Helicases are enzymes that unwind DNA and RNA. They're central to cellular life, implicated in a number of cancers and infections-;and, alas, extraordinarily difficult to target with drugs.
Mar 9 2024The Rockefeller University Helicases are enzymes that unwind DNA and RNA. They're central to cellular life, implicated in a number of cancers and infections-;and, alas, extraordinarily difficult to target with drugs.
"High-resolution structural and biochemical data alone are not sufficient for finding druggable sites in conformationaly dynamic enzymes such as helicases. Our approach can identify these sites and also provide chemical starting points for developing drugs that target helicases.
Helicase inhibitors, however, are hard to come by. By testing thousands of small molecules, drug companies have occasionally happened upon methods for grinding one helicase or another to a halt, but these occurences have proven rare. "The same was true in our lab," Ramsey says. "We were unable to identifiy helicase inhibitors using typical approaches such as high-throughput screening.
Once they found likely binding sites on the helicase, they promoted the scouts to soldiers. "We just had to take a minimally elaborated electrophilic molecule, identify where it binds with mass spectrometry, and then use medicinal chemistry to modify it and screen a few versions of to achieve a potent, specific inhibitor," Ramsey says.
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