Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:3.4.24.3 (collagenase)
 18,340 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The levels of collagenolytic activity of strains HM-1:1 MSS (HM-1), (HM-1), 200-NIH, and HK-9 of Entamoeba histolytica were compared. Collagen degradation was evaluated by sodium dodecyl sulfate-polyacrylamide gel electrophoresis. Conditioned media as well as extracts of the highly virulent strain HM-1 effectively degraded native type I collagen. Significantly lower activity was found in the analogous fractions of strains 200-NIH and HK-9, which are not as virulent. The collagenolytic activity of strain HM-1 was associated with the isolated plasma membrane fraction and could be eluted from the membranes by buffers of high ionic strength, indicating that it is not an integral membrane protein. Unlike the vertebrate and the clostridial collagenases, the collagenolytic activity of E. histolytica HM-1 was enhanced in presence of dithiothreitol and was inhibited by N-ethylmaleimide. The correlation between virulence of the individual strains and their collagenolytic activity suggests that collagenase might play a role in pathogenesis of amoebiasis. The localization of the enzyme on the plasma membrane and its presence in the extracellular medium favor this view.
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PMID:Correlation of virulence and collagenolytic activity in Entamoeba histolytica. 629 42

The transcription factor ETS-1 is induced in endothelial cells (ECs) by angiogenic growth factors and the specific elimination of ETS-1 synthesis by antisense oligodeoxynucleotide inhibited angiogenesis in vitro (Iwasaka et al., 1996, J Cell Physiol 169:522-531). To understand the precise role of ETS-1 in angiogenesis, we established both high and low ETS-1 expression EC lines and compared angiogenic properties of these cell lines with those of the parental murine EC line, MSS-31. Although growth rate was almost identical for each cell line, the invasiveness was markedly enhanced in high ETS-1 expression cells and reduced in low ETS-1 expression cells compared with that of parental cells. The gene expressions of matrix metalloproteinases (MMP-1, MMP-3, and MMP-9) and gelatinolytic activity of MMP-9 were significantly increased in high ETS-1 expression cells. Low ETS-1 expression cells could not spread on a vitronectin substratum, and the phosphorylation of focal adhesion kinase was markedly impaired because of the reduced expression of integrin beta3. These results indicate that ETS-1 is a principal regulator that converts ECs to the angiogenic phenotype.
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PMID:ETS-1 converts endothelial cells to the angiogenic phenotype by inducing the expression of matrix metalloproteinases and integrin beta3. 1004 76

The SAR of a series of sterically hindered sulfonamide hydroxamic acids with relatively large P1' groups is described. The compounds typically spare MMP-1 while being potent inhibitors of MMP-13. The metabolically more stable compounds in the series contain either a monocyclic or bicyclic pyran ring adjacent to the hydroxamate group. Despite the sparing of MMP-1, pre-clinical and clinical studies revealed that fibrosis in rats and MSS in humans is still produced.
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PMID:Pyran-containing sulfonamide hydroxamic acids: potent MMP inhibitors that spare MMP-1. 1517 39