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Approaches for discovering anti-prion compounds: lessons learned and challenges ahead

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Fabio Moda, Maria Laura Bolognesi & Giuseppe Legname. (2019) Novel screening approaches for human prion diseases drug discovery. Expert Opinion on Drug Discovery 14:10, pages 983-993.
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Yeong-Gon Choi, Byungki Jang, Jeong-Ho Park, Min-Woo Choi, Gong Yeal Lee, Dae Jin Cho, Hong Youp Kim, Hae Kyoung Lim, Won Jae Lee, Eun-Kyoung Choi & Yong-Sun Kim. (2023) Radotinib Decreases Prion Propagation and Prolongs Survival Times in Models of Prion Disease. International Journal of Molecular Sciences 24:15, pages 12241.
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Matteo Staderini, Silvia Vanni, Arianna Colini Baldeschi, Gabriele Giachin, Marco Zattoni, Luigi Celauro, Chiara Ferracin, Edoardo Bistaffa, Fabio Moda, Daniel I. Pérez, Ana Martínez, M. Antonia Martín, Olmo Martín-Cámara, Ángel Cores, Giulia Bianchini, Robert Kammerer, J. Carlos Menéndez, Giuseppe Legname & Maria Laura Bolognesi. (2023) Bifunctional carbazole derivatives for simultaneous therapy and fluorescence imaging in prion disease murine cell models. European Journal of Medicinal Chemistry 245, pages 114923.
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Ghulam Mustafa, Muhammad Zia-ur-Rehman, Sajjad Hussain Sumrra, Muhammad Ashfaq, Wardha Zafar & Maryam Ashfaq. (2022) A critical review on recent trends on pharmacological applications of pyrazolone endowed derivatives. Journal of Molecular Structure 1262, pages 133044.
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Wei Yang, Cao Chen, Jia Chen, Ying Xia, Chao Hu, Lin Wang, Yue-Zhang Wu, Qi Shi, Zhi-Bao Chen & Xiao-Ping Dong. (2022) PrPSc Inhibition and Cellular Protection of DBL on a Prion-Infected Cultured Cell via Multiple Pathways. Molecular Neurobiology 59:5, pages 3310-3321.
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Carlo Mustazza, Marco Sbriccoli, Paola Minosi & Carla Raggi. (2020) Small Molecules with Anti-Prion Activity. Current Medicinal Chemistry 27:33, pages 5446-5479.
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Ludovica Zaccagnini, Giulia Rossetti, Thanh Hoa Tran, Giulia Salzano, Annachiara Gandini, Arianna Colini Baldeschi, Maria Laura Bolognesi, Paolo Carloni & Giuseppe Legname. (2020) In silico/in vitro screening and hit evaluation identified new phenothiazine anti-prion derivatives. European Journal of Medicinal Chemistry 196, pages 112295.
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Óscar López-Pérez, Janne Markus Toivonen, Alicia Otero, Laura Solanas, Pilar Zaragoza, Juan José Badiola, Rosario Osta, Rosa Bolea & Inmaculada Martín-Burriel. (2020) Impairment of autophagy in scrapie-infected transgenic mice at the clinical stage. Laboratory Investigation 100:1, pages 52-63.
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Takao Ishikawa & Kamil Lisiecki. (2020) Anti-prion drug screening system in Saccharomyces cerevisiae based on an artificial [LEU2+] prion. Fungal Genetics and Biology 134, pages 103280.
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Zhiqiang Du, Stephanie Valtierra, Luzivette Robles Cardona, Sara Fernandez Dunne, Chi-Hao Luan & Liming Li. (2019) Identifying Anti-prion Chemical Compounds Using a Newly Established Yeast High-Throughput Screening System. Cell Chemical Biology 26:12, pages 1664-1680.e4.
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Erica Corda, Xiaotang Du, Su Yeon Shim, Antonia N. Klein, Jessica Siltberg-Liberles & Sabine Gilch. (2018) Interaction of Peptide Aptamers with Prion Protein Central Domain Promotes α-Cleavage of PrPC. Molecular Neurobiology 55:10, pages 7758-7774.
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Katharina Annick Wüsten, Pasham Parameshwar Reddy, Andrej Smiyakin, Maria Eugenia Bernis & Gültekin Tamgüney. (2018) A Bioluminescent Cell Assay to Quantify Prion Protein Dimerization. Scientific Reports 8:1.
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N. C. Ferreira, L. M. Ascari, A. G. Hughson, G. R. Cavalheiro, C. F. Góes, P. N. Fernandes, J. R. Hollister, R. A. da Conceição, D. S. Silva, A. M. T. Souza, M. L. C. Barbosa, F. A. Lara, R. A. P. Martins, B. Caughey & Y. Cordeiro. (2018) A Promising Antiprion Trimethoxychalcone Binds to the Globular Domain of the Cellular Prion Protein and Changes Its Cellular Location. Antimicrobial Agents and Chemotherapy 62:2.
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Basant A. Abdulrahman, Dalia Abdelaziz, Simrika Thapa, Li Lu, Shubha Jain, Sabine Gilch, Stefan Proniuk, Alexander Zukiwski & Hermann M. Schatzl. (2017) The celecoxib derivatives AR-12 and AR-14 induce autophagy and clear prion-infected cells from prions. Scientific Reports 7:1.
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Adriano Aguzzi & Yingjun Liu. (2017) A role for astroglia in prion diseases. Journal of Experimental Medicine 214:12, pages 3477-3479.
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S. Vanni, F. Moda, M. Zattoni, E. Bistaffa, E. De Cecco, M. Rossi, G. Giaccone, F. Tagliavini, S. Haïk, J. P. Deslys, G. Zanusso, J. W. Ironside, I. Ferrer, G. G. Kovacs & G. Legname. (2017) Differential overexpression of SERPINA3 in human prion diseases. Scientific Reports 7:1.
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Luise Linsenmeier, Hermann C. Altmeppen, Sebastian Wetzel, Behnam Mohammadi, Paul Saftig & Markus Glatzel. (2017) Diverse functions of the prion protein – Does proteolytic processing hold the key?. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research 1864:11, pages 2128-2137.
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Giuseppe Legname. (2017) Elucidating the function of the prion protein. PLOS Pathogens 13:8, pages e1006458.
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Ludovica Zaccagnini, Simone Brogi, Margherita Brindisi, Sandra Gemma, Giulia Chemi, Giuseppe Legname, Giuseppe Campiani & Stefania Butini. (2017) Identification of novel fluorescent probes preventing PrP Sc replication in prion diseases. European Journal of Medicinal Chemistry 127, pages 859-873.
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Annachiara Gandini & Maria Laura Bolognesi. 2017. Prion Protein. Prion Protein 433 453 .
M.L. Bolognesi. 2017. Comprehensive Medicinal Chemistry III. Comprehensive Medicinal Chemistry III 74 106 .
Elisa Uliassi, Federica Prati, Salvatore Bongarzone & Maria Laura Bolognesi. 2017. Design of Hybrid Molecules for Drug Development. Design of Hybrid Molecules for Drug Development 259 277 .
Kenta Teruya, Ayumi Oguma, Keiko Nishizawa, Maki Kawata, Yuji Sakasegawa, Hiroshi Kamitakahara & Katsumi Doh-ura. (2016) A Single Subcutaneous Injection of Cellulose Ethers Administered Long before Infection Confers Sustained Protection against Prion Diseases in Rodents. PLOS Pathogens 12:12, pages e1006045.
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Maria Laura Bolognesi, Salvatore Bongarzone, Suzana Aulic, Hoang Ngoc Ai Tran, Federica Prati, Paolo Carloni & Giuseppe Legname. (2015) Rational approach to an antiprion compound with a multiple mechanism of action. Future Medicinal Chemistry 7:16, pages 2113-2120.
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