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PMID:21173178
| Citation |
Toh, EC, Dashper, SG, Huq, NL, Attard, TJ, O'Brien-Simpson, NM, Chen, YY, Cross, KJ, Stanton, DP, Paolini, RA and Reynolds, EC (2011) Porphyromonas gingivalis cysteine proteinase inhibition by kappa-casein peptides. Antimicrob. Agents Chemother. 55:1155-61 |
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| Abstract |
Porphyromonas gingivalis is a major pathogen associated with chronic periodontitis, an inflammatory disease of the supporting tissues of the teeth. The Arg-specific (RgpA/B) and Lys-specific (Kgp) cysteine proteinases of P. gingivalis are major virulence factors for the bacterium. In this study κ-casein(109-137) was identified in a chymosin digest of casein as an inhibiting peptide of the P. gingivalis proteinases. The peptide was synthesized and shown to inhibit proteolytic activity associated with P. gingivalis whole cells, purified RgpA-Kgp proteinase-adhesin complexes, and purified RgpB proteinase. The peptide κ-casein(109-137) exhibited synergism with Zn(II) against both Arg- and Lys-specific proteinases. The active region for inhibition was identified as κ-casein(117-137) using synthetic peptides. Kinetic studies revealed that κ-casein(109-137) inhibits in an uncompetitive manner. A molecular model based on the uncompetitive action and its synergistic ability with Zn(II) was developed to explain the mechanism of inhibition. Preincubation of P. gingivalis with κ-casein(109-137) significantly reduced lesion development in a murine model of infection. |
| Links |
PubMed PMC3067070 Online version:10.1128/AAC.00466-10 |
| Keywords |
Amino Acid Sequence; Animals; Anti-Bacterial Agents; Bacterial Proteins/antagonists & inhibitors; Caseins/chemistry; Cysteine Proteases/metabolism; Cysteine Proteinase Inhibitors/chemical synthesis; Cysteine Proteinase Inhibitors/chemistry; Cysteine Proteinase Inhibitors/pharmacology; Mice; Mice, Inbred BALB C; Molecular Sequence Data; Peptides/chemical synthesis; Peptides/chemistry; Peptides/pharmacology; Porphyromonas gingivalis/drug effects; Porphyromonas gingivalis/enzymology |
| edit table |
Significance
Annotations
| Gene product | Qualifier | GO Term | Evidence Code | with/from | Aspect | Extension | Notes | Status |
|---|---|---|---|---|---|---|---|---|
| GO:0004860: protein kinase inhibitor activity |
ECO:0000315: |
F |
Figure 4. |
complete | ||||
See also
References
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