Journal ArticleDOI
Histone deacetylase inhibitors.
TLDR
Design of a second generation ofHDACs was based upon data affording potent HDACs such as LAQ824 and PDX101 currently under phase I clinical trials, and two of them, MS-275 and CI-994, have reached phase II and I clinical Trials, respectively.About:
This article is published in European Journal of Medicinal Chemistry.The article was published on 2005-01-01. It has received 819 citations till now. The article focuses on the topics: Histone deacetylase & Phenylbutyrate.read more
Citations
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Journal ArticleDOI
Identification of novel small-molecule histone deacetylase inhibitors by medium-throughput screening using a fluorigenic assay.
Dennis Wegener,Christian Hildmann,Daniel Riester,Andreas Schober,Franz-Josef Meyer-Almes,Hedwig E. Deubzer,Ina Oehme,Olaf Witt,Siegmund Lang,Martina Jaensch,Vadim Makarov,Corinna Lange,Benedikt Busse,Andreas Schwienhorst +13 more
TL;DR: Screening of a compound library using FB188 HDAH as model enzyme identified several promising new lead structures for further development of novel HDAC inhibitors, including potent inhibitors of eukaryotic HDACs.
Journal ArticleDOI
Effects of the histone deacetylase inhibitor valproic acid on human pericytes in vitro.
Jakob Karén,Alejandro Rodriguez,Tomas Friman,Lennart Dencker,Christian Sundberg,Christian Sundberg,Birger Scholz +6 more
TL;DR: The present in vitro study demonstrates that VPA influences several aspects of microvascular pericyte biology and suggests an alternative mechanism by which HDAC inhibition affects blood vessels.
Journal ArticleDOI
Energy-optimised pharmacophore approach to identify potential hotspots during inhibition of Class II HDAC isoforms.
TL;DR: A computational approach that combines in silico docking and energy-optimised pharmacophore mapping of 18 known HDAC inhibitors and has identified structural variations that regulate their interactions against the six Class II HDAC enzymes considered for the study establishes that inhibitors possessing higher number of aromatic rings in different structural regions might function as potent inhibitors, while inhibitors with scarce ring structures might point to compromised potency.
Journal ArticleDOI
Anti-tumor effect in human lung cancer by a combination treatment of novel histone deacetylase inhibitors: SL142 or SL325 and retinoic acids.
Shaoteng Han,Shaoteng Han,Takuya Fukazawa,Tomoki Yamatsuji,Junji Matsuoka,Hiroyuki Miyachi,Yutaka Maeda,Mary L. Durbin,Yoshio Naomoto +8 more
TL;DR: The results suggest that the combination treatment of SL142 or SL325 with retinoic acids exerts significant anti-tumor activity and is a promising therapeutic candidate to treat human lung cancer.
Journal ArticleDOI
Interference of CREB‐dependent transcriptional activation by expanded polyglutamine stretches – augmentation of transcriptional activation as a potential therapeutic strategy for polyglutamine diseases
Mitsuteru Shimohata,Takayoshi Shimohata,Shuichi Igarashi,Satoshi Naruse,Shoji Tsuji,Shoji Tsuji +5 more
TL;DR: It is suggested that the interference of CREB‐dependent transcriptional activation by expanded polyglutamine stretches is involved in the pathogenetic mechanisms underlying neurodegeneration, and that the augmentation ofCREB‐ dependent transcriptionalactivation is a potential strategy in treating polyglUTamine diseases.
References
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Journal ArticleDOI
Crystal structure of the nucleosome core particle at 2.8 Å resolution
TL;DR: The X-ray crystal structure of the nucleosome core particle of chromatin shows in atomic detail how the histone protein octamer is assembled and how 146 base pairs of DNA are organized into a superhelix around it.
Journal ArticleDOI
hSIR2SIRT1 Functions as an NAD-Dependent p53 Deacetylase
Homayoun Vaziri,Scott K. Dessain,Scott K. Dessain,Elinor Ng Eaton,Shin-ichiro Imai,Roy A. Frye,Tej K. Pandita,Leonard Guarente,Robert A. Weinberg +8 more
TL;DR: It is proposed that hSir2, the human homolog of the S. cerevisiae Sir2 protein known to be involved in cell aging and in the response to DNA damage, binds and deacetylates the p53 protein with a specificity for its C-terminal Lys382 residue.
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Negative Control of p53 by Sir2α Promotes Cell Survival under Stress
Jianyuan Luo,Anatoly Y. Nikolaev,Shin-ichiro Imai,Delin Chen,Fei Su,Ariel L. Shiloh,Leonard Guarente,Wei Gu +7 more
TL;DR: It is shown that mammalian Sir2alpha physically interacts with p53 and attenuates p53-mediated functions, and Nicotinamide inhibits an NAD-dependent p53 deacetylation induced by Sir2 alpha, and also enhances the p53 acetylation levels in vivo.
Journal ArticleDOI
Potent and specific inhibition of mammalian histone deacetylase both in vivo and in vitro by trichostatin A.
TL;DR: Results clearly indicate that TSA is a potent and specific inhibitor of the histone deacetylase and that the in vivo effect of TSA on cell proliferation and differentiation can be attributed to the inhibition of the enzyme.
Journal ArticleDOI
Valproic acid defines a novel class of HDAC inhibitors inducing differentiation of transformed cells
Martin Göttlicher,Saverio Minucci,Ping Zhu,Oliver H. Krämer,Annemarie Schimpf,Sabrina Giavara,Jonathan P. Sleeman,Francesco Lo Coco,Clara Nervi,Pier Giuseppe Pelicci,Thorsten Heinzel +10 more
TL;DR: Valproic acid induces differentiation of carcinoma cells, transformed hematopoietic progenitor cells and leukemic blasts from acute myeloid leukemia patients, and tumor growth and metastasis formation are significantly reduced in animal experiments, suggesting that it might serve as an effective drug for cancer therapy.