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The Applications of Kinase Screening and Profiling Services in Target-based Drug Discovery

Kinase is a large family with 518 members, representing one of the most important and largest drug target superfamily, and is the main research field of the pharmaceutical industry and academic research. The kinase signaling pathway plays a major role in regulating cell proliferation, metabolism and death, which indicates that changes in kinase activity can lead to several disease states, even cancer. Therefore, these remarkable properties make kinases one of the most interesting target families in drug discovery. In the past few years, people have realized that kinases are an important class of drug targets. It seems that the selection of specific and potent drug candidates for kinases has become a popular and meaningful choice in the drug discovery industry.

 

Drug discovery efforts usually focus on targeting individual targets and optimizing compounds for these targets to achieve therapeutic efficacy. However, due to the conserved active sites and high structural homology between kinases, the development of selective kinase inhibitors is particularly challenging. In this way, in order to better understand the structure/activity relationship, support the avoidance of toxic targets, and ultimately select better drug candidates, the new kinase inhibitor program has become a wide range of analytical needs.

 

Based on a comprehensive collection of biochemical and cell-based kinase assays, Creative Biogene can provide the gold standard filter-bound radiokinase activity assay, TR-FRET technology and mobility assay to measure substrate phosphorylation, and to detect ATP consumption And ADP is generated. By integrating different technology platforms, kinase knowledge, and cell-based detection technologies, it can also provide more and more homogeneous and functional detection menus for identifying activated kinases in whole cells. These powerful assay platforms can be used alone or in combination, can be used in all stages of drug discovery, and are ideal for identifying highly efficient and selective kinase inhibitors.

 

Kinases are an indispensable target category for drug research. By transferring terminal phosphate molecules from ATP to the serine, threonine or tyrosine residues of the protein, which are a key component of the cell signaling pathway. Recently, the approval of new chemical entities has demonstrated the value of targeted kinases in the treatment of various diseases. The kits of assays and reagents used to determine the kinase activity of purified proteins in biochemical assays provide many opportunities.

 

Meanwhile, cell-based analysis (including the activity of hit compounds and detection of protein interactions) constitutes an important part of the selection of candidate drugs for in vivo testing. Creative Biogene provides a series of cell-based assays, including activity assessment, compound binding assay, protein interaction assay, cell selective screening and compound screening, etc. Combined with our kinase biochemical assays, we can provide you with the best quality services in assay development, high-throughput screening and selective analysis for kinase-based drug discovery.

 

Radiation-based assays are the most reliable and stable method for detecting kinase reactions. Therefore, they are the preferred method for kinase profiling. Compared with those non-radioactive methods, it is considered to be a radiation-based filtering and binding assay, which is the “gold standard” method. In this assay format, the kinase reaction is performed in the presence of 32P-γ-ATP or 33P-γ-ATP. By combining the final radioisotope-labeled product with the filter, unreacted phosphate can be washed away without interfering with the detection of the true phosphorylation product. In addition, scintillation proximity assay (SPA) is also used in radiokinase activity testing.

 

FRET analysis is a technique suitable for automation. The assay uses “donor” and “acceptor” fluorophores nearby, and the excited donor fluorophore exhibits non-radiative energy transfer to the acceptor fluorophore. Creative Biogene offers a filter-combined radiokinase activity assay, which has long been established as the most reliable, reliable and gold standard assay for all other assay formats. When a higher level of throughput is required to support high-throughput screening, Creative Biogene can also provide TR-FRET technology to measure the phosphorylation of the substrate.

 

Creative Biogene provides a wide range of platforms and assay formats for kinase biochemical assays. With years of experience in this field, Creative Biogene is committed to providing radiological analysis and FRET analysis services with the best results. The services provided are very flexible and can meet the special needs of customers for kinase screening and analysis. Experienced experts will work closely with the customer’s team to effectively support compound screening and analysis.

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