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Learn MoreIdentifying and characterizing promising therapeutic targets is the first step in the process of developing new drugs for brain tumors. Validation of these targets becomes critical before additional time and resources are invested in development. Target validation is the process of further screening of candidate targets, as the candidate targets identified by target identification are not necessarily the target targets and may be mixed with false-positive results.
Alfa Cytology identifies promising targets in early drug discovery. We develop and implement high-throughput target ID screens that characterize a wide range of analytes from small molecular fragments to biologics. We utilize non-labeled binding technologies such as bio-layer interference (BLI) and surface plasmon resonance (SPR) systems to rapidly establish high-throughput binding screens. Our services can be used to identify binding targets and accurately characterize complex formation rates, complex stability, and affinity.
Services | Description |
Target-based screening services | We can effectively screen for biologically active small molecules by target-based screening targeted at specific target proteins, e.g., kinases, histone deacetylases, G protein-coupled receptors, etc. The small molecule active substances obtained by this method have a strong effect on the target. |
Phenotypic screening service | Compared to traditional target-based screening methods, phenotypic screening is a fast and effective way to screen for high-potential drug targets. We screen the entire genome, covering all targets and signaling pathways associated with the screened phenotype. The screening process takes into account absorption, distribution, metabolism, and excretion factors. This screening service is well suited for screening targets in brain tumor diseases with unknown mechanisms. After the phenotypic screening, the targets and pathways of drug action are still unclear, so we also identify intracellular targets through positive phenotypic screening and perform further validation. |
Target validation service | We use multiple target identification methods to obtain drug targets that can only be used as a preliminary target screening method, and then validate the candidate target to confirm whether it regulates the biological activity of the compound in cellular assays. We silence genes associated with brain tumor disease by RNA interference technology to form mice lacking a specific target to see if they have the symptoms of normal mice after drug action. Alternatively, we inject the drug into the knockout mice and if the drug does not cause an effect, it indicates that the drug is acting through this specific target. In addition to RNA interference techniques, we will also use cDNA overexpression to establish drug-target action relationships. Overexpression of the target may inhibit the activity of the drug, and this approach is extremely important for validating membrane targets. |
Target characterization services | Once the hypothetical target is validated by functional experiments, we quantify the affinity of the small molecule and the target using SPR or isothermal calorimetry techniques. If the hypothetical target is an enzyme, we measure the enzymatic activity of the substance by enzyme kinetics experiments. Finally, we also perform more rigorous validation by NMR or co-crystallization experiments to obtain the three-dimensional structure of the drug-target complex. This information not only verifies the physical correlation but also provides you with criteria for the identification of binding models for later drug optimization. |
Successful development of brain tumor drugs begins with target validation and discovery. Finding targets that can be developed into therapeutic agents is critical to the success of brain tumor drug development, and Alfa Cytology' advanced genetic manipulation technology platform provides our clients with powerful support in identifying and validating known or novel targets relevant to brain tumors therapy. Our services enable you to decide to continue or discontinue a project as soon as possible, effectively reducing the risk of your investment in drug development projects. Please contact us to learn how we can contribute to the successful development of brain tumor drugs.