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Inhibition of the RacGEF VAV3 by the small molecule IODVA1 impedes RAC signaling and overcomes resistance to tyrosine kinase inhibition in acute lymphoblastic leukemia

Aberrant RHO guanine nucleotide exchange factor (RhoGEF) activation is chief mechanism driving abnormal activation of their GTPase targets in transformation and tumorigenesis. Consequently, a small-molecule inhibitor of RhoGEF can make an anti-cancer drug. We used cellular, mouse, and humanized mode...

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Detalles Bibliográficos
Autores principales: Hegde, Shailaja, Gasilina, Anjelika, Wunderlich, Mark, Lin, Yuan, Buchholzer, Marcel, Krumbach, Oliver H. F., Akbarzadeh, Mohammad, Ahmadian, Mohammad Reza, Seibel, William, Zheng, Yi, Perentesis, John P., Mizukawa, Benjamin E., Vinnedge, Lisa Privette, Cancelas, José A., Nassar, Nicolas N.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group UK 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8885421/
https://www.ncbi.nlm.nih.gov/pubmed/34711926
http://dx.doi.org/10.1038/s41375-021-01455-3