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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Detalhes bibliográficos
Publicado no:J Biol Chem
Main Authors: 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: Artigo
Idioma:Inglês
Publicado em: American Society for Biochemistry and Molecular Biology 2021
Assuntos:
Research Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC8079283/
https://ncbi.nlm.nih.gov/pubmed/33753169
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.jbc.2021.100568
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