Screening assays for tyrosine kinase inhibitors: A review

Abstract

Tyrosine kinases have been intensively investigated as drug targets for several decades, since they regulate many cellular processes including cell growth, differentiation, and proliferation. Indeed, the deregulation of tyrosine kinases has been confirmed to play a vital role in the pathophysiology of many diseases. During the last few years, varieties of techniques have been developed to search for new tyrosine kinase inhibitors for cancer therapy, such as traditional filtration binding assay, scintillation proximity assay and some high-throughput screening methods. In this review, we describe the basic rules, merits and demerits, and application of a number of general and advanced technologies. The purpose of this review is to provide an insight into the numerous assays to achieve the exploration of new tyrosine kinase inhibitors.

Keywords: Inhibitor screening assay; Non-receptor tyrosine kinases; Receptor tyrosine kinases; Tyrosine kinase.