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https://www.readbyqxmd.com/read/27902771/piceatannol-attenuates-renal-fibrosis-induced-by-unilateral-ureteral-obstruction-via-downregulation-of-histone-deacetylase-4-5-or-p38-mapk-signaling
#1
Sin Young Choi, Zhe Hao Piao, Li Jin, Jung Ha Kim, Gwi Ran Kim, Yuhee Ryu, Ming Quan Lin, Hyung-Seok Kim, Hae Jin Kee, Myung Ho Jeong
Piceatannol, a resveratrol metabolite, is a phenolic compound found in red wine and grapes. We investigated the effect of piceatannol on renal fibrosis and histone deacetylase (HDAC) expression in a mouse model of unilateral ureteral obstruction (UUO). Fibrosis was established by UUO and piceatannol was intraperitoneally injected for 2 weeks. Piceatannol suppressed extracellular matrix (ECM) protein deposition including collagen type I and fibronectin as well as connective tissue growth factor (CTGF) and α-smooth muscle actin (α-SMA) in UUO kidneys...
2016: PloS One
https://www.readbyqxmd.com/read/27901049/glucocorticoid-receptor-and-histone-deacetylase-6-mediate-the-differential-effect-of-dexamethasone-during-osteogenesis-of-mesenchymal-stromal-cells-mscs
#2
Marilyn G Rimando, Hao-Hsiang Wu, Yu-An Liu, Chien-Wei Lee, Shu-Wen Kuo, Yin-Ping Lo, Kuo-Fung Tseng, Yi-Shiuan Liu, Oscar Kuang-Sheng Lee
Lineage commitment and differentiation of mesenchymal stromal cells (MSCs) into osteoblasts in vitro is enhanced by a potent synthetic form of glucocorticoid (GC), dexamethasone (Dex). Paradoxically, when used chronically in patients, GCs exert negative effects on bone, a phenomenon known as glucocorticoid-induced osteoporosis in clinical practice. The mechanism on how GC differentially affects bone precursor cells to become mature osteoblasts during osteogenesis remains elusive. In this study, the dose and temporal regulation of Dex on MSC differentiation into osteoblasts were investigated...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27900262/impaired-histone-deacetylases-5-and-6-expression-mimics-the-effects-of-obesity-and-hypoxia-on-adipocyte-function
#3
Julien Bricambert, Dimitri Favre, Saška Brajkovic, Amélie Bonnefond, Raphael Boutry, Roberto Salvi, Valérie Plaisance, Mohamed Chikri, Giulia Chinetti-Gbaguidi, Bart Staels, Vittorio Giusti, Robert Caiazzo, François Pattou, Gérard Waeber, Philippe Froguel, Amar Abderrahmani
OBJECTIVE: The goal of the study was to investigate the role of histone deacetylases (HDACs) in adipocyte function associated with obesity and hypoxia. METHODS: Total proteins and RNA were prepared from human visceral adipose tissues (VAT) of human obese and normal weight subjects and from white adipose tissue (WAT) of C57Bl6-Rj mice fed a normal or high fat diet (HFD) for 16 weeks. HDAC activity was measured by colorimetric assay whereas the gene and protein expression were monitored by real-time PCR and by western blotting, respectively...
December 2016: Molecular Metabolism
https://www.readbyqxmd.com/read/27886544/3-aroylindoles-display-antitumor-activity-in%C3%A2-vitro-and-in%C3%A2-vivo-effects-of-n1-substituents-on-biological-activity
#4
Hsueh-Yun Lee, Jiann-Fong Lee, Sunil Kumar, Yi-Wen Wu, Wei-Chun HuangFu, Mei-Jung Lai, Yu-Hsuan Li, Hsiang-Ling Huang, Fei-Chiao Kuo, Che-Jen Hsiao, Chun-Chun Cheng, Chia-Ron Yang, Jing-Ping Liou
A series of 3-aroylindole hydroxamic acids (10-17) were developed based on the concept of a structural combination of tubulin and histone deacetylase (HDAC) inhibitors. This was accomplished by introducing hydroxamic acid-containing moieties at the N1 position of the tubulin assembly inhibitor, compound 9 (SCB01A, BPR0L075, phase II trial). Most of synthetic compounds produced in this way displayed comparable HDAC inhibitory activity, and four (10, 12-14) of them also inhibit tubulin assembly. Notably, compound 12 possesses not only tubulin and HDAC inhibitory activity but also shows HDAC6 selectivity over other HDAC isoforms...
November 15, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27884726/deacetylase-inhibitors-as-a-novel-modality-in-the-treatment-of-multiple-myeloma
#5
REVIEW
Paul G Richardson, Philippe Moreau, Jacob P Laubach, Michelle E Maglio, Sagar Lonial, Jesus San-Miguel
Deacetylase enzymes remove acetyl groups from histone and nonhistone proteins. Dysregulation of deacetylase activity is a hallmark of malignancy, including multiple myeloma (MM). Deacetylase inhibitors (DACi) cause epigenetic modification and inhibition of the aggresome pathway, resulting in death of MM cells. Panobinostat, a pan-DACi, has shown significant clinical benefit and is the first DACi approved for the treatment of MM. It is approved for use in combination with bortezomib and dexamethasone for the treatment of patients with relapsed or relapsed and refractory MM who have received ≥2 prior regimens including bortezomib and an immunomodulatory drug...
November 21, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27881643/inclusion-body-fusion-of-human-parainfluenza-virus-type-3-regulated-by-acetylated-%C3%AE-tubulin-enhances-viral-replication
#6
Shengwei Zhang, Yanliang Jiang, Qi Cheng, Zhong Yi, Yali Qin, Mingzhou Chen
: Viral inclusion bodies (IBs) or replication factories are unique structures generated by viral proteins together with some cellular proteins as a platform for efficient viral replication, but little is known about the mechanism underlying IB formation and fusion. Our previous study demonstrated that the interaction between the nucleoprotein (N) and phosphoprotein (P) of human parainfluenza virus type 3 (HPIV3), an enveloped virus of great medical impact, can form IBs. In this study, we found that small IBs can fuse with each other to form large IBs that enhance viral replication...
November 23, 2016: Journal of Virology
https://www.readbyqxmd.com/read/27827303/an-hdac6-inhibitor-confers-protection-and-selectively-inhibits-b-cell-infiltration-in-dss-induced-colitis-in-mice
#7
Anh Do, Robert C Reid, Rink-Jan Lohman, Matthew J Sweet, David P Fairlie, Abishek Iyer
Small molecule histone deacetylase (HDAC) inhibitors with anti-inflammatory activity may be candidates for targeting intestinal inflammatory pathways in inflammatory bowel disease (IBD). This study investigated whether treatment with a potent HDAC6 inhibitor, BML-281, could protect against colonic inflammation and prevent inflammatory cell infiltration into the colon to drive disease pathology in a mouse model of acute DSS-colitis. Control and acute DSS-colitis mice were treated with BML-281 (1mg/kg/day s.c...
November 8, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27816334/pilot-phenotype-and-natural-history-study-of-hereditary-neuropathies-caused-by-mutations-in-the-hspb1-gene
#8
Alexander M Rossor, Jasper M Morrow, James M Polke, Sinead M Murphy, Henry Houlden, Matilde Laura, Hadi Manji, Julian Blake, Mary M Reilly
Mutations in HSPB1 are one of the commonest causes of distal Hereditary Motor Neuropathy (dHMN). Transgenic mouse models of the disease have identified HDAC6 inhibitors as promising treatments for the condition paving the way for human trials. A detailed phenotype and natural history study of HSPB1 neuropathy is therefore required in order to inform the duration and outcome measures of any future trials. Clinical and neurophysiological data and lower limb muscle MRI were collected both prospectively and retrospectively from patients with mutations in HSPB1...
October 8, 2016: Neuromuscular Disorders: NMD
https://www.readbyqxmd.com/read/27809521/largazole-analogues-embodying-radical-changes-in-the-depsipeptide-ring-development-of-a-more-selective-and-highly-potent-analogue
#9
Jehad Almaliti, Ayad A Al-Hamashi, Ahmed T Negmeldin, Christin L Hanigan, Lalith Perera, Mary Kay H Pflum, Robert A Casero, L M Viranga Tillekeratne
A number of analogues of the marine-derived histone deacetylase inhibitor largazole incorporating major structural changes in the depsipeptide ring were synthesized. Replacing the thiazole-thiazoline fragment of largazole with a bipyridine group gave analogue 7 with potent cell growth inhibitory activity and an activity profile similar to that of largazole, suggesting that conformational change accompanying switching hybridization from sp3 to sp2at C-7 is well tolerated. Analogue 7 was more class I selective compared to largazole, with at least 464-fold selectivity for class I HDAC proteins over class II HDAC6 compared to a 22-fold selectivity observed with largazole...
November 3, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27807597/analysis-of-the-interplay-between-all-trans-retinoic-acid-and-histone-deacetylase-inhibitors-in-leukemic-cells
#10
Katrin Noack, Nisintha Mahendrarajah, Dorle Hennig, Luisa Schmidt, Florian Grebien, Dagmar Hildebrand, Markus Christmann, Bernd Kaina, Andreas Sellmer, Siavosh Mahboobi, Katharina Kubatzky, Thorsten Heinzel, Oliver H Krämer
The treatment of acute promyelocytic leukemia (APL) with all-trans retinoic acid (ATRA) induces granulocytic differentiation. This process renders APL cells resistant to cytotoxic chemotherapies. Epigenetic regulators of the histone deacetylases (HDACs) family, which comprise four classes (I-IV), critically control the development and progression of APL. We set out to clarify the parameters that determine the interaction between ATRA and histone deacetylase inhibitors (HDACi). Our assays included drugs against class I HDACs (MS-275, VPA, and FK228), pan-HDACi (LBH589, SAHA), and the novel HDAC6-selective compound Marbostat-100...
November 2, 2016: Archives of Toxicology
https://www.readbyqxmd.com/read/27807097/ricolinostat-may-enhance-lenalidomide-and-dexamethasone-efficacy
#11
(no author information available yet)
The HDAC6 inhibitor ricolinostat was well tolerated in combination therapy for multiple myeloma.
November 2016: Cancer Discovery
https://www.readbyqxmd.com/read/27799547/discovery-of-selective-small-molecule-hdac6-inhibitor-for-overcoming-proteasome-inhibitor-resistance-in-multiple-myeloma
#12
Teru Hideshima, Jun Qi, Ronald M Paranal, Weiping Tang, Edward Greenberg, Nathan West, Meaghan E Colling, Guillermina Estiu, Ralph Mazitschek, Jennifer A Perry, Hiroto Ohguchi, Francesca Cottini, Naoya Mimura, Güllü Görgün, Yu-Tzu Tai, Paul G Richardson, Ruben D Carrasco, Olaf Wiest, Stuart L Schreiber, Kenneth C Anderson, James E Bradner
Multiple myeloma (MM) has proven clinically susceptible to modulation of pathways of protein homeostasis. Blockade of proteasomal degradation of polyubiquitinated misfolded proteins by the proteasome inhibitor bortezomib (BTZ) achieves responses and prolongs survival in MM, but long-term treatment with BTZ leads to drug-resistant relapse in most patients. In a proof-of-concept study, we previously demonstrated that blocking aggresomal breakdown of polyubiquitinated misfolded proteins with the histone deacetylase 6 (HDAC6) inhibitor tubacin enhances BTZ-induced cytotoxicity in MM cells in vitro...
November 15, 2016: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/27783058/ubiquitin-in-influenza-virus-entry-and-innate-immunity
#13
REVIEW
Alina Rudnicka, Yohei Yamauchi
Viruses are obligatory cellular parasites. Their mission is to enter a host cell, to transfer the viral genome, and to replicate progeny whilst diverting cellular immunity. The role of ubiquitin is to regulate fundamental cellular processes such as endocytosis, protein degradation, and immune signaling. Many viruses including influenza A virus (IAV) usurp ubiquitination and ubiquitin-like modifications to establish infection. In this focused review, we discuss how ubiquitin and unanchored ubiquitin regulate IAV host cell entry, and how histone deacetylase 6 (HDAC6), a cytoplasmic deacetylase with ubiquitin-binding activity, mediates IAV capsid uncoating...
October 24, 2016: Viruses
https://www.readbyqxmd.com/read/27769671/synthesis-and-investigation-of-novel-6-1-2-3-triazol-4-yl-4-aminoquinazolin-derivatives-possessing-hydroxamic-acid-moiety-for-cancer-therapy
#14
Chao Ding, Shaopeng Chen, Cunlong Zhang, Guangnan Hu, Wei Zhang, Lulu Li, Yu Zong Chen, Chunyan Tan, Yuyang Jiang
By merging the critical pharmacophore of EGFR/HER2 and HDAC inhibitors into one compound, a novel series of EGFR, HER-2, and HDAC multitarget inhibitors were synthesized. Compounds 9a-l contained 4-anilinoquinazolines with C-6 triazole-linked long alkyl chains of hydroxamic acid and displayed excellent inhibition against these enzymes (compound 9d exhibited the best inhibitory potency on wild-type EGFR, HDAC1, and HDAC6 with IC50 values 0.12nM, 0.72nM and 3.2nM individually). Furthermore, compounds 9b and 9d potently inhibited proliferation of five human cancer cell lines (with IC50 values between 0...
October 10, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27761834/how-to-distinguish-between-the-activity-of-hdac1-3-and-hdac6-with-western-blot
#15
Mandy Beyer, Nicole Kiweler, Siavosh Mahboobi, Oliver H Krämer
Histone deacetylases (HDACs) catalyze the deacetylation of lysine residues in their target proteins. This biochemical modification can have profound effects on the functions of these proteins and a dysregulation of HDAC activity contributes to severe diseases, including neoplastic transformation. In the following chapter, we present a strategy that allows to distinguish between the inhibition of the class I HDACs HDAC1, 2, and 3 and of the class IIb HDAC HDAC6. This method is based on Western blot and relies on the detection of hyperacetylated substrates of class I or class IIb HDACs in lysates from cells that were treated with histone deacetylase inhibitors (HDACi)...
2017: Methods in Molecular Biology
https://www.readbyqxmd.com/read/27759399/metal-free-direct-amidation-of-naphthoquinones-using-hydroxamic-acids-as-an-amide-source-application-in-the-synthesis-of-an-hdac6-inhibitor
#16
Cheng Zhang, C James Chou
A novel synthetic approach to amidoquinones by the reaction of naphthoquinones with hydroxamic acids under basic conditions was developed. The reaction is mild and operationally simple, and it affords high yields of amidoquinones. With this new method, a novel, very strong HDAC6 inhibitor, which showed high toxicity to AML cells, was successfully synthesized.
October 19, 2016: Organic Letters
https://www.readbyqxmd.com/read/27754697/hematopoietic-pbx-interaction-protein-promotes-breast-cancer-sensitivity-to-paclitaxel-through-a-microtubule-dependent-mechanism
#17
Bing Yu, Xiaoxuan Tian, Lin Zhang, Rui Feng
AIMS: Recently, microtubule-binding proteins (MBPs) have been implicated in modulation of paclitaxel sensitivity in many cancers, highlighting their potential as biomarkers predictive of treatment outcomes and as therapeutic targets that can be pharmacologically manipulated. This study is aimed to determine the impact of the MBP hematopoietic PBX-interaction protein (HPIP) on breast cancer cell sensitivity to paclitaxel. RESULTS: In this study, we show that breast cancer cells (MCF-7 and MDA-MB-231) overexpressing HPIP were more sensitive to paclitaxel treatment as evaluated by MTT assay, exhibiting a significant reduction in IC50 of paclitaxel compared with the control...
October 18, 2016: DNA and Cell Biology
https://www.readbyqxmd.com/read/27739328/mc1568-inhibits-hdac6-8-activity-and-influenza-a-virus-replication-in-lung-epithelial-cells-role-of-hsp90-acetylation
#18
Simona Panella, Maria Elena Marcocci, Ignacio Celestino, Sergio Valente, Clemens Zwergel, Domenica Donatella Li Puma, Lucia Nencioni, Antonello Mai, Anna Teresa Palamara, Giovanna Simonetti
AIM: Histone deacetylases (HDACs) regulate the life-cycle of several viruses. We investigated the ability of different HDAC-inhibitors, to interfere with influenza virus A/Puerto Rico/8/34/H1N1 (PR8 virus) replication in Madin-Darby canine kidney and NCI cells. RESULTS: 3-(5-(3-Fluorophenyl)-3-oxoprop-1-en-1-yl)-1-methyl-1H-pyrrol-2-yl)-N-hydroxyacrylamide (MC1568) inhibited HDAC6/8 activity and PR8 virus replication, with decreased expression of viral proteins and their mRNAs...
October 14, 2016: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/27737934/rescue-of-camdi-deletion-induced-delayed-radial-migration-and-psychiatric-behaviors-by-hdac6-inhibitor
#19
Toshifumi Fukuda, Shun Nagashima, Takaya Abe, Hiroshi Kiyonari, Ryoko Inatome, Shigeru Yanagi
The DISC1-interacting protein CAMDI has been suggested to promote radial migration through centrosome regulation. However, its physiological relevance is unclear. Here, we report the generation and characterization of CAMDI-deficient mice. CAMDI-deficient mice exhibit delayed radial migration with aberrant neural circuit formation and psychiatric behaviors including hyperactivity, repetitive behavior, and social abnormality typically observed in autism spectrum disorder patients. Analyses of direct targets of CAMDI identify HDAC6 whose α-tubulin deacetylase activity is inhibited by CAMDI at the centrosome...
October 13, 2016: EMBO Reports
https://www.readbyqxmd.com/read/27733371/tlr-adaptor-protein-myd88-mediates-sensitivity-to-hdac-inhibitors-via-a-cytokine-dependent-mechanism
#20
Maria New, Semira Sheikh, Mina Bekheet, Heidi Olzscha, Marie-Laetitia Thezenas, Matthew A Care, Susan Fotheringham, Reuben M Tooze, Benedikt M Kessler, Nicholas B La Thangue
Histone deacetylase (HDAC) inhibitors have proven useful therapeutic agents for certain haematological cancers. However, HDAC inhibition causes diverse cellular outcomes, and identification of cancer-relevant pathways within these outcomes remains unresolved. In this study, we utilized an unbiased loss-of-function screen and identified the Toll-like receptor (TLR) adaptor protein MYD88 as a key regulator of the anti-proliferative effects of HDAC inhibition. High expression of MYD88 exhibited increased sensitivity to HDAC inhibitors; conversely, low expression coincided with reduced sensitivity...
October 12, 2016: Cancer Research
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