ArticleNature chemical biology2016
Thermal profiling reveals phenylalanine hydroxylase as an off-target of panobinostat.
Article in Nature chemical biology, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 106 papers.
What it found
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Who cites it
106 citing papers in PubMed, 252 citations in OpenAlex.
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- Gene Families, Structural and Functional Contexts Shape Protein Thermostability and Paralog Divergence inPlants (Basel, Switzerland) · 2026Article
- A covalent PFKL activator suppresses tumor growth.Nature chemical biology · 2026Article
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- Biophysical Sensing Tools in Drug Discovery: Integrating Kinetics, Thermodynamics, Cellular Target Engagement and Structure.Sensors (Basel, Switzerland) · 2026Review
- Above-Filter Digestion Proteomics Reveals Drug Targets and Localizes Ligand Binding Site.Journal of proteome research · 2026Article
- Proteomics in Antitumor Drug Target Discovery, Toxicity, Resistance, and Precision Oncology.Drug design, development and therapy · 2026Review
- A BRET biosensor for measuring uncompetitive engagement of PRMT5 complexes in cells.Nature communications · 2025Article
- Top-Down Thermal Proteome Profiling (TD-TPP) for Functional Characterization of the Intact Proteoforms in Complex Samples.Journal of mass spectrometry : JMS · 2025Article
- Expanding the Reach of Membrane Protein-Ligand Interaction Studies Through the Integration of Mass Spectrometry and Membrane Mimetics.Proteomics · 2025Review
- Human gut bacteria bioaccumulate per- and polyfluoroalkyl substances.Nature microbiology · 2025Article
- Thermal Proteome Profiling Reveals Meltome Upon NLRP3 Inflammasome Activation.Molecular & cellular proteomics : MCP · 2025Article
- TargetSeeker-MS: A Bayesian Inference Approach for Drug-Target Discovery Using Protein Fractionation Coupled to Mass Spectrometry.Journal of the American Society for Mass Spectrometry · 2025Article
- Article
- Integrated thermal proteome and thermal proximity co-aggregation profiling identifies ATP6V1C1 as a novel anti-cancer drug target.International journal of biological sciences · 2025Article
- Studying Target-Engagement of Anti-Infectives by Solvent-Induced Protein Precipitation and Quantitative Mass Spectrometry.ACS infectious diseases · 2024Article
- Aromatic Amino Acid Hydroxylases as Off-Targets of Histone Deacetylase Inhibitors.ACS chemical neuroscience · 2024Article
- Large-scale characterization of drug mechanism of action using proteome-wide thermal shift assays.eLife · 2024Article
- Progress in mass spectrometry approaches to profiling protein-protein interactions in the studies of the innate immune system.Journal of proteins and proteomics · 2024Article
46 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
13 authors at 3 institutions in 3 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
We describe a two-dimensional thermal proteome profiling strategy that can be combined with an orthogonal chemoproteomics approach to enable comprehensive target profiling of the marketed histone deacetylase inhibitor panobinostat. The N-hydroxycinnamide moiety is identified as critical for potent and tetrahydrobiopterin-competitive inhibition of phenylalanine hydroxylase leading to increases in phenylalanine and decreases in tyrosine levels. These findings provide a rationale for adverse clinical observations and suggest repurposing of the drug for treatment of tyrosinemia.
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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.