4-P-PDOT, MT2 selective melatonin receptor antagonist

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.

Activity summary

The target 'RGS4 Melatonin Receptor 1A/MTNR1A Melatonin Receptor 1B/MTNR1B' involves a group of important proteins in cellular signaling. RGS4 also known as Regulator of G-protein Signaling 4 regulates G-protein signaling by accelerating the GTPase activity of the alpha subunit of G-proteins which serves as a turning-off mechanism for G-protein-coupled receptor signaling. RGS4 has a molecular mass of approximately 25-30 kDa and is mainly expressed in the brain and heart tissues. Melatonin Receptor 1A (MTNR1A) and Melatonin Receptor 1B (MTNR1B) bind melatonin a hormone produced by the pineal gland that influences circadian rhythms and reproduction. These two receptors are expressed in various tissues including the brain and retina.

Biological function summary

The proteins work in signaling pathways that affect physiological processes. RGS4 modulates the signaling complexity by interacting with other G-protein coupled receptors and is not usually found as part of a complex but influences them by its regulatory activities. Both MTNR1A and MTNR1B are key in the transduction of melatonin signals and affect sleep-wake cycles and mood regulation. They operate as part of receptor-ligand binding events and facilitate the entry of the hormone to initiate downstream effects impacting neurotransmitter release and cellular signaling cascades.

Pathways

The roles of these proteins are significant. RGS4 intervenes in pathways that regulate heart rate and neurotransmitter release working alongside G-proteins to modulate signaling strength and duration. It interacts with proteins such as G-protein alpha subunits. MTNR1A and MTNR1B are components of the melatonin signaling pathway which influences circadian rhythms and interacts with other circadian regulatory proteins. Their activity can affect proteins involved in sleep regulation and other neurobiological processes.

Associated diseases and disorders

These targets play roles that have been linked to several health conditions. Dysregulation of RGS4 is associated with psychiatric disorders such as schizophrenia due to its effects on neurotransmitter systems. Other relevant proteins in these pathways include dopamine receptors which are also involved in these psychiatric conditions. MTNR1A and MTNR1B are connected to disorders such as insomnia and depression as the disruption of normal melatonin signaling can lead to impaired circadian rhythm. In these cases altered function of proteins within related pathways can lead to the described clinical manifestations.