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

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

  • Bioorg Med Chem Lett. 2007 Dec 15;17(24):6860-3. doi: 10.1016/j.bmcl.2007.10.021.
Malcolm S Buchanan 1,  Anthony R Carroll,  Gregory A Fechner,  Anthony Boyle,  Moana M Simpson,  Rama Addepalli,  Vicky M Avery,  John N A Hooper,  Nancy Su,  Huawei Chen,  Ronald J Quinn
Affiliations

Affiliation

  • 1 Eskitis Institute, Griffith University, Brisbane, Qld 4111, Australia.
PMID: 17964784 DOI: 10.1016/j.bmcl.2007.10.021
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.

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