Sandbox Reserved 1170: Difference between revisions
From Proteopedia
Jump to navigationJump to search
Whitney Hart (talk | contribs) No edit summary |
Whitney Hart (talk | contribs) No edit summary |
||
| Line 10: | Line 10: | ||
=== Binding Sites === | === Binding Sites === | ||
[[Image:HGPR40bind2.png|200 px|right|thumb|Figure 1. Second proposed binding site of hGPR40.]] | [[Image:HGPR40bind2.png|200 px|right|thumb|Figure 1. Second proposed binding site of hGPR40.]] | ||
[[Image:HGPR40bind3.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.<ref name="Srivastava"/> [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 (Figure 1). 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 (Figure 2).<ref name="Srivastava"/> These binding sites could potentially serve as regulation points for hGPR40. Many proteins are regulated by the binding of inhibitors. | [[Image:HGPR40bind3.png|200 px|right|thumb|Figure 2. Third proposed binding site of hGPR40.]][http://metislabs.com/radioligand-binding-assays Radioligand binding studies] identified multiple [https://en.wikipedia.org/wiki/Binding_site binding sites] in hGPR40.<ref name="Srivastava"/> [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 (Figure 1). 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 (Figure 2).<ref name="Srivastava"/> These binding sites could potentially serve as regulation points for hGPR40. Many proteins are regulated by the binding of inhibitors. | ||
=== Charge Network === | === Charge Network === | ||