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All studied iRFPs exhibited efficient binding of the endogenous biliverdin chromophore in cultured neurons and in the mammalian brain and can be readily applied to neuroimaging.
Despite loss of the SET domain in MLL fusion proteins, they can actively increase binding of the endogenous and intact MLL to the target genes 5 to 15 fold, leading to increased H3K4 trimethylation [48].
Second, studies of naturally occurring loss-of-function mutations in MC4R from obese subjects [23] [27], in conjunction with structure-function studies [28], [29], have identified several key regions of the receptor that are required for binding of the endogenous ligand, α-MSH.
Taking into account that these A2AR antagonists behave similarly than the A2AR agonist CGS-21680 in terms of binding to A1R-A2AR and A2AR-D2R heteromers, it is expected that these four compounds compete equally for the binding of the endogenous agonist at pre- and at postsynaptic sites.
To block the binding of the endogenous Sema3 with Nrps, we used function-blocking antibodies that specifically blocked ligand-binding sites in Nrps.
Methods: We used X-ray crystallography to obtain atomic detail of the binding modes of TBBPA and 3-OH-BDE-47 to estrogen sulfotransferase for comparison with binding of the endogenous substrate estradiol.
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By presenting the antigen in its native conformation for immunisation and hybridoma selection, this procedure promotes the generation of antibodies capable of binding to the endogenous protein.
Furthermore, antibodies generated against a purified recombinant protein are frequently incapable of binding to the endogenous protein in its native context.
Consistent with this model, overexpression of wild-type XIAP increased the amount of p65 binding to the endogenous Beclin 1 promoter (assessed by chromatin immunoprecipitation), whereas the overexpression of XIAPH467A failed to reproduce this effect (Fig. 4B).
As shown in Fig. 4, there was marked enrichment of palladin binding to the endogenous SMA promoter region in both A404 and R518 cells (p<0.05).
Low concentrations of cAMP (0.5 µM-2.5 µM) drastically reduced the binding of both the endogenous PKA-RIβ, and of cAMP sponge, which was completely abolished at concentrations above 10 µM (Figure 3b and supplementary Figure S1).
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