Concept

Reuptake inhibitor

Related publications (36)

Crosslinking Allosteric Sites on the Nucleosome

Paul Joseph Dyson, Lucinda Kate Batchelor, Thibaud Edouard Alistair von Erlach

Targeting defined histone protein sites in chromatin is an emerging therapeutic approach that can potentially be enhanced by allosteric effects within the nucleosome. Here we characterized a novel hetero-bimetallic compound with a design based on a nucleos ...

WILEY-V C H VERLAG GMBH2019

ER-to-lysosome-associated degradation of proteasome-resistant ATZ polymers occurs via receptor-mediated vesicular transport

Maurizio Molinari, Paolo Paganetti

Maintenance of cellular proteostasis relies on efficient clearance of defective gene products. For misfolded secretory proteins, this involves dislocation from the endoplasmic reticulum (ER) into the cytosol followed by proteasomal degradation. However, po ...

2018

Organometallic Glutathione S-Transferase Inhibitors

Paul Joseph Dyson, Rosario Scopelliti, Mylène Soudani, Emilia Paunescu

A new family of organometallic p-cymene ruthenium(II) and osmium(II) complexes conjugated to ethacrynic acid, a glutathione transferase (GST) inhibitor, is reported. The ethacrynic acid moiety (either one or two) is tethered to the arene ruthenium(II) and ...

2017

Neuronal Depolarization Drives Increased Dopamine Synaptic Vesicle Loading via VGLUT

Brian Donal McCabe

The ability of presynaptic dopamine terminals to tune neurotransmitter release to meet the demands of neuronal activity is critical to neurotransmission. Although vesicle content has been assumed to be static, in vitro data increasingly suggest that cell a ...

Cell Press2017

Discovery of a Selective Aurora A Kinase Inhibitor by Virtual Screening

Pierre Gönczy, Maria Josefina Marcaida Lopez, Sachin Kotak, Jean-Louis Reymond

Here we report the discovery of a selective inhibitor of Aurora A, a key regulator of cell division and potential anticancer target. We used the atom category extended ligand overlap score (xLOS), a 3D ligand-based virtual screening method recently develop ...

2016

A Gating Mechanism of the Serotonin 5-HT3 Receptor

Horst Vogel, Shuguang Yuan

Our recently solved high-resolution structure of the serotonin 5-HT3 receptor (5-HT3R) delivered the first detailed structural insights for a mammalian pentameric ligand-gated ion channel. Based on this structure, we here performed a total of 2.8-μs all-at ...

Cell Press2016

Development and application of the adverse outcome pathway framework for understanding and predicting chronic toxicity: II. A focus on growth impairment in fish

Kristin Schirmer

Adverse outcome pathways (AOPs) organize knowledge on the progression of toxicity through levels of biological organization. By determining the linkages between toxicity events at different levels, AOPs lay the foundation for mechanism-based alternative te ...

Pergamon-Elsevier Science Ltd2015

Peripubertal stress-induced behavioral changes are associated with altered expression of genes involved in excitation and inhibition in the amygdala

Maria del Carmen Sandi Perez, Stamatina Tzanoulinou, Orbicia Riccio Wicht

Early-life stress is a critical risk factor for developing psychopathological alterations later in life. This early adverse environment has been modeled in rats by exposure to stress during the peripubertal period-that is, corresponding to childhood and pu ...

Nature Publishing Group2014

Vesicular glutamate transporter-3 in the rodent brain: Vesicular colocalization with vesicular γ-aminobutyric acid transporter

Mats Julius Stensrud

Vesicular glutamate transporters (VGLUT1–3) carry glutamate into synaptic vesicles. VGLUT3 has been reported to be localized in nonglutamatergic neuronal populations in the brain. However, detailed subcellular localization of VGLUT3 has not been shown. In ...

2013

Overexpression of parkin in the rat nigrostriatal dopamine system protects against methamphetamine neurotoxicity

Bernard Schneider

Methamphetamine (METH) is a central nervous system psychostimulant with a high potential for abuse. At high doses, METH causes a selective degeneration of dopaminergic terminals in the striatum, sparing other striatal terminals and cell bodies. We previous ...

Elsevier2013

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