Beyond the nucleus: Plastic chemicals activate G protein-coupled receptors

M McPartland, S Stevens, Z Bartosova… - Environmental …, 2024 - ACS Publications
G protein-coupled receptors (GPCRs) are central mediators of cell signaling and
physiological function. Despite their biological significance, GPCRs have not been widely …

Melatonin receptor structure and signaling

HH Okamoto, E Cecon, O Nureki… - Journal of Pineal …, 2024 - Wiley Online Library
Abstract Melatonin (5‐methoxy‐N‐acetyltryptamine) binds with high affinity and specificity to
membrane receptors. Several receptor subtypes exist in different species, of which the …

The location, physiology, pathology of hippocampus Melatonin MT2 receptor and MT2-selective modulators

Y Feng, X Jiang, W Liu, H Lu - European Journal of Medicinal Chemistry, 2023 - Elsevier
Melatonin, a neurohormone secreted by the pineal gland and regulated by the
suprachiasmatic nucleus (SCN) of the hypothalamus, is synthesized and directly released …

[HTML][HTML] Structure-based virtual screening of ultra-large library yields potent antagonists for a lipid GPCR

AA Sadybekov, RL Brouillette, E Marin, AV Sadybekov… - Biomolecules, 2020 - mdpi.com
Cysteinyl leukotriene G protein-coupled receptors, CysLT1R and CysLT2R, regulate
bronchoconstrictive and pro-inflammatory effects and play a key role in allergic disorders …

Melatonin receptors, brain functions, and therapies

A Oishi, F Gbahou, R Jockers - Handbook of Clinical Neurology, 2021 - Elsevier
In mammals, including humans, the neurohormone melatonin is mainly secreted from the
pineal gland at night and acts on two high-affinity G protein-coupled receptors, the melatonin …

[HTML][HTML] Structural Basis for Agonistic Activity and Selectivity toward Melatonin Receptors hMT1 and hMT2

M Cantarini, D Rusciano, R Amato, A Canovai… - International Journal of …, 2023 - mdpi.com
Glaucoma, a major ocular neuropathy originating from a progressive degeneration of retinal
ganglion cells, is often associated with increased intraocular pressure (IOP). Daily IOP …

Structure-based virtual screening accelerates GPCR drug discovery

L Liu, R Jockers - Trends in Pharmacological Sciences, 2020 - cell.com
Virtual ligand screening (VLS) against high-resolution structures of G-protein-coupled
receptors (GPCRs) is likely to become the next-generation drug design approach of choice …

[HTML][HTML] Molecular characterization and pharmacology of melatonin receptors in animals

E Cecon, JA Boutin, R Jockers - Receptors, 2023 - mdpi.com
Melatonin, the hormone of darkness, is secreted in minute amounts during the night and is
virtually undetectable during the day. Melatonin mainly acts on high-affinity G protein …

In silico drug discovery of melatonin receptor ligands with therapeutic potential

GM Elisi, L Scalvini, A Lodola, A Bedini… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction The neurohormone melatonin (N-acetyl-5-methoxytryptamine) regulates
circadian rhythms exerting a variety of effects in the central nervous system and in periphery …

The circadian machinery links metabolic disorders and depression: a review of pathways, proteins and potential pharmacological interventions

E Pitsillou, J Liang, A Hung, TC Karagiannis - Life Sciences, 2021 - Elsevier
Circadian rhythms are responsible for regulating a number of physiological processes. The
central oscillator is located within the suprachiasmatic nucleus (SCN) of the hypothalamus …