Abstract

MCL1 INHIBITOR BRD-810 KILLS CANCER CELLS WHILE MINIMIZING RISK OF CARDIOTOXICITY

Akanksha N. Mote* and Karan D. Atpadkar

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Abstract

The MCL1 gene is regularly increased in cancer and codes for the antiapoptotic protein myeloid cell leukemia 1 (MCL1), which confers resistance to the current standard of care. In this manner, MCL1 is an attractive anticancer target. Here we depict BRD-810 as a strong and particular MCL1 inhibitor and its key design guideline of fast systemic clearance to possibly minimize region beneath the curve-driven toxicities associated with MCL1 inhibition. Cell death escape is one of the most prominent features of cancer cells and closely connected to the dysregulation of members of the Bcl-2 family of proteins. Among those, the anti-apoptotic family member myeloid cell leukemia-1 (MCL-1) acts as a master regulator of apoptosis in different human malignancies. Irrespective of its unfavorable structure profile, independent research efforts recently led to the era of highly strong MCL-1 inhibitors that are currently assessed in clinical trials.

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