Shane D. Hellyer
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Structure-based discovery of positive allosteric modulators of the A <sub>1</sub> adenosine receptor Open
Allosteric modulation of G protein–coupled receptors (GPCRs) is an exciting strategy for developing new therapeutic agents, and it has several advantages over more commonly used orthosteric drugs. Recently determined GPCR structures have r…
View article: Pharmacological characterisation of allosteric modulators at human mGlu5
Pharmacological characterisation of allosteric modulators at human mGlu5 Open
The metabotropic glutamate receptor 5 (mGlu5) is a Class C G protein-coupled receptor, ubiquitously expressed throughout the central nervous system (CNS). With major roles in cognition, learning and memory, mGlu5 dysfunction is linked with…
View article: Pharmacological characterisation of allosteric modulators at human mGlu <sub>5</sub>
Pharmacological characterisation of allosteric modulators at human mGlu <sub>5</sub> Open
The metabotropic glutamate receptor 5 (mGlu 5 ) is a Class C G protein-coupled receptor, ubiquitously expressed throughout the CNS. With major roles in cognition, learning and memory, mGlu 5 dysfunction is linked with numerous neurodegener…
<i>DUSP6</i> loss enhances dopamine secretion and modulate neurodevelopment in ADHD iPSC-derived dopaminergic neurons Open
Although the gene DUSP6 has been implicated as a risk gene for attention deficit hyperactivity disorder (ADHD) in recent GWAS studies, its functional role in the aetiology of the condition remains poorly understood. DUSP6 is reported to re…
Pharmacology, Signaling and Therapeutic Potential of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators Open
Metabotropic glutamate receptors are a family of eight class C G protein-coupled receptors regulating higher order brain functions including cognition and motion. Metabotropic glutamate receptors have thus been heavily investigated as pote…
Unlocking the secrets of trace amine-associated receptor 1 agonists: new horizon in neuropsychiatric treatment Open
For over seven decades, dopamine receptor 2 (D 2 receptor) antagonists remained the mainstay treatment for neuropsychiatric disorders. Although it is effective for treating hyperdopaminergic symptoms, it is often ineffective for treating n…
Transcriptome profiling of dopaminergic neurons derived from an ADHD induced pluripotent stem cell (iPSC) model Open
The most recent ADHD – GWAS meta – analysis highlighted the potential role of 76 genes enriched among genes expressed in early brain development and associated with midbrain dopaminergic neurons. However, the precise functional importance …
SCA44‐ and SCAR13‐associated <i>GRM1</i> mutations affect metabotropic glutamate receptor 1 function through distinct mechanisms Open
Background and Purpose Metabotropic glutamate receptor 1 (mGlu 1 ) is a promising therapeutic target for neurodegenerative CNS disorders including spinocerebellar ataxias (SCAs). Clinical reports have identified naturally‐occurring mGlu 1 …
Trace amine associated receptor 1: predicted effects of single nucleotide variants on structure-function in geographically diverse populations Open
Trace Amine Associated Receptor 1 (TAAR1) is a novel pharmaceutical target under investigation for the treatment of several neuropsychiatric conditions. TAAR1 single nucleotide variants (SNV) have been found in patients with schizophrenia …
Trace amine associated receptor 1: Predicted effects of single nucleotide variants on structure-function in geographically diverse populations Open
Trace Amine Associated Receptor 1 (TAAR1) is a novel pharmaceutical target under investigation for the treatment of several neuropsychiatric conditions. TAAR1 single nucleotide variants (SNV) have been found in patients with schizophrenia …
Trace amine associated receptor 1: Predicted effects of single nucleotide variants on structure-function in geographically diverse populations Open
Trace Amine Associated Receptor 1 (TAAR1) is a novel pharmaceutical target under investigation for the treatment of several neuropsychiatric conditions. TAAR1 single nucleotide variants (SNV) have been found in patients with schizophrenia …
SCA44- and SCAR13-associated <i>GRM1</i> mutations affect metabotropic glutamate receptor 1 function through distinct mechanisms Open
Metabotropic glutamate receptor 1 (mGlu 1 ) is a promising therapeutic target for neurodegenerative CNS disorders including spinocerebellar ataxias (SCAs). Clinical reports have identified naturally-occurring mGlu 1 mutations in rare SCA s…
Publisher Correction to: Adenosine receptor signalling in Alzheimer’s disease Open
Alzheimer's disease (AD) is the most common dementia in the elderly and its increasing prevalence presents treatment challenges.Despite a better understanding of the disease, the current mainstay of treatment cannot modify pathogenesis or …
Adenosine receptor signalling in Alzheimer’s disease Open
Alzheimer’s disease (AD) is the most common dementia in the elderly and its increasing prevalence presents treatment challenges. Despite a better understanding of the disease, the current mainstay of treatment cannot modify pathogenesis or…
Metabotropic glutamate receptor 5 (mGlu<sub>5</sub>)‐positive allosteric modulators differentially induce or potentiate desensitization of mGlu<sub>5</sub> signaling in recombinant cells and neurons Open
Allosteric modulators of metabotropic glutamate receptor 5 (mGlu 5 ) are a promising therapeutic strategy for a number of neurological disorders. Multiple mGlu 5 ‐positive allosteric modulator (PAM) chemotypes have been discovered that act…
Identification of monellin as the first naturally derived proteinaceous allosteric agonist of metabotropic glutamate receptor 5 Open
Allosteric modulators bind sites distinct from orthosteric ligands, allowing for improved spatiotemporal control of receptors and greater subtype selectivity. However, we recently showed that allosteric ligands previously classified as sel…
Coincident activation of adenosine A1 receptors and metabotropic glutamate receptor 5 differentially influences signalling in primary brain cell cultures Open
G protein-coupled receptors (GPCRs) are highly 'druggable' proteins and represent the largest class of current therapeutic targets. Two distinct neuromodulatory GPCRs, the adenosine A1 receptor (A1AR) and the metabotropic glutamate recepto…