(S)-3,5-DHPG (mM/ml), group I mGlu agonist

Supplementary info

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

Activity summary

Cytochrome P450 3A4 commonly known as CYP3A4 is an enzyme with a mass of approximately 57 kDa. It participates in the metabolism of various substances including drugs and xenobiotics in the liver and intestines. This enzyme is part of the larger cytochrome P450 family which are heme-containing proteins. Metabotropic Glutamate Receptors (mGluRs) including mGluR2 mGluR3 mGluR1a mGluR5 mGluR4 (also known as MGLUR4) mGluR7 (MGLUR7) and mGluR8 (MGLUR8) are G protein-coupled receptors involved in modulating neurotransmission in the central nervous system and are expressed throughout the brain. The structure and expression of these targets enable them to play significant roles in both enzymatic activity and neurotransmission.

Biological function summary

CYP3A4 plays a role in the oxidation of small organic molecules making it critical for drug metabolism and drug-drug interactions. It operates as part of a large enzymatic complex in the endoplasmic reticulum. Metabotropic Glutamate Receptors contribute to modulating synaptic plasticity and neuronal excitability. These receptors function as homo- or heterodimers and are linked to signaling pathways that regulate several neurotransmitters. The activity of these mGluRs significantly affects cognitive functions learning memory and responsiveness to stress.

Pathways

CYP3A4 is a central player in the drug metabolism pathway influencing the biotransformation of pharmaceuticals and endogenous compounds. It is related to the regulation of the xenobiotic detoxification pathway. Metabotropic Glutamate Receptors are involved in the glutamate signaling pathway which has strong connections to synaptic plasticity. These receptors are associated with other proteins like NMDA and AMPA receptors influencing neurotransmitter release and signal modulation in neuronal networks.

Associated diseases and disorders

CYP3A4 is associated with altered drug metabolism which can lead to drug-induced liver injury and adverse drug reactions. Additionally altered CYP3A4 activity is linked to conditions affecting the intestines and liver. Metabotropic Glutamate Receptors are connected to neurological disorders such as schizophrenia and anxiety. Dysregulation of these mGluRs can affect proteins like NMDA receptors impacting synaptic signaling and contributing to the pathophysiology of these disorders. Understanding the roles of these targets aids in developing therapies for related diseases.