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687 results on '"Liang, Gaolin"'

26. 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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43. CBT‐Cys click reaction for optical bioimaging in vivo.

Author

Hu, Xinyi, Tang, Runqun, Bai, Lin, Liu, Songqin, Liang, Gaolin, and Sun, Xianbao

Subjects
LINEAR polymers, OPTICAL images, RATE coefficients (Chemistry), CONDENSATION reactions, OLIGOMERS, DNA nanotechnology
Abstract

Derived from the D‐luciferin regeneration pathway in firefly body, the click condensation reaction between 2‐cyanobenzothiazole (CBT) and D‐cysteine (Cys) (CBT‐Cys click reaction) possesses unique advantages, including superior biocompatibility, high second order reaction rate, and metal‐free mild conditions, emerging as a powerful bioorthogonal tool for a variety of chemical biological applications. Moreover, owing to its programmable controllability (e.g., pH, reduction, or enzyme), CBT‐Cys click reaction is exploited to fabricate stimuli‐activatable imaging probes with self‐assembling behaviors in physiological context. At stimuli‐rich pathological lesions of interest, these probes undergo CBT‐Cys click reaction to form cyclic dimers/oligomers or linear polymers, and further self‐assemble into nanostructures. The in situ formed nanostructures promote the selective accumulation and retention of imaging agent cargos at pathological lesions, thus enabling precise and enhanced in vivo imaging of diseases (especially tumors). To address the significance and recent breakthroughs of smart CBT‐Cys probes for enhanced optical imaging of tumors/other diseases, we herein propose this mini‐review, in which advances (particularly in recent 5 years) and potential challenges (or chances) in this field are emphasized. [ABSTRACT FROM AUTHOR]

Published
2023
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