Structural basis of the ligand binding and signaling mechanism of melatonin receptors
Q Wang, Q Lu, Q Guo, M Teng, Q Gong, X Li… - Nature …, 2022 - nature.com
Melatonin receptors (MT1 and MT2 in humans) are family AG protein–coupled receptors that
respond to the neurohormone melatonin to regulate circadian rhythm and sleep. Numerous …
respond to the neurohormone melatonin to regulate circadian rhythm and sleep. Numerous …
Structure-based discovery of potent and selective melatonin receptor agonists
Melatonin receptors MT1 and MT2 are involved in synchronizing circadian rhythms and are
important targets for treating sleep and mood disorders, type-2 diabetes and cancer. Here …
important targets for treating sleep and mood disorders, type-2 diabetes and cancer. Here …
Cryo-EM structure of the human MT1–Gi signaling complex
HH Okamoto, H Miyauchi, A Inoue… - Nature Structural & …, 2021 - nature.com
Melatonin receptors (MT1 and MT2) transduce inhibitory signaling by melatonin (N-acetyl-5-
methoxytryptamine), which is associated with sleep induction and circadian rhythm …
methoxytryptamine), which is associated with sleep induction and circadian rhythm …
Molecular organization and dynamics of the melatonin MT1 receptor/RGS20/Gi protein complex reveal asymmetry of receptor dimers for RGS and Gi coupling
Functional asymmetry of G‐protein‐coupled receptor (GPCR) dimers has been reported for
an increasing number of cases, but the molecular architecture of signalling units associated …
an increasing number of cases, but the molecular architecture of signalling units associated …
Melatonin receptor structures shed new light on melatonin research
The tryptophan derivative melatonin is an evolutionary old molecule that is involved in a
pleiotropy of physiological functions. In humans, age‐related decline of circulating melatonin …
pleiotropy of physiological functions. In humans, age‐related decline of circulating melatonin …
Structural insights into melatonin receptors
The long‐anticipated high‐resolution structures of the human melatonin G protein‐coupled
receptors MT1 and MT2, involved in establishing and maintaining circadian rhythm, were …
receptors MT1 and MT2, involved in establishing and maintaining circadian rhythm, were …
Homology models of melatonin receptors: challenges and recent advances
Melatonin exerts many of its actions through the activation of two G protein-coupled
receptors (GPCRs), named MT1 and MT2. So far, a number of different MT1 and MT2 …
receptors (GPCRs), named MT1 and MT2. So far, a number of different MT1 and MT2 …
A molecular and chemical perspective in defining melatonin receptor subtype selectivity
KH Chan, YH Wong - International Journal of Molecular Sciences, 2013 - mdpi.com
Melatonin is primarily synthesized and secreted by the pineal gland during darkness in a
normal diurnal cycle. In addition to its intrinsic antioxidant property, the neurohormone has …
normal diurnal cycle. In addition to its intrinsic antioxidant property, the neurohormone has …
Melatonin receptor signaling: impact of receptor oligomerization on receptor function
A Oishi, E Cecon, R Jockers - International Review of Cell and Molecular …, 2018 - Elsevier
The melatonin receptor subfamily is composed of three members, MT 1 and MT 2, which are
binding to melatonin, and GPR50, which shows high sequence homology to MT 1 and MT 2 …
binding to melatonin, and GPR50, which shows high sequence homology to MT 1 and MT 2 …
MT1 and MT2 Melatonin Receptors: Ligands, Models, Oligomers, and Therapeutic Potential
Numerous physiological functions of the pineal gland hormone melatonin are mediated via
activation of two G-protein-coupled receptors, MT1 and MT2. The melatonergic drugs on the …
activation of two G-protein-coupled receptors, MT1 and MT2. The melatonergic drugs on the …