Crystal structures of NUDT15 variants enabled by a potent inhibitor reveal the structural basis for thiopurine sensitivity

The enzyme NUDT15 efficiently hydrolyzes the active metabolites of thiopurine drugs, which are routinely used for treating cancer and inflammatory diseases. Loss-of-function variants in NUDT15 are strongly associated with thiopurine intolerance, such as leukopenia, and preemptive NUDT15 genotyping h...

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Detalles Bibliográficos
Autores principales: Rehling, Daniel, Zhang, Si Min, Jemth, Ann-Sofie, Koolmeister, Tobias, Throup, Adam, Wallner, Olov, Scaletti, Emma, Moriyama, Takaya, Nishii, Rina, Davies, Jonathan, Desroses, Matthieu, Rudd, Sean G., Scobie, Martin, Homan, Evert, Berglund, Ulrika Warpman, Yang, Jun J., Helleday, Thomas, Stenmark, Pål
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Society for Biochemistry and Molecular Biology 2021
Materias:
Research Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8079283/
https://www.ncbi.nlm.nih.gov/pubmed/33753169
http://dx.doi.org/10.1016/j.jbc.2021.100568

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