NEW YORK, April 20 (UPI) — U.S. and Canadian scientists say they have created a class of drugs that target the protein BCL6, which causes the most common type of non-Hodgkin’s lymphoma.
Researchers from Weill Cornell Medical College and colleagues said the experimental compound may effectively block the cancer-causing actions of BCL6 by attaching to a critical “hot spot” on its surface, thus killing the cancer cells.
“BCL6 mediates its cancer-causing actions by attaching to other proteins,” said Dr. Ari Melnick, a Weill Cornell associate professor who led the study. “Traditionally protein-protein interactions have been viewed as being too difficult to block with small-molecule drugs.”
Melnick and his team said they identified a critical “hot spot” that appeared to be amenable to designing a drug. Dr. Alexander Mackerell of the University of Maryland then used computational modeling to identify chemical structures that could attack the hot spot.
“We tested the ability of a large number of these chemicals to bind and block BCL6,” said Melnick, “and then Dr. Gilbert Prive from the University of Toronto performed nuclear magnetic resonance and X-ray crystallography studies to show that a specific BCL6 inhibitor compound hit exactly in the center of the predicted hot spot.
“Our results show that given the right scientific approach it is quite possible to design drugs against key protein regulatory factors like BCL6.”
The study appears in the April 13 issue of the journal Cancer Cell.
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