GPCRomics: an approach to discover GPCR drug targets

PA Insel, K Sriram, MW Gorr, SZ Wiley… - Trends in …, 2019 - cell.com
G protein-coupled receptors (GPCRs) are targets for∼ 35% of approved drugs but only∼
15% of the∼ 800 human GPCRs are currently such targets. GPCRomics, the use of …

[HTML][HTML] Understanding the habenula: A major node in circuits regulating emotion and motivation

JL Ables, K Park, I Ibañez–Tallon - Pharmacological research, 2023 - Elsevier
Over the last decade, the understanding of the habenula has rapidly advanced from being
an understudied brain area with the Latin name 'habena” meaning “little rein”, to being …

Compensatory CSF2-driven macrophage activation promotes adaptive resistance to CSF1R inhibition in breast-to-brain metastasis

F Klemm, A Möckl, A Salamero-Boix, T Alekseeva… - Nature cancer, 2021 - nature.com
Tumor microenvironment-targeted therapies are emerging as promising treatment options
for different cancer types. Tumor-associated macrophages and microglia (TAMs) represent …

G-protein-coupled receptors in CNS: a potential therapeutic target for intervention in neurodegenerative disorders and associated cognitive deficits

S Azam, ME Haque, M Jakaria, SH Jo, IS Kim, DK Choi - Cells, 2020 - mdpi.com
Neurodegenerative diseases are a large group of neurological disorders with diverse
etiological and pathological phenomena. However, current therapeutics rely mostly on …

Application of mathematical modeling in prediction of COVID-19 transmission dynamics

A AlArjani, MT Nasseef, SM Kamal, BVS Rao… - Arabian Journal for …, 2022 - Springer
The entire world has been affected by the outbreak of COVID-19 since early 2020. Human
carriers are largely the spreaders of this new disease, and it spreads much faster compared …

Intrinsically disordered proteins and proteins with intrinsically disordered regions in neurodegenerative diseases

O Coskuner-Weber, O Mirzanli, VN Uversky - Biophysical Reviews, 2022 - Springer
Many different intrinsically disordered proteins and proteins with intrinsically disordered
regions are associated with neurodegenerative diseases. These types of proteins including …

Brain-wide functional architecture remodeling by alcohol dependence and abstinence

A Kimbrough, DJ Lurie, A Collazo… - Proceedings of the …, 2020 - National Acad Sciences
Alcohol abuse and alcohol dependence are key factors in the development of alcohol use
disorder, which is a pervasive societal problem with substantial economic, medical, and …

Molecular pharmacology of metabotropic receptors targeted by neuropsychiatric drugs

BL Roth - Nature structural & molecular biology, 2019 - nature.com
Metabotropic receptors are responsible for so-called 'slow synaptic transmission'and
mediate the effects of hundreds of peptide and non-peptide neurotransmitters and …

Update on GPCR-based targets for the development of novel antidepressants

I Mantas, M Saarinen, ZQD Xu, P Svenningsson - Molecular psychiatry, 2022 - nature.com
Traditional antidepressants largely interfere with monoaminergic transport or degradation
systems, taking several weeks to have their therapeutic actions. Moreover, a large …

Discovery of TAK-041: a potent and selective GPR139 agonist explored for the treatment of negative symptoms associated with schizophrenia

HA Reichard, HH Schiffer, H Monenschein… - Journal of Medicinal …, 2021 - ACS Publications
The orphan G-protein-coupled receptor GPR139 is highly expressed in the habenula, a
small brain nucleus that has been linked to depression, schizophrenia (SCZ), and substance …