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学者姓名：王娟
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摘要 ：
To obtain new anticancer agents with antimetastatic adjunct efficacy, a series of novel N-4-hydrazone derivatives of 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one were designed and synthesized by an eight-step reaction, with appropriate yields. All the synthesized compounds were evaluated for their antiproliferative activity against A549 and MCF-7 cells and for antiplatelet aggregation activity in vitro. The results showed that compounds 25 and 35 not only showed potent antiproliferative activity against the A549 (IC50 = 15.3 and 21.4 mu M) and MCF-7 (IC50 = 15.6 and 10.9 mu M) cell lines but also showed certain antiplatelet aggregation activity (inhibition rates: 47.0% and 45.8%). These results indicated that the structural modification on the N-4-hydrazone moiety of 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one is promising to obtain novel anticancer compounds with antimetastatic adjunct efficacy. In addition, a molecular docking study was performed to investigate the possible targets, and these results indicated that compounds 25 and 35 have the potential to target EGFR, HER2, and P2Y(12).
关键词 ：
3-d]pyrimidin-6-one 3-d]pyrimidin-6-one anticancer anticancer antimetastatic antimetastatic hydrazone hydrazone pyrrolo[2 pyrrolo[2 synthesis synthesis
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| GB/T 7714 | Zhao, Zhichang , Wang, Hongjun , Tian, Nana et al. Synthesis and biological evaluation of N-4-hydrazone derivatives of 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one as novel anticancer agents with antimetastatic adjunct efficacy [J]. | ARCHIV DER PHARMAZIE , 2021 , 354 (11) . |
| MLA | Zhao, Zhichang et al. "Synthesis and biological evaluation of N-4-hydrazone derivatives of 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one as novel anticancer agents with antimetastatic adjunct efficacy" . | ARCHIV DER PHARMAZIE 354 . 11 (2021) . |
| APA | Zhao, Zhichang , Wang, Hongjun , Tian, Nana , Yan, Hong , Wang, Juan . Synthesis and biological evaluation of N-4-hydrazone derivatives of 5,7-dihydro-6H-pyrrolo[2,3-d]pyrimidin-6-one as novel anticancer agents with antimetastatic adjunct efficacy . | ARCHIV DER PHARMAZIE , 2021 , 354 (11) . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
Autophagy is a conserved degradation process crucial to maintaining the primary function of cellular and organismal metabolism. Impaired autophagy could develop numerous diseases, including cancer, cardiomyopathy, neurodegenerative disorders, and aging. N6-methyladenosine (m6A) is the most common RNA modification in eukaryotic cells, and the fate of m6A modified transcripts is controlled by m6A RNA binding proteins. m6A modification influences mRNA alternative splicing, stability, translation, and subcellular localization. Intriguingly, recent studies show that m6A RNA methylation could alter the expression of essential autophagy-related (ATG) genes and influence the autophagy function. Thus, both m6A modification and autophagy could play a crucial role in the onset and progression of various human diseases. In this review, we summarize the latest studies describing the impact of m6A modification in autophagy regulation and discuss the role of m6A modification-autophagy axis in different human diseases, including obesity, heart disease, azoospermatism or oligospermatism, intervertebral disc degeneration, and cancer. The comprehensive understanding of the m6A modification and autophagy interplay may help in interpreting their impact on human diseases and may aid in devising future therapeutic strategies.
关键词 ：
Autophagy Autophagy Azoospermatism Azoospermatism Cancer Cancer Ischemic heart disease Ischemic heart disease m6A m6A Obesity Obesity RNA methylation RNA methylation
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| GB/T 7714 | Chen, Xuechai , Wang, Jianan , Tahir, Muhammad et al. Current insights into the implications of m6A RNA methylation and autophagy interaction in human diseases [J]. | CELL AND BIOSCIENCE , 2021 , 11 (1) . |
| MLA | Chen, Xuechai et al. "Current insights into the implications of m6A RNA methylation and autophagy interaction in human diseases" . | CELL AND BIOSCIENCE 11 . 1 (2021) . |
| APA | Chen, Xuechai , Wang, Jianan , Tahir, Muhammad , Zhang, Fangfang , Ran, Yuanyuan , Liu, Zongjian et al. Current insights into the implications of m6A RNA methylation and autophagy interaction in human diseases . | CELL AND BIOSCIENCE , 2021 , 11 (1) . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
Purpose Non-small cell lung cancer (NSCLC) is the most common type of lung cancer and ranked top in terms of incidence and mortality in men and women. Recently, improvements in treatment approaches for NSCLC have reported, but still, there is a need to devise innovative treatment strategies, especially to manage the advanced and metastatic stage of NSCLC. Aloperine (ALO), an herbal alkaloid, has exerted anti-cancer effects in many cancers. However, the use of any chemotherapeutic agents is dose limited due to possible adverse effects and drug-resistance issues. Therefore, a combination of chemotherapy with viral-based targeted gene therapy may provide a novel treatment strategy for NSCLC. Methods/results In this study, the results of the MTT and flow cytometry-based assays showed that Aloperine-Adbic (adenoviral vector expressing p14(ARF)/p53) combined treatment on NSCLC cells synergistically produced anti-proliferative effects, induced apoptosis, and arrested cell cycle at the G1 phase. Furthermore, the expression analysis suggested that the p53/p21 pathway might contribute to achieving aforesaid cytotoxic effects. The ALO-Adbic combined treatment prolonged the percent survival of NSCLC xenograft models. Conclusion In conclusion, ALO-Adbic combination can produce synergistic anti-cancer effects at low doses, and may offer a more effective and less toxic new treatment strategy for NSCLC.
关键词 ：
Adenoviral vectors Adenoviral vectors Aloperine Aloperine NSCLC NSCLC p53 p53 Synergy Synergy
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| GB/T 7714 | Muhammad, Tahir , Sakhawat, Ali , Khan, Aamir Ali et al. Aloperine in combination with therapeutic adenoviral vector synergistically suppressed the growth of non-small cell lung cancer [J]. | JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY , 2020 , 146 (4) : 861-874 . |
| MLA | Muhammad, Tahir et al. "Aloperine in combination with therapeutic adenoviral vector synergistically suppressed the growth of non-small cell lung cancer" . | JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY 146 . 4 (2020) : 861-874 . |
| APA | Muhammad, Tahir , Sakhawat, Ali , Khan, Aamir Ali , Huang, Hua , Khan, Haroon Rashid , Huang, Yinghui et al. Aloperine in combination with therapeutic adenoviral vector synergistically suppressed the growth of non-small cell lung cancer . | JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY , 2020 , 146 (4) , 861-874 . |
| 导入链接 | NoteExpress RIS BibTex |
摘要 ：
Autophagy starts with the initiation and nucleation of isolation membranes, which further expand and seal to form autophagosomes. The regulation of isolation membrane closure remains poorly understood. CK1 delta is a member of the casein kinase I family of serine/threonine specific kinases. Although CK1 delta is reported to be involved in various cellular processes, its role in autophagy is unknown. Here, we show that CK1 delta regulates the progression of autophagy from the formation of isolation membranes to autophagosome closure, and is essential for macroautophagy. CK1 delta depletion results in impaired autophagy flux and the accumulation of unsealed isolation membranes. The association of LC3 with ATG9A, ATG14L, and ATG16L1 was found to be increased in CK1 delta-depleted cells. The role of CK1 delta in autophagosome completion appears to be conserved between yeasts and humans. Our data reveal a key role for CK1 delta/Hrr25 in autophagosome completion.
关键词 ：
autophagosome closure autophagosome closure autophagy autophagy CK1 delta CK1 delta Hrr25 Hrr25 isolation membrane isolation membrane
引用：
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| GB/T 7714 | Li, Yuting , Chen, Xuechai , Xiong, Qianqian et al. Casein Kinase 1 Family Member CK1 delta/Hrr25 Is Required for Autophagosome Completion [J]. | FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY , 2020 , 8 . |
| MLA | Li, Yuting et al. "Casein Kinase 1 Family Member CK1 delta/Hrr25 Is Required for Autophagosome Completion" . | FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY 8 (2020) . |
| APA | Li, Yuting , Chen, Xuechai , Xiong, Qianqian , Chen, Yong , Zhao, Hongyu , Tahir, Muhammad et al. Casein Kinase 1 Family Member CK1 delta/Hrr25 Is Required for Autophagosome Completion . | FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY , 2020 , 8 . |
| 导入链接 | NoteExpress RIS BibTex |
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