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Tegavivint Mechanism of Action

Beta Cat has the only potent and selective inhibitor of the Wnt/beta catenin pathway. The major distinguishing factor for Tegavivint is the target of inhibition: the protein-protein interaction between beta catenin and another protein called TBL1 (Transducin Beta-like Protein One). TBL1 brings beta catenin into the nucleus and supports the activation of target oncogenes leading to tumor growth and dissemination. Importantly, this event occurs at the bottom of the Wnt pathway and does not overlap with related Wnt pathway proteins important for normal stem cell function. Tegavivint is therefore exceptionally selective for aberrant beta catenin gene activation, as opposed to other therapies that broadly drug the Wnt pathway and cause harmful side effects to healthy tissue relying on other aspects of Wnt.    

                                           

 

Experiments in various hematological and solid tumor cell lines confirm the primary mechanism of action of Tegavivint (BC-2059) to be disruption of TBL1 interactions with beta catenin. After treatment with Tegavivint, cellular levels of non-membrane beta catenin are dramatically reduced in the nucleus.  Nuclear beta catenin is the oncogenic event that needs to be suppressed.  Gene reporter assays validate compound selectivity for the Wnt pathway. Even though research into TBL1 is still budding, it has begun to stand out as a prognostic marker for disease aggressiveness and survival.

 

© 2017 Betacat Pharma Inc.