ArticleACS chemical biology2018
Discovery and Optimization of Inhibitors of the Parkinson's Disease Associated Protein DJ-1.
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 21 papers.
What it found
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Who cites it
21 citing papers in PubMed.
- Glyoxalase activities of Parkinson's disease relevant protein DJ-1/PARK7: Past discoveries and future perspectives.Proceedings of the Japan Academy. Series B, Physical and biological sciences · 2026Review
- DJ-1 Protects Human Retinal Endothelial Cells From Diabetes-Related Conditions and Prevents Ischemic Damage in Mouse Retinal Capillaries.Investigative ophthalmology & visual science · 2025Article
- The reaction mechanism for glycolysis side product degradation by Parkinson's disease-linked DJ-1.The Journal of cell biology · 2025Article
- Development and use of DJ-1 affinity microcolumns to screen and study small drug candidates for Parkinson's disease.Analytica chimica acta · 2025Article
- The origin of esterase activity of Parkinson's disease causative factor DJ-1 implied by evolutionary trace analysis of its prokaryotic homolog HchA.The Journal of biological chemistry · 2024Article
- Development of Inhibitors, Probes, and PROTAC Provides a Complete Toolbox to Study PARK7 in the Living Cell.Journal of medicinal chemistry · 2024Article
- Cellular Exposure to Chloroacetanilide Herbicides Induces Distinct Protein Destabilization Profiles.ACS chemical biology · 2023Article
- Leveraging histone glycation for cancer diagnostics and therapeutics.Trends in cancer · 2023Review
- Chemical Toolkit for PARK7: Potent, Selective, and High-Throughput.Journal of medicinal chemistry · 2022Article
- Review
- Unfolding is the driving force for mitochondrial import and degradation of the Parkinson's disease-related protein DJ-1.Journal of cell science · 2021Article
- Non-enzymatic Covalent Modifications as a New Chapter in the Histone Code.Trends in biochemical sciences · 2021Review
- Deglycase-activity oriented screening to identify DJ-1 inhibitors.RSC medicinal chemistry · 2021Article
- Bis-isatin derivatives: design, synthesis, and biological activity evaluation as potent dimeric DJ-1 inhibitors.Acta pharmacologica Sinica · 2021Article
- The C terminus of DJ-1 determines its homodimerization, MGO detoxification activity and suppression of ferroptosis.Acta pharmacologica Sinica · 2021Article
- Knockdown of the DJ-1 (Molecular therapy oncolytics · 2021Article
- Small Substrate or Large? Debate Over the Mechanism of Glycation Adduct Repair by DJ-1.Cell chemical biology · 2020Review
- Novel Insights into PARK7 (DJ-1), a Potential Anti-Cancer Therapeutic Target, and Implications for Cancer Progression.Journal of clinical medicine · 2020Review
- Synthesis of an Alkynyl Methylglyoxal Probe to Investigate Nonenzymatic Histone Glycation.The Journal of organic chemistry · 2020Article
- Shining light on cysteine modification: connecting protein conformational dynamics to catalysis and regulation.Journal of synchrotron radiation · 2019Article
Corrections and comments
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Authors and funding
10 authors.
Funding
Abstract
DJ-1 is a Parkinson's disease associated protein endowed with enzymatic, redox sensing, regulatory, chaperoning, and neuroprotective activities. Although DJ-1 has been vigorously studied for the past decade and a half, its exact role in the progression of the disease remains uncertain. In addition, little is known about the spatiotemporal regulation of DJ-1, or the biochemical basis explaining its numerous biological functions. Progress has been hampered by the lack of inhibitors with precisely known mechanisms of action. Herein, we have employed biophysical methodologies and X-ray crystallography to identify and to optimize a family of compounds inactivating the critical Cys106 residue of human DJ-1. We demonstrate these compounds are potent inhibitors of various activities of DJ-1 in vitro and in cell-based assays. This study reports a new family of DJ-1 inhibitors with a defined mechanism of action, and contributes toward the understanding of the biological function of DJ-1.
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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.