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Naltrexone is a competitive antagonist for opioid receptors, effectively blocking the effects of endorphins and opiates.
Cetuximab, a chimeric Mab, is a competitive antagonist for EGFR.
To determine whether the action of DEX on Ostf1 expression was receptor-mediated, a competitive antagonist for glucocorticoid receptor (GR) RU486 was used for the co-treatment study.
The use of a competitive antagonist for mineralocorticoid receptor (MR), spironolactone in DEX co-treatment did not exhibit noticeable effects on DEX-induced Ostf1 expression.
NK4 has been isolated as a competitive antagonist for HGF and the c-Met receptor [ 12], and subsequent studies have shown that NK4 also inhibits the angiogenic response induced by basic fibroblast growth factor (bFGF) and VEGF [ 13].
This effect is not due to MAA acting as a competitive antagonist for ERα, as MAA does not compete with E2 for binding to ERα (Jansen et al. 2004).
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In VAC, the K3L ORF functions as an eIF2α decoy homolog; the E3L ORF encodes a double-stranded RNA binding protein that inhibits 2'5'-OAS, the RNaseL system, and PKR (EIF2AK2); and the B18R and B8R ORFs are predicted to encode soluble and cell surface receptors that may act as competitive antagonists for type I and type II interferons, respectively (for review, see [8]).
They are competitive antagonists for PI hydrolysis mediated via Gq but have agonist activity that results in activation of ERK via Gi.
First, they may be released (Corradi et al., 1995; Levine et al., 1997; Muzio et al., 1999; Wilson et al., 2004; Evans et al., 2006) and act as competitive antagonists for IL-1RI, in a similar manner to sIL-1RA.
185 HTS has also been used to discover two classes of competitive antagonists for the interaction B7.1/CD28, involved into the T-cell response augmentation, with potential therapeutic applications in immunotherapy after transplantation or autoimmune diseases.
Current opinion suggests that classical competitive antagonists for PXR that bind in the ligand-binding pocket may be difficult to identify (Xue et al. 2007a) compared with allosteric antagonists that bind elsewhere on the protein surface (Ekins et al. 2007, 2008a).
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