2006
DOI: 10.1158/1535-7163.mct-05-0494
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Detection of histone deacetylase inhibition by noninvasive magnetic resonance spectroscopy

Abstract: Histone deacetylase (HDAC) inhibitors are new and promising antineoplastic agents. Current methods for monitoring early response rely on invasive biopsies or indirect blood-derived markers. Our goal was to develop a magnetic resonance spectroscopy (MRS) -based method to detect HDAC inhibition. The fluorinated lysine derivative Boc-Lys-(Tfa)-OH (BLT) was investigated as a 19 F MRS molecular marker of HDAC activity together with 31 P MRS of endogenous metabolites. In silico modeling of the BLT-HDAC interaction a… Show more

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Cited by 32 publications
(36 citation statements)
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“…Significant increases in PC were seen in HT29 cells after LAQ824 ( Figure 1A) and SAHA treatment . A rise in PC was also observed in PC3 prostate cancer cells after treatment with an analogue of SAHA (Sankaranarayanapillai et al, 2006).…”
Section: Mrs-detectable Pd Biomarkers Of Targeted Cancer Therapiesmentioning
confidence: 78%
“…Significant increases in PC were seen in HT29 cells after LAQ824 ( Figure 1A) and SAHA treatment . A rise in PC was also observed in PC3 prostate cancer cells after treatment with an analogue of SAHA (Sankaranarayanapillai et al, 2006).…”
Section: Mrs-detectable Pd Biomarkers Of Targeted Cancer Therapiesmentioning
confidence: 78%
“…In most cases, a therapeutic effect is associated with a decrease in tCho or PCho. However, the opposite effect is seen with histone deacetylase inhibitors, which repeatedly have been shown to increase tCho concentrations in vivo and ex vivo [141,142]. GPC concentrations may both increase and decrease following drug treatment, complicating the overall picture.…”
Section: Phospholipid Metabolism In Evaluation Of Response To Therapymentioning
confidence: 99%
“…Increased PC and total choline levels were found in SAHA-treated cell extracts, and these changes were inversely correlated with resulting growth inhibition, cell-cycle arrest and apoptosis, and HDAC activity. 96 P-NMR spectra of LAQ824-treated tumor extracts when compared with controls. An increase in PC was also found in LAQ-treated HT29 cell extracts.…”
Section: Hdac Inhibitorsmentioning
confidence: 99%