ArticleACS chemical biology2018
Detection of Chemical Engagement of Solute Carrier Proteins by a Cellular Thermal Shift Assay.
Article in ACS chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 40 citations in OpenAlex.
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- Structure, Function, and Inhibition of Adenylosuccinate Lyase (ADSL) fromACS infectious diseases · 2026Article
- DABPU-DE targeting host adipose triglyceride lipase provides broad-spectrum anti-coronavirus effectsFrontiers in pharmacology · 2026Article
- Calcium Channel Blocker Lacidipine Promotes Antitumor Immunity by Reprogramming Tryptophan Metabolism.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Determining the In Vitro Ligand-Target Interaction by Cellular Thermal Shift Assay and Isothermal Dose-Response Fingerprint Assay.Bio-protocol · 2024Article
- Deep learning based CETSA feature prediction cross multiple cell lines with latent space representation.Scientific reports · 2024Article
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- The vacuolar iron transporter mediates iron detoxification in Toxoplasma gondii.Nature communications · 2023Article
- Corynoxine B targets at HMGB1/2 to enhance autophagy forActa pharmaceutica Sinica. B · 2023Article
- The GFP thermal shift assay for screening ligand and lipid interactions to solute carrier transporters.Nature protocols · 2021Review
- The Transporter-Mediated Cellular Uptake and Efflux of Pharmaceutical Drugs and Biotechnology Products: How and Why Phospholipid Bilayer Transport Is Negligible in Real Biomembranes.Molecules (Basel, Switzerland) · 2021Review
- A study of the dopamine transporter using the TRACT assay, a novel in vitro tool for solute carrier drug discovery.Scientific reports · 2021Article
- An Overview of Cell-Based Assay Platforms for the Solute Carrier Family of Transporters.Frontiers in pharmacology · 2021Review
- A machine learning-based chemoproteomic approach to identify drug targets and binding sites in complex proteomes.Nature communications · 2020Article
- Thermal proteome profiling for interrogating protein interactions.Molecular systems biology · 2020Review
- Plasmodium Perforin-Like Protein Pores on the Host Cell Membrane Contribute in Its Multistage Growth and Erythrocyte Senescence.Frontiers in cellular and infection microbiology · 2020Article
- Article
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
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 routinely applicable to membrane transporters such as SLCs. We used SLC16A1 (MCT1) and SLC1A2 (EAAT2) as targets to establish robust conditions by which chemical engagement of SLCs can be detected. Using immunoblotting, we demonstrate that treatment with the SLC16A1 inhibitors AZD3965 and AR-C155858 stabilized endogenous SLC16A1 in HEK293 cell lysates as well as intact cells. In addition, the high-affinity ligand of SLC16A1, l-lactate, and the low-affinity ligand, formate, resulted in strong and weak stabilization of SLC16A1, respectively. Moreover, we observed stabilization of SLC1A2 upon treatment with the selective inhibitor WAY-213613. We propose that the experimental approach presented here should be generally and easily applicable for monitoring the engagement of chemical ligands by SLCs in cellular settings and thus assisting in their deorphanization.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.