ArticleBioorganic & medicinal chemistry letters2013
Radionuclide labeling and evaluation of candidate radioligands for PET imaging of histone deacetylase in the brain.
Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Who cites it
21 citing papers in PubMed, 34 citations in OpenAlex.
- Can Nuclear Imaging Detect Trained Immunity in Cardiovascular Disease?Arteriosclerosis, thrombosis, and vascular biology · 2026Review
- High-Contrast PET Imaging with [Journal of medicinal chemistry · 2023Article
- Introducing HDAC-Targeting Radiopharmaceuticals for Glioblastoma Imaging and Therapy.Pharmaceuticals (Basel, Switzerland) · 2023Review
- HDAC Inhibitors: Innovative Strategies for Their Design and Applications.Molecules (Basel, Switzerland) · 2022Review
- Unprotected peptide macrocyclization and stapling via a fluorine-thiol displacement reaction.Nature communications · 2022Article
- Design, synthesis, biochemical evaluation, radiolabeling and in vivo imaging with high affinity class-IIa histone deacetylase inhibitor for molecular imaging and targeted therapy.European journal of medicinal chemistry · 2022Article
- A Baboon Brain Atlas for Magnetic Resonance Imaging and Positron Emission Tomography Image Analysis.Frontiers in neuroanatomy · 2021Article
- Design, Synthesis, and Blood-Brain Barrier Transport Study of Pyrilamine Derivatives as Histone Deacetylase Inhibitors.ACS medicinal chemistry letters · 2018Article
- Advances in the Development of PET Ligands Targeting Histone Deacetylases for the Assessment of Neurodegenerative Diseases.Molecules (Basel, Switzerland) · 2018Review
- Article
- Evaluation of Fluorine-18-Labeled α1(I)-N-Telopeptide Analogs as Substrate-Based Radiotracers for PET Imaging of Melanoma-Associated Lysyl Oxidase.Frontiers in chemistry · 2018Article
- HDAC6 Brain Mapping with [ACS central science · 2017Article
- Using Protein-Confined Proximity To Determine Chemical Reactivity.Journal of the American Chemical Society · 2016Article
- Kinetic Analysis and Quantification of [¹¹C]Martinostat for in Vivo HDAC Imaging of the Brain.ACS chemical neuroscience · 2015Article
- Novel Histone Deacetylase Class IIa Selective Substrate Radiotracers for PET Imaging of Epigenetic Regulation in the Brain.PloS one · 2015Article
- A philosophy for CNS radiotracer design.Accounts of chemical research · 2014Review
- In vivo imaging of histone deacetylases (HDACs) in the central nervous system and major peripheral organs.Journal of medicinal chemistry · 2014Article
- Image-guided synthesis reveals potent blood-brain barrier permeable histone deacetylase inhibitors.ACS chemical neuroscience · 2014Article
- Epigenetics and nutritional environmental signals.Integrative and comparative biology · 2014Review
- Targeting histone deacetylase in lung cancer for early diagnosis: (18)F-FAHA PET/CT imaging of NNK-treated A/J mice model.American journal of nuclear medicine and molecular imaging · 2014Article
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 2 countries.
Funding
Abstract
Histone deacetylases (HDACs) regulate gene expression by inducing conformational changes in chromatin. Ever since the discovery of a naturally occurring HDAC inhibitor, trichostatin A (TSA) stimulated the recent development of suberoylanilide (SAHA, Zolinza®), HDAC has become an important molecular target for drug development. This has created the need to develop specific in vivo radioligands to study epigenetic regulation and HDAC engagement for drug development for diseases including cancer and psychiatric disorders. 6-([(18)F]Fluoroacetamido)-1-hexanoicanilide ([(18)F]FAHA) was recently developed as a HDAC substrate and shows moderate blood-brain barrier (BBB) permeability and specific signal (by metabolic trapping/or deacetylation) but rapid metabolism. Here, we report the radiosynthesis of two carbon-11 labeled candidate radiotracers (substrate- and inhibitor-based radioligand) for HDAC and their evaluation in non-human primate brain. PET studies showed very low brain uptake and rapid metabolism of both labeled compounds but revealed a surprising enhancement of brain penetration by F for H substitution when comparing one of these to [(18)F]FAHA. Further structural refinement is needed for the development of brain-penetrant, metabolically stable HDAC radiotracers and to understand the role of fluorine substitution on brain penetration.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.