Kinases/Phosphatases as Therapeutic TargetsINQUIRY
Creative BioMart has established a plethora of assays and continues to develop new approaches to support integrated kinase/phosphatase drug discovery programs, starting with initial steps of target identification and validation. Our scientists are experienced at discovering understudied kinases as targets and drugging the undruggable phosphatases.
Reversible phosphorylation, which is widely recognized as one of the major post-translational modifications (PTMs), is an important regulatory mechanism vital to virtually all cellular processes. Kinases and phosphatases coordinate with each other to control phosphorylation, thereby mediating protein-protein interactions and regulating the catalytic activity of enzymes. Disruption of kinase/phosphatase balance may directly cause or to be a consequence of many pathological conditions, such as cancer, diabetes, inflammation, neurodegenerative disorders, and cardiovascular diseases. These understandings have made these enzymes be potential and important targets for the development of therapeutic drugs. It is estimated that the field of phosphorylation already accounts for approximately 30% of research and development in the pharmaceutical industry.
Figure 1. Selected protein kinase and phosphatase pathways indicating chemical inhibitors with therapeutic potential. (Ventura J J & Nebreda Á R., 2006)
Identification of Kinase Targets
Kinases have attracted a great deal of attention as potential targets for new drug development. Creative BioMart enables kinase drug discovery with integrated solutions for target identification. We offer a wide range of in vitro and in vivo assays as well as advanced technologies such as mass spectrometry to help our customers identify kinase substrates in high-throughput and map kinase-substrate interactions.
Identification of Druggable Phosphatase Targets
Phosphatases have been widely dismissed as “undruggable”. Creative BioMart has long been committed in the development of therapeutics targeting of previously undruggable phosphatases. Our scientists can provide comprehensive support to our customers based on our state-of-the-art technology platform and their extensive drug discovery experience to help facilitate the identification of the druggable phosphatase targets and drug the previously undruggable phosphatases.
Target deconvolution is the subsequence process of target identification to further elucidate compound mechanism of action and to identify the target of small molecules. Creative BioMart offers chemical proteomic-based approaches, expression cloning techniques, and in silico approaches to help globally map small molecule-target interactions and develop small molecules targeting kinase/phosphatase signaling networks.
Creative BioMart leverages our expertise and a comprehensive set of tools covering in vitro and in vivo techniques to help our customers determine the biological functions of a given target, determine its role in a disease process, and elucidate its druggable attributes. Our in-depth knowledge of phosphorylation pathways will greatly facilitate the transition of potential kinase/phosphatase targets into pharmacological candidates, driving the success of drug discovery programs.
In Vitro Kinase Screening & Profiling
In Vitro Phosphatase Screening & Profiling
Analysis of Phosphorylation In Vitro
In Vivo Functional Characterization
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 discovery project.
- Ventura J J & Nebreda Á R. Protein kinases and phosphatases as therapeutic targets in cancer. Clinical and Translational Oncology, 2006, 8(3): 153-160.
- Cohen P, et al. Kinase drug discovery 20 years after imatinib: progress and future directions. Nature Reviews Drug Discovery, 2021: 1-19.