Sentence examples for modification with p-Bromophenacyl from inspiring English sources
Its chemical modification with p-Bromophenacyl Bromide abolishes the enzymatic activity without affecting the antiangiogenic effect.
Chemical modification with p-bromophenacyl bromide abolished the enzymatic activity of MVL-PLA2 without affecting its anti-tumor effect, suggesting the presence of 'pharmacological sites' distinct from the catalytic site in snake venom phospholipase A2.
In vitro angiogenesis assays were thus performed using HMEC-1 cells treated with various concentrations of native MVL-PLA2 or with MVL-PLA2 catalytically inactivated by incubation with p-bromophenacyl bromide (BPB).
Indeed, when the esterase activity of the basic PLA2 was eliminated by treatment with p-bromophenacyl bromide, the enzyme retained cytotoxic potency inducing necrosis of certain tumor cells grown in vitro, but not of other cells, such as erythrocytes, for which concomitant esterase activity was also necessary.
Figure 6 shows the scores and the loadings plot of the surface modification with Pd(CH3CN 4 BF4 2.
The docking scores for these calculations were 36.78, 35.29 and 26.63, respectively, showing a better affinity between the PrTX-III target and harpalycin 2, in comparison with aristolochic acid and p-bromophenacyl bromide.
Harpalycin 2 (HP-2) showed a potent inhibitory capacity when compared to the classical sPLA2 inhibitor p-bromophenacyl bromide (p-BPB), with an IC50 calculated at 11.34 ± 0.28 μg per well, whereas p-BPB showed only a marginal inhibition of PrTX-III catalytic active.
The MVL-PLA2 was purified and its phospholipase catalytic activity was inactivated by p-bromophenacyl bromide (BPB) alkylation as described in a previous work [20].
Aggregation experiments were performed with 10 μg of PrTX-III and PrTX-III: HP-2., PrTX-III: aristolochic acid or PrTX-III: p-bromophenacyl bromide.
Aristolochic acid and p-bromophenacyl bromide were used as gold standards sPLA2 inhibitors.
The literature describes that PLA2 loses its catalytic activity when His48 undergoes alkylation by p-bromophenacyl bromide (BPB).
