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Nature Chemical Biology

April 22, 2013

A potent and selective small-molecule inhibitor of the pro-survival protein BCL-XL is reported this week in Nature Chemical Biology. The work raises the possibility of developing BCL-XL-specific anticancer drugs.

BCL-XL is in a family of proteins that can help cancer cells survive and is often overexpressed in tumors. Because this family of proteins is difficult to target with small molecules, only a small number of compounds have progressed into clinical development. To date, none of these compounds are selective for specific family members, which could contribute to undesirable toxicities of these drugs.

Guillaume Lessene and colleagues now engineer a selective and potent inhibitor of BCL-XL. They go on to validate that this compound called WEHI-539 retains both its potency and selectivity in cells and demonstrate that it promotes cell death by acting on target. WEHI-539 is an important tool that scientists can use to better understand the relationship between BCL-XL and cancer cell survival and opens the door for the development of BCL-XL-specific anticancer drugs.

DOI:10.1038/nchembio.1246 | Original article

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