Identification of novel small-molecule inhibitors of glioblastoma cell growth and invasion by high-throughput screening

Wang, Lulu; Zhao, Hong; Cui, Kemi; Yao, Lishuang; Ren, Min; Hao, Aijun; Smollen, P.; Nie, Fang; Jin, Guangxu; Liu, Qian; Wong, Stephen T.C.

doi:10.5582/bst.2012.v6.4.192

Cited by 11 publications

(10 citation statements)

References 28 publications

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“…The α-adrenoceptor antagonist also showed anti-tumor potential against prostate cancer cell lines and GBM cells [5,7]. Previous studies suggested that PHEN might be a potential inhibitor of GBM cell growth and invasion through a high-throughput screening [7], which allows for concurrent screening of thousands of compounds on account of its high sensitivity, broad linearity, and robustness [9,10]. In the current study, we tested the anti-tumor effect of PHEN in glioma cells and conducted a preliminary study to explore the molecular mechanism, finding that PHEN was able to induce an anti-tumor effect both in vitro and in vivo.…”

Section: Discussionmentioning

confidence: 99%

“…It was first used in the early 1950s as an anti-pheochromocytoma drug [8]. The α-adrenoceptor antagonist also showed anti-tumor potential against prostate cancer cell lines and GBM cells [5,7]. Previous studies suggested that PHEN might be a potential inhibitor of GBM cell growth and invasion through a high-throughput screening [7], which allows for concurrent screening of thousands of compounds on account of its high sensitivity, broad linearity, and robustness [9,10].…”

Section: Discussionmentioning

confidence: 99%

“…In addition, PHEN could irreversibly inhibit calmodulin gene expression, knowing that calmodulin plays an important role in the maintenance of astrocytoma cell viability [6]. Importantly, PHEN was supposed to be a novel smallmolecule inhibitor of glioblastoma multiform (GBM) cell growth and invasion in a high-throughput screening study [7]. However, the intrinsic molecular mechanism underlying its anti-cancer property remains to be clarified.…”

Section: Introductionmentioning

confidence: 99%

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Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells

et al. 2015

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Phenoxybenzamine hydrochloride (PHEN) is a selective antagonist of both α-adrenoceptor and calmodulin that exhibits anticancer properties. The aim of this study was to explore the anti-tumor function of PHEN in glioma. Cell proliferation assay was used to assess glioma cell growth. Migration and invasion capacity of glioma cells was monitored by wound-healing and transwell assay, respectively. Neurosphere formation test was adopted for the tumorigenesis of glioma cells, which was also confirmed by soft agar cloning formation test in vitro and a nude mouse model in vivo. Finally, we explored the potential pathway utilized by PHEN using Western blot and immunofluoresce staining. PHEN exhibited a significant inhibitory effect on the proliferation of both U251 and U87MG glioma cell lines in a positive dose-dependent manner. PHEN apparently attenuated the malignancy of glioma in terms of migration and invasion and also suppressed the tumorigenic capacity both in vitro and in vivo. Mechanism study showed that PHEN promoted tumor suppression by inhibiting the TrkB-Akt pathway. The results of the present study demonstrated that PHEN suppressed the proliferation, migration, invasion, and tumorigenesis of glioma cells, induced LINGO-1 expression, and inhibited the TrkB-Akt pathway, which may prove to be the mechanisms underlying the anti-tumor effect of PHEN on glioma cells.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells

et al. 2015

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“…Therefore, there are uninterrupted endeavor of trying to find an effectively therapeutic method to inhibit the bloodcurdling tumor domestic and overseas [19,20]. There are increasing reports that gene therapy has distinct effect and bright future.…”

Section: Discussionmentioning

confidence: 99%

Novel Gelatin–Siloxane Nanoparticles Multiple Modified by Cationic Peptide and Aptamers as Efficient Gene Vector

Tian¹,

Wang²,

Feng³

et al. 2017

JAN

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Abstract. An excellent gene vector is of great importance for the development of the gene therapy. Gelatin-siloxane nanoparticles (GS NPs) with controlled size and surface charge were synthesized through a two-step sol-gel process for gene vector. In order to increase the efficiency of tumour targeting, HIV-derived Tat peptide and TTA1, a kind of modified RNA aptamer, were further grafted onto GS NPs (GS-PEG-TTA1/TAT NPs). It was demonstrated in this article that gelatin-siloxane nanoparticles (GS NPs) have the significant characteristic of being innocuous, small, covered with positive charge and even have been modified with PEG, TTA1, and TAT. The modified nanoparticles, GS-PEG-TTA1/TAT, not only have the ability of crossing the cell membrane with DNA accompanied effectively, but also could target the U251 cells and impel the DNA express right in the cells with the help of aptamer TTA1.

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“…Integration of in vivo/ in situ imaging and therapy will provide some more possibilities for intraoperative diagnosis and therapeutic (17,(24)(25)(26)(27)(28)(29)96). With respect to tumor resection in soft biological tissue, OCT-guided laser ablation is a novel theranostics method, especially in brain tumor resection.…”

Section: Integrated Oct and Laser Ablation System For Realtime Treatmmentioning

confidence: 99%

Optical coherence tomography for precision brain imaging, neurosurgical guidance and minimally invasive theranostics

Fan

Xia

Zhang

et al. 2018

BST

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Identification of novel small-molecule inhibitors of glioblastoma cell growth and invasion by high-throughput screening

Cited by 11 publications

References 28 publications

Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells

Anti-tumor activity of phenoxybenzamine hydrochloride on malignant glioma cells

Novel Gelatin–Siloxane Nanoparticles Multiple Modified by Cationic Peptide and Aptamers as Efficient Gene Vector

Optical coherence tomography for precision brain imaging, neurosurgical guidance and minimally invasive theranostics

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