Tiny compound kills large B cell lymphomas

Small molecules may help researchers develop a targeted therapy for lymphoma, according to a study published in Cancer Cell (2010;17(4):400-411).

The study, led by Ari Melnick, from Weill Cornell Medical College, focused on disrupting the activity of BCL6, the most commonly involved oncogene in diffuse large B cell lymphomas (DLBCL), by using structure-based strategies to determine the best point of attack.

Researchers were able to identify small molecule compounds that specifically interacted with BCL6 at an exposed groove within the BCL6 BTB domain. One compound, called 79-6, was found to bind specifically to the BTB groove and effectively kill BCL6-positive DLBCL cell lines. Additionally, 79-6 was shown to significantly reduce BCL6-dependent tumors in mice that had received transplants of human lymphoma cells and specifically killed primary human DLBCL cells.

“Our work demonstrates that oncogenic transcriptional repressors can be therapeutically targeted with small molecules and presents a rationally designed therapy approach for treatment of lymphomas,” concluded Dr. Melnick. “Future efforts will be taken to systematically improve the therapeutic potential of these compounds with the goal of developing BCL6 targeted therapy for DLBCL.

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