ArticleNeoplasia (New York, N.Y.)2008
Noninvasive magnetic resonance spectroscopic pharmacodynamic markers of a novel histone deacetylase inhibitor, LAQ824, in human colon carcinoma cells and xenografts.
Article in Neoplasia (New York, N.Y.), 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 48 citations in OpenAlex.
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- Metabolomic Profiling Reveals Cellular Reprogramming of B-Cell Lymphoma by a Lysine Deacetylase Inhibitor through the Choline Pathway.EBioMedicine · 2018Article
- Response Detection of Castrate-Resistant Prostate Cancer to Clinically Utilised and Novel Treatments by Monitoring Phospholipid Metabolism.BioMed research international · 2017Article
- The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate-Lactate Exchange in BRAF-Mutant Human Melanoma Cells.Molecular cancer therapeutics · 2016Article
- Choline kinase alpha-Putting the ChoK-hold on tumor metabolism.Progress in lipid research · 2016Review
- Metabolic Effects of Known and Novel HDAC and SIRT Inhibitors in Glioblastomas Independently or Combined with Temozolomide.Metabolites · 2014Article
- High-field small animal magnetic resonance oncology studies.Physics in medicine and biology · 2014Review
- Metabolic biomarkers for response to PI3K inhibition in basal-like breast cancer.Breast cancer research : BCR · 2013Article
- Histone acetylation regulates intracellular pH.Molecular cell · 2013Article
- HDAC inhibition induces increased choline uptake and elevated phosphocholine levels in MCF7 breast cancer cells.PloS one · 2013Article
- Histone deacetylase inhibition increases levels of choline kinase α and phosphocholine facilitating noninvasive imaging in human cancers.Cancer research · 2012Article
- Metabolic consequences of treatment with AKT inhibitor perifosine in breast cancer cells.NMR in biomedicine · 2012Article
- Pharmacodynamic modelling of biomarker data in oncology.ISRN pharmacology · 2012Article
- Metabolic effects of signal transduction inhibition in cancer assessed by magnetic resonance spectroscopy.Molecular oncology · 2011Review
- Dinosaurs and ancient civilizations: reflections on the treatment of cancer.Neoplasia (New York, N.Y.) · 2010Article
- Modulation of melanoma cell phospholipid metabolism in response to heat shock protein 90 inhibition.Oncotarget · 2010Article
Corrections and comments
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Authors and funding
11 authors at 4 institutions in 3 countries.
Funding
Abstract
The aim of this work was to use phosphorus magnetic resonance spectroscopy ((31)P MRS) to investigate the pharmacodynamic effects of LAQ824, a histone deacetylase (HDAC) inhibitor. Human HT29 colon carcinoma cells were examined by (31)P MRS after treatment with LAQ824 and another HDAC inhibitor, suberoylanilide hydroxamic acid. HT29 xenografts and tumor extracts were also examined using (31)P MRS, pre- and post-LAQ824 treatment. Histone H3 acetylation was determined using Western blot analysis, and tumor microvessel density by immunohistochemical staining of CD31. Phosphocholine showed a significant increase in HT29 cells after treatment with LAQ824 and suberoylanilide hydroxamic acid. In vivo, the ratio of phosphomonoester/total phosphorus (TotP) signal was significantly increased in LAQ824-treated HT29 xenografts, and this ratio was inversely correlated with changes in tumor volume. Statistically significant decreases in intracellular pH, beta-nucleoside triphosphate (beta-NTP)/TotP, and beta-NTP/inorganic phosphate (Pi) and an increase in Pi/TotP were also seen in LAQ824-treated tumors. Tumor extracts showed many significant metabolic changes after LAQ824 treatment, in parallel with increased histone acetylation and decreased microvessel density. Treatment with LAQ824 resulted in altered phospholipid metabolism and compromised tumor bioenergetics. The phosphocholine and phosphomonoester increases may have the potential to act as pharmacodynamic markers for noninvasively monitoring tumor response after treatment with LAQ824 or other HDAC inhibitors.
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