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Vascular Endothelial Growth Factor Receptor KDR Tyrosine Kinase Activity Is Increased by Autophosphorylation of Two Activation Loop Tyrosine Residues*
It is demonstrated that tyrosine kinase antagonists can preferentially inhibit either the unactivated or activated form of the enzyme, which is a consequence of an increased affinity for both ATP and the peptide substrate and has no effect on k cat, the intrinsic catalytic activity of the enzymes.
Potent hFPRL1 (ALXR) agonists as potential anti-inflammatory agents.
Discovery and optimization of chromenotriazolopyrimidines as potent inhibitors of the mouse double minute 2-tumor protein 53 protein-protein interaction.
Tumor protein 53 (p53) is a critical regulator of cell cycle and apoptosis that is frequently disabled in human tumors. In many tumor types, p53 is deleted or mutated, but in others p53 is
New 'chemical probes' to examine the role of the hFPRL1 (or ALXR) receptor in inflammation.
Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease.
1 (AMG319), a compound with an IC50 of 16 nM in a human whole blood assay (HWB), excellent selectivity over a large panel of protein kinases, and a high level of in vivo efficacy as measured by two rodent disease models of inflammation are identified.
Dipeptidyl-quinolone derivatives inhibit hypoxia inducible factor-1α prolyl hydroxylases-1, -2, and -3 with altered selectivity.
The synthesis and activity of dipeptidyl analogues derived from a potent but non-selective quinolone scaffold are reported, found to be ∼10-fold more potent against PHD1 and PHD3 than againstPHD2, whereas the specific parent compound had shown no appreciable selectivity among the different PHD isoforms.
Discovery of potent LPA2 (EDG4) antagonists as potential anticancer agents.