CHAPTER 6. Discovery and Use of Natural Products and Derivatives as Chemical Probes

Among various structurally and functionally diverse natural products, some compounds modulate protein–protein interactions (PPIs). The anti-tumour macrolide aplyronine A is a PPI stabilizer between tubulin and actin and prevents spindle formation and mitosis. As a case study of using natural products as chemical probes, target identification and mode of action studies of aplyronines are presented. A new methodology using an amidopyrene tag and label-assisted laser desorption/ionization mass spectrometry (LA-LDI-MS) for binding position analysis of ligands on target biomacromolecules is also highlighted.