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Edward A. McKenzie talks
with ScienceWatch.com and answers a few
questions about this month's New Hot Paper in the field
of Pharmacology & Toxicology. The author has
also sent along images of their work.
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Article Title: Heparanase: a target for drug
discovery in cancer and inflammation
Authors:
McKenzie,
EA
Journal: BRIT J PHARMACOL
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Figures and descriptions:
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Figure 1:
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Figure 1:
The active heparanase enzyme capable of
digesting heparan sulfate is generated
by proteolytic cleavage of the latent
pro- form of the enzyme. Inhibitors
have been shown to block a number of
heparanase mediated processes such as
invasion, motility and
angiogenesis.
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Figure 2:
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Figure 2:
Heparanase has an important
housekeeping role in degrading recycled
glycosaminoglycan chains of
internalized HSPG molecules. In the
scenario of a malignant tumour cell
however, it is proposed that a
combination of increased heparanase
expression and secretion could rapidly
mobilize ECM components required for
proliferation and metastases (adapted
from Shafat et al.,
2006a).
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Figure 3:
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Figure 3:
The OGS high throughput screening assay
(a) shows the route to identify drugs
that inhibit heparanase cleavage of
heparan sulphate bound to growth
factors. The OGS inhibitor OGT 2492 (b)
was identified in this screen as a
potent angiogenesis inhibitor.
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2008 : September 2008 - New Hot Papers : Edward A. McKenzie - Figures & Descriptions
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