Cationic Pillar[6]arene Induces Cell Apoptosis by Inhibiting Protein Tyrosine Phosphorylation Via Host-Guest Recognition.

International Journal of Molecular Sciences
Can-Peng LiYa-Ping Zhang

Abstract

We reported for the first time that cationic pillar[6]arene (cPA6) could tightly bind to peptide polymer (MW~20-50 kDa), an artificial substrate for tyrosine (Tyr) phosphorylation, and efficiently inhibit Tyr protein phosphorylation through host-guest recognition. We synthesized a nanocomposite of black phosphorus nanosheets loaded with cPA6 (BPNS@cPA6) to explore the effect of cPA6 on cells. BPNS@cPA6 was able to enter HepG2 cells, induced apoptosis, and inhibited cell proliferation by reducing the level of Tyr phosphorylation. Furthermore, BPNS@cPA6 showed a stronger ability of inhibiting cell proliferation in tumor cells than in normal cells. Our results revealed the supramolecular modulation of enzymatic Tyr phosphorylation by the host-guest recognition of cPA6.

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Citations

Apr 28, 2021·Chemistry : a European Journal·Lucía TapiaIgnacio Alfonso
Jun 1, 2021·Chembiochem : a European Journal of Chemical Biology·Yan Zhao

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Methods Mentioned

BETA
isothermal titration calorimetry
circular
nuclear magnetic resonance
fluorescence titration
X-ray
atomic force microscopy
AFM
fluorescence assay
Assay
protein assay

Software Mentioned

UCSF Chimera
Dock Prep
PyMOL
IN Cell Analyzer
Chimera
IN Cell Analyzer 2200
DOCK
DOCK6

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Apoptosis

Apoptosis is a specific process that leads to programmed cell death through the activation of an evolutionary conserved intracellular pathway leading to pathognomic cellular changes distinct from cellular necrosis