4-Pyridin-5-yl-2-(3,4,5-trimethoxyphenylamino)pyrimidines: potent and selective inhibitors of ZAP 70.
Activation of the tyrosine kinase ZAP 70 has been shown to be crucial to the transduction of the T-cell receptor signalling pathway, which leads ultimately to proliferation, cytokine gene expression and T-cell effector functions. A series of 2-phenylaminopyrimidines have been identified as potent and selective inhibitors of ZAP 70.
Moffat
D
D
Celltech Therapeutics Limited, Slough, UK. dmoffat@celltech.co.uk
Davis
P
P
Hutchings
M
M
Davis
J
J
Berg
D
D
Batchelor
M
M
Johnson
J
J
O'Connell
J
J
Martin
R
R
Crabbe
T
T
Delgado
J
J
Perry
M
M
D010766:Phosphorylation; D011505:Protein-Tyrosine Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism; D011743:Pyrimidines / Q000737:chemistry / Q000494:pharmacology*; D015398:Signal Transduction; D051746:ZAP-70 Protein-Tyrosine Kinase
D011743:Pyrimidines; D011505:Protein-Tyrosine Kinases; D051746:ZAP-70 Protein-Tyrosine Kinase