Double your pleasure

SignalRx Pharmaceuticals Inc. has developed an in silico platform for designing small molecule dual inhibitors that is more targeted and efficient than the standard approach of experimentally screening vast chemical libraries to find a molecule with the desired specificities. The company is using the platform to create a line of compounds that inhibit PI3K plus a second cancer target, and has shown in preclinical models that a dual inhibitor of PI3Kα and BRD4 produces less toxicity than separate inhibitors of the two targets.

Founder Donald Durden, vice chair of research in the Department of Pediatrics at the University of California San Diego, told BioCentury the company's strategy is to attack MYC-fueled tumors by two mechanisms that can work together to prevent development of drug resistance. For example, Durden said PI3K prevents degradation of MYC, while the epigenetic regulator BRD4 promotes its transcription. ...