PROJECT TITLE :

Investigating receptor enzyme activity using time-scale analysis

ABSTRACT:

At early drug discovery, purified protein-based assays are often used to characterise compound potency. Within the context of dose response, it is often perceived that a time-freelance inhibitor is reversible and a time-dependent inhibitor is irreversible. The legitimacy of this argument is investigated employing a easy kinetics model, where it's revealed by model-primarily based analytical analysis and numerical studies that dose response of an irreversible inhibitor may appear time-independent below sure parametric conditions. Hence, the observation of time-independence cannot be used as sole evidence for identification of inhibitor reversibility. It has additionally been discussed how the synthesis and degradation of a target receptor affect drug inhibition in an in vitro cell-based mostly assay setting. These processes could conjointly influence dose response of an irreversible inhibitor in such a method that it seems time-independent beneath certain conditions. Furthermore, model-based steady-state analysis reveals the complexity nature of the drug–receptor method.


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