Discovery of novel hydroxamates as highly potent tumor necrosis factor-α converting enzyme inhibitors. Part II: Optimization of the S3′ pocket

2008 ◽  
Vol 18 (21) ◽  
pp. 5809-5814 ◽  
Author(s):  
Robert D. Mazzola ◽  
Zhaoning Zhu ◽  
Lisa Sinning ◽  
Brian McKittrick ◽  
Brian Lavey ◽  
...  
Keyword(s):  
Tumor Necrosis Factor ◽  
Tumor Necrosis ◽  
Tumor Necrosis Factor Α ◽  
Enzyme Inhibitors ◽  
Converting Enzyme ◽  
Converting Enzyme Inhibitors ◽  
Factor Α ◽  
Necrosis Factor ◽  
Potent Tumor

Tumor Necrosis Factor-α-converting Enzyme (TACE) Levels in Periodontal Diseases

2008 ◽  
Vol 87 (3) ◽  
pp. 273-277 ◽  
Author(s):  
N. Bostanci ◽  
G. Emingil ◽  
B. Afacan ◽  
B. Han ◽  
T. Ilgenli ◽  
...  
Keyword(s):  
Tumor Necrosis Factor ◽  
Tumor Necrosis ◽  
Tumor Necrosis Factor Α ◽  
Periodontal Diseases ◽  
Immunosuppressive Treatment ◽  
Aggressive Periodontitis ◽  
Converting Enzyme ◽  
Factor Α ◽  
Necrosis Factor ◽  
Healthy Persons

Tumor necrosis factor-α-converting enzyme (TACE) is a metalloprotease which can shed several cytokines from the cell membrane, including receptor activator of NF-κB ligand (RANKL). This study aimed to investigate the hypothesis that TACE would be elevated in the gingival crevicular fluid (GCF) of persons with periodontitis. Total TACE amounts in GCF were higher in persons with chronic and aggressive periodontitis than in those with gingivitis or in healthy persons. TACE concentrations in GCF were higher in persons with chronic and aggressive periodontitis than in those with gingivitis, although not significantly higher than in healthy persons. Persons with chronic periodontitis receiving immunosuppressive treatment exhibited over 10-fold lower TACE levels than the other periodontitis groups. TACE was positively correlated with probing pocket depth, clinical attachment levels, and RANKL concentrations in GCF. In conclusion, the increased GCF TACE levels in persons with periodontitis and their positive correlation with RANKL may indicate an association of this enzyme with alveolar bone loss, and may warrant special attention in future therapeutic approaches.

Discovery of Novel Hydantoins as Selective Non-Hydroxamate Inhibitors of Tumor Necrosis Factor-α Converting Enzyme (TACE).

ChemInform ◽  
2007 ◽  
Vol 38 (29) ◽  
Author(s):  
James E. II Sheppeck ◽  
John L. Gilmore ◽  
Anle Yang ◽  
Xiao-Tao Chen ◽  
Chu-Biao Xue ◽  
...  
Keyword(s):  
Tumor Necrosis Factor ◽  
Tumor Necrosis ◽  
Tumor Necrosis Factor Α ◽  
Converting Enzyme ◽  
Factor Α ◽  
Necrosis Factor
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