ArticleACS medicinal chemistry letters2014
Oxathiazolones Selectively Inhibit the Human Immunoproteasome over the Constitutive Proteasome.
Article in ACS medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 43 citations in OpenAlex.
- Identification of a new class of proteasome inhibitors based on a naphthyl-azotricyclic-urea-phenyl scaffold.RSC medicinal chemistry · 2023Article
- Site-Specific Proteasome Inhibitors.Biomolecules · 2021Review
- Review
- Microbial proteasomes as drug targets.PLoS pathogens · 2021Review
- A Nut for Every Bolt: Subunit-Selective Inhibitors of the Immunoproteasome and Their Therapeutic Potential.Cells · 2021Review
- Review
- Anti-tumor activity of a novel proteasome inhibitor D395 against multiple myeloma and its lower cardiotoxicity compared with carfilzomib.Cell death & disease · 2021Article
- Noncytotoxic Inhibition of the Immunoproteasome Regulates Human Immune Cells In Vitro and Suppresses Cutaneous Inflammation in the Mouse.Journal of immunology (Baltimore, Md. : 1950) · 2021Article
- Synthesis and Biochemical Evaluation of Warhead-Decorated Psoralens as (Immuno)Proteasome Inhibitors.Molecules (Basel, Switzerland) · 2021Article
- Mechanistic and thermodynamic characterization of oxathiazolones as potent and selective covalent immunoproteasome inhibitors.Computational and structural biotechnology journal · 2021Article
- Article
- Structure-Activity Relationships of Noncovalent Immunoproteasome β5i-Selective Dipeptides.Journal of medicinal chemistry · 2020Article
- Psoralen Derivatives as Inhibitors ofMolecules (Basel, Switzerland) · 2020Article
- A focused structure-activity relationship study of psoralen-based immunoproteasome inhibitors.MedChemComm · 2019Article
- Selective Phenylimidazole-Based Inhibitors of theJournal of medicinal chemistry · 2019Article
- Discovery of Immunoproteasome Inhibitors Using Large-Scale Covalent Virtual Screening.Molecules (Basel, Switzerland) · 2019Article
- Antimalarial proteasome inhibitor reveals collateral sensitivity from intersubunit interactions and fitness cost of resistance.Proceedings of the National Academy of Sciences of the United States of America · 2018Article
- Structure of human immunoproteasome with a reversible and noncompetitive inhibitor that selectively inhibits activated lymphocytes.Nature communications · 2017Article
- The crystal structures of two isomers of 5-(phenyl-iso-thia-zol-yl)-1,3,4-oxa-thia-zol-2-one.Acta crystallographica. Section E, Crystallographic communications · 2017Article
- The Proteasome in Modern Drug Discovery: Second Life of a Highly Valuable Drug Target.ACS central science · 2017Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Selective inhibitors for the human immunoproteasome LMP7 (β5i) subunit over the constitutive proteasome hold promise for the treatment of autoimmune and inflammatory diseases and hematologic malignancies. Here we report that oxathiazolones inhibit the immunoproteasome β5i with up to 4700-fold selectivity over the constitutive proteasome, are cell permeable, and inhibit proteasomes inside cells.
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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.