Presenters

MD. MOHIUDDIN 2008-3-70-049 MAHFUJUR RAHMAN 2008-3-70-029 A. K. M. RADOWAN AHMAD 2008-3-70-018

G-protein coupled Receptor is the large super family of receptors. Found only in eukaryotes, and animals. Also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors and G protein-linked receptors (GPLR), GPCRs. These type of receptor contain distinct heterotrimeric GTP-binding regulatory proteins known as G-proteins.

G protein-coupled receptors are involved in many diseases, and are also the target of approximately 30% of all modern medicinal drugs. GPCRs include: Biogenic amines Eicosanoids Peptide hormones Opioids Amino acids such as GABA ,-adrenergic receptor proteins Other peptide and Protein ligands

G-protein regulated effectors include: Adenylyl cyclase Phospholipase C Phosphodiesterases Ca2+ channels K+ channels

Divided into three main classes of family Class A: The largest class by far, contain nearly 85% of the GPCR genes. Half of these are predicted to encode olfactory receptors, the remaining are classified as orphan receptors. Class B: Secreting receptor family. A protein family which is a group of evolutionarily-related proteins. Many secreting receptors are regulated by peptide hormones. Class C: A type of glutamate receptors which are active through an indirect

Gs: The first G-protein alpha subunit to be identified was Gs. this is responsible for stimulating adenylate cyclase and is ADP-ribosylated and activated by CTx. Some evidence shows that this subunit can also enhance the activity of the cardiac L-type Ca ion channels, independently of their phosphorylation by cAMP stimulated protein kinase A. Golf: Golf is a cyclase-stimulating homolog in the olfactory epithelium, activated by the large family of olfactory receptors. Gi: Gi is the G-protein responsible for inhibiting adenylate cyclase. The inhibition is mediated by the alpha subunit and is ADP-ribosylated and activated by PTx. It also activates inward rectifier K ion channels and this activation is mediated by subunits. It has three isomers

Go: Gos main function is to reduce the opening probability of those voltage gated Ca ion channels involve in neurotransmitter release. Hence, it is large responsible for the widespread auto inhibition of transmitter secretion by pre-synaptic receptors and this effect is mediated through released subunits. There are two main isomers of this: Go1 Go2 Gt: Gt is responsible for stimulating phosphodiesterase. Ggust: Ggust is a phosphodiesterase stimulating homolog in tounge taste buds involve in bitter taste reception. Activation of the Ggust also stimulates phospholipase C via the subunits. Gq & G11: Both are closely related and widely

G14 & G15: Both are more distantly related PTx insensitive G-proteins those can stimulate phospholipase C. G12 & G13: Both are other PTx insensitive Gproteins related to Gq. G16: It is interesting because it lacks receptor specificity and so acts as a universal phospholipase C transducer.

Structurally GPCRs are characterized by an extracellular amino-terminus and an intracellular carboxyl-terminus The GPCR arranges itself into a tertiary structure resembling a container like structure, with the seven transmembrane helices forming a cavity within the plasma membrane which serves a ligand-binding domain as a result of GPCR activation. GPCRs respond to extra cellular signals mediated by a huge diversity of agonists, ranging from proteins to biogenic amines to protons, But All transduce this signal via a mechanism of G-

The production and secretion of glucose from the liver cell to blood stream Action of Epinephrine

Autonomic nervous system

transmission Cell density The sense of smell Behavioral and mood regulation Regulation of immune system activity and inflammation