New Spisulosine Derivative promotes robust autophagic response to cancer cells

Ganesher Asha; Chaturvedi Priyank; Sahai Rohit; Meena Sanjeev; Mitra Kalyan; Datta Dipak; Panda Gautam

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New Spisulosine Derivative promotes robust autophagic response to cancer cells

机译：新的施霉素衍生物促进对癌细胞的稳健自噬反应

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Therapy resistance by evasion of apoptosis is one of the hallmarks of human cancer. Therefore, restoration of cell death by non-apoptotic mechanisms is critical to successfully overcome therapy resistance in cancer. By rational drug design approach, here we try to provide evidence that subtle changes in the chemical structure of spisulosine completely switched its cytotoxic function from apoptosis to autophagy. Our most potent molecule (26b) in a series of 16 synthesized derivatives showed robust autophagic cell death in diverse cancer cells sparing normal counterpart. Compound 26b mediated lethal autophagy induction was confirmed by formation of characteristic autophagic vacuoles, LC3 puncta formation, upregulation of signature autophagy markers like Beclin and Atg family proteins. Altogether, we have detected novel autophagy inducer small molecule which can be tested further for drug discovery research. (C) 2020 Elsevier Masson SAS. All rights reserved.

机译：抑制细胞凋亡的治疗耐药是人类癌症的标志之一。因此，通过非凋亡机制恢复细胞死亡对于成功克服癌症治疗抗性至关重要。通过合理的药物设计方法，我们尝试提供证据，即施霉素的化学结构的细微变化完全切换其从细胞凋亡到自噬的细胞毒性功能。我们最有效的分子（26b）在一系列16个合成衍生物中显示出在不同癌细胞中施加正常对应的不同癌细胞中的鲁棒性动物死亡。通过形成特征自噬液泡，LC3斑点形成，拟标志性自噬标志物的上调，介导致死的致命自噬诱导介导的致死自噬诱导，如BECLIN和ATG家族蛋白。完全，我们检测到新型的自噬诱导剂小分子，可以进一步测试用于药物发现研究。（c）2020 Elsevier Masson SAS。版权所有。

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《European Journal of Medicinal Chemistry: Chimie Therapeutique》 |2020年第1期|共14页
作者
Ganesher Asha; Chaturvedi Priyank; Sahai Rohit; Meena Sanjeev; Mitra Kalyan; Datta Dipak; Panda Gautam;
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作者单位

Cent Drug Res Inst CSIR Med &

Proc Chem Div Sitapur Rd Lucknow 226031 UP India;

Cent Drug Res Inst CSIR Div Canc Biol Sitapur Rd Lucknow 226031 UP India;

Cent Drug Res Inst CSIR Sophisticated Analyt Instrument Facil Electron Microscopy Unit Sect 10;

Cent Drug Res Inst CSIR Div Canc Biol Sitapur Rd Lucknow 226031 UP India;

Cent Drug Res Inst CSIR Sophisticated Analyt Instrument Facil Electron Microscopy Unit Sect 10;

Cent Drug Res Inst CSIR Div Canc Biol Sitapur Rd Lucknow 226031 UP India;

Cent Drug Res Inst CSIR Med &

Proc Chem Div Sitapur Rd Lucknow 226031 UP India;

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原文格式 PDF
正文语种 eng
中图分类药学;
关键词
Sphingoid; Chemotherapy; Autophagy; Resistance; Structure-activity relationship;

机译：泪水;化疗;自噬;抵抗;结构 - 活动关系;

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专利

1. New Spisulosine Derivative promotes robust autophagic response to cancer cells [J] . Ganesher Asha, Chaturvedi Priyank, Sahai Rohit, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2020,第1期

机译：新的施霉素衍生物促进对癌细胞的稳健自噬反应
2. Sulfabenzamide promotes autophagic cell death in T-47D breast cancer cells through p53/ DRAM pathway [J] . Raziye MOHAMMADPOUR, Shahrokh SAFARIAN, Soroor FARAHNAK, Journal of Cell and Molecular Biology . 2012,第1期

机译：磺胺苯甲酰胺通过p53 / DRAM途径促进T-47D乳腺癌细胞自噬细胞死亡
3. Neuregulin promotes autophagic cell death of prostate cancer cells. [J] . Tal Or P, Di Segni A, Lupowitz Z, The Prostate . 2003,第2期

机译：神经调节蛋白促进前列腺癌细胞的自噬细胞死亡。
4. Invasion-promoting extracellular matrix composition enhances photodynamic therapy response in 3D pancreatic cancer models [C] . Gwendolyn M. Cramer, Hamid El-Hamidi, Jonathan P. Celli Optical methods for tumor treatment and detection: mechanisms and techniques in photodynamic therapy XXVI . 2017

机译：促进侵袭的细胞外基质成分增强了3D胰腺癌模型的光动力治疗反应
5. Mechanisms mediating tocotrienol derivative in vitro and in vivo anticancer effects and inhibition of compensatory responses to hypoxia in the highly malignant mouse +SA mammary cancer cells. [D] . Ananthula, Suryatheja. 2014

机译：在高度恶性的小鼠+ SA乳腺癌细胞中介导生育三烯酚衍生物的体内外抗癌作用和对缺氧的代偿反应的抑制机制。
6. The quinone-based derivative HMNQ induces apoptotic and autophagic cell death by modulating reactive oxygen species in cancer cells [O] . Eun Byul Lee, Min Gyeong Cheon, Jun Cui, 2017

机译：基于醌的衍生物HMNQ通过调节癌细胞中的活性氧来诱导凋亡和自噬细胞死亡
7. YAP enhances autophagic flux to promote breast cancer cell survival in response to nutrient deprivation. [O] . Qinghe Song, Beibei Mao, Jinbo Cheng, 2015

机译：Yap增强自噬通量，以促进乳腺癌细胞存活以应对营养缺乏。

New Spisulosine Derivative promotes robust autophagic response to cancer cells

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