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Synthesis and structure–activity relationships of tyrosine-based inhibitors of autotaxin (ATX)

✍ Scribed by James E. East; Andrew J. Kennedy; Jose L. Tomsig; Alexandra R. De Leon; Kevin R. Lynch; Timothy L. Macdonald

Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 844 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.09.030

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✦ Synopsis

Autotaxin (ATX) is a secreted soluble enzyme that generates lysophosphatidic acid (LPA) through its lysophospholipase D activity. Because of LPA's role in neoplastic diseases, ATX is an attractive therapeutic target due to its involvement in LPA biosynthesis. Here we describe the SAR of ATX inhibitor, VPC8a202, and apply this SAR knowledge towards developing a high potency inhibitor. We found that electron density in the pyridine region greatly influences activity of our inhibitors at ATX.

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