Small ligands interacting with the phosphotyrosine binding pocket of the Src SH2 protein
Various small fragments bearing phosphate, phosphonate or phosphonic acid moieties have been prepared through parallel synthesis and their binding potencies evaluated on the Src SH2 protein using a BIAcore assay. This provided us insight into the requirement of the Src SH2 pTyr binding pocket and some promising small ligands have been characterised.
Novel hydroxyphosphonate inhibitors of CD-45 tyrosine phosphatase
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.
Frechette, Roger F.,Ackerman, Caridad,Beers, Scott,Look, Rich,Moore, John
p. 2169 - 2172
(2007/10/03)
Phosphonate-containing inhibitors of tyrosine-specific protein kinases
Tyrosine-specific protein kinases (TPK) are important signal transducing enzymes involved in normal cellular growth and differentiation and have been implicated in the etiology of a number of human neoplastic processes. Efforts to develop agents which inh
Burke Jr.,Li,Bolen,Marquez
p. 1577 - 1581
(2007/10/02)
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