Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors.

Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Research Abstract Details 

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Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Abstract Text:

Peng Cui,Jose L Tomsig,William F McCalmont,Sangderk Lee,Christopher J Becker,Kevin R Lynch,Timothy L Macdonald,

Autotaxin (ATX) is an autocrine motility factor that promotes cancer cell invasion, cell migration, and angiogenesis. ATX, originally discovered as a nucleotide phosphodiesterase, is known now to be responsible for the lysophospholipid-preferring phospholipase D activity in plasma. As such, it catalyzes the production of lysophosphatidic acid (LPA) from lysophophatidylcholine (LPC). ATX is thus an attractive drug target; small molecular inhibitors might be efficacious in slowing the spread of cancers. With this study we have generated a series of beta-keto and beta-hydroxy phosphonate derivatives of LPA, some of which are potent ATX inhibitors.

Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Publishing Authors By Initials

P Cui,JL Tomsig,WF McCalmont,S Lee,CJ Becker,KR Lynch,TL Macdonald,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Journal Published:

PUBLICATION TYPE: Research Support, N.I.H., Extr

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 1634-40

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 13

MONTH: 01

YEAR: 2007

Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Information

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LANGUAGE: eng

NlmUniqueID: 9107377

Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: antagonists & inhibitors

Chemical & Substance for Abstract: Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors. Information

Substance Name: Pyrophosphatases

Registry Number: EC 3.6.1.-

Grant and Affiliation Information for Synthesis and biological evaluation of phosphonate derivatives as autotaxin (ATX) inhibitors.

AFFILIATION: Department of Chemistry, University of Virginia, McCormick Road, Charlottesville, VA 22904, USA. pc3n@virginia.edu

Country: England

AGENCY: United States NIGMS

GRANT: R01 GM 052722

ACRONYM: GM

MEDLINETA: Bioorg Med Chem Lett

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