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Lysosomes of brain capillary endothelial cells are implicated in nicotine acetylcholine receptor (nAChR)‐mediated transcytosis and act as an enzymatic barrier for the transport of peptide ligands to the brain. A D‐peptide ligand of nAChRs (termed DCDX), which binds to nAChRs with an IC50 value of 84.5 nM, was developed by retro–inverso isomerization. DCDX displayed exceptional stability in lysosomal...
Peptidliganden …︁ …︁ vermitteln den Transport von Wirkstoffen in das Gehirn, indem sie kognate Rezeptoren auf Gehirn‐Endothelzellen “entführen". Ein Problem dabei ist, dass Enzyme L‐Peptide inaktivieren und die Transportfähigkeit beschneiden. In ihrer Zuschrift auf S. 3066 ff. identifizieren W. Lu, C. Zhan et al. einen D‐Peptidliganden von Nicotinacetylcholin‐Rezeptoren, der resistent gegen Proteolyse...
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