Suppression of Pathogenicity of Porphyromonas gingivalis by Newly Developed Gingipain Inhibitors

@article{Kadowaki2004SuppressionOP,
  title={Suppression of Pathogenicity of Porphyromonas gingivalis by Newly Developed Gingipain Inhibitors},
  author={Tomoko Kadowaki and Atsuyo Baba and Naoko Abe and Ryosuke Takii and Munetaka Hashimoto and Takayuki Tsukuba and Shinji Okazaki and Yoshimitsu Suda and Tetsuji Asao and Kenji Yamamoto},
  journal={Molecular Pharmacology},
  year={2004},
  volume={66},
  pages={1599 - 1606}
}
Arg-gingipain (Rgp) and Lys-gingipain (Kgp) are cysteine proteinases produced by Porphyromonas gingivalis, a major etiological bacterium of periodontal diseases. Here we show a series of small peptide analogs able to inhibit either Rgp or Kgp, which are synthesized on the basis of the cleavage site specificity of human salivary histatins by each enzyme. Among this series of compounds, carbobenzoxy-Lys-Arg-CO-Lys-N-(CH3)2 (KYT-1) and carbobenzoxy-Glu(NHN(CH3)Ph)-Lys-CO-NHCH2Ph (KYT-36) were… Expand
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The present study sets the pace for the development of tailored next-generation drugs to tackle P. gingivalis by reporting the high-resolution complex structure of Kgp with KYT-36, a peptide-derived, potent, bioavailable and highly selective inhibitor. Expand
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TLDR
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Enzymatic Characteristics and Activities of Gingipains from Porphyromonas gingivalis.
  • T. Kadowaki
  • Medicine, Biology
  • Methods in molecular biology
  • 2021
TLDR
This chapter describes the methods used to analyze gingipains, which play crucial roles in the virulence of P. gingivalis and are critical in processing fimbriae and several bacterial proteins that contribute to hemagglutination, coaggregation, and hemoglobin binding. Expand
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A molecular model based on the uncompetitive action and its synergistic ability with Zn(II) was developed to explain the mechanism of inhibition and κ-casein(109-137) inhibits in an uncompetitive manner. Expand
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TLDR
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TLDR
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A role for gingipains in cellular responses and bacterial survival in Porphyromonas gingivalis-infected cells.
TLDR
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TLDR
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Gingipains from Porphyromonas gingivalis promote the transformation and proliferation of vascular smooth muscle cell phenotypes.
TLDR
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