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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

Boronic Acid Based Inhibitors of Autotaxin: Understanding their Biological Role in Terms of Quantitative Structure Activity Relationships (QSAR)

Author(s): Sotirios Katsamakas and Dimitra Hadjipavlou-Litina

Volume 10 , Issue 1 , 2013

Page: [11 - 18] Pages: 8

DOI: 10.2174/1570180811309010011

Price: $65


Autotaxin (ATX or NPP2) is a newly discovered secreted glycoprotein lyso-phospholipase D (lysoPLD). Its main role is the lysoPLD activity, which transforms lyso-phosphatidylcholine (LPC) into lyso-phosphatidic acid (LPA). ATX contributes to tumor progression, inflammation, obesity and diabetes and constitutes a target for drug design. Various synthetic phospholipid analogues have been explored as ATX inhibitors. However, potent and selective non-lipid inhibitors of ATX are currently not available. Some new ATX inhibitors have been subjected to a Quantitative-Structure Activity Relationships (QSAR) analysis. CMR represents the calculated molar refractivity of the molecules and seems to govern the ATX inhibition. Steric factors are obviously important. No role for lipophilicity was found. Electronic parameters are not found to be present.

Keywords: Boronic Acid based Autotaxin Inhibitors, Hydrophobicity, Molar Refractivity, QSAR, lyso-phosphatidic, cell proliferation, phospholipase, macromolecular systems

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