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Pharmaceuticals

Bleomycin Potency Boost

Combinatorial biosynthesis produces analog with uniquely high activity

by Stu Borman
August 6, 2012 | APPEARED IN VOLUME 90, ISSUE 32

Bleomycins are approved drugs used in cocktails with other medicines for conditions such as testicular cancer, but they have serious side effects, including lung inflammation. Now, a team has used combinator­ial biosynthesis (genetic engineering of biosynthetic pathways) to create a designed bleomycin with uniquely high potency, which could lead to anticancer agents with improved side-effect profiles. The work was carried out by Yanwen Duan of Hunan Engineering Research Center of Combinatorial Biosynthesis & Natural Product Drug Discovery, in China; Ben Shen of Scripps Research Institute; and coworkers (J. Am. Chem. Soc., DOI: 10.1021/ja3056535). The researchers previously cloned and characterized the biosynthetic gene clusters that bacteria use to produce bleomycins. By analyzing the clusters, they were able to devise a plan for engineering analogs with potentially higher activity, and they succeeded by creating 6′-deoxybleomycin Z, the most potent bleomycin analog to date. The analog could lead to “new bleomycin chemotherapy regimens with reduced dosage, thereby lessening dose-limiting side effects and the incidence of lung toxicity,” Shen says.

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