Product Overview
DARTS (Drug Affinity Responsive Target Stability) is a label-free drug target identification method based on the principle of protein hydrolysis protection. Its core principle is that after a small molecule drug or ligand specifically binds to a target protein, it induces the target protein to become more compact or masks the protease recognition site, thereby reducing its sensitivity to degradation by a broad spectrum of proteases. By comparing the undegraded protein bands or peptides in the drug-treated group and the control group using SDS-PAGE combined with mass spectrometry, the target protein directly bound to the drug can be identified.
DARTS technology does not require chemical modification of drugs, does not rely on the inherent activity of drugs (such as enzyme inhibitory activity), is suitable for water-insoluble drugs and crude extracts of natural products, and can be carried out under near-physiological conditions. Therefore, it is widely used in drug target discovery, mechanism of action analysis, and off-target effect assessment.
DARTS Schematic Diagram
Technical Process
Schematic diagram of DARTS process route
Applications
English Title：5-aza-2'-deoxycytidine potentiates anti-tumor immunity in colorectal peritoneal metastasis by modulating ABC A9-mediated cholesterol accumulation in macrophages
Impact Factor：13.3
Journal：Theranostics
Research Content：This paper successfully identified ABCA9, the direct target of 5Aza, using DARTS technology, and elucidated a novel mechanism by which it inhibits peritoneal metastasis of colorectal cancer by regulating the macrophage cholesterol metabolism-inflammatory polarization-T cell activation axis.
English Title：Unveiling Vacuolar H+-ATPase Subunit a as the Primary Target of the Pyridinylmethyl-Benzamide Fungicide, Fluopicolide
Impact Factor：6.2
Journal：Journal of Agricultural and Food Chemistry
Research Content： This study successfully identified the direct target of fluopyram as the vacuole H⁺-ATPase a subunit (PcVHA-a) using DARTS combined with BSA-seq. This provides an efficient and chemical-modification-free general strategy for target discovery in agrochemicals and other small molecule drugs.
Sample Submission Requirements
- Sample
- Cell
- Specification
- T75 /set
- Notes
- 1*10^7/ set
- Sample
- Bacteria
- Specification
- OD600~0.6 / set
- Notes
- Sample
- Tissue
- Specification
- 100mg / set
- Notes
- Sample
- Small Molecule Drugs
- Specification
- 100 mM，50 uL
- Notes
- The dosage concentration and preparation solvent must be provided.
- Sample
- DMSO
- Specification
- 50 uL
- Notes
| Sample | Specification | Notes |
|---|---|---|
| Cell | T75 /set | 1*10^7/ set |
| Bacteria | OD600~0.6 / set | |
| Tissue | 100mg / set | |
| Small Molecule Drugs | 100 mM，50 uL | The dosage concentration and preparation solvent must be provided. |
| DMSO | 50 uL |
References
Ren YS, Li HL, Piao XH, et al Drug affinity responsive target stability (DARTS) accelerated small molecules target discovery: Principles and application Biochem Pharmacol, 2021;194:114798.DOI: 10.1016/j.bcp.2021.114798
Shi R, Zhao K, Wang T, et al 5-aza-2'-deoxycytidine potentiates anti-tumor immunity in colorectal peritoneal metastasis by modulating ABC A9-mediated cholesterol accumulation in macrophages Theranostics, 2022;12(2):875-890.DOI: 10.7150/thno.66420
Dai T, Yang J, Zhao C, et al Unveiling Vacuolar H+-ATPase Subunit a as the Primary Target of the Pyridinylmethyl-Benzamide Fungicide, Fluopicolide J Agric Food Chem, 2024;72(3):1527-1538.DOI: 10.1021/acs.jafc.3c08485
Shenzhen Wininnovate Bio Co., Ltd.
Innovative mass spectrometry and AI technologies provide protein and metabolite mass spectrometry multi-omics solutions for life science research, empowering the growth of the biotechnology, pharmaceutical, and healthcare industries.
