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20S Proteasome and Its Inhibitors:  Crystallographic Knowledge for Drug Development

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Charité (CCM), Institut für Biochemie, AG Strukturforschung, Monbijoustrasse 2, 10117 Berlin, Germany
Cite this: Chem. Rev. 2007, 107, 3, 687–717
Publication Date (Web):February 23, 2007
Copyright © 2007 American Chemical Society

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    80. Alexei F. Kisselev. Site-Specific Proteasome Inhibitors. Biomolecules 2022, 12 (1) , 54.
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    88. Zhang-Xu He, Yun-Peng Gong, Xin Zhang, Li-Ying Ma, Wen Zhao. Pyridazine as a privileged structure: An updated review on anticancer activity of pyridazine containing bioactive molecules. European Journal of Medicinal Chemistry 2021, 209 , 112946.
    89. Sirin Uysal, Zeynep Soyer, Merve Saylam, Ayse H. Tarikogullari, Sinem Yilmaz, Petek Ballar Kirmizibayrak. Design, synthesis and biological evaluation of novel naphthoquinone-4-aminobenzensulfonamide/carboxamide derivatives as proteasome inhibitors. European Journal of Medicinal Chemistry 2021, 209 , 112890.
    90. Youdong Mao. Structure, Dynamics and Function of the 26S Proteasome. 2021, 1-151.
    91. Levente M. Mihalovits, György G. Ferenczy, György M. Keserű. Mechanistic and thermodynamic characterization of oxathiazolones as potent and selective covalent immunoproteasome inhibitors. Computational and Structural Biotechnology Journal 2021, 19 , 4486-4496.
    92. Jyoti Singh, Amruta Suryan, Sandeep Kumar, Shweta Sharma. Phthalazinone Scaffold: Emerging Tool in the Development of Target Based Novel Anticancer Agents. Anti-Cancer Agents in Medicinal Chemistry 2020, 20 (18) , 2228-2245.
    93. Yajun Yang, Ke Wang, Bo Wu, Ying Yang, Fangfang Lai, Xiaoguang Chen, Zhiyan Xiao. Design, synthesis and biological evaluation of triaryl compounds as novel 20S proteasome inhibitors. Bioorganic & Medicinal Chemistry Letters 2020, 30 (21) , 127508.
    94. Anna Maria Santoro, Alessandro D’Urso, Alessandra Cunsolo, Danilo Milardi, Roberto Purrello, Diego Sbardella, Grazia R. Tundo, Donatella Diana, Roberto Fattorusso, Antonio Di Dato, Antonella Paladino, Marco Persico, Massimo Coletta, Caterina Fattorusso. Cooperative Binding of the Cationic Porphyrin Tris-T4 Enhances Catalytic Activity of 20S Proteasome Unveiling a Complex Distribution of Functional States. International Journal of Molecular Sciences 2020, 21 (19) , 7190.
    95. G.R. Tundo, D. Sbardella, A.M. Santoro, A. Coletta, F. Oddone, G. Grasso, D. Milardi, P.M. Lacal, S. Marini, R. Purrello, G. Graziani, M. Coletta. The proteasome as a druggable target with multiple therapeutic potentialities: Cutting and non-cutting edges. Pharmacology & Therapeutics 2020, 213 , 107579.
    96. Paula Guzmán-Téllez, Diana Martínez-Valencia, Angélica Silva-Olivares, Rosa M. del Ángel, Jesús Serrano-Luna, Mineko Shibayama. Naegleria fowleri and Naegleria gruberi 20S proteasome: identification and characterization. European Journal of Cell Biology 2020, 99 (5) , 151085.
    97. Imen Boualia, Abdelmadjid Debache, Raouf Boulcina, Thierry Roisnel, Fabienne Berrée, Joëlle Vidal, Bertrand Carboni. Synthesis of novel 3-(quinazol-2-yl)-quinolines via SNAr and aluminum chloride-induced (hetero) arylation reactions and biological evaluation as proteasome inhibitors. Tetrahedron Letters 2020, 61 (17) , 151805.
    98. Anna Maria Santoro, Valeria Lanza, Francesco Bellia, Diego Sbardella, Grazia R. Tundo, Alessandra Cannizzo, Giuseppe Grasso, Mariaconcetta Arizzi, Vincenzo G. Nicoletti, Stefano Alcaro, Giosuè Costa, Adriana Pietropaolo, Gaetano Malgieri, Gianluca D'Abrosca, Roberto Fattorusso, Sara García‐Viñuales, Ikhlas M. M. Ahmed, Massimiliano Coletta, Danilo Milardi. Pyrazolones Activate the Proteasome by Gating Mechanisms and Protect Neuronal Cells from β‐Amyloid Toxicity. ChemMedChem 2020, 15 (3) , 302-316.
    99. Stanley C. Xie, Lawrence R. Dick, Alexandra Gould, Stephen Brand, Leann Tilley. The proteasome as a target for protozoan parasites. Expert Opinion on Therapeutic Targets 2019, 23 (11) , 903-914.
    100. Guedes, Aniceto, Andrade, Salvador, Guedes. Chemical Patterns of Proteasome Inhibitors: Lessons Learned from Two Decades of Drug Design. International Journal of Molecular Sciences 2019, 20 (21) , 5326.
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