Cargando…
Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS
Mutations activating KRAS underlie many forms of cancer, but are refractory to therapeutic targeting. Here, we develop Poloppin, an inhibitor of protein-protein interactions via the Polo-box domain (PBD) of the mitotic Polo-like kinases (PLKs), in monotherapeutic and combination strategies to target...
Autores principales: | Narvaez, Ana J., Ber, Suzan, Crooks, Alex, Emery, Amy, Hardwick, Bryn, Guarino Almeida, Estrella, Huggins, David J., Perera, David, Roberts-Thomson, Meredith, Azzarelli, Roberta, Hood, Fiona E., Prior, Ian A., Walker, David W., Boyce, Richard, Boyle, Robert G., Barker, Samuel P., Torrance, Christopher J., McKenzie, Grahame J., Venkitaraman, Ashok R. |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Cell Press
2017
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5563081/ https://www.ncbi.nlm.nih.gov/pubmed/28807782 http://dx.doi.org/10.1016/j.chembiol.2017.07.009 |
Ejemplares similares
-
Development of a Novel Cell-Permeable Protein–Protein
Interaction Inhibitor for the Polo-box Domain of Polo-like Kinase
1
por: Huggins, David J., et al.
Publicado: (2019) -
Computational Analysis of Phosphopeptide Binding to the Polo-Box Domain of the Mitotic Kinase PLK1 Using Molecular Dynamics Simulation
por: Huggins, David J., et al.
Publicado: (2010) -
A cryptic hydrophobic pocket in the polo-box domain of the polo-like kinase PLK1 regulates substrate recognition and mitotic chromosome segregation
por: Sharma, Pooja, et al.
Publicado: (2019) -
Allosteric modulation of AURKA kinase activity by a small-molecule inhibitor of its protein-protein interaction with TPX2
por: Janeček, Matej, et al.
Publicado: (2016) -
Overcoming Chemical, Biological, and Computational Challenges in the Development of Inhibitors Targeting Protein-Protein Interactions
por: Laraia, Luca, et al.
Publicado: (2015)