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Target protein degradation is an emerging strategy in the field of drug discovery and development, aimed at treating diseases, particularly cancer. In traditional drug design, it's common to intervene in the function or activity of proteins to influence disease processes. However, target protein degradation achieves the regulation of disease-related signaling pathways by facilitating the degradation of specific target proteins.
Currently, mass spectrometry-based methods enable highly selective protein degradation through precise protein identification and quantification. This approach offers a novel therapeutic strategy. In comparison to traditional inhibitors, protein degraders can more thoroughly target proteins, including those considered "undruggable". This provides hope for developing new treatment modalities, overcoming drug resistance, and addressing refractory diseases. Mass spectrometry-based targeted protein degradation methods also facilitate rapid optimization and development of more effective protein degraders through accurate analysis of drug-protein interactions. This aids in expediting the drug development process and shortening time to market for pharmaceuticals.
As a leading and pioneering proteomic company, our exclusive platforms, built upon mass spectrometry, effectively tackle these requirements and revolutionize the process of discovering and developing novel protein degrader drugs for their expedited clinical translation.
1. On-target and Off-target Degradation
◉ A total of 8528 proteins identified (with over 160,000 peptide sequences).
◉ Both target and off-target proteins can be accurately detected.
◉ Degradation efficiency results highly correlate with Western Blot results.
◉ The degradation specificity of the PROTAC-B2 molecule surpasses that of the PROTAC-B3 molecule.
2. Targeted quantification of POI by targeted proteomics
◉ The standard curve of synthesized peptides exhibits a strong correlation with excellent fitting (R2 > 0.99).
◉ The limit of detection (LOD) for quantitative detection is as low as 0.05 fmol/μg.
◉ Dose-dependent degradation of the target protein was observed in both cell lines.
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