A molecule capable of targeting multiple cancer cell targets at once could be the basis of a potential new cancer drug class. 

Created by researchers at the University of California San Diego School of Medicine and Moores Cancer Center in collaboration with Rady Children’s Hospital-San Diego, the University of Colorado School of Medicine and pharma company SignalRx, the molecule inhibits two major cancer targets responsible for growth and metastasis.

SF2523 inhibits the action of both PI3K and BRD4 which in turn blocks the activation of a major cancer target called MYC.

MYC is one of the most frequently mutated genes found in cancer but at the same time has proven to be difficult to target with therapeutics.

The gene is a regulator gene meaning it controls the expression of other genes and encodes molecules involved in many essential cellular processes.

As SF2523 indirectly inhibits MYC, the drug also prevents the abnormal activity of many signalling cascades affected by the gene’s mutation.

When tested in mouse models of cancer, SF2523 was found to significantly decrease both cancer growth and metastasis as well as demonstrating a low level of toxicity in the host.

“Most anti-cancer drugs have a single target,” said study co-senior author Donald Durden. “They try to do one thing, such as block a single receptor or signalling pathway. This paper is proof-of-concept of a completely different mode of drug discovery clearly separated from the standard practice of one drug, one target.

“These findings suggest that dual-activity inhibitors are a highly promising lead compound for developing new anticancer therapeutics.”

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