Neuroscience: Pharmacology & Drug Discovery
43 views | +0 today
Follow
Your new post is loading...
Your new post is loading...
Scooped by Juan Piña-Crespo
Scoop.it!

Mental Immunity: The Microbiome’s Influence on Two Critical Body Systems | Insight & Intelligence™ | GEN

Mental Immunity: The Microbiome’s Influence on Two Critical Body Systems | Insight & Intelligence™ | GEN | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
The pragmatic nature of science grounds the haughty opinions we fabricate about ourselves.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Seeking Cures for Terrible Brain Diseases

Seeking Cures for Terrible Brain Diseases | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
A researcher explains the promise of stem cells for treating neurodegenerative disease
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Alzheimer disease: Antimicrobial role of amyloid-β

The accumulation of amyloid-β (Aβ) in the brain is believed to have a pivotal role in Alzheimer disease (AD) pathology. Kumar et al. now provide in vivo evidence that Aβ may also perform a protective antimicrobial function.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Fragile X disappointments upset autism ambitions

Nature Reviews Drug Discovery 14, 151 (2015).
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

The Alzheimer’s enigma

The Alzheimer’s enigma | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
The cause of Alzheimer’s disease has troubled the science world’s best detectives. Can such a mystery really be solved if we gather enough clues?
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

New mouse model could revolutionize research in Alzheimer's disease - Medical Xpress

New mouse model could revolutionize research in Alzheimer's disease - Medical Xpress | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
Medical Xpress
New mouse model could revolutionize research in Alzheimer's disease
Medical Xpress
Alzheimer's disease, the primary cause of dementia in the elderly, imposes a tremendous social and economic burden on modern society.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Advances in the pharmacological treatment of Parkinson's disease: targeting neurotransmitter systems

Advances in the pharmacological treatment of Parkinson's disease: targeting neurotransmitter systems | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

NMDA Receptor Antagonists for Treatment of Depression

Depression is a psychiatric disorder that affects millions of people worldwide. Individuals battling this disorder commonly experience high rates of relapse, persistent residual symptoms, functional impairment, and diminished well-being.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Study finds brivaracetam well tolerated but with unclear efficacy : Internal Medicine News

Study finds brivaracetam well tolerated but with unclear efficacy : Internal Medicine News | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
Brivaracetam was found to be a safe and tolerable add-on treatment for uncontrolled epilepsy in adults, in a phase III, randomized, double-blind placebo-controlled trial.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

FDA approvals in the first 6 months of 2016 : FDA approvals for the first 6 months of 2016 : Nature Reviews Drug Discovery : Nature Research

Brivaracetam (Briviact- UCB) for Partial-onset seizures     Pimavanserin tartrate (Nuplazid - Acadia) for hallucinations and delusions associated with Parkinson's disease psychosis           Gallium Ga 68 dotatate (Netspot - AAA) for neuroendocrine tumours
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Failed trials for central nervous system disorders do not necessarily invalidate preclinical models and drug targets

A recent article identified five key technical determinants that make substantial contributions to the outcome of drug R&D projects (Lessons learned from the fate of AstraZeneca's drug pipeline: a five-dimensional framework.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Biotech R&D spend jumps by more than 15%

Two reports show big increases in R&D spending among both biotech and pharmaceutical drug developers.In an annual review of the biotech sector, analysts at EY (formerly Ernst & Young) found that biotech companies spent US$40.1 billion on R&D...
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Making strides against Alzheimer’s

Making strides against Alzheimer’s | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
In the innovative research and development process, setbacks are in many ways as important as successes, helping to identify more promising areas to pursue.
more...
No comment yet.
Rescooped by Juan Piña-Crespo from Alzheimer's Disease R&D Review
Scoop.it!

Inhibitor of the Tyrosine Phosphatase STEP Reverses Cognitive Deficits in a Mouse Model of Alzheimer's Disease

Inhibitor of the Tyrosine Phosphatase STEP Reverses Cognitive Deficits in a Mouse Model of Alzheimer's Disease | Neuroscience: Pharmacology & Drug Discovery | Scoop.it

Abstract

 

STEP (STriatal-Enriched protein tyrosine Phosphatase) is a neuron-specific phosphatase that regulates N-methyl-D-aspartate receptor (NMDAR) and α-amino-3-hydroxy-5-methyl-4-isoxazolepropionicacid receptor (AMPAR) trafficking, as well as ERK1/2, p38, Fyn, and Pyk2 activity. STEP is overactive in several neuropsychiatric and neurodegenerative disorders, including Alzheimer's disease (AD). The increase in STEP activity likely disrupts synaptic function and contributes to the cognitive deficits in AD. AD mice lacking STEP have restored levels of glutamate receptors on synaptosomal membranes and improved cognitive function, results that suggest STEP as a novel therapeutic target for AD. Here we describe the first large-scale effort to identify and characterize small-molecule STEP inhibitors. We identified the benzopentathiepin 8-(trifluoromethyl)-1,2,3,4,5-benzopentathiepin-6-aminehydrochloride (known as TC-2153) as an inhibitor of STEP with an IC50 of 24.6 nM. TC-2153 represents a novel class of PTP inhibitors based upon a cyclic polysulfide pharmacophore that forms a reversible covalent bond with the catalytic cysteine in STEP. In cell-based secondary assays, TC-2153 increased tyrosine phosphorylation of STEP substrates ERK1/2, Pyk2, and GluN2B, and exhibited no toxicity in cortical cultures. Validation and specificity experiments performed in wild-type (WT) and STEP knockout (KO) cortical cells and in vivo in WT and STEP KO mice suggest specificity of inhibitors towards STEP compared to highly homologous tyrosine phosphatases. Furthermore, TC-2153 improved cognitive function in several cognitive tasks in 6- and 12-mo-old triple transgenic AD (3xTg-AD) mice, with no change in beta amyloid and phospho-tau levels.


Via Krishan Maggon
more...
Krishan Maggon 's curator insight, August 7, 2014 6:40 AM

open access full text

 

Inhibitor of the Tyrosine Phosphatase STEP Reverses Cognitive Deficits in a Mouse Model of Alzheimer's DiseaseJian Xu,  Manavi Chatterjee,  Tyler D. Baguley,  Jonathan Brouillette,  Pradeep Kurup,  Debolina Ghosh,  Jean Kanyo,  Yang Zhang,  Kathleen Seyb, Chimezie Ononenyi,  Ethan Foscue,  George M. Anderson,  Jodi Gresack,  [ ... ], Paul J. Lombroso mail , [ view all ]Published: August 05, 2014DOI: 10.1371/journal.pbio.1001923

 

Citation: Xu J, Chatterjee M, Baguley TD, Brouillette J, Kurup P, et al. (2014) Inhibitor of the Tyrosine Phosphatase STEP Reverses Cognitive Deficits in a Mouse Model of Alzheimer's Disease. PLoS Biol 12(8): e1001923. doi:10.1371/journal.pbio.1001923

Scooped by Juan Piña-Crespo
Scoop.it!

The discovery of first-in-class drugs: origins and evolution

Nature Reviews Drug Discovery 13, 577 (2014).
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

1 in 68 Children Now Has a Diagnosis of Autism Spectrum Disorder. Why? - The Atlantic

1 in 68 Children Now Has a Diagnosis of Autism Spectrum Disorder. Why? - The Atlantic | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
The Atlantic
1 in 68 Children Now Has a Diagnosis of Autism Spectrum Disorder. Why?
The Atlantic
Rates of autism spectrum disorder (ASD) are not creeping up so much as leaping up.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Mitochondria targeted therapeutic approaches in Parkinson's and Huntington's diseases

Mitochondria targeted therapeutic approaches in Parkinson's and Huntington's diseases | Neuroscience: Pharmacology & Drug Discovery | Scoop.it

Abstract

Substantial evidence from both genetic and toxin induced animal and cellular models and postmortem human brain tissue indicates that mitochondrial dysfunction plays a central role in pathophysiology of the neurodegenerative disorders including Parkinson's disease (PD), and Huntington's disease (HD). This review discusses the emerging understanding of the role of mitochondrial dysfunction including bioenergetics defects, mitochondrial DNA mutations, familial nuclear DNA mutations, altered mitochondrial fusion/fission and morphology, mitochondrial transport/trafficking, altered transcription and increased interaction of pathogenic proteins with mitochondria in the pathogenesis of PD and HD. This review recapitulates some of the key therapeutic strategies applied to surmount mitochondrial dysfunction in these debilitating disorders. We discuss the therapeutic role of mitochondrial bioenergetic agents such as creatine, Coenzyme-Q10, mitochondrial targeted antioxidants and peptides, the SIRT1 activator resveratrol, and the pan-PPAR agonist bezafibrate in toxin and genetic cellular and animal models of PD and HD. We also summarize the phase II-III clinical trials conducted using some of these agents. Lastly, we discuss PGC-1α, TORC and Sirtuins as potential therapeutic targets for mitochondrial dysfunction in neurodegenerative disorders. This article is part of a Special Issue entitled 'Mitochondrial function and dysfunction in neurodegeneration'

more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Trial watch: Phase II boost for glutamate-targeted antidepressants

Nature Reviews Drug Discovery 12, 897 (2013).
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

P2X receptors as targets for the treatment of status epilepticus | Frontiers in Cellular Neuroscience

Prolonged seizures are amongst the most common neurological emergencies.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

NMDA Receptor Modulators in the Treatment of Drug Addiction

Glutamate plays a pivotal role in drug addiction, and the N-methyl-D-aspartate (NMDA) glutamate receptor subtype serves as a molecular target for several drugs of abuse.
more...
No comment yet.
Scooped by Juan Piña-Crespo
Scoop.it!

Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain : Nature Reviews Drug Discovery : Nature Publishing Group

Glycine transporters as novel therapeutic targets in schizophrenia, alcohol dependence and pain : Nature Reviews Drug Discovery : Nature Publishing Group | Neuroscience: Pharmacology & Drug Discovery | Scoop.it
more...
No comment yet.