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13. Fibroblast Growth Factor Receptor 1-Specific Dehydrogelation to Release Its Inhibitor for Enhanced Lung Tumor Therapy

Author

Tang, Runqun, Zhang, Ziyi, Liu, Xiaoyang, Zhu, Liangxi, Xu, Yuting, Chai, Renjie, Zhan, Wenjun, Shen, Shurong, and Liang, Gaolin

Abstract

Fibroblast growth factor receptor 1 (FGFR1) is emerging as a promising molecular target of lung cancer, and various FGFR1 inhibitors have exhibited significant therapeutic effects on lung cancer in preclinical research. Due to their low targeting ability or bioavailability, direct administration of these inhibitors may cause side effects. Herein, a hydrogelator, Nap-Phe-Phe-Phe-Glu-Thr-Glu-Leu-Tyr-OH (Nap-Y), was rationally designed to coassemble with an FGFR1 inhibitor nintedanib (Nin) to form a peptide hydrogel Gel Y/Ninfor localized administration and FGFR1-triggered release of Nin. Upon specific phosphorylation by FGFR1 overexpressed on lung cancer cells, Nap-Yin Gel Y/Ninis converted to the hydrophilic product Nap-Phe-Phe-Phe-Glu-Thr-Glu-Leu-Tyr(H2PO3)-OH (Nap-Yp), leading to dehydrogelation of the gel and subsequent Ninrelease. In vitroexperiments demonstrate that the release of Ninin a sustained manner from Gel Y/Ninsignificantly suppresses the survival, migration, and invasion of A549 cells by inhibiting FGFR1 expression and its phosphorylation function on downstream signaling molecules. Nude mouse studies show that Gel Y/Ninexhibits enhanced therapeutic efficacy on lung tumor than free Nin. We anticipate that Gel Y/Ninwill be utilized for lung cancer treatment in clinical settings in the near future.

Published
2024
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34. Aurora Kinase B‐Instruct Release of AZD1152‐HQPA from Hydrogel to Enhance Cervical Cancer Suppression.

Author

Xu, Guangqiong, Weng, Qiao, Zhang, Lei, Song, Yaye, Zhan, Wenjun, Yin, Yuan, Liang, Gaolin, and Wang, Fuqiang

Subjects
AURORA kinases, CERVICAL cancer, SMALL molecules, DRUG target
Abstract

Aurora kinase B (AURKB) is an attractive and potential molecular target for cervical cancer therapy. To date, a variety of AURKB inhibitors are developed to suppress cervical tumors. Nevertheless, direct use of these small molecule inhibitors may cause severe side effects to patients, limiting their further clinical applications. Herein, a rationally designed hydrogelator Nap‐Phe‐Phe‐Arg‐Arg‐Lys‐Ser‐OH (S) is employed to co‐assemble AZD1152‐HQPA (AZD, an AURKB inhibitor) to develop an AURKB‐responsive hydrogel Gel S/AZD for enhanced cervical tumor suppression. Upon AURKB activation, hydrogelator S in Gel S/AZD evolves into its hydrophilic phosphate Nap‐Phe‐Phe‐Arg‐Arg‐Lys‐Ser(H2PO3)‐OH (Sp), triggering the disassembly of Gel S/AZD to release AZD in a sustained manner. Cell assays reveal that AURKB‐responsive release of AZD from Gel S/AZD potently induces the growth arrest and apoptosis of cervical cancer cells by downregulating the expression level of AURKB downstream protein phospho‐histone H3 (pH3). In vivo studies demonstrate that compared with free AZD, Gel S/AZD shows a superior tumor suppressive effect in orthotropic cervical tumor models. It is envisioned that the Gel S/AZD might be applied in clinic cervical cancer treatment in the near future. [ABSTRACT FROM AUTHOR]

Published
2024
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