A philosophy for CNS radiotracer design

GC Van de Bittner, EL Ricq… - Accounts of chemical …, 2014 - ACS Publications
Conspectus Decades after its discovery, positron emission tomography (PET) remains the
premier tool for imaging neurochemistry in living humans. Technological improvements in …

Introducing HDAC-targeting radiopharmaceuticals for glioblastoma imaging and therapy

L Everix, EN Seane, T Ebenhan, I Goethals, J Bolcaen - Pharmaceuticals, 2023 - mdpi.com
Despite recent advances in multimodality therapy for glioblastoma (GB) incorporating
surgery, radiotherapy, chemotherapy and targeted therapy, the overall prognosis remains …

PET neuroimaging reveals histone deacetylase dysregulation in schizophrenia

TM Gilbert, NR Zürcher, CJ Wu… - The Journal of …, 2019 - Am Soc Clin Investig
BACKGROUND. Patients with schizophrenia (SCZ) experience chronic cognitive deficits.
Histone deacetylases (HDACs) are enzymes that regulate cognitive circuitry; however, the …

Neuroepigenetic signatures of age and sex in the living human brain

TM Gilbert, NR Zürcher, MC Catanese… - Nature …, 2019 - nature.com
Age-and sex-related alterations in gene transcription have been demonstrated, however the
underlying mechanisms are unresolved. Neuroepigenetic pathways regulate gene …

HDAC 2 dysregulation in the nucleus basalis of Meynert during the progression of Alzheimer's disease

L Mahady, M Nadeem, M Malek‐Ahmadi… - Neuropathology and …, 2019 - Wiley Online Library
Aims Alzheimer's disease (AD) is characterized by degeneration of cholinergic basal
forebrain (CBF) neurons in the nucleus basalis of Meynert (nbM), which provides the major …

Frontal cortex epigenetic dysregulation during the progression of Alzheimer's disease

L Mahady, M Nadeem, M Malek-Ahmadi… - Journal of …, 2018 - content.iospress.com
Although the frontal cortex plays an important role in cognitive function and undergoes
neuronal dysfunction in Alzheimer's disease (AD), the factors driving these cellular …

Fluid and imaging biomarkers for Alzheimer's disease: Where we stand and where to head to

AD Henriques, AL Benedet, EF Camargos… - Experimental …, 2018 - Elsevier
There is increasing evidence that a number of potentially informative biomarkers for
Alzheimer disease (AD) can improve the accuracy of diagnosing this form of dementia …

Expression of HDAC2 but Not HDAC1 Transcript Is Reduced in Dorsolateral Prefrontal Cortex of Patients with Schizophrenia

FA Schroeder, TM Gilbert, N Feng… - ACS chemical …, 2017 - ACS Publications
Postmortem brain studies support dysregulated expression of the histone deacetylase
enzymes, HDAC1 and HDAC2, as a central feature in diseases including schizophrenia …

In vivo human brain expression of histone deacetylases in bipolar disorder

CEJ Tseng, TM Gilbert, MC Catanese… - Translational …, 2020 - nature.com
The etiology of bipolar disorder (BD) is unknown and the neurobiological underpinnings are
not fully understood. Both genetic and environmental factors contribute to the risk of BD …

Design, synthesis and biological evaluation of a series of CNS penetrant HDAC inhibitors structurally derived from amyloid-β probes

MA Choi, SY Park, HY Chae, Y Song, C Sharma… - Scientific Reports, 2019 - nature.com
To develop novel CNS penetrant HDAC inhibitors, a new series of HDAC inhibitors having
benzoheterocycle were designed, synthesized, and biologically evaluated. Among the …