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These new analogues were found to be moderately active to inhibit H661 cell proliferation.
In our study, it was the most active to inhibit BChE and TYR, while several other Origanum species have been demonstrated to display inhibitory property on cholinesterases to some extent such as Origanum syriacum, Origanum ehrenbergii [28, 29], Origanum vulgare var.
The hexameric condensed tannin was more active to inhibit the pigmentation of the acapsular strain Cap 67 than the capsular strains.
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The latter was used both in active and non-active forms, meaning the activity to inhibit HMG-CoA reductase.
The inability of a primer template that is bound to the polymerase active site to inhibit exonuclease activity indicates that the two activities have independent binding domains.
As to whether Mar is also an active chemical to inhibit proteasome activity, we initiated our studies to examine the effects of Mar on the purified 20 S proteasome by monitoring chymotrypsin-like (ChT-L), trypsin-like (Try-L) and peptidyl-glutamyl peptide-hydrolyzing (PGPH) activities in vitro.
These inhibitors, WEE1 for example, phosphorylate the kinase active site to inhibit cyclin/CDK complex activity (Additional file 2: Table S3) [ 16, 17].
In a study, out of 10 flavonoids isolated from Intsia palembanica methanolic extract, fustin, ampelopsin and 4′-dehydroxyrobidanol were found to be the most active compounds to inhibit the lipase activity of P. acnes using the 2,3-dimercapto-1-propanol tributyrate (BALB) method with IC50 values of 13.7 μM, 36.1 μM, and 40.0 μM, respectively, [ 122].
Active measures to inhibit complement include the use of pharmacological inhibitors of complement as well as surface engineering of the baculoviral vectors through the use of synthetic polymers, pseudotyping or display of complement inhibitors.
However, while sufficient biologically active drug to inhibit HIV and HSV-2 infection was retained in cervicovaginal lavage (CVL) collected following gel application [1], [4], the antiviral activity was markedly reduced when virus was introduced in seminal plasma, reflecting interference by seminal proteins with the antiviral activity of PRO 2000 [3].
Because of the proposed role of PPARγ in inflammation, we investigated the potential of orally active THR0921 to inhibit the pathogenesis of collagen-induced arthritis (CIA).
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