Inhibitors of BRAF dimers using an allosteric site
FDA-approved RAF inhibitors poorly inhibit BRAF dimers, which limits their clinical efficacy in tumors expressing BRAFV600E mutant monomers. Here the authors identify FDA-approved Ponatinib as an effective inhibitor of BRAF monomers and dimers and designed PHI1, an inhibitor with a unique mode of ac...
Main Authors: | Xiomaris M. Cotto-Rios, Bogos Agianian, Nadege Gitego, Emmanouil Zacharioudakis, Orsi Giricz, Yang Wu, Yiyu Zou, Amit Verma, Poulikos I. Poulikakos, Evripidis Gavathiotis |
---|---|
Format: | Article |
Language: | English |
Published: |
Nature Publishing Group
2020-09-01
|
Series: | Nature Communications |
Online Access: | https://doi.org/10.1038/s41467-020-18123-2 |
Similar Items
-
Eltrombopag directly inhibits BAX and prevents cell death
by: Adam Z. Spitz, et al.
Published: (2021-02-01) -
Exploring Molecular Mechanisms of Paradoxical Activation in the BRAF Kinase Dimers: Atomistic Simulations of Conformational Dynamics and Modeling of Allosteric Communication Networks and Signaling Pathways.
by: Amanda Tse, et al.
Published: (2016-01-01) -
Molecular Basis for p85 Dimerization and Allosteric Ligand Recognition
by: Aljedani, Safia
Published: (2018) -
Identification of allosteric inhibitors of the ecto-5'-nucleotidase (CD73) targeting the dimer interface.
by: Rahila Rahimova, et al.
Published: (2018-01-01) -
Unbiased discovery of druggable genomic targets by Click-sequencing (Click-seq)
by: Zacharioudakis, Emmanouil
Published: (2015)