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Kinases belong to the family of phosphotransferases and play critical roles in the process known as phosphorylation in which a phosphorylated substrate and ADP are produced. Kinases are associated with many complex cellular pathways including cell metabolism, cell signaling, cell transport etc., which makes them very important to human physiology. Since many kinases can enhance cell proliferation, cell migration and cell survival, loss-of-function or gain-of-function mutations in kinases can lead to various types of cancer and some human disorders in immune, neurological and infectious diseases.
Because of their important cellular functions, kinases have become important drug targets in drug discovery and development for the treatment of human diseases especially diverse cancers. Small-molecule kinase inhibitors against these targets have shown prominent roles in the treatment of many cancers. With decades of experience in cell line engineering and drug discovery, Creative Biogene has developed a large collection of kinase stable cell lines that can be used for in vitro cell-based kinase assays. The use of these cell lines allows for broad set of assays and reduced assay development time.
Key Features of Our Kinases Stable Cell Lines:
Kinases are a large family of enzymes, with more than 500 enzymes encoded in the human genome, and all share highly conserved kinase domains. Based on the substrates on which they act, they can be broadly divided into three categories: protein kinases, carbohydrate kinases, and lipid kinases. Because kinases play different roles in cells, they have been implicated in many diseases, including cancer.
Although only slightly more than 50 of the 518 kinases have become drug targets to date, kinase inhibitors are expected to remain a major growth area for drug development over the next 20 years. Next-generation inhibitors will emphasize improved specificity, reduced drug resistance, and the ability to penetrate the blood-brain barrier. Cell-based assays are often required for gene functional analysis, target discovery and validation, assay development, and compound screening. Stable cell lines expressing the kinase gene of interest via transgene integration into the host genome provide an efficient method for performing such analyses.
Applications for Kinase stable cell lines include:
Case Study 1
Researchers analyzed the effects of EGFR inhibition on VEGF and HIF-1α in an in vitro NSCLC model. They determined the efficacy of VEGF inhibition in xenografts and analyzed the impact of acquired EGFR inhibitor resistance on VEGF and HIF-1α.
Figure 1. In NSCLC cells with EGFR-activating mutations, VEGF is elevated and regulated by EGFR. (Ba/F3 cells were obtained from Creative-Biogene) (Nilsson M B, et al., 2021)
Case Study 2
RET is a tyrosine kinase receptor with restricted tissue expression and association with cancer. Researchers describe RET::GRB2, a unique fusion in sporadic pheochromocytoma in which RET serves as the upstream component of the hybrid protein. Studies have shown that the kinase activity of RET and GRB2 located downstream of RET are both necessary for the transforming potential of the fusion and that the growth of RET::GRB2-expressing cells is readily inhibited by selpercatinib and pralsetinib.
Figure 2. RET::GRB2 fusion is oncogenic and sensitive to clinical grade RET inhibitors. (Ba/F3 cells were obtained from Creative-Biogene) (Estrada-Zuniga C M, et al. 2022)
Q: What are kinases?
A: Protein kinases are key regulators of cellular function and constitute one of the largest and most functionally diverse gene families. By adding phosphate groups to substrate proteins, they direct the activity, localization, and overall function of many proteins and serve to coordinate the activity of nearly all cellular processes.
Q: How many kinases are encoded by the human genome?
A: Over 500 kinases are encoded by the human genome.
Q: How are kinases classified based on their substrates?
A: Kinases are classified into distinct families based on their substrates: lipid, nucleotide, carbohydrate, and protein.
Q: What are the cellular responses elicited by activated targets of kinases?
A: The activated targets elicit cellular responses that include the promotion of cell growth and division, protein translation, and other physiological responses.
Q: What are the consequences of dysregulation of kinase activity?
A: Dysregulation of kinase activity can lead to many human diseases, especially cancer.
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