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Discovery and Optimization of Salicylic Acid-Derived Sulfonamide Inhibitors of the WD Repeat-Containing Protein 5 (WDR5)–MYC Protein–Protein Interaction

The treatment of tumors driven by overexpression or amplification of MYC oncogenes remains a significant challenge in drug discovery. Here, we present a new strategy towards the inhibition of MYC via the disruption of the protein-protein-interaction between MYC and its chromatin cofactor WDR5. Block...

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Publicat a:J Med Chem
Autors principals: Macdonald, Jonathan D., Simon, Selena Chacón, Han, Changho, Wang, Feng, Shaw, J. Grace, Howes, Jennifer E., Sai, Jiqing, Yuh, Joannes P., Camper, Demarco, Alicie, Bethany M., Alvarado, Joseph, Nikhar, Sameer, Payne, William, Aho, Erin R., Bauer, Joshua A., Zhao, Bin, Phan, Jason, Thomas, Lance R., Rossanese, Olivia W., Tansey, William P., Waterson, Alex G., Stauffer, Shaun R., Fesik, Stephen W.
Format: Artigo
Idioma:Inglês
Publicat: 2019
Matèries:
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC6933084/
https://ncbi.nlm.nih.gov/pubmed/31724864
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.9b01411
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