Drug discovery and development are challenged by costly and time-consuming high attrition rates. Early knowledge of targets and unintended off-targets can improve success rates at all stages of drug development and increase the chance of developing a potent drug with minimal side-effects.
Drug mechanism of action
A multitude of approaches is required to identify target(s) and unintended off-target effects and to understand drug mechanisms of action. Chemical proteomics and quantitative mass spectrometry offer an array of novel methodologies for target deconvolution, discovery of drug response biomarkers and disease pathway analysis for pre-clinical target validation.
Most drugs interact with multiple targets
Target deconvolution is essential for rational drug design and an important aspect for efficient progression of hit compounds. Knowledge of target-specific toxicity and side effects can be addressed in the early phases, supporting cost effective drug development and reducing late-stage drug candidate failure. Target deconvolution approaches have the potential to elucidate highly valued information about drug mode of action (MoA), to aid in rational compound structure optimization and thereby facilitate knowledge-based decisions throughout the drug discovery and development process.
DTI can assist you by providing
- Complementary technologies to deselect hits caused by non-specific binding
- Identify molecular targets of active hits from phenotypic screening
- Monitoring drug-protein interactions by chromatographic co-elution
- Specialized MS-protocols for identification of drugs mitigating protein misfolding
- Identification of targets using Drug Affinity Responsive Target Stability (DARTS)
- Pulldown and Affinity-based MS Protocols for Target Identification
- Discovery and development of ligands using peptide phage display
- Activity based protein profiling to monitor specific target classes