204130-63-2Relevant academic research and scientific papers
Nitroarylhydroxymethylphosphonic acids as inhibitors of CD45
Beers, Scott A.,Malloy, Elizabeth A.,Wu, Wei,Wachter, Michael P.,Gunnia, Uma,Cavender, Druie,Harris, Crafford,Davis, Janet,Brosius, Ruth,Pellegrino-Gensey, J. Lee,Siekierka, John
, p. 2203 - 2211 (2007/10/03)
A series of nitroarylhydroxymethylphosphonic acids was synthesized and evaluated as inhibitors of CD45. It was discovered that both the alpha hydroxy and nitro groups are essential for activity. Potency is enhanced by the addition of a large lipophilic group on the aryl ring adjacent to the phosphonic acid moiety. Kinetics studies have shown that these compounds are competitive inhibitors and thus bind at the active site of this enzyme.
Novel hydroxyphosphonate inhibitors of CD-45 tyrosine phosphatase
Frechette, Roger F.,Ackerman, Caridad,Beers, Scott,Look, Rich,Moore, John
, p. 2169 - 2172 (2007/10/03)
CD-45 tyrosine phosphatase [E.C. 3.1.3.48] is an important player in the regulation of cell activation and proliferation in hematopoetic cells. As part of a program in immune response modulation, we prepared the first series of small organic molecule inhibitors of CD-45. The preparation and in vitro screening of these hydroxyphosphonates is described herein.
