Sandbox Reserved 1652: Difference between revisions
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However, the orientation of <scene name='86/868185/L515/1'>L515</scene> and <scene name='86/868185/M547/1'>M547</scene> makes this region of the vanilloid pocket narrow, which considerably limits the nature of the fragments tolerated. | However, the orientation of <scene name='86/868185/L515/1'>L515</scene> and <scene name='86/868185/M547/1'>M547</scene> makes this region of the vanilloid pocket narrow, which considerably limits the nature of the fragments tolerated. | ||
The aromatic part of resiniferatoxin is located deeper in the sub-pocket near <scene name='86/868185/Y511/2'>Y511</scene> and is oriented almost parallel to the aromatic side chain of <scene name='86/868185/Y511/2'>Y511</scene>, so it establishes a strong interaction π-π. The aromatic hydroxyl and methoxy groups of the RTX form strong hydrogen bonds with <scene name='86/868185/E570/2'>E570</scene>, <scene name='86/868185/R557/1'>R557</scene> and S512. The ester group is linked to <scene name='86/868185/Y511/2'>Y511</scene> and T550 by hydrogen bonds.<ref>K. Elokely et al., « Understanding TRPV1 activation by ligands: Insights from the binding modes of capsaicin and resiniferatoxin », Proc. Natl. Acad. Sci., vol. 113, no 2, p. E137‑E145, janv. 2016, doi:10.1073/pnas.1517288113.</ref> | The aromatic part of resiniferatoxin is located deeper in the sub-pocket near <scene name='86/868185/Y511/2'>Y511</scene> and is oriented almost parallel to the aromatic side chain of <scene name='86/868185/Y511/2'>Y511</scene>, so it establishes a strong interaction π-π. The aromatic hydroxyl and methoxy groups of the RTX form strong hydrogen bonds with <scene name='86/868185/E570/2'>E570</scene>, <scene name='86/868185/R557/1'>R557</scene> and <scene name='86/868185/S512/1'>S512</scene>. The ester group is linked to <scene name='86/868185/Y511/2'>Y511</scene> and T550 by hydrogen bonds.<ref>K. Elokely et al., « Understanding TRPV1 activation by ligands: Insights from the binding modes of capsaicin and resiniferatoxin », Proc. Natl. Acad. Sci., vol. 113, no 2, p. E137‑E145, janv. 2016, doi:10.1073/pnas.1517288113.</ref> | ||
=== Regulation === | === Regulation === | ||
