys192 of the Human Mast Cell Chymase Markedly Affect the Activity of Five Potent Human Chymase Inhibitors

PLoS ONE

Volumn 8, Issue 6, 2013, Pages

  Ahooghalandari, Parvin ^a   Hanke, Nina ^b,c   Thorpe, Michael ^a   Witte, Andreas ^b   Messinger, Josef ^b,d   Hellman, Lars ^a  

^a UPPSALA UNIVERSITY   (Sweden)

^b ABBOTT GMBH AND CO KG   (Germany)

^c ElexoPharm GmbH   (Germany)

^d ORION CORPORATION   (Finland)

Author keywords

[No Author keywords available]

Indexed keywords

ANGIOTENSIN I; ARGININE; CHYMASE; CHYMASE INHIBITOR; ISOLEUCINE; LYSINE; METHIONINE; TYROSINE; 2-(4-(5-FLUORO-3-METHYLBENZO(B)THIOPHEN-2-YL)SULFONAMIDE-3-METHANESULFONYLPHENYL)OXAZOLE-4-CARBOXYLIC ACID; ENZYME INHIBITOR; OXAZOLE DERIVATIVE; SULFONAMIDE;

AMINO TERMINAL SEQUENCE; ARTICLE; CHEMICAL BOND; CONTROLLED STUDY; EMBRYO; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME INACTIVATION; ENZYME INHIBITION; ENZYME SPECIFICITY; HUMAN; HUMAN CELL; MAST CELL; MOLECULAR INTERACTION; MUTATION RATE; PROTEIN EXPRESSION; RESIDUE ANALYSIS; WILD TYPE; CHEMISTRY; GENETICS; METABOLISM; MOLECULAR MODEL; MUTATION; PHENOTYPE; X RAY CRYSTALLOGRAPHY;

ANGIOTENSIN I; ARGININE; CHYMASES; CRYSTALLOGRAPHY, X-RAY; ENZYME INHIBITORS; HUMANS; LYSINE; MODELS, MOLECULAR; MUTATION; OXAZOLES; PHENOTYPE; SUBSTRATE SPECIFICITY; SULFONAMIDES;

EID: 84879241209     PISSN: None     EISSN: 19326203     Source Type: Journal    
DOI: 10.1371/journal.pone.0065988     Document Type: Article

References (32)

1. Kunder CA, St John AL, Abraham SN, (2011) Mast cell modulation of the vascular and lymphatic endothelium. Blood 118: 5383-5393.
2. Lutzelschwab C, Pejler G, Aveskogh M, Hellman L, (1997) Secretory granule proteases in rat mast cells. Cloning of 10 different serine proteases and a carboxypeptidase A from various rat mast cell populations. J Exp Med 185: 13-29.
3. Caughey GH, (2007) Mast cell tryptases and chymases in inflammation and host defense. Immunol Rev 217: 141-154.
4. Pejler G, Ronnberg E, Waern I, Wernersson S, (2010) Mast cell proteases: multifaceted regulators of inflammatory disease. Blood 115: 4981-4990.
5. Galli SJ, Grimbaldeston M, Tsai M, (2008) Immunomodulatory mast cells: negative, as well as positive, regulators of immunity. Nat Rev Immunol 8: 478-486.
6. Forsberg E, Pejler G, Ringvall M, Lunderius C, Tomasini-Johansson B, et al. (1999) Abnormal mast cells in mice deficient in a heparin-synthesizing enzyme. Nature 400: 773-776.
7. Humphries DE, Wong GW, Friend DS, Gurish MF, Qiu WT, et al. (1999) Heparin is essential for the storage of specific granule proteases in mast cells. Nature 400: 769-772.
8. Serafin WE, Reynolds DS, (1990) Neutral proteases of mouse mast cells. Monogr Allergy 27: 31-50.
9. Huang RY, Blom T, Hellman L, (1991) Cloning and structural analysis of MMCP-1, MMCP-4 and MMCP-5, three mouse mast cell-specific serine proteases. Eur J Immunol 21: 1611-1621.
10. Huang R, Hellman L, (1994) Genes for mast-cell serine protease and their molecular evolution. Immunogenetics 40: 397-414.
11. Chandrasekharan UM, Sanker S, Glynias MJ, Karnik SS, Husain A, (1996) Angiotensin II-forming activity in a reconstructed ancestral chymase. Science 271: 502-505.
12. Gallwitz M, Reimer JM, Hellman L, (2006) Expansion of the mast cell chymase locus over the past 200 million years of mammalian evolution. Immunogenetics 58: 655-669.
13. Andersson MK, Enoksson M, Gallwitz M, Hellman L, (2009) The extended substrate specificity of the human mast cell chymase reveals a serine protease with well-defined substrate recognition profile. Int Immunol 21: 95-104.
14. Andersson MK, Karlson U, Hellman L, (2008) The extended cleavage specificity of the rodent beta-chymases rMCP-1 and mMCP-4 reveal major functional similarities to the human mast cell chymase. Mol Immunol 45: 766-775.
15. Andersson MK, Thorpe M, Hellman L, (2010) Arg143 and Lys192 of the human mast cell chymase mediate the preference for acidic amino acids in position P2' of substrates. Febs J 277: 2255-2267.
16. Vernersson M, Ledin A, Johansson J, Hellman L, (2002) Generation of therapeutic antibody responses against IgE through vaccination. Faseb J 16: 875-877.
17. Neuhoff V, Arold N, Taube D, Ehrhardt W, (1988) Improved staining of proteins in polyacrylamide gels including isoelectric focusing gels with clear background at nanogram sensitivity using Coomassie Brilliant Blue G-250 and R-250. Electrophoresis 9: 255-262.
18. Lehtonen JV, Still DJ, Rantanen VV, Ekholm J, Bjorklund D, et al. (2004) BODIL: a molecular modeling environment for structure-function analysis and drug design. J Comput Aided Mol Des 18: 401-419.
19. Puente XS, Sanchez LM, Overall CM, Lopez-Otin C, (2003) Human and mouse proteases: a comparative genomic approach. Nat Rev Genet 4: 544-558.
20. Southan C, (2001) A genomic perspective on human proteases as drug targets. Drug Discov Today 6: 681-688.
21. Reimer JM, Enoksson M, Samollow PB, Hellman L, (2008) Extended substrate specificity of opossum chymase-Implications for the origin of mast cell chymases. Mol Immunol 45: 2116-2125.
22. Karlson U, Pejler G, Tomasini-Johansson B, Hellman L, (2003) Extended substrate specificity of rat mast cell protease 5, a rodent alpha-chymase with elastase-like primary specificity. J Biol Chem 278: 39625-39631.
23. Caughey GH, Beauchamp J, Schlatter D, Raymond WW, Trivedi NN, et al. (2008) Guinea pig chymase is leucine-specific: a novel example of functional plasticity in the chymase/granzyme family of serine peptidases. J Biol Chem 283: 13943-13951.
24. Itoh H, Murakumo Y, Tomita M, Ide H, Kobayashi T, et al. (1996) Cloning of the cDNAs for mast-cell chymases from the jejunum of Mongolian gerbils, Meriones unguiculatus, and their sequence similarities with chymases expressed in the connective-tissue mast cells of mice and rats. Biochem J 314 (Pt 3): 923-929.
25. Gallwitz M, Enoksson M, Thorpe M, Ge X, Hellman L, (2010) The extended substrate recognition profile of the dog mast cell chymase reveals similarities and differences to the human chymase. Int Immunol 22: 421-431.
26. Kervinen J, Crysler C, Bayoumy S, Abad MC, Spurlino J, et al. (2010) Potency variation of small-molecule chymase inhibitors across species. Biochem Pharmacol 80: 1033-1041.
27. Kinoshita A, Urata H, Bumpus FM, Husain A, (1991) Multiple determinants for the high substrate specificity of an angiotensin II-forming chymase from the human heart. J Biol Chem 266: 19192-19197.
28. Sanker S, Chandrasekharan UM, Wilk D, Glynias MJ, Karnik SS, et al. (1997) Distinct multisite synergistic interactions determine substrate specificities of human chymase and rat chymase-1 for angiotensin II formation and degradation. J Biol Chem 272: 2963-2968.
29. Pereira PJ, Wang ZM, Rubin H, Huber R, Bode W, et al. (1999) The 2.2 A crystal structure of human chymase in complex with succinyl-Ala-Ala-Pro-Phe-chloromethylketone: structural explanation for its dipeptidyl carboxypeptidase specificity. J Mol Biol 286: 163-173.
30. Muilenburg DJ, Raymond WW, Wolters PJ, Caughey GH, (2002) Lys40 but not Arg143 influences selectivity of angiotensin conversion by human alpha-chymase. Biochim Biophys Acta 1596: 346-356.
31. Saito K, Muto T, Tomimori Y, Imajo S, Maruoka H, et al. (2003) Mouse mast cell protease-1 cleaves angiotensin I to form angiotensin II. Biochem Biophys Res Commun 302: 773-777.
32. Guo C, Ju H, Leung D, Massaeli H, Shi M, et al. (2001) A novel vascular smooth muscle chymase is upregulated in hypertensive rats. J Clin Invest 107: 703-715.