Characterization of a novel AICARFT inhibitor which potently elevates ZMP and has anti-tumor activity in murine models

AICARFT is a folate dependent catalytic site within the ATIC gene, part of the purine biosynthetic pathway, a pathway frequently upregulated in cancers. LSN3213128 is a potent (16 nM) anti-folate inhibitor of AICARFT and selective relative to TS, SHMT1, MTHFD1, MTHFD2 and MTHFD2L. Increases in ZMP,...

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Detalles Bibliográficos
Autores principales: Brooks, Harold B., Meier, Timothy I., Geeganage, Sandaruwan, Fales, Kevin R., Thrasher, Kenneth J., Konicek, Susan A., Spencer, Charles D., Thibodeaux, Stefan, Foreman, Robert T., Hui, Yu-Hua, Roth, Kenneth D., Qian, Yue-Wei, Wang, Tao, Luo, Shuang, Torrado, Alicia, Si, Chong, Toth, James L., Mc Cowan, Jefferson R., Frimpong, Kwame, Lee, Matthew R., Dally, Robert D., Shepherd, Timothy A., Durham, Timothy B., Wang, Yong, Wu, Zhipei, Iversen, Philip W., Njoroge, F. George
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2018
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6193938/
https://www.ncbi.nlm.nih.gov/pubmed/30337562
http://dx.doi.org/10.1038/s41598-018-33453-4

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