Protein Interaction Studies with Low Molecular Weight Ligands : Applications for Drug Discovery, Basic Research and Diagnostic Tool Design

摘要: The screening of extracts from marine organisms is a widely used strategy to discover new drug leads. A common problem in the process generation false positive hits through unspecific effects complex chemical composition crude extracts. In this study, we explored combination fluorescence resonance energy transfer (FRET) based activity assay and surface plasmon (SPR) binding avoid problem. An aqueous extract was prepared rest raw material Norwegian spring spawning herring, further fractionated by methanol solubility solid phase extraction. FRET assays were determine influence each on different proteases. Several showed more than 50% inhibition. inhibition mechanisms elucidated SPR competition experiments with known inhibitors. For secreted aspartic proteases 1, 2, 3 HIV-1 protease, results indicated that some contain inhibitors interacting specifically active site enzymes. study shows an powerful tool identify potent Furthermore, vertebrates offer interesting source for bioactive compounds, although they have rarely been purpose.