Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands
G protein coupled receptors (GPCRs) bind diverse classes of ligands, and depending on the receptor, these may bind in their transmembrane or the extracellular domains, demonstrating the principal ability of GPCRs to bind ligand in either domains. Most recently, it was also observed that small molecu...
| Main Authors: | , |
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| Format: | Article |
| Language: | English |
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MDPI AG
2010-10-01
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| Series: | Pharmaceuticals |
| Subjects: | |
| Online Access: | http://www.mdpi.com/1424-8247/3/10/3324/ |
| _version_ | 1818208145380474880 |
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| author | Naveena Yanamala Judith Klein-Seetharaman |
| author_facet | Naveena Yanamala Judith Klein-Seetharaman |
| author_sort | Naveena Yanamala |
| collection | DOAJ |
| description | G protein coupled receptors (GPCRs) bind diverse classes of ligands, and depending on the receptor, these may bind in their transmembrane or the extracellular domains, demonstrating the principal ability of GPCRs to bind ligand in either domains. Most recently, it was also observed that small molecule ligands can bind in the cytoplasmic domain, and modulate binding and response to extracellular or transmembrane ligands. Thus, all three domains in GPCRs are potential sites for allosteric ligands, and whether a ligand is allosteric or orthosteric depends on the receptor. Here, we will review the evidence supporting the presence of putative binding pockets in all three domains of GPCRs and discuss possible pathways of communication between these pockets. |
| first_indexed | 2024-12-12T04:40:10Z |
| format | Article |
| id | doaj.art-ee9c1f9e4525416b9137586b3ea18619 |
| institution | Directory Open Access Journal |
| issn | 1424-8247 |
| language | English |
| last_indexed | 2024-12-12T04:40:10Z |
| publishDate | 2010-10-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceuticals |
| spelling | doaj.art-ee9c1f9e4525416b9137586b3ea186192022-12-22T00:37:51ZengMDPI AGPharmaceuticals1424-82472010-10-013103324334210.3390/ph3103324Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular LigandsNaveena YanamalaJudith Klein-SeetharamanG protein coupled receptors (GPCRs) bind diverse classes of ligands, and depending on the receptor, these may bind in their transmembrane or the extracellular domains, demonstrating the principal ability of GPCRs to bind ligand in either domains. Most recently, it was also observed that small molecule ligands can bind in the cytoplasmic domain, and modulate binding and response to extracellular or transmembrane ligands. Thus, all three domains in GPCRs are potential sites for allosteric ligands, and whether a ligand is allosteric or orthosteric depends on the receptor. Here, we will review the evidence supporting the presence of putative binding pockets in all three domains of GPCRs and discuss possible pathways of communication between these pockets.http://www.mdpi.com/1424-8247/3/10/3324/rhodopsinmetabotropic glutamate receptorsallosteric networkcommunicationmembrane proteins |
| spellingShingle | Naveena Yanamala Judith Klein-Seetharaman Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands Pharmaceuticals rhodopsin metabotropic glutamate receptors allosteric network communication membrane proteins |
| title | Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands |
| title_full | Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands |
| title_fullStr | Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands |
| title_full_unstemmed | Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands |
| title_short | Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands |
| title_sort | allosteric modulation of g protein coupled receptors by cytoplasmic transmembrane and extracellular ligands |
| topic | rhodopsin metabotropic glutamate receptors allosteric network communication membrane proteins |
| url | http://www.mdpi.com/1424-8247/3/10/3324/ |
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