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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Patent
Combination therapy using an HDAC inhibitor, carboplatin and paclitaxel for treating ovarian cancer
Henri Lichenstein,Jeffers Mike,Xiaozhang Qian,Maxwell Sehested,Kamille Dumong Petersen,James Ritchie +5 more
TL;DR: In this paper, a method for treating cancer such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount OR dose of carboplatin/paclitaxel, wherein the first and second amounts or doses together comprise a therapeutically effective amount.
Patent
Procedes et compositions pour favoriser la croissance neuronale et le traitement de l'asociabilite et des troubles affectifs
Ciaran Regan,Andrew G. Foley +1 more
TL;DR: In this paper, an invention concerne l'utilisation d'au moins un inhibiteur de la Histone Deacetylase (HDAC) for the fabrication of un medicament devant favoriser la croissance neuronale.
Síntesis y evaluación de nuevos inhibidores de las HDAC
Mavys Tabraue Chavez,S. Panadero-Fajardo,M. Arévalo-Ruiz,Jose Francisco Dominguez Seglar,José Antonio Gómez Vidal +4 more
Patent
Combination therapy using an HDAC inhibitor and erlotinib for treating lung cancer
Henri Lichenstein,Jeffers Mike,Xiaozhang Qian,Maxwell Sehested,Kamille Dumong Petersen,James Ritchie +5 more
TL;DR: In this article, a method for treating cancer such as lung cancer, multiple myeloma, lymphoma, and epithelial ovarian cancer, comprising the administration to a patient in need thereof a first amount or dose of a histone deacetylase (HDAC) inhibitor, such as PXD-101, and a second amount OR dose of erlotinib, wherein the first and second amounts or doses together comprise a therapeutically effective amount.
Dissertation
Conception et synthèse d'inhibiteurs de métalloprotéases et de cibles à ligand acide
TL;DR: In this article, a set of nouvelles voies d'obtention de produits acides potentiellement ligand du zinc dans le cadre d'un projet plus vaste mene au laboratoire sur de two cibles biologiques appartenant a la famille des metalloproteases a zinc, l'aggrecanase and l'enzyme de conversion de l'angiotensine de type 2.
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.
Journal ArticleDOI
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.