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ID: ALA1138281

Journal: Bioorg Med Chem Lett

Title: Spermatinamine, the first natural product inhibitor of isoprenylcysteine carboxyl methyltransferase, a new cancer target.

Authors: Buchanan MS, Carroll AR, Fechner GA, Boyle A, Simpson MM, Addepalli R, Avery VM, Hooper JN, Su N, Chen H, Quinn RJ.

Abstract: Isoprenylcysteine methyltransferase (Icmt) catalyzes the carboxyl methylation of oncogenic proteins in the final step of a series of post-translational modifications. The inhibition of Icmt provides an attractive and novel anticancer target. A natural product high-throughput screening campaign was conducted to discover inhibitors of Icmt. The Australian marine sponge, Pseudoceratina sp., yielded spermatinamine, a novel alkaloid with a bromotyrosyl-spermine-bromotyrosyl sequence, as the bioactive constituent. Its structure was determined by 1D and 2D NMR spectroscopy. Spermatinamine is the first natural product inhibitor of Icmt.

CiteXplore: 17964784

DOI: 10.1016/j.bmcl.2007.10.021