Discovery of Therapeutic Kinase InhibitorsINQUIRY
Creative BioMart aims to provide our customers with integrated solutions, from target identification to lead optimization, to accelerate their drug discovery process for kinase inhibitors. Our team of scientists with diverse disciplinary backgrounds provides our customers with deep expertise and extensive drug development experience.
Kinase dysfunction has been shown to play a key role in cancer, cardiovascular diseases, degenerative diseases, autoimmune disorders, inflammation, and many other diseases. Since the first kinase inhibitor, imatinib, was approved by the FDA in 2001, the number of approved kinase inhibitors has increased each year and these compounds have had a significant impact on the way diseases are treated. Their druggability and safety have made kinases one of the most intensively studied and successful families of drug targets. However, there are still a large number of kinases that have not been well studied, suggesting that the field of kinase inhibitor discovery remains immature. In addition, "pseudokinases" represent an attractive unexplored area of drug development and deserve more attention in the future.
Figure 1. Timeline depicting important events in the development and approval of kinase inhibitors over the past 20 years since imatinib was approved for treatment of CML in 2001. (Cohen P, et al., 2021)
Kinase Inhibitor Discovery from Target to Lead
The discovery of kinase inhibitors is a very active field as the kinase family is a very large, druggable target class associated with diverse diseases. Creative BioMart offers an optimized one-stop solution for kinase inhibitor discovery from target identification to lead optimization. Our scientists leverage our high-throughput kinase screening & profiling platform and their extensive experience in kinase inhibitor development to help our customers significantly accelerate their drug discovery process.
Discovery of Natural Product-based Kinase Inhibitors
Natural products from microorganisms or plants have emerged as a continuing source for the development of novel kinase inhibitors. Creative BioMart has a team of natural product chemists specializing in the extraction, isolation, and characterization of bioactive compounds from biological sources, as well as the design and chemical synthesis of natural products. We have a proven track record of successfully developing natural products as lead compounds for kinase inhibitor discovery.
Selectivity Enhancement of Kinase Inhibitors
The development of kinase inhibitors is often hindered by a lack of selectivity. A number of new technologies that enable rapid selectivity assessment of kinase inhibitors are driving significant advances in selectivity enhancement. Creative BioMart provides comprehensive analysis of kinase inhibitor selectivity and chemical biology insights to guide improvements in selectivity of kinase inhibitors and increase the success rate in transforming optimized leads into clinical candidates.
Overcoming Resistance to Kinase Inhibitors
Resistance to kinase inhibitors is a major obstacle to the development of these potential drugs. Attention should be paid to both primary and acquired drug resistance. Creative BioMart offers advanced strategies for identifying drug resistance mutations and developing next-generation kinase inhibitors, such as multi-target kinase inhibitors, with enhanced selectivity and reduced adverse effects to overcome the challenges of drug resistance.
Ligand Binding Assays
Kinase Functional Assays
Kinase Substrate Screening
Small Molecule Screening against Kinases
Assay Development and Validation
Creative BioMart is a trusted solution provider with many years of experience in kinase/phosphatase biology research and drug development. We have always been committed to providing our customers with high-quality products and customized services to accelerate their cutting-edge research and drug development pipeline. We fully support your project every step of the way to success.
Contact us to find out how our scientists can help you with your drug development project.
- Cohen P, et al. Kinase drug discovery 20 years after imatinib: progress and future directions. Nature Reviews Drug Discovery, 2021: 1-19.
- Ferguson F M & Gray N S. Kinase inhibitors: the road ahead. Nature reviews Drug discovery, 2018, 17(5): 353-377.