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Bioorg Med Chem. 2011 Jul 15;19(14):4377-85. doi: 10.1016/j.bmc.2011.05.009. Epub 2011 May 27.

Generation of 'Unnatural Natural Product' library and identification of a small molecule inhibitor of XIAP.

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Department of Biosciences and Informatics, Faculty of Science and Technology, Keio University, 3-14-1 Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan.

Erratum in

  • Bioorg Med Chem. 2012 Apr 1;20(7):2479.


Natural products have been utilized for drug discovery. To increase the source diversity, we generated a new chemical library consisting of chemically modified microbial metabolites termed 'Unnatural Natural Products' by chemical conversion of microbial metabolites in crude broth extracts followed by purification of reaction products with the LC-photo diode array-MS system. Using this library, we discovered an XIAP inhibitor, C38OX6, which restored XIAP-suppressed enzymatic activity of caspase-3 in vitro. Furthermore, C38OX6 sensitized cancer cells to anticancer drugs, whereas the unconverted natural product did not. These findings suggest that our library could be a useful source for drug seeds.

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