ArticleBioorganic & medicinal chemistry letters2014
Selective immunoproteasome inhibitors with non-peptide scaffolds identified from structure-based virtual screening.
Article in Bioorganic & medicinal chemistry letters, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 18 citations in OpenAlex.
- A Nut for Every Bolt: Subunit-Selective Inhibitors of the Immunoproteasome and Their Therapeutic Potential.Cells · 2021Review
- Synthesis and Biochemical Evaluation of Warhead-Decorated Psoralens as (Immuno)Proteasome Inhibitors.Molecules (Basel, Switzerland) · 2021Article
- 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
- Discovery of Immunoproteasome Inhibitors Using Large-Scale Covalent Virtual Screening.Molecules (Basel, Switzerland) · 2019Article
- In Silico Studies in Drug Research Against Neurodegenerative Diseases.Current neuropharmacology · 2018Review
- Brief treatment with a highly selective immunoproteasome inhibitor promotes long-term cardiac allograft acceptance in mice.Proceedings of the National Academy of Sciences of the United States of America · 2016Article
- Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview.Molecules (Basel, Switzerland) · 2016Review
- Fundamental reaction pathway and free energy profile of proteasome inhibition by syringolin A (SylA).Organic & biomolecular chemistry · 2015Article
- Proteasome inhibitors with pyrazole scaffolds from structure-based virtual screening.Journal of medicinal chemistry · 2015Article
- Subunit specific inhibitors of proteasomes and their potential for immunomodulation.Current opinion in chemical biology · 2014Review
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Authors and funding
4 authors at 1 institution in 1 country.
Funding
Abstract
As a major component of the crucial nonlysosomal protein degradation pathway in the cells, the proteasome has been implicated in many diseases such as Alzheimer's disease, Huntington's disease, inflammatory bowel diseases, autoimmune diseases, multiple myeloma (MM) and other cancers. There are two main proteasome subtypes: the constitutive proteasome which is expressed in all eukaryotic cells and the immunoproteasome which is expressed in immune cells and can be induced in other cell types. Majority of currently available proteasome inhibitors are peptide backbone-based, having short half-lives in the body. It is highly desirable to identify novel, immunoproteasome-selective inhibitors with non-peptide scaffolds for development of novel therapeutics. Through combined virtual screening and experimental studies targeting the immunoproteasome, we have identified a set of novel immunoproteasome inhibitors with diverse non-peptide scaffolds. Some of the identified inhibitors have significant selectivity for the immunoproteasome over the constitutive proteasome. Unlike most of the currently available proteasome inhibitors, these new inhibitors lacking electrophilic pharmacophores are not expected to form a covalent bond with proteasome after the binding. These non-peptide scaffolds may provide a new platform for future rational drug design and discovery targeting the immunoproteasome.
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