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Allosteric Modulation of G Protein Coupled Receptors by Cytoplasmic, Transmembrane and Extracellular Ligands
| Content Provider | Semantic Scholar |
|---|---|
| Author | Yanamala, Naveena Klein-Seetharaman, Judith |
| Copyright Year | 2010 |
| Abstract | 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. |
| Starting Page | 3324 |
| Ending Page | 3342 |
| Page Count | 19 |
| File Format | PDF HTM / HTML |
| Alternate Webpage(s) | http://ftp.ncbi.nlm.nih.gov/pub/pmc/f8/8c/pharmaceuticals-03-03324.PMC3760430.pdf |
| Alternate Webpage(s) | http://www.mdpi.com/1424-8247/3/10/3324/pdf |
| Alternate Webpage(s) | http://www.mdpi.com/1424-8247/3/10/3324/pdf?y=1 |
| PubMed reference number | 24009470 |
| Volume Number | 3 |
| Journal | Pharmaceuticals |
| Language | English |
| Access Restriction | Open |
| Subject Keyword | Allosteric Regulation Binding Sites Class G-Protein-Coupled Receptors Ligand Binding Ligands Small Molecule research grants |
| Content Type | Text |
| Resource Type | Article |
