Y Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective

Gao Yuan; Zhang Hang; Lirussi Frederic; Garrido Carmen; Ye Xiang-Yang; Xie Tian

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Y Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective

机译：组蛋白脱乙酰酶和其他与癌症相关靶标的y双抑制剂：药理学观点

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Epigenetic enzymes histone deacetylases (HDACs) are clinically validated anticancer drug targets which have been studied intensively in the past few decades. Although several drugs have been approved in this field, they are still limited to a subset of hematological malignancies (in particular T-cell lymphomas), with therapeutic potential not fully realized and the drug-resistance occurred after a certain period of use. To maximize the therapeutic potential of these classes of anticancer drugs, and to extend their application to solid tumors, numerous combination therapies containing an HDACi and an anticancer agent from other mechanisms are currently ongoing in clinical trials. Recently, dual targeting strategy comprising the HDACs component has emerged as an alternative approach for combination therapies. In this perspective, we intend to gather all HDACs-containing dual inhibitors related to cancer therapy published in literature since 2015, classify them into five categories based on targets' biological functions, and discuss the rationale why dual acting agents should work better than combinatorial therapies using two separate drugs. The article discusses the pharmacological aspects of these dual inhibitors, including in vitro biological activities, pharmacokinetic studies, in vivo efficacy studies,

机译：表观遗传酶组蛋白脱乙酰酶（HDACs）是临床验证的抗癌药物靶标，这些目标在过去几十年中被密集地研究。虽然在该领域已经批准了几种药物，但它们仍然仅限于血液天动学恶性肿瘤（特别是T细胞淋巴瘤）的子集，治疗潜力没有完全实现，并且在一定时期后发生耐药性。为了最大限度地提高这些类抗癌药物的治疗潜力，并将其应用延伸到实体瘤中，目前在临床试验中正在进行含有HDACI和抗癌剂的许多组合疗法。最近，包括HDACS组分的双靶向策略作为组合疗法的替代方法。在这一观点中，我们打算自2015年以来收集与文学中发表的癌症治疗有关的含HDACs的双重抑制剂，将它们分为基于目标的生物学功能的五类，并讨论了双代理代理应该比组合治疗更好地工作的理由使用两种单独的药物。本文讨论了这些双重抑制剂的药理学方面，包括体外生物活性，药代动力学研究，体内疗效研究，

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《Biochemical Pharmacology》 |2020年第1期|共29页
作者
Gao Yuan; Zhang Hang; Lirussi Frederic; Garrido Carmen; Ye Xiang-Yang; Xie Tian;
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作者单位

Key Lab Elemene Class Anticanc Chinese Med Zhejia Hangzhou Zhejiang Peoples R China;

Key Lab Elemene Class Anticanc Chinese Med Zhejia Hangzhou Zhejiang Peoples R China;

INSERM U1231 Label LipSTIC Dijon France;

INSERM U1231 Label LipSTIC Dijon France;

Key Lab Elemene Class Anticanc Chinese Med Zhejia Hangzhou Zhejiang Peoples R China;

Key Lab Elemene Class Anticanc Chinese Med Zhejia Hangzhou Zhejiang Peoples R China;

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原文格式 PDF
正文语种 eng
中图分类药理学;
关键词
Histone deacetylases (HDACs); Dual inhibitor; Anticancer drugs; Kinases; Epigenetics; Enzymes; Receptors; Synergistic effects;

机译：组蛋白脱乙酰酶（HDAC）;双抑制剂;抗癌药物;激酶;表观酶;酶;受体;协同效应;

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1. Inhibitory Effect of Histone Deacetylase Inhibitor on the Proliferation of Leukemia Cells and Its Anti-Tumor Pharmacology [J] . Shubo Wang 生物科学与医学（英文） . 2021,第001期
2. Evodiamine-inspired dual inhibitors of histone deacetylase 1(HDAC1) and topoisomerase 2(TOP2) with potent antitumor activity [J] . Yahui Huang, Shuqiang Chen, Shanchao Wu, 药学学报：英文版 . 2020,第007期
3. Evodiamine-inspired dual inhibitors of histone deacetylase 1 (HDAC1) and topoisomerase 2 (TOP2) with potent antitumor activity [J] . Yahui Huang, Shuqiang Chen, Shanchao Wu, 药学学报（英文版） . 2020,第007期
4. P21-Driven Multifusion Gene System for Evaluating the Efficacy of Histone Deacetylase Inhibitors by In Vivo Molecular Imaging and for Transcription Targeting Therapy of Cancer Mediated by Histone Deacetylase Inhibitor [J] . Ya-Ju Hsieh, Luen Hwu, Yi-Chieh Chen, The Journal of Nuclear Medicine . 2014,第4期

机译：P21驱动的多重融合基因系统，用于通过体内分子成像评估组蛋白去乙酰化酶抑制剂的功效以及组蛋白去乙酰化酶抑制剂介导的癌症的转录靶向治疗
5. P21-driven multifusion gene system for evaluating the efficacy of histone deacetylase inhibitors by in vivo molecular imaging and for transcription targeting therapy of cancer mediated by histone deacetylase inhibitor. [J] . Ya-Ju Hsieh, Luen Hwu, Yi-Chieh Chen, The Journal of Nuclear Medicine . 2014,第4期

机译：P21驱动的多融合基因系统，用于通过体内分子成像评估组蛋白脱乙酰基酶抑制剂的功效，以及通过组蛋白脱乙酰基酶抑制剂介导的癌症的转录靶向治疗。
6. P21-driven multifusion gene system for evaluating the efficacy of histone deacetylase inhibitors by in vivo molecular imaging and for transcription targeting therapy of cancer mediated by histone deacetylase inhibitor. [J] . Ya-Ju Hsieh, Luen Hwu, Yi-Chieh Chen, The Journal of Nuclear Medicine . 2014,第4期

机译：P21驱动的多化基因系统，用于评估组蛋白脱乙酰酶抑制剂的体内分子成像和组蛋白脱乙酰酶抑制剂介导的癌症的转录靶向治疗的疗效。
7. The Tricyclic Antidepressant Amitriptyline Inhibits D-Cyclin Transactivation and Induces Myeloma Cell Apoptosis by Inhibiting Histone Deacetylases: In Vitro and In Silico Evidence [C] . Xinliang Mao, Depei Wu, Suzanne Trudel, International conference of molecular simulations and applied informatics technologies . 2012

机译：三环抗抑郁药阿米替林通过抑制组蛋白脱乙酰基酶抑制D-cyclin反式激活并诱导骨髓瘤细胞凋亡：体外和计算机证据。
8. P27 as a molecular target for cancer therapeutics: Discovering small molecule inhibitors of p27 proteolysis and structure-activity relationship and mechanistic studies of largazole, a potent inhibitor of histone deacetylase . [D] . Ungermannova, Dana. 2010

机译：P27作为癌症治疗的分子靶标：发现p27蛋白水解和结构活性关系的小分子抑制剂以及组蛋白脱乙酰基酶的有效抑制剂largazole的机理研究。
9. Antitumor activity and pharmacologic characterization of the depsipeptide analog as a novel histone deacetylase/ phosphatidylinositol 3‐kinase dual inhibitor [O] . Ken Saijo, Hiroo Imai, Sonoko Chikamatsu, 2017

机译：作为新型组蛋白脱乙酰基酶/磷脂酰肌醇3-激酶双重抑制剂的十肽类似物的抗肿瘤活性和药理学表征
10. Phenylhexyl isothiocyanate has dual function as histone deacetylase inhibitor and hypomethylating agent and can inhibit myeloma cell growth by targeting critical pathways [O] . Gallagher Ruth, Zhao Xiangmin, Feng Jean, 2008

机译：异硫氰酸苯酯具有组蛋白去乙酰化酶抑制剂和低甲基化剂的双重功能，可通过靶向关键途径抑制骨髓瘤细胞生长
11. Targeting MTA1/HIF-1alpha Signaling by Pterostilbene in Combination with Histone Deacetylase Inhibitor Attenuates Prostate Cancer Progression (Open Access). [R] . Butt, N. A., Kumar, A., Dhar, S., 2017

机译：通过紫檀芪与组蛋白去乙酰化酶抑制剂组合靶向mTa1 / HIF-1α信号减弱前列腺癌进展（开放存取）。

Y Dual inhibitors of histone deacetylases and other cancer-related targets: A pharmacological perspective

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