When expressed at high levels, these DN mutants reduce or eliminate RTK activity by dimerizing with wild-type receptors in a ligand-dependent manner, producing inactive complexes that cannot undergo transphosphorylation because they have only one kinase domain.
The active DDT metabolites o,p´-DDT, p,p´-DDT, and o,p´-DDD potentiated CBP transactivation in a dose-dependent manner, whereas the inactive DDT metabolite, p,p´-DDA, had no effect.
We demonstrate that UTX, in a demethylase activity-independent manner, facilitates conversion of inactive enhancers in embryonic stem cells to an active (H3K4me1+/H3K27ac+) state by recruiting and coupling the enzymatic functions of MLL4 and p300.
Each of these points of view is stated with clear positions, waging debates with each other in a tit-for-tat manner, breaking the dull and inactive situation of many years in the academic field of "nation studies" (Ma Rong, 2015).
Recombinant Fam20C phosphorylated each of these proteins in a time-dependent manner in vitro, whereas an inactive Fam20C D478A mutant did not.
Conversely, overexpression of kinase-dead NDR resulted in a 2.7-fold increase, suggesting that catalytically inactive NDR acts in a dominant-negative manner as already reported in another setting [ 15].
Treatment of MDA-MB-231 cells with F1 and F2 induced a decrease in the level of the inactive caspase-3 in a dose dependent manner indicating its cleavage into activated form.
As expected, the expression of CD-zTERT in the zTERT morphants did not restore telomerase activity, confirming that this mutant is catalytically inactive, and also functioned in a dominant-negative manner against authentic telomerase activity (Figure 6C, a, b).
Previous Phase I/II studies had shown that, while flavopiridol induces apoptosis in CLL cells in a p53-independent manner in vitro, the drug is inactive using a 24- to 72-h CIVI schedule.
Indeed, treatment of WT neurons with CP2 increased levels of NADH in a dose-dependent manner compared to vehicle or an inactive CP2 analog, a neutral tricyclic pyrone compound TP17 (Hong et al., 2009) (Fig. 5G).
