A5080870364- Neuroscience and Neuropharmacology Research
- Neuroinflammation and Neurodegeneration Mechanisms
- Adenosine and Purinergic Signaling
- Pluripotent Stem Cells Research
- Receptor Mechanisms and Signaling
- Wnt/β-catenin signaling in development and cancer
- Cellular transport and secretion
- Synthesis and biological activity
- Sphingolipid Metabolism and Signaling
- Trace Elements in Health
- Cancer Mechanisms and Therapy
- Cancer-related gene regulation
- Genetics and Neurodevelopmental Disorders
- RNA Interference and Gene Delivery
- Cancer, Stress, Anesthesia, and Immune Response
- 3D Printing in Biomedical Research
- Protein Kinase Regulation and GTPase Signaling
- Management, Economics, and Public Policy
- Click Chemistry and Applications
- Alzheimer's disease research and treatments
- Photoreceptor and optogenetics research
- Nuclear Receptors and Signaling
- Pharmacological Receptor Mechanisms and Effects
- 14-3-3 protein interactions
Université de Montpellier
2019
Centre National de la Recherche Scientifique
2019
Czech Academy of Sciences
2019
Charles University
2019
Czech Academy of Sciences, Institute of Molecular Genetics
2019
Inserm
2019
Italian Institute of Technology
2017-2018
Sapienza University of Rome
2005-2007
In this work, we describe the identification of 1,2,4-triazolo[4,3-a]pyrazin-3-one as a new versatile scaffold for development adenosine human (h) receptor antagonists. The chemotype ensued from molecular simplification approach applied to our previously reported 1,2,4-triazolo[4,3-a]quinoxalin-1-one series. Hence, set novel 8-amino-2-aryl-1,2,4-triazolopyrazin-3-one derivatives, featured by different substituents on 2-phenyl ring (R) and at position 6 (R6), was synthesized with main purpose...
Abstract Glycogen synthase kinase 3β (GSK‐3β) and casein 1δ (CK‐1δ) are emerging targets for the treatment of neuroinflammatory disorders, including Parkinson's disease. An inhibitor able to target these two kinases was developed by docking‐based design. Compound 12 , 3‐(7‐amino‐5‐(cyclohexylamino)‐[1,2,4]triazolo[1,5‐ a ][1,3,5]triazin‐2‐yl)‐2‐cyanoacrylamide, showed combined inhibitory activity against GSK‐3β CK‐1δ [IC 50 (GSK‐3β)=0.17 μ m ; IC (CK‐1δ)=0.68 ]. In particular, classical ATP...
We have shown that endogenous activation of type 5 metabotropic glutamate (mGlu5) receptors supports the maintenance a pluripotent, undifferentiated state in D3 mouse embryonic stem cells cultured presence leukaemia inhibitory factor (LIF). Here, we examined interaction between LIF and mGlu5 using as read-out immediate early gene, c-Myc. The selective receptor antagonist, 2-methyl-6-(phenylenthynyl)pyridine (MPEP; 1 mum), reduced increase c-Myc protein levels induced by enhancing...
Alzheimer's disease (AD) is a slow-progressing of the brain characterized by symptoms such as impairment memory and other cognitive functions. AD associated with an inflammatory process that involves astrocytes microglial cells, among components. Astrocytes are most abundant type glial cells in central nervous system (CNS). They involved inducing neuroinflammation. The present study uses astrocyte-neuron cocultures to investigate how ARN14494, serine palmitoyltransferase (SPT) inhibitor,...
The orphan G-protein–coupled receptor (GPCR) GPR158 is expressed in the brain, where it involved osteocalcin effect on cognitive processes, and at periphery, may contribute to glaucoma cancers. forms a complex with RGS7-<i>β</i>5, leading regulation of neighboring GPCR-induced Go protein activity. also interacts <i>α</i>o, although no canonical coupling has been reported. displays three VCPWE motifs its C-terminal domain that are putatively G-protein regulation. Here, we addressed...
We examined the effect of Wnt1 and Wnt7a on cell proliferation using undifferentiated PC12 cells, which originate from neural crest are widely employed as a neuronal model. Heterologous expression enhanced [3H]thymidine incorporation cyclin D1 cylin E in cells. Opposite effects were observed cells expressing Wnt7a. Searching for mechanisms underlying opposite proliferation, we activation canonical beta-catenin/T-cell-lymphoid enhancer-binding protein transcription factor pathway 'calcium...