Andrastin A is potent inhibitor of protein farnesyltransferase (PFTase) isolated by Omura and co-workers at the Kitasato Institute, Japan in 1996. Andrastin A is a meroterpenoid with an androstane skeleton biosynthesized from a sesquiterpene and a tetraketide. The cyclopentane ring of andrastin A exhibits characteristic keto-enol tautomerism. Andrastin A is potently active against mammalian tumor cell lines and is devoid of antimicrobial activity.
- Andrastins A ~ C, new protein farnesyltransferase inhibitors produced by Penicillium sp. FO-3929.I. Producing strain, fermentation, isolation and biological activities. Omura S. et al., J. Antibiot. 1996, 49, 414.
- Andrastins A ~ C, new protein farnesyltransferase inhibitors produced by Penicillium sp. FO-3929.II. Structure elucidation and biosynthesis. Uchida R. et al., J. Antibiot. 1996, 49, 418.
- Reconstituted biosynthesis of fungal meroterpenoid andrastin A. Matsuda Y. et al., Tetrahedron 2013, 69, 8199.