CHAPTER 6: Discovery and Use of Natural Products and Derivatives as Chemical Probes
Published:17 Nov 2020
M. Kita and H. Kigoshi, in The Discovery and Utility of Chemical Probes in Target Discovery, ed. P. Brennan and S. V. Rodriguez, The Royal Society of Chemistry, 2020, pp. 124-149.
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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.