Results 71 to 80 of about 81,753 (307)

The first-in-class alkylating deacetylase inhibitor molecule tinostamustine shows antitumor effects and is synergistic with radiotherapy in preclinical models of glioblastoma [PDF]

, 2018
Background: The use of alkylating agents such as temozolomide in association with radiotherapy (RT) is the therapeutic standard of glioblastoma (GBM).
Chen, Yi, Colapietro, Alessandro, Cristiano, Loredana, Delle Monache, Simona, Festuccia, Claudio, Gravina, Giovanni Luca, Mancini, Andrea, Marampon, Francesco, Mehrling, Thomas, Pompili, Simona, Tombolini, Vincenzo, Vetuschi, Antonella, Vitale, Flora   +12 more
core   +2 more sources

Discovery of a Novel DNMT1 Inhibitor with Improved Efficacy in Treating β‐Thalassemia

Advanced Science, EarlyView.
Context of Research: β‐thalassemia affects millions worldwide. DNMT inhibitors are effective HbF‐inducers that benefit patients with β‐thalassemia. Existing DNMT inhibitors are not approved for β‐thalassemia treatment due to dose‐limiting toxicity.What We Find: DMT207 traps DNMT1 into helix‐kinked inactive conformation and enhances its interaction with
Yijie Shen, Jiale Wei, Shibing Tang, Dongliang Wu, Liangyi Zong, Shuyuan Ma, Qing Xiong, Ruijie Gong, Siyuan Xu, Chuxuan Peng, Qin Feng, Songchen Liu, Qitong Liu, Yuhua Ye, Quan Zhao, Cheng Luo, Peng Huang, Zhihai Li, Xiangqian Kong, Xianjiang Lan   +19 more
wiley   +1 more source

HDAC inhibitor ITF2357 reduces resistance of mutant-KRAS non-small cell lung cancer to pemetrexed through a HDAC2/miR-130a-3p-dependent mechanism

Journal of Translational Medicine, 2023
Background Histone deacetylases (HDAC) contribute to oncogenic program, pointing to their inhibitors as a potential strategy against cancers. We, thus, studied the mechanism of HDAC inhibitor ITF2357 in resistance of mutant (mut)-KRAS non-small cell lung
Jian Cui, Fei Xu, Wei Bai, Tiantian Zhao, Junbo Hong, Wei Zuo   +5 more
doaj   +1 more source

Translating HDAC inhibitors in Friedreich’s ataxia [PDF]

Expert Opinion on Orphan Drugs, 2016
Friedreich's ataxia (FRDA) is an autosomal recessive neurodegenerative disease caused by expansion of a GAA·TTC triplet in the first intron of the FXN gene, encoding the essential mitochondrial protein frataxin. Repeat expansion results in transcriptional silencing through an epigenetic mechanism, resulting in significant decreases in frataxin protein ...
Elisabetta, Soragni, Joel M, Gottesfeld
openaire   +2 more sources

Material‐Induced Nuclear Deformation Controls Chromatin Architecture in Adipose Stem Cells

Advanced Science, EarlyView.
Tuning cell and cytoskeleton mechanics modulated nuclear shape and heterochromatin organization in ASCs. Distinct cytoskeletal architectures induced nuclear morphologies from oblate to prolate ellipsoids. Large elongated cells with a structured actin cap exhibited high nuclear strain, driving nuclear envelope deformation and heterochromatin ...
Carlo F. Natale, Luca Messina, Valeria Panzetta, Stefania Saporito, Costantino Menna, Maurizio Ventre, Paolo A. Netti   +6 more
wiley   +1 more source

Antimalarial activity of the anticancer histone deacetylase inhibitor SB939 [PDF]

, 2012
Histone deacetylase (HDAC) enzymes posttranslationally modify lysines on histone and nonhistone proteins and play crucial roles in epigenetic regulation and other important cellular processes. HDAC inhibitors (e.g., suberoylanilide hydroxamic acid [SAHA;
Andrews, Katherine T., Do, Tram Anh, Fairlie, David P., Goodman, Christopher D., Haque, Ashraful, Lucke, Andrew J., McFadden, Geoffrey I., Sahama, Ishani, Skinner-Adams, Tina, Sumanadasa, Subathdrage D. M.   +9 more
core   +1 more source

A Trypsin‐Like Serine Protease ZmNAL1a Fine‐Tunes Maize Floral Transition and Flowering Time

Advanced Science, EarlyView.
This study identifies a trypsin‐like serine protease, ZmNAL1a, that moves from leaves to the shoot apical meristem. ZmNAL1a promotes the floral transition by degrading TOPLESS‐like corepressor REL2, which thereby enhances the expression of key flowering genes through elevating histone acetylation and relieving REL2–ZmEREBP147‐mediated transcriptional ...
Nan Li, Qiang Ning, Zhen Li, Qian Zhang, Peilu Zhu, Jimin Zhan, Yunfu Li, Zhen Li, Liang Dong, Qing Xiong, Jiahao Liao, Jie Liu, David Jackson, Munenori Kitagawa, Zuxin Zhang, Lei Liu   +15 more
wiley   +1 more source

Epigenetic and antitumor effects of platinum(IV)-octanoato conjugates [PDF]

, 2017
We present the anticancer properties of cis, cis, trans-[Pt(IV)(NH3)2Cl2(OA)2] [Pt(IV)diOA] (OA = octanoato), Pt(IV) derivative of cisplatin containing two OA units appended to the axial positions of a six-coordinate Pt(IV) center.
Brabec, Viktor, Gandin, Valentina, Gibson, Dan, Kasparkova, Jana, Marzano, Cristina, Novohradsky, Vojtech, Osella, Domenico, Pracharova, Jitka, Zanellato, Ilaria   +8 more
core   +1 more source

Targeting Lactate and Lactylation in Cancer Metabolism and Immunotherapy

Advanced Science, EarlyView.
Lactate, once deemed a metabolic waste, emerges as a central regulator of cancer progression. This review elucidates how lactate and its epigenetic derivative, protein lactylation, orchestrate tumor metabolism, immune suppression, and therapeutic resistance.
Jiajing Gong, Yuhang Xie, Zhijie Weng, Yongzhi Wu, Longjiang Li, Bo Li   +5 more
wiley   +1 more source

Enhanced efficacy of histone deacetylase inhibitor combined with bromodomain inhibitor in glioblastoma

Journal of Experimental & Clinical Cancer Research, 2018
Background Glioblastoma (GBM) is the most common and most malignant primary brain cancer in adults. Despite multimodality treatment, the prognosis is still poor.
Wei Meng, Baocheng Wang, Weiwei Mao, Jiajia Wang, Yang Zhao, Qifeng Li, Chenran Zhang, Yujie Tang, Jie Ma   +8 more
doaj   +1 more source