ArticleCell chemical biology2018
Tetracyclines Modify Translation by Targeting Key Human rRNA Substructures.
Article in Cell chemical biology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed, 57 citations in OpenAlex.
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- Comparative analysis of alkyne- and desthiobiotinylated photoaffinity probes for chemotranscriptomic profiling.RSC chemical biology · 2026Article
- RNA functional modulation by Mitoxantrone via RNA structural ensemble repartitioning.Nature communications · 2026Article
- Atypical tetracyclines promote longevity and ferroptotic neuroprotection via translation attenuation.bioRxiv : the preprint server for biology · 2026Article
- SHAPE-Based Chemical Probes for Studying preQACS chemical biology · 2025Article
- Molecular mechanisms of 10-butyl ether minocycline, a novel nonantibiotic tetracycline, as a potential treatment for inflammatory and neuroimmune-related disorders.The Journal of pharmacology and experimental therapeutics · 2025Article
- An approach to characterize mechanisms of action of anti-amyloidogenic compounds in vitro and in situ.NPJ Parkinson's disease · 2025Article
- The G-quadruplex ligand CX-5461: an innovative candidate for disease treatment.Journal of translational medicine · 2025Review
- Tetracyclines enhance antitumor T-cell immunity via the Zap70 signaling pathway.Journal for immunotherapy of cancer · 2024Article
- Mitoribosomal synthetic lethality overcomes multidrug resistance in MYC-driven neuroblastoma.Cell death & disease · 2023Article
- Oh my gut! Is the microbial origin of neurodegenerative diseases real?Infection and immunity · 2023Review
- Rescue of Dopamine Neurons from Iron-Dependent Ferroptosis by Doxycycline and Demeclocycline and Their Non-Antibiotic Derivatives.Antioxidants (Basel, Switzerland) · 2023Article
- Article
- Targeting RNA structures with small molecules.Nature reviews. Drug discovery · 2022Review
- COL-3-Induced Molecular and Ultrastructural Alterations in K562 Cells.Journal of personalized medicine · 2022Article
- Doxycycline attenuates l-DOPA-induced dyskinesia through an anti-inflammatory effect in a hemiparkinsonian mouse model.Frontiers in pharmacology · 2022Article
- Oncogenic KRAS creates an aspartate metabolism signature in colorectal cancer cells.The FEBS journal · 2021Article
- A chemical probe based on the PreQNature communications · 2021Article
- Reprogramming of Protein-Targeted Small-Molecule Medicines to RNA by Ribonuclease Recruitment.Journal of the American Chemical Society · 2021Article
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Authors and funding
11 authors at 4 institutions in 2 countries.
Funding
Abstract
Apart from their antimicrobial properties, tetracyclines demonstrate clinically validated effects in the amelioration of pathological inflammation and human cancer. Delineation of the target(s) and mechanism(s) responsible for these effects, however, has remained elusive. Here, employing quantitative mass spectrometry-based proteomics, we identified human 80S ribosomes as targets of the tetracyclines Col-3 and doxycycline. We then developed in-cell click selective crosslinking with RNA sequence profiling (icCL-seq) to map binding sites for these tetracyclines on key human rRNA substructures at nucleotide resolution. Importantly, we found that structurally and phenotypically variant tetracycline analogs could chemically discriminate these rRNA binding sites. We also found that tetracyclines both subtly modify human ribosomal translation and selectively activate the cellular integrated stress response (ISR). Together, the data reveal that targeting of specific rRNA substructures, activation of the ISR, and inhibition of translation are correlated with the anti-proliferative properties of tetracyclines in human cancer cell lines.
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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.