Reduction‐Responsive RGD‐Docetaxel Conjugate: Synthesis, In Vitro Drug Release and In Vitro Antitumor Activity DOI Open Access
Qingqing Li, Yufeng Liu,

Yi‐Lin Cheng

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 86(1)

Published: Dec. 25, 2024

Poor selectivity to tumor cells is a major drawback in the clinical application of antitumor drug docetaxel (DTX). Peptide-drug conjugates (PDCs) constructed by modifying drugs with peptide ligands that have high affinity certain overexpressed receptors are increasingly assessed for their possibility tumor-selective delivery. In present research, DTX condensed 3-(pyridin-2-yldisulfanyl) propanoic acid via ester bond obtain intermediate Py-SS-DTX. Two GSS-DTX and RGDC-SS-DTX were obtained conjugation Py-SS-DTX glutathione (GSH) RGDC through thiol-disulfide exchange reaction. Afterwards, these two peptide-DTX characterized proton nuclear magnetic resonance, Fourier transform infrared spectroscopy, high-resolution mass spectrometry. The further evaluated terms release, cell cycle inhibition, apoptosis, cytotoxicity. results show both exhibit reduction-responsive release higher reduction-responsiveness. vitro activity study shows exhibits enhanced G2/M phase arrest, apoptosis rate, cytotoxicity as compared free DTX. Besides, reduced on normal synthesized this represents novel conjugate effectively selectively inhibit cells.

Language: Английский

A brain-targeted and ROS-responsive natural polysaccharide nanogel for enhancing antidepressant therapy DOI
Dong Xu,

Tao Qiao,

Yan-Ming Zhou

et al.

Chemical Engineering Journal, Journal Year: 2025, Volume and Issue: unknown, P. 160719 - 160719

Published: Feb. 1, 2025

Language: Английский

Citations

1
RGD peptide/dextran sulfate-based nanocarriers loaded with triptolide for double-targeted apoptosis of both tumor cells and M2-like TAMs in pancreatic cancer therapy DOI

Yaning Ge,

Xin Zhu,

Zhengxian Zhang

et al.

International Journal of Biological Macromolecules, Journal Year: 2025, Volume and Issue: unknown, P. 144032 - 144032

Published: May 1, 2025

Language: Английский

Citations

0
Reduction‐Responsive RGD‐Docetaxel Conjugate: Synthesis, In Vitro Drug Release and In Vitro Antitumor Activity DOI Open Access
Qingqing Li, Yufeng Liu,

Yi‐Lin Cheng

et al.

Drug Development Research, Journal Year: 2024, Volume and Issue: 86(1)

Published: Dec. 25, 2024

Poor selectivity to tumor cells is a major drawback in the clinical application of antitumor drug docetaxel (DTX). Peptide-drug conjugates (PDCs) constructed by modifying drugs with peptide ligands that have high affinity certain overexpressed receptors are increasingly assessed for their possibility tumor-selective delivery. In present research, DTX condensed 3-(pyridin-2-yldisulfanyl) propanoic acid via ester bond obtain intermediate Py-SS-DTX. Two GSS-DTX and RGDC-SS-DTX were obtained conjugation Py-SS-DTX glutathione (GSH) RGDC through thiol-disulfide exchange reaction. Afterwards, these two peptide-DTX characterized proton nuclear magnetic resonance, Fourier transform infrared spectroscopy, high-resolution mass spectrometry. The further evaluated terms release, cell cycle inhibition, apoptosis, cytotoxicity. results show both exhibit reduction-responsive release higher reduction-responsiveness. vitro activity study shows exhibits enhanced G2/M phase arrest, apoptosis rate, cytotoxicity as compared free DTX. Besides, reduced on normal synthesized this represents novel conjugate effectively selectively inhibit cells.

Language: Английский

Citations

1