Vortrag
The Discovery of Potent WDR5 Inhibitors for the Treatment of Cancer
Veranstaltungen
21.10.21
14:00 – 15:00
Medizinische Chemie
Dies ist ein Online Event
Stephen Fesik
Vanderbilt University School of Medicine, Nashville, TN, USA
WDR5 is a component of multiple epigenetic regulatory complexes, including the mixed lineage leukemia (MLL)/SET complexes that deposit histone H3 lysine 4 methylation. Overexpression of WDR5 correlates with a poor clinical outcome in many human cancers, and WDR5 has emerged as an attractive target for therapy. We discovered potent WDR5 inhibitors using fragment-based methods and structure-based design. These inhibitors have been optimized for their drug-like properties and show potent oral activity in tumor xenograft mouse models. They act not by altering histone methylation but by displacing WDR5 from chromatin at protein synthesis genes, choking the translational capacity of these cells, and inducing death via a nucleolar stress response. Our inhibitors could thus have broad therapeutic utility as anti-cancer agents.
Kontaktperson
Alexander Lorey
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Interessen
Medizinische Chemie
Veranstaltungsdetails
21.10.21
14:00 – 15:00
Medizinische Chemie
Dies ist ein Online Event
Stephen Fesik
Vanderbilt University School of Medicine, Nashville, TN, USA
Kontaktperson
Alexander Lorey
Zu Ihrem Kalender hinzufügen
In andere Kalender herunterladen
