Structural insights into the potency and selectivity of covalent pan-FGFR inhibitors

FIIN-2, TAS-120 (Futibatinib) and PRN1371 are highly potent pan-FGFR covalent inhibitors targeting the p-loop cysteine of FGFR proteins, of which TAS-120 and PRN1371 are currently in clinical trials. It is critical to analyze their target selectivity and their abilities to overcome gatekeeper mutati...

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Detalles Bibliográficos
Autores principales: Qu, Lingzhi, Chen, Xiaojuan, Wei, Hudie, Guo, Ming, Dai, Shuyan, Jiang, Longying, Li, Jun, Yue, Sitong, Chen, Zhuchu, Chen, Yongheng
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2022
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9814232/
https://www.ncbi.nlm.nih.gov/pubmed/36697561
http://dx.doi.org/10.1038/s42004-021-00623-x

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9814232/
https://www.ncbi.nlm.nih.gov/pubmed/36697561
http://dx.doi.org/10.1038/s42004-021-00623-x

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