ArticleMolecules (Basel, Switzerland)2011
Synthesis and SAR study of novel peptide aldehydes as inhibitors of 20S proteasome.
Article in Molecules (Basel, Switzerland), 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.
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Who cites it
6 citing papers in PubMed, 16 citations in OpenAlex.
- Navigating bioactivity space in anti-tubercular drug discovery through the deployment of advanced machine learning models and cheminformatics tools: a molecular modeling based retrospective study.Frontiers in pharmacology · 2023Review
- Exploring the Role of Ubiquitin-Proteasome System in Parkinson's Disease.Molecular neurobiology · 2022Review
- Nostocyclopeptides as New Inhibitors of 20S Proteasome.Biomolecules · 2021Article
- Computational Approaches for the Discovery of Human Proteasome Inhibitors: An Overview.Molecules (Basel, Switzerland) · 2016Review
- Incorporation of metabolically stable ketones into a small molecule probe to increase potency and water solubility.Bioorganic & medicinal chemistry letters · 2015Article
- Theory and applications of covalent docking in drug discovery: merits and pitfalls.Molecules (Basel, Switzerland) · 2015Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
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Abstract
Based on the analysis of the crystal structure of MG101 (1) and 20S proteasomes, a new series of peptide aldehyde derivatives were designed and synthesized. Their ability to inhibit 20S proteasome was assayed. Among them, Cbz-Glu(OtBu)-Phe-Leucinal (3c), Cbz-Glu(OtBu)-Leu-Leucinal (3d), and Boc-Ser(OBzl)-Leu-Leucinal (3o) exhibited the most activity, which represented an order of magnitude enhancement compared with MG132 (2). The covalent docking protocol was used to explore the binding mode. The structure-activity relationship of the peptide aldehyde inhibitors is discussed.
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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.