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From Proteopedia
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| - | G-Protein Coupled Receptors (GPCR), also known as 7 transmembrane receptors [because of its 7 constituent alpha helices] are the largest groups of transmembrane protein receptors in eukaryotes. There are many different classes GPCRs depending on their functionality. These include the classes A, B, C, D, E, AND F. Beta adrenergic receptors fall the class C with other metabotropic hormones. All studied GPCRs have a particular structure that can be subdivided into; the amino-terminal extracellular domain, the three extracellular loops (EC1), (EC2), (EC3), the seven spanning transmembrane domains (7TM), three intracellular domains (IC1, ...IC3) and the carboxyl-terminal intracellular domain. The binding of the receptor | + | G-Protein Coupled Receptors (GPCR), also known as 7 transmembrane receptors [because of its 7 constituent alpha helices] are the largest groups of transmembrane protein receptors in eukaryotes. There are many different classes GPCRs depending on their functionality. These include the classes A, B, C, D, E, AND F. Beta adrenergic receptors fall the class C with other metabotropic hormones. All studied GPCRs have a particular structure that can be subdivided into; the amino-terminal extracellular domain, the three extracellular loops (EC1), (EC2), (EC3), the seven spanning transmembrane domains (7TM), three intracellular domains (IC1, ...IC3) and the carboxyl-terminal intracellular domain. The binding of the receptor to a ligand causes a structural change in the intracellular domains that leads to the exchange of GDP for GTP. |
'''FUNCTIONS''' | '''FUNCTIONS''' | ||
GPCRs act as a bridge and communicate the conditions of the cell to the nucleus to induce transcription or affect the processivity of catalytic pathway. They bind to wide varieties of ligands such as epinephrine, glucagon, insulin, light, and sugars. Upon binding the ligand epinephrine, it causes a conformational change that leads to the exchange of the Guanine nucleotide (GDP to GTP) and that mechanism "turns" the switch on. The apha subunit then dissociate from the beta and gamma subunits and activates adenylate cyclase which makes cAMP. The cAMP activates Protein Kinase A by binding to its regulatory subunits, and that releases the catalytic subunits to further phosphorylate other proteins in the cell. | GPCRs act as a bridge and communicate the conditions of the cell to the nucleus to induce transcription or affect the processivity of catalytic pathway. They bind to wide varieties of ligands such as epinephrine, glucagon, insulin, light, and sugars. Upon binding the ligand epinephrine, it causes a conformational change that leads to the exchange of the Guanine nucleotide (GDP to GTP) and that mechanism "turns" the switch on. The apha subunit then dissociate from the beta and gamma subunits and activates adenylate cyclase which makes cAMP. The cAMP activates Protein Kinase A by binding to its regulatory subunits, and that releases the catalytic subunits to further phosphorylate other proteins in the cell. | ||
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| + | Manu GPCRs have become targets of many pharmaceutical drugs because they control many metabolic activities in the cell. | ||
Revision as of 04:32, 21 November 2018
| This Sandbox is Reserved from November 5 2018 through January 1, 2019 for use in the course "CHEM 4923: Senior Project taught by Christina R. Bourne at the University of Oklahoma, Norman, USA. This reservation includes Sandbox Reserved 1471 through Sandbox Reserved 1478. |
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References
- ↑ Hanson, R. M., Prilusky, J., Renjian, Z., Nakane, T. and Sussman, J. L. (2013), JSmol and the Next-Generation Web-Based Representation of 3D Molecular Structure as Applied to Proteopedia. Isr. J. Chem., 53:207-216. doi:http://dx.doi.org/10.1002/ijch.201300024
- ↑ Herraez A. Biomolecules in the computer: Jmol to the rescue. Biochem Mol Biol Educ. 2006 Jul;34(4):255-61. doi: 10.1002/bmb.2006.494034042644. PMID:21638687 doi:10.1002/bmb.2006.494034042644
THE GENUIS OF GPCRs.
INTRODUCTION.
Within the course of our daily activities, we experience several situations that cause us to jump on our feet and also, initiate some kind of response to these situations. Our bodies have an outstanding way of preparing us for such events as to whether flee or fight and it does this by making energy in the form of glucose available in the blood to support our reactions to these events. Our response is effectively mediated through reflex actions which are propagated through networks of neurons that are wired all over our body and eventually to the brain. One of the neurotransmitters produced through the coordination of these neuronal networks is epinephrine. Epinephrine serves as a ligand that bind to a transmembrane protein called GPCR and initiates a sequence of cascading pathways further downstream, that eventually results in the release of glucose into the blood to support the response we carry out.
'STRUCTURE HIGHLIGHTS'
G-Protein Coupled Receptors (GPCR), also known as 7 transmembrane receptors [because of its 7 constituent alpha helices] are the largest groups of transmembrane protein receptors in eukaryotes. There are many different classes GPCRs depending on their functionality. These include the classes A, B, C, D, E, AND F. Beta adrenergic receptors fall the class C with other metabotropic hormones. All studied GPCRs have a particular structure that can be subdivided into; the amino-terminal extracellular domain, the three extracellular loops (EC1), (EC2), (EC3), the seven spanning transmembrane domains (7TM), three intracellular domains (IC1, ...IC3) and the carboxyl-terminal intracellular domain. The binding of the receptor to a ligand causes a structural change in the intracellular domains that leads to the exchange of GDP for GTP.
FUNCTIONS
GPCRs act as a bridge and communicate the conditions of the cell to the nucleus to induce transcription or affect the processivity of catalytic pathway. They bind to wide varieties of ligands such as epinephrine, glucagon, insulin, light, and sugars. Upon binding the ligand epinephrine, it causes a conformational change that leads to the exchange of the Guanine nucleotide (GDP to GTP) and that mechanism "turns" the switch on. The apha subunit then dissociate from the beta and gamma subunits and activates adenylate cyclase which makes cAMP. The cAMP activates Protein Kinase A by binding to its regulatory subunits, and that releases the catalytic subunits to further phosphorylate other proteins in the cell.
"DISEASE"
Manu GPCRs have become targets of many pharmaceutical drugs because they control many metabolic activities in the cell.
