Chemistry is an experimental science, and the best way to enjoy it and learn about it is performing experiments. Quality Control of 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine. Introducing a new discovery about 22013-33-8, Name is 2,3-Dihydrobenzo[b][1,4]dioxin-6-amine
Selective Targeting of the TPX2 Site of Importin-alpha Using Fragment-Based Ligand Design
Protein-protein interactions are difficult therapeutic targets, and inhibiting pathologically relevant interactions without disrupting other essential ones presents an additional challenge. Herein we report how this might be achieved for the potential anticancer target, the TPX2-importin-a interaction. Importina is a nuclear transport protein that regulates the spindle assembly protein TPX2. It has two binding sites – major and minor – to which partners bind. Most nuclear transport cargoes use the major site, whereas TPX2 binds principally to the minor site. Fragment-based approaches were used to identify small molecules that bind importin-a, and crystallographic studies identified a lead series that was observed to bind specifically to the minor site, representing the first ligands specific for this site. Structure-guided synthesis informed the elaboration of these fragments to explore the source of ligand selectivity between the minor and major sites. These ligands are starting points for the development of i hibitors of this protein-protein interaction.
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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem