Chemical Proteomics Drug Target Identification
Chemical Proteomics, as an important branch of proteomics, integrates various methods including synthetic chemistry, cell biology, and mass spectrometry,aims to design small molecule probes to understand the mode of action of small molecules and protein functions in drug discovery, in the context of natural products, chemical proteomics can be used to identify protein binding partners or targets of small molecules in living cells.Chemical Proteomicsconsists of two key steps: (1) probe design and synthesis; (2) target fishing and protein identification.Currentlyhave developed4different types of probes to screen small molecules with different structurestargets;after targeting, there are also various protein identification methods suitable for different situations.Chemical proteomics provides a range of novel methods for target deconvolution, discovery of drug response biomarkers, and disease pathway analysis for preclinical target validation, inpharmacological researchfield,has beenwidely used foridentifying drug targets and studying theirmechanism of action.
Applications of Chemical Proteomics
Biotech Company (BTP) has developed and validatedcutting-edge chemical proteomics technology,which can be used in biomarker research, drug and target discovery, pathway modeling, mechanism of action studies, and many other fields,aiming to provide customerswith high-quality, comprehensive target deconvolution services.We offer a variety of methods to identify and validate new drug targets,to meetdifferentneeds.
Design and synthesis of probes are the initial and critical steps in the target identification of chemical proteomics methods. BTP offers four common probes including(1) Immobilized Probes: Bioactive natural products are covalently immobilized on biocompatible inert resins (such as agarose and magnetic beads) as bait to screen target proteins from active proteomes;(2) Activity-Based Probes (ABP): ABPs take into account the activity of drug molecules, allowing them to interact with proteins in the active proteome prior to enrichment and even cross cell membranes to bind with target proteins in living cells, potentially reflecting the true interaction of drugs and targets under intracellular physiological conditions;(3) Click Chemistry Probes: These probes undergo bio-orthogonal click reactions with their complement (such as azides, alkynes, etc.) to covalently link the probe to affinity tags (biotin-azide, biotin-cyclopropane, etc.) or fluorescent tags (rhodamine-azide, FITC-azide, etc.) for subsequent enrichment and target identification;(4) Photoaffinity Probes: Photoaffinity probes consist of a click chemistry probe scaffold and a photoaffinity group used to fix the binding between the probe and the target. Under specific wavelength light, the photoaffinity group generates highly active radicals that promote covalent binding of the active molecule with the target.
Chen, X.; et al. Sig Transduct Target Ther. 2020.
General molecular structures of different types of chemical proteomics probes
Forsomewithout suitable modification sitesoraffect activity after modificationofnatural products,BTP also offers based ondrug affinity responsive target stability(DARTS) and MS-based thermal stability profiling non-label chemical proteomics methods.DARTSrelies on the proteolytic protection conferred to the target protein through interaction with small molecules, firstsimply treat aliquots of cell lysates with the target compound and vehicle control or inactive analogue, then perform limited proteolysis of proteins in the cell lysates with a protease,then separate samples by SDS-PAGE and stain to identify protein bands protected from small molecule proteolysisfinallyuse MS to identify proteins present in each band.
Chen, X.; et al. Sig Transduct Target Ther. 2020.
Workflow of non-label chemical proteomics methods
Biotech Company's comprehensive chemical proteomics solutions include fromexperimental design,sample preparation, probe synthesis, target identification, to data analysis, providing you with one-stop worry-free service to meet your diverse needs in biomarker research, drug and target discovery, pathway modeling, and drug mechanism studies in the fields of drug development and drug discovery. With our comprehensive solutions, you won't waste timeand costson wrong candidate drugs and can optimize the success rate of drug development and discovery plans. Feel free to contact us for a free consultation to learn more about our services!
Chinese/English Project Report
In the technical report, Biotech Company will provide you with a detailed bilingual technical report in Chinese and English, including:
1. Experimental steps (Chinese/English)
2. Related mass spectrometry parameters (Chinese/English)
3. Details of chemical proteomics
4. Mass spectrometry images
5. Raw data
Related Services
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