Class I HDAC imaging using [<sup>3</sup>H]CI-994 autoradiography

Wang, Yajie; Zhang, Yanling; Hennig, Krista M.; Gale, Jennifer; Hong, Yi-Jia; Cha, Anna; Riley, Misha M.; Wagner, Florence F.; Haggarty, Stephen J.; Holson, Edward B.; Hooker, Jacob M.

doi:10.4161/epi.25202

Cited by 27 publications

(24 citation statements)

References 39 publications

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“…Good correlation between in vitro and in vivo derived kinetic binding parameters for HDACs 1, 2 and 3 has been demonstrated using brain tissue autoradiography. 20 As described in a previous report, 16 this simulation helps define HDAC isoform selectivity in the dynamic in vivo context.…”

Section: Surface Binding Domainmentioning

confidence: 95%

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors

Wagner

Weïwer

Steinbacher³

et al. 2016

Bioorganic & Medicinal Chemistry

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Section: Surface Binding Domainmentioning

confidence: 95%

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors

Wagner

Weïwer

Steinbacher³

et al. 2016

Bioorganic & Medicinal Chemistry

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“…In a different study, investigators used phosphor imaging and re-calibrated commercial standards to determine the concentration of tritium-labeled Cl-994 ( 3 H-Cl-994), which is a benzamide that inhibits class I histone deacetylase (HDAC) (Wang et al 2013). The goal of this study was to use 3 H-Cl-994 as a probe for the ex vivo binding to, and thus localization of, HDAC in the rat brain.…”

Section: Receptor Autoradiography Studiesmentioning

confidence: 99%

Autoradiography techniques and quantification of drug distribution

Solon¹

2015

Cell Tissue Res

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The use of radiolabeled drug compounds offers the most efficient way to quantify the amount of drug and/or drug-derived metabolites in biological samples. Autoradiography is a technique using X- ray film, phosphor imaging plates, beta imaging systems, or photo-nuclear emulsion to visualize molecules or fragments of molecules that have been radioactively labeled, and it has been used to quantify and localize drugs in tissues and cells for decades. Quantitative whole-body autoradiography or autoradioluminography (QWBA) using phosphor imaging technology has revolutionized the conduct of drug distribution studies by providing high resolution images of the spatial distribution and matching tissue concentrations of drug-related radioactivity throughout the body of laboratory animals. This provides tissue-specific pharmacokinetic (PK) compartmental analysis which has been useful in toxicology, pharmacology, and drug disposition/patterns, and to predict human exposure to drugs and metabolites, and also radioactivity, when a human radiolabeled drug study is necessary. Microautoradiography (MARG) is another autoradiographic technique that qualitatively resolves the localization of radiolabeled compounds to the cellular level in a histological preparation. There are several examples in the literature of investigators attempting to obtain drug concentration data from MARG samples; however, there are technical issues which make that problematic. These issues will be discussed. This review will present a synopsis of both techniques and examples of how they have been used for drug research in recent years.

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“…To date, however, the mechanistic insights from studies correlating peripheral epigenetic changes with brain imaging are limited. The development of positron emission tomography ligands based on compounds targeting epigenetic mechanisms, such as, for example, HDAC1 inhibitors, may also further our understanding of the contribution of these mechanisms in stress-related psychiatric disorders (Wang et al, 2013).…”

Section: Epigenetic Modifications As a Potential Target Of Psychiatrimentioning

confidence: 99%

Epigenetics of Stress-Related Psychiatric Disorders and Gene × Environment Interactions

Klengel

Binder

2015

Neuron

283

184

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A deeper understanding of the pathomechanisms leading to stress-related psychiatric disorders is important for the development of more efficient preventive and therapeutic strategies. Epidemiological studies indicate a combined contribution of genetic and environmental factors in the risk for disease. The environment, particularly early life severe stress or trauma, can lead to lifelong molecular changes in the form of epigenetic modifications that can set the organism off on trajectories to health or disease. Epigenetic modifications are capable of shaping and storing the molecular response of a cell to its environment as a function of genetic predisposition. This provides a potential mechanism for gene-environment interactions. Here, we review epigenetic mechanisms associated with the response to stress and trauma exposure and the development of stress-related psychiatric disorders. We also look at how they may contribute to our understanding of the combined effects of genetic and environmental factors in shaping disease risk.

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Class I HDAC imaging using [³H]CI-994 autoradiography

Cited by 27 publications

References 39 publications

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors

Autoradiography techniques and quantification of drug distribution

Epigenetics of Stress-Related Psychiatric Disorders and Gene × Environment Interactions

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Class I HDAC imaging using [3H]CI-994 autoradiography

Cited by 27 publications

References 39 publications

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors

Kinetic and structural insights into the binding of histone deacetylase 1 and 2 (HDAC1, 2) inhibitors

Autoradiography techniques and quantification of drug distribution

Epigenetics of Stress-Related Psychiatric Disorders and Gene × Environment Interactions

Contact Info

Product

Resources

About

Class I HDAC imaging using [³H]CI-994 autoradiography