• Proceedings of the PSK Conference
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• 2002.04a
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• pp.109.1-109.1
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• 2002

• Proceedings of the PSK Conference
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• 2003.04a
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• pp.133.1-133.1
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• 2003

Cathepsin K (CK) is a cysteine protease that plays a major and essential role in osteoclast-mediated degradation of collagen matrix of bone. Its tissue-limited distribution and pivotal contribution to bone resorption meet the requirements as the potential therapeutic target of the disease with excessive bone loss such as osteoporosis. In a search for potent CK inhibitors. we found OST-5440 that effectively inhibited bone resorption in vivo as well as in vitro. (omitted)

• Maxillofacial Plastic and Reconstructive Surgery
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• v.33 no.1
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• pp.26-31
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• 2011

Purpose: Chronic inflammatory gingival lesions occur as pyogenic granulomas or non-specific chronic suppurative lesions. Methods: Of the 59 chronic inflammatory gingival lesions examined, plasma cell granuloma (n=14), which showed an intense antibody-mediated immune reaction with the increased infiltration of plasma cells, was observed as a pseudotumor-like gingival overgrowth and myofibroblastic or fibrohistiocytitc proliferation of stromal cells with a heavy collection of plasma cells. The levels of CD3, CD20, CD31, CD68, RANKL, cathepsin G, cathepsin K, lysozyme, TNF${\alpha}$, MMP-2, and MMP-9 in the 14 cases of gingival plasma cell granuloma with immunohistochemical detection were measured to determine the pathogenetic progresses of the plasma cell granuloma compared to the common pyogenic granuloma (n=45) in the gingiva. Results: The gingival lesions of the plasma cell granuloma could be divided into three histological types, plasma cell predominant type (PPT, n=8), mixed inflammatory cell type (MICT, n=2), and sclerosed fibrosis type (SFT, n=4). The PPT showed a condensed infiltration of plasma cells into the perivascular spaces of the granulomatous lesion with frequent formation of Russel's body in their cytoplasm. The MICT showed the concomitant infiltration of many macrophages together with plasma cells, resulting in the diffuse destruction of stromal fibrous tissue. The SFT showed granulomatous lesions replaced gradually by thick collagenous fibrous tissue, resembling an inflammatory pseudotumor. The SFT expressed strongly the lymphocytic markers, CD3 and CD20, and the macrophage/monocyte markers, CD31 and CD68, but showed reduced expression of common inflammatory markers, TNF${\alpha}$, cathepsin G, lysozyme, MMP-2, and MMP-9, as well as the reduced expression of osteoclastogenic markers, RANKL and cathepsin K. Conclusion: These results suggest that a gingival plasma cell granuloma shows variable gene expression for cell-mediated immunity and stromal tissue degeneration, undergoing sclerotic fibrosis with a persistent inflammatory reaction.

• Bulletin of the Korean Chemical Society
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• v.35 no.2
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• pp.345-346
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• 2014

• Korean Journal of Food Science and Technology
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• v.41 no.4
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• pp.446-451
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• 2009

In this study, cathepsin S (CTSS) inhibitory fraction was isolated from Paecilomyces tenuipes and anti-obesitic effects of the fraction were evaluated in mice, fed a high-fat diet. Hot water extract of P. tenuipes (DHW) was divided into 2 fractions, water eluate fraction (DHP1) and methanol eluate fraction (DHP2) using Diaion HP-20. $IC_{50}$ values for DHW, DHP1 and DHP2 against CTSS were 108.7, 890.3 and 2.3 ${\mu}g$/mL, respectively. To evaluate anti-obesitic effects of the fractions, each fraction was administrated orally to C57BL/6 mice for 4 weeks with a high-fat diet. DHP2 had the highest inhibitory effect on CTSS activity, causing serious reduction in weight gain, a reduction in the amount of adipose tissue and in serum lipids levels. These results suggest that the inhibition of CTSS by compounds derived from P. tenuipes may be effective in preventing and in ameliorating obesity.

• Proceedings of the Zoological Society Korea Conference
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• 1994.10a
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• pp.219.2-219
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• 1994

No Abstract, See Full Text

• Bulletin of the Korean Chemical Society
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• v.29 no.8
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• pp.1467-1471
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• 2008

The design, synthesis, and biological evaluation of structurally novel N-cyanopyrazolidine and N-cyanohexahydropyridazine derivatives as cathepsin inhibitors are described. In vitro assay reveals that several compounds exhibit highly potent and selective profiles against cathepsins K or S.

• Journal of Microbiology and Biotechnology
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• v.10 no.1
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• pp.81-85
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• 2000

An elastase inhibitor, SMFEI02, was isolated from culture broth of Streptomyces lavendulae SMF11. The inhibitor was purified by ultrafiltration followed by XAD-7 column and Dowex-1 anion-exchange chromatographies, and preparative HPLC. The molecular formula was determined to be $C_{14}H_{16}N_2O_2$ (MW244) by HRFAB-MS analysis. The inhibitor was identified to be a diketopiperazine cyclo(S-Phe-S-Pro) by the optical rotation value and MNR spectral data, and showed inhibitory activities for trypsin, chymotrypsin, cathepsin B, and papain as well as elastase with the Ki values ranging from 1.78mM to $2.86{\;}\mu\textrm{m}$. The inhibition showed a competitive mode for elastase, chymotrypsin, and cathepsin B, whereas it showed a noncompetitive mode for trypsin and papain.

• Journal of Periodontal and Implant Science
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• v.45 no.5
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• pp.169-177
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• 2015

Purpose: Despite the high success rates of endosseous dental implants, their placement is restricted according to the height and volume of bone available. The use of short or mini dental implants could be one way to overcome this limitation. Thus, this study aimed to compare standard, short, and mini dental implants with regard to associated clinical parameters and peri-implant crevicular fluid (PICF) levels of cathepsin-K (CTSK), RANK ligand (RANKL), and osteoprotegerin (OPG), after prosthodontic loading. Methods: A total of 78 non-submerged implants (Euroteknika, $Aesthetica^{+2}$, Sallanches, France) were installed in 30 subjects (13 male, 17 female; range, 26-62 years) who visited the clinic of the Periodontology Department, Faculty of Dentistry, Selcuk University. Sampling and measurements were performed on the loading date (baseline) and 2, 14, and 90 days after loading. Assessment of the peri-implant status for the implant sites was performed using the pocket probing depth (PPD), modified plaque index, modified gingival index, modified sulcular bleeding index, and radiographic signs of bone loss. PICF samples collected from each implant were evaluated for CTSK, RANKL, and OPG levels using the ELISA method. Keratinized tissue and marginal bone loss (MBL) were also noted. Results: Clinical parameters statistically significantly increased in each group but did not show statistical differences between groups without PPD. Although implant groups showed a higher MBL in the upper jaw, only the standard dental group demonstrated a statistically significant difference. At 90 days, the OPG:sRANKL ratio and total amounts of CTSK for each group did not differ from baseline. Conclusions: Within the limitations of this study, both short and mini dental implants were achieving the same outcomes as the standard dental implants in the early period after loading.

• Biomolecules & Therapeutics
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• v.30 no.4
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• pp.348-359
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• 2022

Gastric adenocarcinoma is among the top causes of cancer-related death and is one of the most commonly diagnosed carcinomas worldwide. Benzyl isothiocyanate (BITC) has been reported to inhibit the gastric cancer metastasis. In our previous study, BITC induced apoptosis in AGS cells. The purpose of the present study was to investigate the effect of BITC on autophagy mechanism in AGS cells. First, the AGS cells were treated with 5, 10, or 15 μM BITC for 24 h, followed by an analysis of the autophagy mechanism. The expression level of autophagy proteins involved in different steps of autophagy, such as LC3B, p62/SQSTM1, Atg5-Atg12, Beclin1, p-mTOR/mTOR ratio, and class III PI3K was measured in the BITC-treated cells. Lysosomal function was investigated using cathepsin activity and Bafilomycin A1, an autophagy degradation stage inhibitor. Methods including qPCR, western blotting, and immunocytochemistry were employed to detect the protein expression levels. Acridine orange staining and omnicathepsin assay were conducted to analyze the lysosomal function. siRNA transfection was performed to knock down the LC3B gene. BITC reduced the level of autophagy protein such as Beclin 1, class III PI3K, and Atg5-Atg12. BITC also induced lysosomal dysfunction which was shown as reducing cathepsin activity, protein level of cathepsin, and enlargement of acidic vesicle. Overall, the results showed that the BITC-induced AGS cell death mechanism also comprises the inhibition of the cytoprotective autophagy at both initiation and degradation steps.