title: 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 μM), an attractive target for anticancer drug development.
authors: Center for Marine Biotechnology and Biomedicine, Scripps Institution of Oceanography, University of California at San Diego, La Jolla, CA 92093, USA.
authors: Karla L
authors: KL
authors: Malloy
authors: Hyukjae
authors: H
authors: Choi
authors: Catherine
authors: C
authors: Fiorilla
authors: Fred A
authors: FA
authors: Valeriote
authors: Teatulohi
authors: T
authors: Matainaho
authors: William H
authors: WH
authors: Gerwick
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology; D045744:Cell Line, Tumor; D002626:Chemistry, Pharmaceutical / Q000379:methods; D000458:Cyanobacteria / Q000378:metabolism*; D047630:Depsipeptides / Q000494:pharmacology*; D015195:Drug Design; D006801:Humans; D020128:Inhibitory Concentration 50; D007532:Isoleucine / Q000737:chemistry; D009682:Magnetic Resonance Spectroscopy / Q000379:methods; D008956:Models, Chemical; D009369:Neoplasms / Q000188:drug therapy*; D051736:Proto-Oncogene Proteins c-mdm2 / Q000378:metabolism*; D012270:Ribosomes / Q000378:metabolism; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D053778:Thiazolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D016159:Tumor Suppressor Protein p53 / Q000378:metabolism*
chemical_list: D000970:Antineoplastic Agents; D047630:Depsipeptides; C495901:TP53 protein, human; D013844:Thiazoles; D053778:Thiazolidines; D016159:Tumor Suppressor Protein p53; C574030:hoiamide D; D007532:Isoleucine; C497206:MDM2 protein, human; D051736:Proto-Oncogene Proteins c-mdm2