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Discovery and Characterization of Clinical Candidate LXE408 as a Kinetoplastid-Selective Proteasome Inhibitor for the Treatment of Leishmaniases

[Image: see text] Visceral leishmaniasis is responsible for up to 30,000 deaths every year. Current treatments have shortcomings that include toxicity and variable efficacy across endemic regions. Previously, we reported the discovery of GNF6702, a selective inhibitor of the kinetoplastid proteasome...

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Detalles Bibliográficos
Autores principales: Nagle, Advait, Biggart, Agnes, Be, Celine, Srinivas, Honnappa, Hein, Andreas, Caridha, Diana, Sciotti, Richard J., Pybus, Brandon, Kreishman-Deitrick, Mara, Bursulaya, Badry, Lai, Yin H., Gao, Mu-Yun, Liang, Fang, Mathison, Casey J. N., Liu, Xiaodong, Yeh, Vince, Smith, Jeffrey, Lerario, Isabelle, Xie, Yongping, Chianelli, Donatella, Gibney, Michael, Berman, Ashley, Chen, Yen-Liang, Jiricek, Jan, Davis, Lauren C., Liu, Xianzhong, Ballard, Jaime, Khare, Shilpi, Eggimann, Fabian Kurt, Luneau, Alexandre, Groessl, Todd, Shapiro, Michael, Richmond, Wendy, Johnson, Kevin, Rudewicz, Patrick J., Rao, Srinivasa P. S., Thompson, Christopher, Tuntland, Tove, Spraggon, Glen, Glynne, Richard J., Supek, Frantisek, Wiesmann, Christian, Molteni, Valentina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2020
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7549094/
https://www.ncbi.nlm.nih.gov/pubmed/32667203
http://dx.doi.org/10.1021/acs.jmedchem.0c00499