Sentence examples for cellular engagement from inspiring English sources
Merozoites of the malaria parasite Plasmodium falciparum use several receptors for cellular engagement when they invade human red blood cells.
Cellular target engagement of AR agonists or antagonists by CETSA HT.
Metabolomics and isotope tracer studies demonstrate effective cellular target engagement.
To facilitate identification of direct AR binders, we sought to apply CETSA to measure direct cellular target engagement.
This value represents the intracellular equivalent of an apparent binding affinity as measured by inhibitory constant, Ki, and is determined using a cellular target engagement CETSA HT assay following compound incubation with prostate-cancer derived cells endogenously expressing AR.
As a measure of cellular target engagement, CETSA offers unique benefits through application to physiologically relevant samples without the requirement for any modifications to either the target protein or the test compound.
Taken together, the biochemical experiments with QL47R and BTK C481S and cellular target engagement studies provide strong evidence that QL47 covalently labels BTK in the cellular environment.
Target selectivity is demonstrated by a variety of approaches, including large-scale kinome and GPCR screens in conjunction with cellular target engagement and surrogate pharmacodynamic end points.
Although few phenotypic effects have been reported using these compounds apart from their cellular target engagements, initial data point to a role of BRD9/7 in inflammation.
Viral RNA-binding proteins like HIV-1 Tat and HTLV-1 Rex have evolved to serve virus-specific roles, but consistent with our current findings on P19, they also show RSS activity [ 20, 50], suggesting that they participate in aspects of virus-cellular RNAi engagement [ 6].
Our results illustrate the potential of metabolomics in cellular drug-target engagement studies and consequently have broad implications in future drug development and target validation ventures.
