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9161por Gao, Yuan, Duan, Jilong, Dang, Xiawen, Yuan, Yinghui, Wang, Yu, He, Xingrui, Bai, Renren, Ye, Xiang-Yang, Xie, Tian“…To further improve its antitumor activity and poor solubility, a polar HDACi pharmacophore was incorporated its scaffold. …”
Publicado 2023
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9162por Wang, Peixin, Zhao, Chenqiong, Zhou, Hanjing, Huang, Xiaona, Ying, Hanqi, Zhang, Songying, Pan, Yibin, Zhu, Haiyan“…Mechanistically, using human trophoblast cell models, treatment with HDAC inhibitor (HDACI)-trichostatin A (TSA) can induce autophagy by promoting nuclear translocation and transcriptional activity of the central autophagic regulator transcription factor EB (TFEB). …”
Publicado 2023
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9163por Romeo, Maria Anele, Gilardini Montani, Maria Saveria, Santarelli, Roberta, Benedetti, Rossella, Arena, Andrea, Cirone, Mara“…Also considering that this HDACi did not upregulate PD-L2 and that the supernatant of VPA-treated cancer cells did not increase PD-L1 expression on the surface of macrophages exposed to it. …”
Publicado 2023
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9164“…As a novel histone deacetylase inhibitor (HDACi), LAQ824 (LAQ) effectively inhibits the proliferation of hematological malignancies and solid tumors. …”
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9165por Sikandar, Shaheen, Dizon, Diana, Shen, Xiling, Li, Zuomei, Besterman, Jeffery, Lipkin, Steven M.“…We found that the class I selective histone deacetylase inhibitor (HDACi) MGCD0103 has significant activity against CCIC, and also significantly inhibits non-CCIC CRC cell xenograft formation. …”
Publicado 2010
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9166por Sambathkumar, Rangarajan, Kalo, Eric, Van Rossom, Rob, Faas, Marijke M., de Vos, Paul, Verfaillie, Catherine M.“…We demonstrated that histone deacetylase inhibitor (HDACi) Trichostatin A (TSA) combined with a chromatin remodeling medium (CRM) induced expression of a number of definitive endoderm and early and late pancreatic marker genes. …”
Publicado 2016
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9167por Witt, A E, Lee, C-W, Lee, T I, Azzam, D J, Wang, B, Caslini, C, Petrocca, F, Grosso, J, Jones, M, Cohick, E B, Gropper, A B, Wahlestedt, C, Richardson, A L, Shiekhattar, R, Young, R A, Ince, T A“…We also demonstrate that clinically available HDAC inhibitors (HDACi) targeting HDAC1 and HDAC7 can be used to preferentially target CSCs. …”
Publicado 2017
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9168por Lv, Baojie, Li, Jingjing, Li, Meng, Zhuo, Yujie, Ren, Ke, Li, Erguang, Yang, Guang“…Inhibitors of histone deacetylases (HDACi) are among the commonly reported small molecule compounds which enhance Ad-mediated gene delivery. …”
Publicado 2018
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9169“…Modifications of histones play a crucial role in cerebral ischemic affair development after translation by modulating disrupted acetylation homeostasis. HDAC inhibitors (HDACi) mainly exert neuroprotective effects by enhancing histone and nonhistone acetylation levels and enhancing gene expression and protein modification functions. …”
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9170por Aru, Başak, Günay, Aysel, Demirel, Gülderen Yanıkkaya, Gürek, Ayşe Gül, Atilla, Devrim“…Moreover, peripheral or non-peripheral substitution of HDACi moieties altered cellular localization between ZnPc-1 and ZnPc-2, leading to increased IC(50) values along with decreased anti-cancer activity for non-peripheral substitution. …”
Publicado 2021
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9171“…Given the poor efficacy of intensive conventional treatment, two novel therapies, histone deacetylase inhibitors (HDACi) and bromodomain inhibitors (BETi) are recommended, as both can arrest the growth of tumour cells, and these targeted therapies may extend patient survival time in the future. …”
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9172por Wen, Jingjing, Chen, Yanxin, Yang, Jiajie, Dai, Chunye, Yu, Shenjie, Zhong, Wenting, Liu, Lilin, He, Chengguanng, Zhang, Wenmin, Yang, Ting, Liu, Lingfeng, Hu, Jianda“…To increase the efficacy of CAR-T cell therapy, we tested different strategies, including application of combined checkpoint inhibitors and histone deacetylase inhibitors (HDACi) in vivo and in vitro. We found CD123 and CLL-1 were highly expressed on AML cells. …”
Publicado 2023
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9173“…To address the issue, herein a multifunctional SN38 derivative (compound 9) containing biotin (tumor-targeting group) and valproic acid (histone deacetylase inhibitor, HDACi) was synthesized via click chemistry and evaluated using MTT assay. …”
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9174por Wu, Yunchen, He, Yudan, Liu, Chen, Ehle, Charlotte, Iyer-Bierhoff, Aishwarya, Liu, Bing, Heinzel, Thorsten, Xing, Shaojun“…Histone deacetylase inhibitors (HDACi), such as suberoylanilide hydroxamic acid (SAHA), have been proposed as potent anti-inflammatory agents for treating inflammatory diseases. …”
Publicado 2023
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9175“…MGCD0103, an isotype-selective histone deacetylase inhibitor (HDACi), has been clinically evaluated for the treatment of hematologic malignancies and advanced solid tumors, alone and in combination with standard-of-care agents. …”
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9176por Bhat, Jaydeep, Sosna, Justyna, Fritsch, Jürgen, Quabius, Elgar Susanne, Schütze, Stefan, Zeissig, Sebastian, Ammerpohl, Ole, Adam, Dieter, Kabelitz, Dieter“…Here we report the induction of IL-4δ(13) expression in human γδ T-cells upon treatment with a sublethal dose of histone deacetylase (HDACi) inhibitor valproic acid (VPA). Induction of IL-4δ(13) was associated with increased cytoplasmic IL-4Rα and decreased IL-4 expression, while mRNA for mature IL-4 was concomitantly down-regulated. …”
Publicado 2016
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9177“…The expression of many well-known oncogenes relies on BET proteins function, indicating BET inhibition as a strategy to counteract their activity. BETi and HDACi share many common targets and affect similar cellular processes to the point that combined inhibition of both these classes of proteins is regarded as a strategy to improve the effectiveness of these drugs in cancer. …”
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9178“…Studies of HDAC inhibitors (HDACi) in human neuronal cells show that HDAC6 inhibitors (HDAC6i) increase the acetylation of specific lysine residues in proteins involved in synaptogenesis. …”
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9179por Voss, S. Randal, Ponomareva, Larissa V., Dwaraka, Varun B., Pardue, Kaitlin E., Baddar, Nour W. Al Haj, Rodgers, A. Katherine, Woodcock, M. Ryan, Qiu, Qingchao, Crowner, Anne, Blichmann, Dana, Khatri, Shivam, Thorson, Jon S.“…A relatively large number of compounds (N = 55) inhibited tail regeneration, including 18 histone deacetylase inhibitors (HDACi). In particular, romidepsin, an FDA-approved anticancer drug, potently inhibited tail regeneration when embryos were treated continuously for 7 days. …”
Publicado 2019
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9180“…INTERVENTIONS: Conventional IA induction regimen followed by high-dose cytarabine (HiDAC) regimen. OUTCOMES: Complete absorption of pericardial and pleural effusion after the first cycle of IA induction chemotherapy. …”
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