Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11
G protein coupled receptors (GPCRs) are one of the major classes of cell surface receptors and are associated with a group of G proteins consisting of three subunits termed alpha, beta, and gamma. G proteins are classified into four families according to their α subunit; Gαi, Gαs, Gα12/13, and Gαq....
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Frontiers Media S.A.
2015
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| Online Access: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4671355/ |
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pubmed-46713552015-12-10 Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 Kamato, Danielle Thach, Lyna Bernard, Rebekah Chan, Vincent Zheng, Wenhua Kaur, Harveen Brimble, Margaret Osman, Narin Little, Peter J. Cardiovascular Medicine G protein coupled receptors (GPCRs) are one of the major classes of cell surface receptors and are associated with a group of G proteins consisting of three subunits termed alpha, beta, and gamma. G proteins are classified into four families according to their α subunit; Gαi, Gαs, Gα12/13, and Gαq. There are several downstream pathways of Gαq of which the best known is upon activation via guanosine triphosphate (GTP), Gαq activates phospholipase Cβ, hydrolyzing phosphatidylinositol 4,5-biphosphate into diacylglycerol and inositol triphosphate and activating protein kinase C and increasing calcium efflux from the endoplasmic reticulum. Although G proteins, in particular, the Gαq/11 are central elements in GPCR signaling, their actual roles have not yet been thoroughly investigated. The lack of research of the role on Gαq/11 in cell biology is partially due to the obscure nature of the available pharmacological agents. YM-254890 is the most useful Gαq-selective inhibitor with antiplatelet, antithrombotic, and thrombolytic effects. YM-254890 inhibits Gαq signaling pathways by preventing the exchange of guanosine diphosphate for GTP. UBO-QIC is a structurally similar compound to YM-254890, which can inhibit platelet aggregation and cause vasorelaxation in rats. Many agents are available for the study of signaling downstream of Gαq/11. The role of G proteins could potentially represent a novel therapeutic target. This review will explore the range of pharmacological and molecular tools available for the study of the role of Gαq/11 in GPCR signaling. Frontiers Media S.A. 2015-03-24 /pmc/articles/PMC4671355/ /pubmed/26664886 http://dx.doi.org/10.3389/fcvm.2015.00014 Text en Copyright © 2015 Kamato, Thach, Bernard, Chan, Zheng, Kaur, Brimble, Osman and Little. http://creativecommons.org/licenses/by/4.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms. |
| repository_type |
Open Access Journal |
| institution_category |
Foreign Institution |
| institution |
US National Center for Biotechnology Information |
| building |
NCBI PubMed |
| collection |
Online Access |
| language |
English |
| format |
Online |
| author |
Kamato, Danielle Thach, Lyna Bernard, Rebekah Chan, Vincent Zheng, Wenhua Kaur, Harveen Brimble, Margaret Osman, Narin Little, Peter J. |
| spellingShingle |
Kamato, Danielle Thach, Lyna Bernard, Rebekah Chan, Vincent Zheng, Wenhua Kaur, Harveen Brimble, Margaret Osman, Narin Little, Peter J. Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 |
| author_facet |
Kamato, Danielle Thach, Lyna Bernard, Rebekah Chan, Vincent Zheng, Wenhua Kaur, Harveen Brimble, Margaret Osman, Narin Little, Peter J. |
| author_sort |
Kamato, Danielle |
| title |
Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 |
| title_short |
Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 |
| title_full |
Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 |
| title_fullStr |
Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 |
| title_full_unstemmed |
Structure, Function, Pharmacology, and Therapeutic Potential of the G Protein, Gα/q,11 |
| title_sort |
structure, function, pharmacology, and therapeutic potential of the g protein, gα/q,11 |
| description |
G protein coupled receptors (GPCRs) are one of the major classes of cell surface receptors and are associated with a group of G proteins consisting of three subunits termed alpha, beta, and gamma. G proteins are classified into four families according to their α subunit; Gαi, Gαs, Gα12/13, and Gαq. There are several downstream pathways of Gαq of which the best known is upon activation via guanosine triphosphate (GTP), Gαq activates phospholipase Cβ, hydrolyzing phosphatidylinositol 4,5-biphosphate into diacylglycerol and inositol triphosphate and activating protein kinase C and increasing calcium efflux from the endoplasmic reticulum. Although G proteins, in particular, the Gαq/11 are central elements in GPCR signaling, their actual roles have not yet been thoroughly investigated. The lack of research of the role on Gαq/11 in cell biology is partially due to the obscure nature of the available pharmacological agents. YM-254890 is the most useful Gαq-selective inhibitor with antiplatelet, antithrombotic, and thrombolytic effects. YM-254890 inhibits Gαq signaling pathways by preventing the exchange of guanosine diphosphate for GTP. UBO-QIC is a structurally similar compound to YM-254890, which can inhibit platelet aggregation and cause vasorelaxation in rats. Many agents are available for the study of signaling downstream of Gαq/11. The role of G proteins could potentially represent a novel therapeutic target. This review will explore the range of pharmacological and molecular tools available for the study of the role of Gαq/11 in GPCR signaling. |
| publisher |
Frontiers Media S.A. |
| publishDate |
2015 |
| url |
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4671355/ |
| _version_ |
1613510146125725696 |