Discovery of MOMA-341, a chemically distinct, potent and selective covalent inhibitor of Werner Syndrome Helicase (WRN) in clinical development
Veranstaltungen
16:00 – 17:00
Medizinische Chemie
Dies ist ein Online Event
Dr. Momar Toure
MOMA Therapeutics
MOMA-341 is a chemically distinct, potent and selective clinical stage covalent inhibitor of WRN. Leveraging MOMA's KNOWMATIC platform and the presence of cysteine 727 in an allosteric binding pocket, covalent inhibitors were designed to achieve high potency. Optimization was based on precise refinement of covalent warhead trajectory, compound rigidity, and improvement of binding affinity to drive high kinact/KI. Optimization of potency and ADME properties, guided by in silico prediction of in vivo target occupancy, led to the discovery of MOMA-341, which demonstrates tumor regression at low doses in MSI-H mouse xenograft models. MOMA-341 is currently in clinical development.
Kontaktperson
Dr. Anika Tarasewicz
Zu Ihrem Kalender hinzufügen
Interessen
Veranstaltungsdetails
16:00 – 17:00
Medizinische Chemie
Dies ist ein Online Event
Dr. Momar Toure
MOMA Therapeutics
Kontaktperson
Dr. Anika Tarasewicz
Zu Ihrem Kalender hinzufügen
