Hoiamide D, a marine cyanobacteria-derived inhibitor of p53/MDM2 interaction

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:22

Article

Malloy, Karla L.^1,2  Choi, Hyukjae^1,2  Fiorilla, Catherine³  Valeriote, Fred A.⁴  Matainaho, Teatulohi⁵  Gerwick, William H.^1,2 

[1] Univ Calif San Diego, Scripps Inst Oceanog, Ctr Marine Biotechnol & Biomed, La Jolla, CA 92093 USA

[2] Univ Calif San Diego, Skaggs Sch Pharm & Pharmaceut Sci, La Jolla, CA 92093 USA

[3] Novartis Inst Biomed Res, Cambridge, MA 02139 USA

[4] Henry Ford Hlth Syst, Dept Internal Med, Josephine Ford Canc Ctr, Detroit, MI 48202 USA

[5] Univ Papua New Guinea, Discipline Pharmacol, Sch Med & Hlth Sci, Natl Capital Dist, Papua N Guinea

关键词: Marine cyanobacteria;    Natural products;    Lipopeptide;    Anticancer;    Spectroscopy;   

DOI  :  10.1016/j.bmcl.2011.10.054

来源: Elsevier

【 摘 要 】

Bioassay-guided fractionation of two cyanobacterial extracts from Papua New Guinea has yielded hoiamide D in both its carboxylic acid and conjugate base forms. Hoiamide D is a polyketide synthase (PKS)/non-ribosomal peptide synthetase (NRPS)-derived natural product that features two consecutive thiazolines and a thiazole, as well as a modified isoleucine residue. Hoiamide D displayed inhibitory activity against p53/MDM2 interaction (EC50 = 4.5 mu M), an attractive target for anticancer drug development. (C) 2011 Elsevier Ltd. All rights reserved.

【 授权许可】

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