List of works - Nicholas J Brandon

2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.

scientific article published on 28 February 2012

A cell-based ultra-high-throughput screening assay for identifying inhibitors of D-amino acid oxidase

scientific article published on 7 June 2006

A human-specific AS3MT isoform and BORCS7 are molecular risk factors in the 10q24.32 schizophrenia-associated locus.

scientific article published on 9 May 2016

A survey of rare coding variants in candidate genes in schizophrenia by deep sequencing.

scientific article published on 15 October 2013

Advancing drug discovery for neuropsychiatric disorders using patient-specific stem cell models

scientific article published on 27 January 2016

Altered expression of histamine signaling genes in autism spectrum disorder

scientific article published on 9 May 2017

Altered functional brain network connectivity and glutamate system function in transgenic mice expressing truncated Disrupted-in-Schizophrenia 1

scientific article published on 19 May 2015

Assessing the role of endooligopeptidase activity of Ndel1 (nuclear-distribution gene E homolog like-1) in neurite outgrowth

scientific article published on 10 May 2010

Balanced translocation linked to psychiatric disorder, glutamate, and cortical structure/function

scientific article published on 10 August 2016

Behavioral and biochemical characterization of a mutant mouse strain lacking D-amino acid oxidase activity and its implications for schizophrenia.

scientific article published on 13 July 2006

Biallelic Mutations in PDE10A Lead to Loss of Striatal PDE10A and a Hyperkinetic Movement Disorder with Onset in Infancy ⬇️

scientific journal article

Cell surface stability of gamma-aminobutyric acid type A receptors. Dependence on protein kinase C activity and subunit composition.

scientific article

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

scientific article

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

scientific article published on 24 October 2017

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

scientific article published on 6 May 2017

Chemoproteomics demonstrates target engagement and exquisite selectivity of the clinical phosphodiesterase 10A inhibitor MP-10 in its native environment

scientific article

Clean energy and the hydrogen economy.

scientific article published in July 2017

Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154.

scientific article

Compromising KCC2 transporter activity enhances the development of continuous seizure activity.

scientific article published on 21 April 2016

Compromising the phosphodependent regulation of the GABAAR β3 subunit reproduces the core phenotypes of autism spectrum disorders

scientific article published on 16 November 2015

Constitutive tyrosine phosphorylation of the GABA(A) receptor gamma 2 subunit in rat brain.

scientific article

Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]

scientific article published on 31 July 2018

Current Understanding of PDE10A in the Modulation of Basal Ganglia Circuitry

scientific article published in January 2017

Cytoplasmic Relocalization of TAR DNA-Binding Protein 43 Is Not Sufficient to Reproduce Cellular Pathologies Associated with ALS In vitro.

scientific article published on 24 February 2017

Cytoskeletal changes underlie estrogen's acute effects on synaptic transmission and plasticity

scientific article

D-amino acid oxidase activity is inhibited by an interaction with bassoon protein at the presynaptic active zone.

scientific article published on 23 June 2011

DISC1 and DISC2: discovering and dissecting molecular mechanisms underlying psychiatric illness

scientific article

DISC1 and PDE4B are interacting genetic factors in schizophrenia that regulate cAMP signaling

scientific article

DISC1 as a genetic risk factor for schizophrenia and related major mental illness: response to Sullivan

scientific article published in February 2014

DISC1 at 10: connecting psychiatric genetics and neuroscience

scientific article

DISC1 regulates trafficking and processing of APP and Aβ generation.

scientific article published on 16 September 2014

Deficits in spatial memory correlate with modified {gamma}-aminobutyric acid type A receptor tyrosine phosphorylation in the hippocampus.

scientific article

Deficits in the activity of presynaptic γ-aminobutyric acid type B receptors contribute to altered neuronal excitability in fragile X syndrome

scientific article

Developmental and genetic regulation of the human cortex transcriptome illuminate schizophrenia pathogenesis

scientific article published on 26 July 2018

Developmental seizures and mortality result from reducing GABA receptor α2-subunit interaction with collybistin

scientific article published in Nature Communications

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition

scientific article published on 21 July 2016

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

scientific article

Disrupted in Schizophrenia 1 Interactome: evidence for the close connectivity of risk genes and a potential synaptic basis for schizophrenia

scientific article

Disrupted in Schizophrenia 1 and Nudel form a neurodevelopmentally regulated protein complex: implications for schizophrenia and other major neurological disorders

scientific article (publication date: 2004)

Disrupted in Schizophrenia 1 forms pathological aggresomes that disrupt its function in intracellular transport.

scientific article published on 30 January 2012

Disrupted in schizophrenia 1 and synaptic function in the mammalian central nervous system.

scientific article published on April 2014

Dissecting DISC1 function through protein-protein interactions.

scientific article published on November 2007

Dissecting transcriptomic signatures of neuronal differentiation and maturation using iPSCs

scientific article published on 23 January 2020

Early postnatal GABAA receptor modulation reverses deficits in neuronal maturation in a conditional neurodevelopmental mouse model of DISC1.

scientific article

Effects of a Balanced Translocation between Chromosomes 1 and 11 Disrupting the DISC1 Locus on White Matter Integrity

scientific article

Effects of environmental risks and polygenic loading for schizophrenia on cortical thickness

scientific article

Emerging biology of PDE10A.

scientific article

Estradiol modulates the efficacy of synaptic inhibition by decreasing the dwell time of GABAA receptors at inhibitory synapses.

scientific article

Estrogen receptor neurobiology and its potential for translation into broad spectrum therapeutics for CNS disorders

scientific article

Estrogen receptor ß activity modulates synaptic signaling and structure

scientific journal article

Evidence for non-axial A/P patterning in the nonneural ectoderm of Xenopus and zebrafish pregastrula embryos.

scientific article published in September 1998

Evidence for sustained elevation of IL-6 in the CNS as a key contributor of depressive-like phenotypes.

scientific article published on 4 December 2012

Evidence that many of the DISC1 isoforms in C57BL/6J mice are also expressed in 129S6/SvEv mice

scientific article published on 01 October 2007

Expression of disrupted in schizophrenia 1 (DISC1) protein in the adult and developing mouse brain indicates its role in neurodevelopment.

scientific article published in December 2004

FBXW7 regulates DISC1 stability via the ubiquitin-proteosome system

scientific article published on 20 July 2017

Future Viable Models of Psychiatry Drug Discovery in Pharma ⬇️

scientific article published on 07 February 2013

Fyn kinase contributes to tyrosine phosphorylation of the GABA(A) receptor gamma2 subunit

scientific article

GABAA receptor phosphorylation and functional modulation in cortical neurons by a protein kinase C-dependent pathway.

scientific article published on December 2000

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors

scientific article

How has DISC1 enabled drug discovery?

scientific article published on 23 October 2007

Identification and characterisation of a Maf1/Macoco protein complex that interacts with GABAA receptors in neurons

scientific journal article

Identification of Phosphorylation Consensus Sequences and Endogenous Neuronal Substrates of the Psychiatric Risk Kinase TNIK.

scientific article published on 8 December 2015

Increased burst-firing of ventral tegmental area dopaminergic neurons in D-amino acid oxidase knockout mice in vivo.

scientific article published on 5 July 2014

Intermediate temperature solid oxide fuel cells.

scientific article published on 28 May 2008

Interplay of palmitoylation and phosphorylation in the trafficking and localization of phosphodiesterase 10A: implications for the treatment of schizophrenia.

scientific article published on July 2010

Is sharing specific autobiographical memories a distinct form of self-disclosure?

scientific article published on 25 January 2016

KCC2 activity is critical in limiting the onset and severity of status epilepticus.

scientific article

L-type voltage-gated calcium channel regulation of in vitro human cortical neuronal networks

scientific article published on 25 September 2019

Laboratory study of electro-coagulation-flotation for water treatment.

scientific article published in September 2002

Linking neurodevelopmental and synaptic theories of mental illness through DISC1 ⬇️

scientific article published on November 18, 2011

Locally Reducing KCC2 Activity in the Hippocampus is Sufficient to Induce Temporal Lobe Epilepsy.

scientific article

Misassembly of full-length Disrupted-in-Schizophrenia 1 protein is linked to altered dopamine homeostasis and behavioral deficits.

scientific article

Molecular architecture of potassium chloride co-transporter KCC2.

scientific article published on 28 November 2017

Multiple roles of protein kinases in the modulation of gamma-aminobutyric acid(A) receptor function and cell surface expression.

scientific article

N-Ethylmaleimide increases KCC2 cotransporter activity by modulating transporter phosphorylation

scientific article published in November 2017

Ndel1 alters its conformation by sequestering cAMP-specific phosphodiesterase-4D3 (PDE4D3) in a manner that is dynamically regulated through Protein Kinase A (PKA).

scientific article

Neurodevelopmental mechanisms of schizophrenia: understanding disturbed postnatal brain maturation through neuregulin-1-ErbB4 and DISC1.

scientific article published on 26 August 2009

Novel inhibitors of As(III) S-adenosylmethionine methyltransferase (AS3MT) identified by virtual screening

scientific article published on 14 August 2018

Novel triazines as potent and selective phosphodiesterase 10A inhibitors ⬇️

scientific article published on July 31, 2012

O10.7. INVESTIGATING THE MECHANISMS UNDERLYING THE BENEFICIAL EFFECTS OF ESTROGENS IN SCHIZOPHRENIA.

scientific article

Optimization of M4 positive allosteric modulators (PAMs): The discovery of VU0476406, a non-human primate in vivo tool compound for translational pharmacology

scientific article published on 13 April 2017

Organization of TNIK in dendritic spines

scientific article published on July 2015

PDE10A mutations help to unwrap the neurobiology of hyperkinetic disorders

scientific article published on 02 April 2019

Pharmacokinetics of Oral d-Serine in d-Amino Acid Oxidase Knockout Mice ⬇️

scientific article published on July 26, 2012

Phosphodiesterase 11A in brain is enriched in ventral hippocampus and deletion causes psychiatric disease-related phenotypes.

scientific article

Potentiating KCC2 activity is sufficient to limit the onset and severity of seizures

article published in the Proceedings of the National Academy of Sciences of the United States of America

Pyrrolidin-3-yl-N-methylbenzamides as potent histamine 3 receptor antagonists ⬇️

scientific article published on July 27, 2011

Receptor Cross Talk: Ligand-Gated Ion Channels Start to Communicate ⬇️

scientific article published on October 24, 2000

Receptor for activated C kinase-1 facilitates protein kinase C-dependent phosphorylation and functional modulation of GABA(A) receptors with the activation of G-protein-coupled receptors.

scientific article published in August 2002

Regulation of N-Methyl-D-Aspartate Receptors by Disrupted-in-Schizophrenia-1 ⬇️

scientific article published on July 29, 2013

Regulation of the cytoskeleton by Disrupted-in-Schizophrenia 1 (DISC1) ⬇️

scientific article published on June 12, 2011

SUMOylation of DISC1: a potential role in neural progenitor proliferation in the developing cortex.

scientific article published on 15 March 2016

Schizophrenia drug discovery and development in an evolving era: are new drug targets fulfilling expectations?

scientific article

Schizophrenia risk variants influence multiple classes of transcripts of sorting nexin 19 (SNX19)

scientific article published on 11 January 2019

Schizophrenia-related neural and behavioral phenotypes in transgenic mice expressing truncated Disc1.

scientific article

Searching for cognitive enhancement in the Morris water maze: better and worse performance in D-amino acid oxidase knockout (Dao(-/-)) mice.

scientific article published on February 2016

Seizing Control of KCC2: A New Therapeutic Target for Epilepsy.

scientific article

Selective activation of M4 muscarinic acetylcholine receptors reverses MK-801-induced behavioral impairments and enhances associative learning in rodents

scientific article

Selective inhibition of KCC2 leads to hyperexcitability and epileptiform discharges in hippocampal slices and in vivo

scientific article published on May 2015

Small molecule inducers of ABCA1 and apoE that act through indirect activation of the LXR pathway

scientific article published on 21 March 2018

Sorting nexin 4 and amphiphysin 2, a new partnership between endocytosis and intracellular trafficking

scientific article

State-dependent alterations in sleep/wake architecture elicited by the M4 PAM VU0467154 - Relation to antipsychotic-like drug effects

scientific article published on 23 November 2015

Subcellular targeting of DISC1 is dependent on a domain independent from the Nudel binding site.

scientific article

Subunit-specific association of protein kinase C and the receptor for activated C kinase with GABA type A receptors

scientific article published on 01 November 1999

The ability of BDNF to modify neurogenesis and depressive-like behaviors is dependent upon phosphorylation of tyrosine residues 365/367 in the GABA(A)-receptor γ2 subunit

scientific article published on September 2013

The behavioral and neurochemical effects of a novel D-amino acid oxidase inhibitor compound 8 [4H-thieno [3,2-b]pyrrole-5-carboxylic acid] and D-serine.

scientific article

The cellular target of antidepressants.

scientific article published in October 2015

The clinical trial landscape in amyotrophic lateral sclerosis-Past, present, and future

scientific article published on 11 February 2020

The impact of Disrupted-in-Schizophrenia 1 (DISC1) on the dopaminergic system: a systematic review.

scientific article published on 31 January 2017

The orphan GPCR, GPR88, modulates function of the striatal dopamine system: a possible therapeutic target for psychiatric disorders?

scientific article published on 29 September 2009

The psychiatric disease risk factors DISC1 and TNIK interact to regulate synapse composition and function.

scientific article

The small molecule CLP257 does not modify activity of the K+-Cl- co-transporter KCC2 but does potentiate GABAA receptor activity.

scientific article

Transcriptional regulation of neurodevelopmental and metabolic pathways by NPAS3.

scientific article published on 28 June 2011

Truncation of the TAR DNA-binding protein 43 is not a prerequisite for cytoplasmic relocalization, and is suppressed by caspase inhibition and by introduction of the A90V sequence variant

scientific article

Uncovering the function of Disrupted in Schizophrenia 1 through interactions with the cAMP phosphodiesterase PDE4: Contributions of the Houslay lab to molecular psychiatry.

scientific article published on 29 September 2015

Understanding the role of DISC1 in psychiatric disease and during normal development

scientific article

Verbal working memory and functional large-scale networks in schizophrenia

scientific article published on 23 October 2017

What Happened When the Environment Met DISC1? Showing the Interactive Effects of Poly I:C and DISC1 on Mouse Phenotypes Related to Mood Disorders ⬇️

scientific article published on December 15, 2010

What can we learn from the disrupted in schizophrenia 1 interactome: lessons for target identification and disease biology?

scientific article published on January 2008

What happens inside a fuel cell? Developing an experimental functional map of fuel cell performance.

scientific article

X-ray Characterization and Structure-Based Optimization of Striatal-Enriched Protein Tyrosine Phosphatase Inhibitors

scientific article published on 8 November 2017

d-amino acid oxidase knockout (Dao(-/-) ) mice show enhanced short-term memory performance and heightened anxiety, but no sleep or circadian rhythm disruption

scientific article published on 27 March 2015

List of works by Nicholas J Brandon

2-(Pyrrolidin-1-yl)ethyl-3,4-dihydroisoquinolin-1(2H)-one derivatives as potent and selective histamine-3 receptor antagonists.

A cell-based ultra-high-throughput screening assay for identifying inhibitors of D-amino acid oxidase

A human-specific AS3MT isoform and BORCS7 are molecular risk factors in the 10q24.32 schizophrenia-associated locus.

A survey of rare coding variants in candidate genes in schizophrenia by deep sequencing.

Advancing drug discovery for neuropsychiatric disorders using patient-specific stem cell models

Altered expression of histamine signaling genes in autism spectrum disorder

Altered functional brain network connectivity and glutamate system function in transgenic mice expressing truncated Disrupted-in-Schizophrenia 1

Assessing the role of endooligopeptidase activity of Ndel1 (nuclear-distribution gene E homolog like-1) in neurite outgrowth

Balanced translocation linked to psychiatric disorder, glutamate, and cortical structure/function

Behavioral and biochemical characterization of a mutant mouse strain lacking D-amino acid oxidase activity and its implications for schizophrenia.

Biallelic Mutations in PDE10A Lead to Loss of Striatal PDE10A and a Hyperkinetic Movement Disorder with Onset in Infancy ⬇️

Cell surface stability of gamma-aminobutyric acid type A receptors. Dependence on protein kinase C activity and subunit composition.

Challenges in the development of an M4 PAM in vivo tool compound: The discovery of VU0467154 and unexpected DMPK profiles of close analogs

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides.

Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and in vivo characterization of a series of 3-aminoazetidine-derived amides

Chemoproteomics demonstrates target engagement and exquisite selectivity of the clinical phosphodiesterase 10A inhibitor MP-10 in its native environment

Clean energy and the hydrogen economy.

Cognitive enhancement and antipsychotic-like activity following repeated dosing with the selective M4 PAM VU0467154.

Compromising KCC2 transporter activity enhances the development of continuous seizure activity.

Compromising the phosphodependent regulation of the GABAAR β3 subunit reproduces the core phenotypes of autism spectrum disorders

Constitutive tyrosine phosphorylation of the GABA(A) receptor gamma 2 subunit in rat brain.

Corrigendum to "Challenges in the development of an M4 PAM preclinical candidate: The discovery, SAR, and biological characterization of a series of azetidine-derived tertiary amides" [Bioorg. Med. Chem. Lett. 27(23) (2017) 5179-5184]

Current Understanding of PDE10A in the Modulation of Basal Ganglia Circuitry

Cytoplasmic Relocalization of TAR DNA-Binding Protein 43 Is Not Sufficient to Reproduce Cellular Pathologies Associated with ALS In vitro.

Cytoskeletal changes underlie estrogen's acute effects on synaptic transmission and plasticity

D-amino acid oxidase activity is inhibited by an interaction with bassoon protein at the presynaptic active zone.

DISC1 and DISC2: discovering and dissecting molecular mechanisms underlying psychiatric illness

DISC1 and PDE4B are interacting genetic factors in schizophrenia that regulate cAMP signaling

DISC1 as a genetic risk factor for schizophrenia and related major mental illness: response to Sullivan

DISC1 at 10: connecting psychiatric genetics and neuroscience

DISC1 regulates trafficking and processing of APP and Aβ generation.

Deficits in spatial memory correlate with modified {gamma}-aminobutyric acid type A receptor tyrosine phosphorylation in the hippocampus.

Deficits in the activity of presynaptic γ-aminobutyric acid type B receptors contribute to altered neuronal excitability in fragile X syndrome

Developmental and genetic regulation of the human cortex transcriptome illuminate schizophrenia pathogenesis

Developmental seizures and mortality result from reducing GABA receptor α2-subunit interaction with collybistin

Discovery and SAR of a novel series of potent, CNS penetrant M4 PAMs based on a non-enolizable ketone core: Challenges in disposition

Discovery of VU0467485/AZ13713945: An M4 PAM Evaluated as a Preclinical Candidate for the Treatment of Schizophrenia

Disrupted in Schizophrenia 1 Interactome: evidence for the close connectivity of risk genes and a potential synaptic basis for schizophrenia

Disrupted in Schizophrenia 1 and Nudel form a neurodevelopmentally regulated protein complex: implications for schizophrenia and other major neurological disorders

Disrupted in Schizophrenia 1 forms pathological aggresomes that disrupt its function in intracellular transport.

Disrupted in schizophrenia 1 and synaptic function in the mammalian central nervous system.

Dissecting DISC1 function through protein-protein interactions.

Dissecting transcriptomic signatures of neuronal differentiation and maturation using iPSCs

Early postnatal GABAA receptor modulation reverses deficits in neuronal maturation in a conditional neurodevelopmental mouse model of DISC1.

Effects of a Balanced Translocation between Chromosomes 1 and 11 Disrupting the DISC1 Locus on White Matter Integrity

Effects of environmental risks and polygenic loading for schizophrenia on cortical thickness

Emerging biology of PDE10A.

Estradiol modulates the efficacy of synaptic inhibition by decreasing the dwell time of GABAA receptors at inhibitory synapses.

Estrogen receptor neurobiology and its potential for translation into broad spectrum therapeutics for CNS disorders

Estrogen receptor ß activity modulates synaptic signaling and structure

Evidence for non-axial A/P patterning in the nonneural ectoderm of Xenopus and zebrafish pregastrula embryos.

Evidence for sustained elevation of IL-6 in the CNS as a key contributor of depressive-like phenotypes.

Evidence that many of the DISC1 isoforms in C57BL/6J mice are also expressed in 129S6/SvEv mice

Expression of disrupted in schizophrenia 1 (DISC1) protein in the adult and developing mouse brain indicates its role in neurodevelopment.

FBXW7 regulates DISC1 stability via the ubiquitin-proteosome system

Future Viable Models of Psychiatry Drug Discovery in Pharma ⬇️

Fyn kinase contributes to tyrosine phosphorylation of the GABA(A) receptor gamma2 subunit

GABAA receptor phosphorylation and functional modulation in cortical neurons by a protein kinase C-dependent pathway.

Highly potent, selective, and orally active phosphodiesterase 10A inhibitors

How has DISC1 enabled drug discovery?

Identification and characterisation of a Maf1/Macoco protein complex that interacts with GABAA receptors in neurons

Identification of Phosphorylation Consensus Sequences and Endogenous Neuronal Substrates of the Psychiatric Risk Kinase TNIK.

Increased burst-firing of ventral tegmental area dopaminergic neurons in D-amino acid oxidase knockout mice in vivo.

Intermediate temperature solid oxide fuel cells.

Interplay of palmitoylation and phosphorylation in the trafficking and localization of phosphodiesterase 10A: implications for the treatment of schizophrenia.

Is sharing specific autobiographical memories a distinct form of self-disclosure?

KCC2 activity is critical in limiting the onset and severity of status epilepticus.

L-type voltage-gated calcium channel regulation of in vitro human cortical neuronal networks

Laboratory study of electro-coagulation-flotation for water treatment.

Linking neurodevelopmental and synaptic theories of mental illness through DISC1 ⬇️

Locally Reducing KCC2 Activity in the Hippocampus is Sufficient to Induce Temporal Lobe Epilepsy.

Misassembly of full-length Disrupted-in-Schizophrenia 1 protein is linked to altered dopamine homeostasis and behavioral deficits.

Molecular architecture of potassium chloride co-transporter KCC2.

Multiple roles of protein kinases in the modulation of gamma-aminobutyric acid(A) receptor function and cell surface expression.

N-Ethylmaleimide increases KCC2 cotransporter activity by modulating transporter phosphorylation

Ndel1 alters its conformation by sequestering cAMP-specific phosphodiesterase-4D3 (PDE4D3) in a manner that is dynamically regulated through Protein Kinase A (PKA).

Neurodevelopmental mechanisms of schizophrenia: understanding disturbed postnatal brain maturation through neuregulin-1-ErbB4 and DISC1.

Novel inhibitors of As(III) S-adenosylmethionine methyltransferase (AS3MT) identified by virtual screening

Novel triazines as potent and selective phosphodiesterase 10A inhibitors ⬇️