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Concept

Inhibiteur de la recapture

Publications associées (19)

Powering the social brain: Mitochondria in social behaviour

Maria del Carmen Sandi Perez, Dogukan Hazar Ülgen, Silvie Rosalie Ruigrok

A central role of brain mitochondria in regulating and influencing social behaviour is emerging. In addition to its important roles as the "powerhouses" of the cell, mitochondria possess a plethora of cellular functions, such as regulating ion homeostasis, ...

2023

Dopamine Transporter, PhosphoSerine129 alpha-Synuclein and alpha-Synuclein Levels in Aged LRRK2 G2019S Knock-In and Knock-Out Mice

Salvatore Novello

The G2019S mutation in leucine rich-repeat kinase 2 (LRRK2) is a major cause of familial Parkinson's disease. We previously reported that G2019S knock-in mice manifest dopamine transporter dysfunction and phosphoSerine129 alpha-synuclein (pSer129 alpha-syn ...

MDPI2022

Highly Sensitive Detection of the Antidepressant Fluoxetine With an Extended Gate Field Effect Transistor

Mihai Adrian Ionescu, Shokoofeh Sheibani

Fluoxetine (FL) is one of the selective serotonin reuptake inhibitors, which is used as an anti-depressant, as well as anti-panic drug. In this work, a sensor for label-free recognition of trace amounts of FL is introduced, which is based on an extended ga ...

IEEE-INST ELECTRICAL ELECTRONICS ENGINEERS INC2022

An Oculus to Profile and Probe Target Engagement In Vivo: How T-REX Was Born and Its Evolution into G-REX

Yimon Aye, Chloé Rogg

Here we provide a personal account of innovation and design principles underpinning a method to interrogate precision electrophile signaling that has come to be known as "REX technologies". This Account is framed in the context of trying to improve methods ...

American Chemical Society2021

Extended Gate Field Effect Transistor Based Sensor for Detection of Trace Amounts of Anti-Depressant Drug

Mihai Adrian Ionescu, Shokoofeh Sheibani

Citalopram hydrobromide (CP) is a selective serotonin reuptake inhibitor for the treatment of the depressive disorder. In this work, a novel label-free recognition method based on an extended gate field-effect transistor (EGFET) for selective determination ...

IEEE-INST ELECTRICAL ELECTRONICS ENGINEERS INC2020

Safinamide inhibits in vivo glutamate release in a rat model of Parkinson's disease

Salvatore Novello

To investigate whether the reversible MAO-B inhibitor and sodium channel blocker safinamide impairs glutamate release under parkinsonian conditions in vivo, and this effect is dependent on MAO-B inhibition, safinamide (and rasagiline as a comparator) were ...

PERGAMON-ELSEVIER SCIENCE LTD2020

Macrocycle synthesis strategy based on step-wise “adding and reacting” three components enables screening of large combinatorial libraries

Christian Heinis, Gerardo Turcatti, Alessandro Angelini, Alessandro Zorzi, Jonathan Patrice Vesin, Kaycie Marie Butler, Julien Bortoli Chapalay, Sangram Shivdas Kale, Ganesh Kumar Mothukuri, Carl Leonard Stenbratt

Macrocycles provide an attractive modality for drug development, but generating ligands for new targets is hampered by the limited availability of large macrocycle libraries. We have established a solution-phase macrocycle synthesis strategy in which three ...

2020

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

Maurizio Molinari

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, Emilia Paunescu, Mylène Soudani

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, Sachin Kotak, Maria Josefina Marcaida Lopez

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 Arthur 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

Relationship between physiological measures of excitability and levels of glutamate and GABA in the human motor cortex

Magnetic resonance spectroscopy (MRS) allows measurement of neurotransmitter concentrations within a region of interest in the brain. Inter-individual variation in MRS-measured GABA levels have been related to variation in task performance in a number of r ...

2011

Intracellular 'boosting' of darunavir using known transport inhibitors in primary PBMC

Ruben Hartkoorn

center dot Antiretroviral protease inhibitors such as lopinavir and saquinavir have been shown to be substrates of ABCB1. Co-administration with the potent ABCB1 and CYP3A4 inhibitor, ritonavir, has shown improved pharmacokinetics and subsequent therapeuti ...

2009

The cyanobacterial alkaloid nostocarboline: an inhibitor of acetylcholinesterase and trypsin

Karl Gademann

Preselected cyanobacterial strains (available from culture collections and our own isolates), belonging primarily to the heterocystous cluster, were screened for inhibitors against butyrylcholinesterase. About one-half of the extracts exhibited inhibitory ...

2009

Pyrrolidine derivatives as new inhibitors of alpha-mannosidases and growth inhibitors of human cancer cells

Pierre Vogel, Sandrine Gerber, Hélène Fiaux

New pyrrolidine-3,4-diol derivatives were prepared from D-(-)- and L(+)-phenylglycinol and tested for their ability to inhibit 25 commercial glycosidases. The influence of the substitution of the lateral side chain and of the pyrrolidine ring on the enzyme ...

2006

Functionalized pyrrolidines as alpha-mannosidase inhibitors and growth inhibitors of human glioblastoma and melanoma cells

Pierre Vogel, Sandrine Gerber, Sylvain Favre, Hélène Fiaux

New substituted pyrrolidine-3,4-diol derivatives were prepared from D-(-)- and L-(+)-phenyl glycinol. The influence of the configuration and the substitution of the lateral side chain of these derivatives on the inhibition of 25 commercial glycosidases wer ...

2005