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Antoine Italiano, Jean-Charles Soria, Maud Toulmonde, Jean-Marie Michot, Carlo Lucchesi, Andrea Varga, Jean-Michel Coindre, Stephen J Blakemore, Alicia Clawson, Benjamin Suttle, Alice A McDonald, Mark Woodruff, Scott Ribich, Eric Hedrick, Heike Keilhack, Blythe Thomson, Takashi Owa, Robert A Copeland, Peter T C Ho, Vincent Ribrag
BACKGROUND: Activating enhancer of zeste homolog 2 (EZH2) mutations or aberrations of the switch/sucrose non-fermentable (SWI/SNF) complex (eg, mutations or deletions of the subunits INI1 or SMARCA4) can lead to aberrant histone methylation, oncogenic transformation, and a proliferative dependency on EZH2 activity. In this first-in-human study, we aimed to investigate the safety, clinical activity, pharmacokinetics, and pharmacodynamics of tazemetostat, a first-in-class selective inhibitor of EZH2...
May 2018: Lancet Oncology
Evan J Kyzar, Huaibo Zhang, Amul J Sakharkar, Subhash C Pandey
Alcohol exposure in adolescence is an important risk factor for the development of alcoholism in adulthood. Epigenetic processes are implicated in the persistence of adolescent alcohol exposure-related changes, specifically in the amygdala. We investigated the role of histone methylation mechanisms in the persistent effects of adolescent intermittent ethanol (AIE) exposure in adulthood. Adolescent rats were exposed to 2 g/kg ethanol (2 days on/off) or intermittent n-saline (AIS) during postnatal days (PND) 28-41 and used for behavioral and epigenetic studies...
September 2017: Addiction Biology
Lorna H Mitchell, P Ann Boriack-Sjodin, Sherri Smith, Michael Thomenius, Nathalie Rioux, Michael Munchhof, James E Mills, Christine Klaus, Jennifer Totman, Thomas V Riera, Alejandra Raimondi, Suzanne L Jacques, Kip West, Megan Foley, Nigel J Waters, Kevin W Kuntz, Tim J Wigle, Margaret Porter Scott, Robert A Copeland, Jesse J Smith, Richard Chesworth
SMYD3 has been implicated in a range of cancers; however, until now no potent selective small molecule inhibitors have been available for target validation studies. A novel oxindole series of SMYD3 inhibitors was identified through screening of the Epizyme proprietary histone methyltransferase-biased library. Potency optimization afforded two tool compounds, sulfonamide EPZ031686 and sulfamide EPZ030456, with cellular potency at a level sufficient to probe the in vitro biology of SMYD3 inhibition. EPZ031686 shows good bioavailability following oral dosing in mice making it a suitable tool for potential in vivo target validation studies...
February 11, 2016: ACS Medicinal Chemistry Letters
Alexandra Flemming
No abstract text is available yet for this article.
July 2012: Nature Reviews. Drug Discovery
Alice McCarthy
No abstract text is available yet for this article.
April 22, 2011: Chemistry & Biology
Karen Vickery, Aniko Pajkos, Yvonne Cossart
BACKGROUND: Biofilm consisting of bacteria enclosed in a matrix of exopolysaccharide (EPS) forms on many medical devices such as catheters and implants. Nosocomial infection is, thus, a newly recognized scenario of biofilm development. Biofilm removal by physical methods such as ultrasound and mechanical cleaning is reasonably effective but difficult to supervise in practice. Chemical methods are often ineffective because of biofilm resistance to biocides. In this study, we compared the efficiency of different detergents used in endoscope reprocessing...
May 2004: American Journal of Infection Control
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