RESUMO
The identification of natural product producer organisms remains a problem for both isolation and natural product classification. A concise screen is developed through fluorescent modification of a set of natural products that offer a common activity. Through real-time multicolor microscopy, the processing, storage, and effects of a natural product are rapidly screened at the level of the strain and individual organism.
Assuntos
Produtos Biológicos/análise , Biotecnologia/métodos , Animais , Produtos Biológicos/biossíntese , Dinoflagellida/metabolismo , Dinoflagellida/ultraestrutura , Corantes Fluorescentes/síntese química , Sensibilidade e EspecificidadeRESUMO
A series of acyclic, truncated microcystin analogues, comprised of the dienic beta-amino acid (Adda) and up to four additional amino acids characteristic of the parent toxin, was synthesized and screened for activity as inhibitors of PP1 and PP2A. Despite a recent report to the contrary for a microcystin-derived tetrapeptide degradation product, none approaches the potency of microcystin itself.
Assuntos
Inibidores Enzimáticos/química , Inibidores Enzimáticos/farmacologia , Peptídeos Cíclicos/química , Peptídeos Cíclicos/farmacologia , Fosfoproteínas Fosfatases/antagonistas & inibidores , Toxinas Bacterianas , Concentração Inibidora 50 , Isoenzimas , Toxinas Marinhas , Microcistinas , Oligopeptídeos/síntese química , Oligopeptídeos/farmacologia , Relação Estrutura-AtividadeRESUMO
A series of greatly simplified microcystin analogues comprised only of Adda (the beta-amino acid common to the microcystins, nodularins, and motuporin,) and a single additional amino acid residue was synthesized and screened for inhibition of the protein phosphatases 1 and 2A. Several of the analogues were shown to be mid-nanomolar inhibitors of the enzymes.
