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PAK1 is activated primarily by binding to active Cdc42 or Rac1 [65], which in turn binds and activates MEK to stimulate ERK1/2 activation [66].
ROK-α is a direct effector of the Rho GTPase, which is activated by binding to active Rho [ 63].
By using spectroscopic measurement, they revealed that the inhibition of lipoxygenase 1 activity by curcumin can be due to binding to active center iron and curcumin after binding to the phosphatidylcholine micelles acts as an inhibitor of lipoxygenase 1.
As the specific binding to active targets may have a profound impact on the overall pharmacological activity [32], the effects of a variety pattern of protein binding reflected in the uptake profiles by cell membrane on therapeutic efficacy of drugs could be adapted as a primary screening means.
While plant NOX proteins are directly regulated by calcium, phosphorylation [ 290, 297, 298] and by binding to active Rop GTPases, positive regulatory feedback between NOX-ROS and ROS-activated calcium channels is proposed to operate at the growing tip contributing to the tip-high cytoplasmic free calcium gradient both in pollen tubes and root hairs [ 290, 298].
Substrate binding to active DM-PaDDAH was accompanied by conversion to l-citrulline, which binds to the enzyme with relatively weak affinity, KD DM/ l -cit) = 3.6 mM as measured by NMR.
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The results demonstrated that the nonspecific binding of the radiotracer was washed out rapidly and caused increased tumor-to-background ratio due to the irreversible and selective bindings to active state of EGFR kinase.
Lysine interferes with the activation of plasminogen into plasmin by tissue plasminogen activator by binding to plasminogen active sites, thereby affecting the plasmin-induced MMP activation cascade [ 5].
Many TG2 inhibitors, in addition to inhibiting its enzymatic activity by directly binding to the active site, induce conformational changes in TG2 protein [ 48].
Both of these compounds selectively inhibit PHD2 by binding to the active site within PHD2 where HIFs bind and stimulate HIF activity [ 2].
BSO depletes GSH by binding to the active site of GCLC non-covalently, inhibiting the activity of GCLC [23].
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