Detection of Chemical Engagement of Solute Carrier Proteins by a Cellular Thermal Shift Assay.

ABSTRACT: Solute carriers (SLCs) are transmembrane proteins that transport various nutrients, metabolites, and drugs across cellular membranes. Despite the relevance of SLCs to cell homeostasis, metabolism, and disease states, for the majority of SLCs we lack experimental evidence regarding the nature of the cognate ligands, whether endobiotic or xenobiotic. Moreover, even for the roughly 20 SLCs for which inhibitors have been characterized, engagement assays in cells are limited to the accessibility of radiolabeled or fluorescent probes. The cellular thermal shift assay (CETSA) has been introduced as a powerful method to assess target engagement by monitoring ligand-induced changes in the thermal stability of cellular proteins. We addressed the question of whether CETSA could be modified to become

SUBMITTER: Hashimoto M 

PROVIDER: S-EPMC6067815 | biostudies-literature | 2018 Jun

REPOSITORIES: biostudies-literature