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A novel discovery may improve cancer treatment by enhancing drug metabolism. A group of scientists has improved the uptake of PROTACs, a potential class of cancer-fighting medications that have trouble entering cells due to their size.
The new technique uses CD36, a protein that pulls compounds into cells. The research study found that tailoring medications to employ this CD36 pathway delivered 7.7 to 22.3 times more of the drug to cancer cells, making the treatment up to 23 times more potent.
Mouse studies suggest that improved uptake suppressed tumors without making medicines harder to break down or less stable.
CEMC (endocytic medicinal chemistry) uses endocytosis, a natural process by which cells “swallow” chemicals. It could revolutionize drug design, especially for those too massive to be effective.
This breakthrough could make numerous medications that were unusable due to inadequate absorption into promising illness treatments.
Most medication development tweaks molecules to improve passive diffusion via cell membranes. The new method uses cell surface receptors like CD36 to actively deliver medicines inward. CD36 is prevalent on intestinal, skin, lung, eye, and brain cells.
Large molecules over 500 dalton (Da) have trouble entering cells. They penetrated cells without a defined mechanism until now. This study examined PROTAC medicines over 1,000 Da, which is huge by pharmaceutical standards.
But the enhanced PROTACs entered cells more efficiently and had increased tumor-fighting activity while maintaining stability and solubility.
Since endocytic cellular uptake of chemical compounds was unknown, big molecules were thought to be unable to cross membranes for decades. Researchers found CD36 to be an uptake protein and modified medicines to better connect with it to internalize and reach the target protein.
The method must be tested in clinical trials before it can be employed in cancer drugs.
Sources:
CD36-mediated endocytosis of proteolysis-targeting chimeras, Cell (2025). DOI:10.1016/j.cell.2025.03.036. www.cell.com/cell/fulltext/S0092-8674(25)00386-1
https://phys.org/news/2025-04-scientists-hack-cell-entry-supercharge.html
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