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Conversely, designing probes based on potent ATP-competitive inhibitors such as probe 2 will minimize nonspecific binding, but these probes will not bind to the full kinome.
We set out to determine the ability of the peptide aptamers to bind to the full length RasGAP protein in mammalian cells.
In view of the above results we explored whether PAO could bind to the full length H-Ras protein in vitro, and if so, whether the peptide containing C181 and C184 was the preferred site for interaction.
The ΔN isoforms can bind to the full length transactivating (TA) isoforms of p53, p63 and p73, and antagonize their function.
Efforts have focused on improving the affinity of lead compounds that bind to the full extent of the dimer interface with a 1 modulator/dimer stoichiometry, in some cases using the properties of thiazides with 2 modulator/dimer stoichiometry.
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Unexpectedly, as shown in Fig. 6C, the amino terminal deletion or the mutated RPEL of MRTF-A still bound to the full length of palladin, indicating that other MRTF-A motifs interact with palladin and that palladin does not compete with actin for the RPEL domain.
As shown in Figure 1d, TAp63 α bound to the full length or the WW domain of Pin1, but not the PPIase domain, Pin1(W34A), or Pin1 Y23A).
Dror et al. have shown that the active state of the β2AR bound to the full agonist requires a substantially longer time (>6 μs) to move to the inactive state in the cMD simulations.
The heparin-binding domain was mapped to the RRH 555-557) at the C-terminal region of GEP, implying that HS only binds to the full length GEP but not most of the granulin subunits generated from posttranslational proteolytic cleavage.
All three Rab effectors bound to the full-length LIC1 but not to untreated beads.
Binding to the full-length enzyme was non-stoichiometric, indicating there is more than one site where small molecules can bind non-specifically.
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