Practical strategies and concepts in GPCR allosteric modulator discovery: recent advances with metabotropic glutamate receptors

CW Lindsley, KA Emmitte, CR Hopkins… - Chemical …, 2016 - ACS Publications
Allosteric modulation of GPCRs has initiated a new era of basic and translational discovery,
filled with therapeutic promise yet fraught with caveats. Allosteric ligands stabilize unique …

Genetic association studies of glutamate, GABA and related genes in schizophrenia and bipolar disorder: a decade of advance

SYT Cherlyn, P San Woon, JJ Liu, WY Ong… - Neuroscience & …, 2010 - Elsevier
Schizophrenia (SZ) and bipolar disorder (BD) are debilitating neurobehavioural disorders
likely influenced by genetic and non-genetic factors and which can be seen as complex …

Polygenic transmission and complex neuro developmental network for attention deficit hyperactivity disorder: Genome‐wide association study of both common and …

L Yang, BM Neale, L Liu, SH Lee… - American Journal of …, 2013 - Wiley Online Library
Attention‐deficit hyperactivity disorder (ADHD) is a complex polygenic disorder. This study
aimed to discover common and rare DNA variants associated with ADHD in a large …

ADX71743, a potent and selective negative allosteric modulator of metabotropic glutamate receptor 7: in vitro and in vivo characterization

M Kalinichev, M Rouillier, F Girard, I Royer-Urios… - … of Pharmacology and …, 2013 - ASPET
Metabotropic glutamate receptor 7 (mGlu7) has been suggested to be a promising novel
target for treatment of a range of disorders, including anxiety, post-traumatic stress disorder …

Glutamate receptor, metabotropic 7 (GRM7) gene variations and susceptibility to autism: A case–control study

R Noroozi, M Taheri, A Movafagh… - Autism …, 2016 - Wiley Online Library
Autism spectrum disorder (ASD) as a synaptopathy is revealed to be pertained to aberrant
glutamatergic neurotransmission. Glutamate receptor, metabotropic 7 (GRM7), a receptor …

Metabotropic glutamate receptor 7: at the interface of cognition and emotion

RM O'Connor, BC Finger, PJ Flor, JF Cryan - European journal of …, 2010 - Elsevier
Understanding the complex interaction between stress and genetics that leads to the
manifestation of disorders such as depression, anxiety, and cognitive dysfunction is one of …

GRM7 gene mutations and consequences for neurodevelopment

GA Freitas, CM Niswender - Pharmacology Biochemistry and Behavior, 2023 - Elsevier
The metabotropic glutamate receptor 7 (mGlu 7), encoded by the GRM7 gene in humans, is
a presynaptic, G protein-coupled glutamate receptor that is essential for modulating …

Persistent challenges in the development of an mGlu7 PAM in vivo tool compound: the discovery of VU6046980

JJ Kalbfleisch, AL Rodriguez, X Lei, K Weiss… - Bioorganic & medicinal …, 2023 - Elsevier
Herein, we report on the further chemical optimization of the first reported mGlu 7 positive
allosteric modulator (PAM), VU6027459. Replacement of the quinoline core by a cinnoline …

Identification of positive allosteric modulators VU0155094 (ML397) and VU0422288 (ML396) reveals new insights into the biology of metabotropic glutamate receptor …

N Jalan-Sakrikar, JR Field, R Klar… - ACS Chemical …, 2014 - ACS Publications
Metabotropic glutamate receptor 7 (mGlu7) is a member of the group III mGlu receptors
(mGlus), encompassed by mGlu4, mGlu6, mGlu7, and mGlu8. mGlu7 is highly expressed in …

The GRM7 gene, early response to risperidone, and schizophrenia: a genome-wide association study and a confirmatory pharmacogenetic analysis

E Sacchetti, C Magri, A Minelli, P Valsecchi… - The …, 2017 - nature.com
The search for biomarkers of response to antipsychotic medications is hindered by
difficulties inherent in the topic or related to persistent methodological difficulties, such as …