Crystal Structure of Epoxomicin:20S Proteasome Reveals a Molecular Basis for Selectivity of α‘,β‘-Epoxyketone Proteasome Inhibitors

Michael Groll ,*^‡ Kyung Bo Kim ,^† Norman Kairies ,^‡ Robert Huber ,^‡ and Craig M. Crews *^†^§

Max Planck Institut für Biochemie D-82152 Martinsried, Germany Departments of Molecular, Cellular, and Developmental Biology and Pharmacology, Yale University 219 Prospect Street, New Haven, Connecticut 06520-8103

J. Am. Chem. Soc., 2000, 122 (6), pp 1237–1238

DOI: 10.1021/ja993588m

Publication Date (Web): January 28, 2000

Note: In lieu of an abstract, this is the article's first page.

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Exploiting nature's rich source of proteasome inhibitors as starting points in drug development
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Chemical Communications 2012 48 (10), 1364
Revisiting the role of the immunoproteasome in the activation of the canonical NF-κB pathway
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Molecular BioSystems 2012 8 (9), 2295
Structural features and binding free energies for non-covalent inhibitors interacting with immunoproteasome by molecular modeling and dynamics simulations
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Theoretical Chemistry Accounts 2012, 1203
Exploiting nature's rich source of proteasome inhibitors as starting points in drug development
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Chem. Commun. 2012 48, 1364-1378
Proteasome Inhibitors: An Expanding Army Attacking a Unique Target
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Chemistry & Biology 2012 19, 99-115
Proteasome-based mechanisms of intrinsic and acquired bortezomib resistance in non-small cell lung cancer
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Biochemical Pharmacology 2012 83 (2), 207-217
Semisynthetic neoboutomellerone derivatives as ubiquitin-proteasome pathway inhibitors
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Bioorganic & Medicinal Chemistry 2012 20 (2), 819-831
Molecular Mechanisms of Bortezomib Resistant Adenocarcinoma Cells
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Combined 3D-QSAR, Molecular Docking and Molecular Dynamics Study on Derivatives of Peptide Epoxyketone and Tyropeptin-Boronic Acid as Inhibitors Against the β5 Subunit of Human 20S Proteasome
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International Journal of Molecular Sciences 2011 12 (12), 1807-1835
Probes for activity-based profiling of plant proteases
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Physiologia Plantarum 2011 , no-no
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Chemistry & Biology 2011 18, 608-618
Carfilzomib: a novel second-generation proteasome inhibitor
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Proteasome inhibitors in cancer therapy
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Targeting PKC-β II by Peptides and Peptidomimetics Derived from RACK 1: An In Silico Approach
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Elucidation of the α-Keto-Aldehyde Binding Mechanism: A Lead Structure Motif for Proteasome Inhibition
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Salinosporamide Natural Products: Potent 20 S Proteasome Inhibitors as Promising Cancer Chemotherapeutics
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Salinosporamid-Naturstoffe: potente Inhibitoren des 20S-Proteasoms als vielversprechende Krebs-Chemotherapeutika
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Bioorganic & Medicinal Chemistry Letters 2010 20 (22), 6581-6586
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Biochimie 2010 92, 1530-1545
Characterization of a new series of non-covalent proteasome inhibitors with exquisite potency and selectivity for the 20S β5-subunit
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Biochemical Journal 2010 430 (3), 461-476
Cell Cycle Arrest and Apoptosis Induction by an Anticancer Chalcone Epoxide
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Probing the proteasome cavity in three steps: bio-orthogonal photo-reactive suicide substrates
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Natural Products as Probes of Selected Targets in Tumor Cell Biology and Hypoxic Signaling
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European Journal of Organic Chemistry 2009 2009 (20), 3301-3313
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Bioorganic & Medicinal Chemistry Letters 2009 19 (12), 3220-3224
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Journal of Organometallic Chemistry 2009 694 (12), 1795-1801
The persisting challenge of selective and specific proteasome inhibition
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Journal of Peptide Science 2009 15 (2), 58-66
The Development and Pharmacology of Proteasome Inhibitors for the Management and Treatment of Cancer
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The Structural Basis for the Activation and Peptide Recognition of Bacterial ClpP
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Bioorganic & Medicinal Chemistry Letters 2008 18 (6), 2198-2202
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Proteasome modulators: essential chemical genetic tools for understanding human diseases
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Molecular BioSystems 2008 4 (4), 280
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Organic & Biomolecular Chemistry 2008 6 (3), 424
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Biochemical and Biophysical Research Communications 2008 365, 882-888
Stability of the proteasome can be regulated allosterically through engagement of its proteolytic active sites
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Nature Structural & Molecular Biology 2007 14 (12), 1180-1188
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Highbrow proteasome in high-throughput technology
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Molecular Machines for Protein Degradation
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Simplified Synthetic TMC-95A/B Analogues Retain the Potency of Proteasome Inhibitory Activity
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Probing Structural Determinants Distal to the Site of Hydrolysis that Control Substrate Specificity of the 20S Proteasome
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Communication

Crystal Structure of Epoxomicin:20S Proteasome Reveals a Molecular Basis for Selectivity of α‘,β‘-Epoxyketone Proteasome Inhibitors

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