[HTML][HTML] PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo
PD 098059 has been shown previously to inhibit the dephosphorylated form of mitogen-
activated protein kinase kinase-1 (MAPKK1) and a mutant MAPKK1 (S217E, S221E), which
has low levels of constitutive activity (Dudley, DT, Pang, L., Decker, SJ, Bridges, AJ, and
Saltiel, AR (1995) Proc. Natl. Acad. Sci. USA 92, 7686-7689). Here we report that PD
098059 does not inhibit Raf-activated MAPKK1 but that it prevents the activation of MAPKK1
by Raf or MEK kinase in vitro at concentrations (IC 50= 2-7 μM) similar to those …
activated protein kinase kinase-1 (MAPKK1) and a mutant MAPKK1 (S217E, S221E), which
has low levels of constitutive activity (Dudley, DT, Pang, L., Decker, SJ, Bridges, AJ, and
Saltiel, AR (1995) Proc. Natl. Acad. Sci. USA 92, 7686-7689). Here we report that PD
098059 does not inhibit Raf-activated MAPKK1 but that it prevents the activation of MAPKK1
by Raf or MEK kinase in vitro at concentrations (IC 50= 2-7 μM) similar to those …