PRESS RELEASES
Please quote Nature Chemical Biology as the source of these items.
The November 2008 issue of Nature Chemical Biology is available online.
November 2008
Seeking promiscuity
pp 691 - 699Scientists have designed a small molecule that simultaneously inhibits multiple enzymes, as described online this week in Nature Chemical Biology. The ability to identify chemical compounds that target multiple pathways involved in cellular growth offers potential for more targeted anticancer therapies.
Previously scientists looking for new drugs try to find a small molecule that will selectively block the action of one protein within cells. However, recent studies have shown that certain successful drugs thought to be highly selective for their target proteins actually work by interacting with other proteins as well.
Kevan Shokat and colleagues used this strategy to identify PP121, a molecule that interferes with cancer cell growth by inhibiting two types of enzymes, known as tyrosine kinases and lipid kinases. The discovery offers a lead compound for therapeutic approaches, but also reveals design principles that will aid researchers in finding new multi-target inhibitors.
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases
pp 691 - 699Beth Apsel, Jimmy A Blair, Beatriz Gonzalez, Tamim M Nazif, Morri E Feldman, Brian Aizenstein, Randy Hoffman, Roger L Williams, Kevan M Shokat & Zachary A Knight
Published online: 12 October 2008 | doi 10.1038/nchembio.117
