Discover the proteome with CETSA® Explore
CETSA® Explore for hit evaluation and target deconvolution
Recent years have seen a resurgence in phenotypic drug discovery owing to its potential for delivering first-in-class treatments for diseases with unmet clinical needs1. However, one of the major challenges to phenotypic approaches is the need for target deconvolution and hit confirmation. CETSA® Explore offers unbiased proteome-wide thermal profiling that can provide key insights for phenotypic drug discovery in a disease-relevant, label-free system. The method allows the entire proteome to be simultaneously monitored for changes in protein thermostability during drug treatment.
CETSA® increases the likelihood for drug success
Gaining a clear understanding of how a drug works, which targets it hits, what processes it alters, and which of these actions are required for therapeutic efficacy can help guide drug development and prevent late-stage failures. CETSA® Explore is a valuable tool to deorphanize drug targets and provide an unbiased proteome-wide measure of target engagement in a physiologically-relevant setting.
How can I identify my target? Download CETSA® Explore application note.
Publications
Mayumi Kitagawa, Pei-Ju Liao, Kyung Hee Lee, Jasmine Wong, See Cheng Shang, et al. Dual blockade of the lipid kinase PIP4Ks and mitotic pathways leads to cancer-selective lethality. (2017) Nature Communications. DOI: 10.1038/s41467-017-02287-5
Dziekan JM, Yu H, Chen D, Dai L, et al. Identifying purine nucleoside phosphorylase as the target of quinine using cellular thermal shift assay. (2019) Sci Transl Med. DOI: 10.1126/scitranslmed.aau3174
Friman T. Mass spectrometry-based Cellular Thermal Shift Assay (CETSA®) for target deconvolution in phenotypic drug discovery. (2020) Bioorganic & Medicinal Chemistry. DOI: https://doi.org/10.1016/j.bmc.2019.115174