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

ABSTRACT: 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 (EC(50)=4.5 ?M), an attractive target for anticancer drug development.

SUBMITTER: Malloy KL

PROVIDER: S-EPMC3248991 | biostudies-literature | 2012 Jan

REPOSITORIES: biostudies-literature

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

Malloy Karla L KL Choi Hyukjae H Fiorilla Catherine C Valeriote Fred A FA Matainaho Teatulohi T Gerwick William H WH

Bioorganic & medicinal chemistry letters 20111024 1

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 (EC(50)=4.5 μM), an attractive target for anticancer drug develo ...[more]

PMID: 22104152

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