A Novel Cyclic Mobile Transporter Can Induce Apoptosis by Facilitating Chloride Anion Transport into Cells

Amide
DOI: 10.1021/acsomega.0c00438 Publication Date: 2020-07-03T00:09:52Z
ABSTRACT
We report here the preparation of an aminoxy amide-based pseudopeptide-derived building block using furanoid sugar molecules. Through cyclo-oligomerization reaction, we generate a hybrid triazole/aminoxy amide macrocycle as-prepared block. The novel conformation has been characterized NMR and molecular modeling studies, which show strong resemblance our synthesized compound to d-,l-α-aminoxy acid-based cyclic peptides that contain uniform backbone chirality. observe can efficiently selectively bind Cl- ion transport across lipid bilayer. 1H anion binding studies suggest coherent relationship between acidity N-H triazole C-H proton strength. Using time-based fluorescence assay, acts as mobile transporter follows antiport mechanism. Our imposes cancer cell death by disrupting ionic homeostasis through transport. induced cytochrome c leakage changes in mitochondrial membrane potential along with activation family caspases, suggesting cellular apoptosis occurs caspase-dependent intrinsic pathway. present results possibility biological tool high therapeutic value.
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