CoQ10 selective miscibility and penetration into lipid monolayers with lower lateral packing density

Biochimica et Biophysica Acta, 2017. Garg, et al. BERG, LLC, investigated the biophysical properties of BPM31510, a compound currently in clinical trials for cancer, and demonstrated that the selective incorporation of BPM31510 into cancer cells is dependent upon the lipid density of the cell membrane.

Authors: Sumit Garg, Vandana Swaminathan, Sirisha Dhavala, Michael A. Kiebish, Rangaprasad Sarangarajan, Niven R. Narain

We investigated the properties of our clinical compound, BPM31510 to determine if the components of BPM31510 formulation (lipid and CoQ10) interact to provide compound stability, and how they facilitate the entry of BPM31510 into cells. CoQ10 is a key component of BPM31510 and acts within a pathway utilized by cells for respiration. CoQ10 is also capable of reorganizing cellular membranes, thus effecting a variety of cellular functions. We used a model cell membrane composed of a lipid monolayer floating on top of water in a Langmuir trough system. We measured the effect of BPM31510 incorporation after changing the density of the lipids in the model membrane by compression. We demonstrated that BPM31510 requires a lower membrane density for membrane incorporation, and that CoQ10 participates in several pathways within the cell in addition to its best known role in respiration. Our results may provide insight into the mechanism of action of CoQ10-based cancer therapies such as BPM31510.

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