ArticleAngewandte Chemie (International ed. in English)2021
Inhibition of Autophagy by a Small Molecule through Covalent Modification of the LC3 Protein.
Article in Angewandte Chemie (International ed. in English), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 43 papers.
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Who cites it
43 citing papers in PubMed, 88 citations in OpenAlex.
- Isopsoralen Promotes Mandibular Fracture Healing by Regulating Autophagy.Medical science monitor : international medical journal of experimental and clinical research · 2026Article
- Carfilzomib Induces Cardiotoxicity by Blocking Autophagic Flux Through the cGAS-STING Signaling Pathway.Biomolecules · 2026Article
- NIBV Induces Incomplete Autophagy via AMPK-TFEB, Causing Kidney Injury in Chicks.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2026Article
- Provoking disulfidptosis-enhanced mitophagy by manganese-based nanoplatform via regulating cellular energy supply and redox homeostasis.Materials today. Bio · 2026Article
- Cancer and aging: complex associations and therapeutic targets.Molecular biomedicine · 2026Review
- SOD1 lactylation impair its enzymatic activity by conformational change to aggravate intervertebral disc degeneration.Nature communications · 2026Article
- ATF3 Deficiency Exacerbates Ageing-Induced Atherosclerosis and Clinical Intervention Strategy.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Salidroside Attenuates Cerebral Ischemia-Reperfusion Injury via ERβ/BNIP3-Mediated Mitochondrial Autophagy Activation in a Rat Model.Neurochemical research · 2025Article
- Article
- Post-translational modifications and the reprogramming of tumor metabolism.Discover oncology · 2025Review
- Identifying a non-conserved site for achieving allosteric covalent inhibition of CECR2.Acta pharmacologica Sinica · 2025Article
- Has-miR-30c-1-3p inhibits macrophage autophagy and promotes Mycobacterium tuberculosis survival by targeting ATG4B and ATG9B.Scientific reports · 2025Article
- Exploring Arylidene-Indolinone Ligands of Autophagy Proteins LC3B and GABARAP.ACS medicinal chemistry letters · 2025Article
- FTO Alleviates Hepatic Ischemia-Reperfusion Injury by Regulating Apoptosis and Autophagy.Gastroenterology research and practice · 2025Article
- Effects of Citrus-derived Diosmetin on Melanoma: Induction of Apoptosis and Autophagy Mediated by PI3K/Akt/mTOR Pathway Inhibition.Anti-cancer agents in medicinal chemistry · 2025Article
- Tuina therapy alleviates knee osteoarthritis by modulating PI3K/AKT/mTOR-mediated autophagy: an integrated machine learning andFrontiers in immunology · 2025Article
- Autophagy-mediated regulation of neutrophil inflammatory responses and its relevance to central nervous system diseases.Frontiers in aging neuroscience · 2025Review
- Identification and interaction analysis of hubgenes related to neutrophil ferroptosis in intracranial atherosclerotic stenosis.Genetics and molecular biology · 2025Article
- Region-specific mitophagy in nucleus pulposus, annulus fibrosus, and cartilage endplate of intervertebral disc degeneration: mechanisms and therapeutic strategies.Frontiers in pharmacology · 2025Review
- DIA-based quantitative proteomics explores the mechanism of amelioration of APAP-induced liver injury by anoectochilus roxburghii (Wall.) Lindl.Frontiers in pharmacology · 2025Article
Corrections and comments
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Authors and funding
27 authors at 6 institutions in 3 countries.
Funding
Abstract
The autophagic ubiquitin-like protein LC3 functions through interactions with LC3-interaction regions (LIRs) of other autophagy proteins, including autophagy receptors, which stands out as a promising protein-protein interaction (PPI) target for the intervention of autophagy. Post-translational modifications like acetylation of Lys49 on the LIR-interacting surface could disrupt the interaction, offering an opportunity to design covalent small molecules interfering with the interface. Through screening covalent compounds, we discovered a small molecule modulator of LC3A/B that covalently modifies LC3A/B protein at Lys49. Activity-based protein profiling (ABPP) based evaluations reveal that a derivative molecule DC-LC3in-D5 exhibits a potent covalent reactivity and selectivity to LC3A/B in HeLa cells. DC-LC3in-D5 compromises LC3B lipidation in vitro and in HeLa cells, leading to deficiency in the formation of autophagic structures and autophagic substrate degradation. DC-LC3in-D5 could serve as a powerful tool for autophagy research as well as for therapeutic interventions.
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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.