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TIC10/ONC201: a bend in the road to clinical development.

作者信息

Greer Yoshimi Endo, Lipkowitz Stanley

机构信息

Women's Malignancies Branch, Center for Cancer Research, National Cancer Institute, National Institutes of Health, Bethesda, Maryland.

出版信息

Oncoscience. 2015 Feb 20;2(2):75-6. doi: 10.18632/oncoscience.133. eCollection 2015.

DOI:10.18632/oncoscience.133
PMID:25859547
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4381697/
Abstract
摘要
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1a3/4381697/4deee8aa42ef/oncoscience-02-0075-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1a3/4381697/4deee8aa42ef/oncoscience-02-0075-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c1a3/4381697/4deee8aa42ef/oncoscience-02-0075-g001.jpg

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1
TIC10/ONC201: a bend in the road to clinical development.TIC10/ONC201：临床开发道路上的一个转折点。
Oncoscience. 2015 Feb 20;2(2):75-6. doi: 10.18632/oncoscience.133. eCollection 2015.
2
TIC10/ONC201 synergizes with Bcl-2/Bcl-xL inhibition in glioblastoma by suppression of Mcl-1 and its binding partners in vitro and in vivo.TIC10/ONC201在体外和体内通过抑制Mcl-1及其结合伴侣，与胶质母细胞瘤中的Bcl-2/Bcl-xL抑制协同作用。
Oncotarget. 2015 Nov 3;6(34):36456-71. doi: 10.18632/oncotarget.5505.
3
Small-Molecule ONC201/TIC10 Targets Chemotherapy-Resistant Colorectal Cancer Stem-like Cells in an Akt/Foxo3a/TRAIL-Dependent Manner.小分子 ONC201/TIC10 通过 Akt/Foxo3a/TRAIL 依赖的方式靶向化疗耐药结直肠肿瘤干细胞。
Cancer Res. 2015 Apr 1;75(7):1423-32. doi: 10.1158/0008-5472.CAN-13-3451. Epub 2015 Feb 20.
4
ONC201/TIC10 Is Empowered by 2-Deoxyglucose and Causes Metabolic Reprogramming in Medulloblastoma Cells Independent of C-Myc Expression.ONC201/TIC10受2-脱氧葡萄糖增强作用，且在髓母细胞瘤细胞中引起代谢重编程，与C-Myc表达无关。
Front Cell Dev Biol. 2021 Nov 26;9:734699. doi: 10.3389/fcell.2021.734699. eCollection 2021.
5
The preclinical evaluation of TIC10/ONC201 as an anti-pancreatic cancer agent.TIC10/ONC201作为一种抗胰腺癌药物的临床前评估。
Biochem Biophys Res Commun. 2016 Aug 5;476(4):260-266. doi: 10.1016/j.bbrc.2016.05.106. Epub 2016 May 24.
6
Genetic and Pharmacological Screens Converge in Identifying FLIP, BCL2, and IAP Proteins as Key Regulators of Sensitivity to the TRAIL-Inducing Anticancer Agent ONC201/TIC10.遗传和药理学筛选共同确定FLIP、BCL2和IAP蛋白是对TRAIL诱导的抗癌药物ONC201/TIC10敏感性的关键调节因子。
Cancer Res. 2015 Apr 15;75(8):1668-74. doi: 10.1158/0008-5472.CAN-14-2356. Epub 2015 Feb 13.
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ONC201 Targets AR and AR-V7 Signaling, Reduces PSA, and Synergizes with Everolimus in Prostate Cancer.ONC201 靶向 AR 和 AR-V7 信号通路，降低 PSA，并与依维莫司在前列腺癌中协同作用。
Mol Cancer Res. 2018 May;16(5):754-766. doi: 10.1158/1541-7786.MCR-17-0614. Epub 2018 Mar 27.
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ONC201 kills solid tumor cells by triggering an integrated stress response dependent on ATF4 activation by specific eIF2α kinases.ONC201通过触发一种依赖于特定eIF2α激酶激活ATF4的综合应激反应来杀死实体瘤细胞。
Sci Signal. 2016 Feb 16;9(415):ra18. doi: 10.1126/scisignal.aac4374.
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TIC10/ONC201-a potential therapeutic in glioblastoma.TIC10/ONC201 - 一种胶质母细胞瘤的潜在治疗药物。
Transl Cancer Res. 2017 Dec;6(Suppl 9):S1439-S1440. doi: 10.21037/tcr.2017.10.51.
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Correction: Identification of TRAIL-inducing compounds highlights small molecule ONC201/TIC10 as a unique anti-cancer agent that activates the TRAIL pathway.更正：诱导TRAIL的化合物的鉴定突出了小分子ONC201/TIC10作为一种激活TRAIL途径的独特抗癌剂。
Mol Cancer. 2024 Oct 18;23(1):233. doi: 10.1186/s12943-024-02158-w.

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Comparative study of the anti-tumour effects of the imipridone, ONC201 and its fluorinated analogues on pancreatic cancer cell line.咪吡酮、ONC201及其氟化类似物对胰腺癌细胞系抗肿瘤作用的比较研究
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Imipridones and Dopamine Receptor Antagonism in the Therapeutic Management of Gliomas.米氮平类药物与多巴胺受体拮抗作用在胶质瘤治疗管理中的应用
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Molecular docking appraisal of phytochemicals as potential inhibitor of a key triple-negative breast cancer driver gene.

本文引用的文献

1
The angular structure of ONC201, a TRAIL pathway-inducing compound, determines its potent anti-cancer activity.TRAIL通路诱导化合物ONC201的角状结构决定了其强大的抗癌活性。
Oncotarget. 2014 Dec 30;5(24):12728-37. doi: 10.18632/oncotarget.2890.
2
Pharmacophore reassignment for induction of the immunosurveillance cytokine TRAIL.免疫监视细胞因子 TRAIL 的药效团重定位诱导。
Angew Chem Int Ed Engl. 2014 Jun 23;53(26):6628-31. doi: 10.1002/anie.201402133. Epub 2014 May 18.
3
Dual inactivation of Akt and ERK by TIC10 signals Foxo3a nuclear translocation, TRAIL gene induction, and potent antitumor effects.
植物化学物质作为关键三阴性乳腺癌驱动基因潜在抑制剂的分子对接评估
In Silico Pharmacol. 2023 Jun 14;11(1):15. doi: 10.1007/s40203-023-00152-6. eCollection 2023.
4
Targeting RAS-RAF-MEK-ERK signaling pathway in human cancer: Current status in clinical trials.靶向人类癌症中的RAS-RAF-MEK-ERK信号通路：临床试验现状
Genes Dis. 2022 May 20;10(1):76-88. doi: 10.1016/j.gendis.2022.05.006. eCollection 2023 Jan.
5
Development of small molecule extracellular signal-regulated kinases (ERKs) inhibitors for cancer therapy.用于癌症治疗的小分子细胞外信号调节激酶（ERK）抑制剂的研发。
Acta Pharm Sin B. 2022 May;12(5):2171-2192. doi: 10.1016/j.apsb.2021.12.022. Epub 2022 Jan 4.
6
The Synergistic Activity of Bortezomib and TIC10 against A2058 Melanoma Cells.硼替佐米与TIC10对A2058黑色素瘤细胞的协同活性
Pharmaceuticals (Basel). 2021 Aug 20;14(8):820. doi: 10.3390/ph14080820.
7
Novel Apoptosis-Inducing Agents for the Treatment of Cancer, a New Arsenal in the Toolbox.用于癌症治疗的新型凋亡诱导剂，工具箱中的新武器。
Cancers (Basel). 2019 Jul 31;11(8):1087. doi: 10.3390/cancers11081087.
8
Metabolic reprogramming of glioblastoma cells by L-asparaginase sensitizes for apoptosis in vitro and in vivo.L-天冬酰胺酶对胶质母细胞瘤细胞的代谢重编程使其在体内外对凋亡敏感。
Oncotarget. 2016 Jun 7;7(23):33512-28. doi: 10.18632/oncotarget.9257.
9
Neuro-oncology biotech industry progress report.神经肿瘤学生物技术行业进展报告。
J Neurooncol. 2016 May;128(1):175-182. doi: 10.1007/s11060-016-2087-z. Epub 2016 Feb 20.
10
TIC10/ONC201 synergizes with Bcl-2/Bcl-xL inhibition in glioblastoma by suppression of Mcl-1 and its binding partners in vitro and in vivo.TIC10/ONC201在体外和体内通过抑制Mcl-1及其结合伴侣，与胶质母细胞瘤中的Bcl-2/Bcl-xL抑制协同作用。
Oncotarget. 2015 Nov 3;6(34):36456-71. doi: 10.18632/oncotarget.5505.
TIC10 通过双重抑制 Akt 和 ERK 信号传导，促进 Foxo3a 核转位、TRAIL 基因诱导，发挥强大的抗肿瘤作用。
Sci Transl Med. 2013 Feb 6;5(171):171ra17. doi: 10.1126/scitranslmed.3004828.
4
Proapoptotic DR4 and DR5 signaling in cancer cells: toward clinical translation.促进凋亡的 DR4 和 DR5 信号在癌细胞中的作用：迈向临床转化。
Curr Opin Cell Biol. 2010 Dec;22(6):837-44. doi: 10.1016/j.ceb.2010.08.001. Epub 2010 Aug 31.
5
The TRAIL to targeted therapy of breast cancer.乳腺癌靶向治疗之路。
Adv Cancer Res. 2009;103:43-73. doi: 10.1016/S0065-230X(09)03003-6.
6
Death receptors: signaling and modulation.死亡受体：信号传导与调节
Science. 1998 Aug 28;281(5381):1305-8. doi: 10.1126/science.281.5381.1305.
7
Identification and characterization of a new member of the TNF family that induces apoptosis.一种诱导细胞凋亡的肿瘤坏死因子（TNF）家族新成员的鉴定与特性分析
Immunity. 1995 Dec;3(6):673-82. doi: 10.1016/1074-7613(95)90057-8.