Sandbox Reserved 1170: Difference between revisions
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=== Binding Sites === | === Binding Sites === | ||
[[Image: | [[Image:HGPR40bind2.png|200 px|right|thumb|Figure 1. Second proposed binding site of hGPR40.]] | ||
[[Image:4phubind3.png|200 px|right|thumb|Figure 2. Third proposed binding site of hGPR40.]][http://metislabs.com/radioligand-binding-assays Radioligand binding studies] identified multiple binding sites in hGPR40. [https://en.wikipedia.org/wiki/Agonist Full agonists] and [https://en.wikipedia.org/wiki/Partial_agonist partial agonists] were shown to bind in separate sites with positive [http://www.britannica.com/science/cooperativity cooperativity].<ref name="Lin">PMID:22859723</ref> The <scene name='72/721541/Tak_binding_site/4'>binding site for the partial agonist TAK-875</scene> has been identified, but other binding sites were hypothesized. TAK-875 binds between transmembrane helices 3, 4, and 5 and underneath ECL2. By visual inspection, a second possible binding site was proposed between transmembrane helices 3, 4, and 5 on the intracellular side of the transmembrane helices. Also by visual inspection, a third possible binding site was proposed between transmembrane helices 1, 2, and 7 on the extracellular side of hGPR40, close to the TAK-875 binding site.<ref name="Srivastava"/> | [[Image:4phubind3.png|200 px|right|thumb|Figure 2. Third proposed binding site of hGPR40.]][http://metislabs.com/radioligand-binding-assays Radioligand binding studies] identified multiple binding sites in hGPR40. [https://en.wikipedia.org/wiki/Agonist Full agonists] and [https://en.wikipedia.org/wiki/Partial_agonist partial agonists] were shown to bind in separate sites with positive [http://www.britannica.com/science/cooperativity cooperativity].<ref name="Lin">PMID:22859723</ref> The <scene name='72/721541/Tak_binding_site/4'>binding site for the partial agonist TAK-875</scene> has been identified, but other binding sites were hypothesized. TAK-875 binds between transmembrane helices 3, 4, and 5 and underneath ECL2. By visual inspection, a second possible binding site was proposed between transmembrane helices 3, 4, and 5 on the intracellular side of the transmembrane helices. Also by visual inspection, a third possible binding site was proposed between transmembrane helices 1, 2, and 7 on the extracellular side of hGPR40, close to the TAK-875 binding site.<ref name="Srivastava"/> | ||
