Sandbox Reserved 1719: Difference between revisions
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=== Toggle switch === | === Toggle switch === | ||
The conserved <scene name='90/904324/5ht2a_toggle_switch/3'>toggle switch</scene> of class A GPCRs functions to activate or inhibit the transduction of the signaling cascade. Typical class A GPCRs contain the conserved ‘toggle switch’ Trp336. In MRGPRX2, this residue is replaced by <scene name='90/904324/Toggle_switch/7'>Gly236</scene>.<ref name="Can"/> By substituting the larger Trp residue with a smaller Gly residue, TM6 is shifted closer to TM3 on the extracellular side of the membrane and contributes to the more tightly packed and shallow binding pocket as compared to other canonical structures. The occluded binding pocket contributes the surface level binding depicted in '''Figure 5''', and allows for a greater variety of ligands interactions with MRGPRX2 as compared to other class A GPCRs, such as [https://proteopedia.org/wiki/index.php/5-hydroxytryptamine_receptor 5-HT<sub>2A</sub>R], [https://proteopedia.org/wiki/index.php/Adrenergic_receptor A<sub>2A</sub>R], and [https://proteopedia.org/wiki/index.php/Beta-2_Adrenergic_Receptor β<sub>2</sub>AR].<ref name="Can"/> | The conserved <scene name='90/904324/5ht2a_toggle_switch/3'>toggle switch</scene> of class A GPCRs functions to activate or inhibit the transduction of the signaling cascade. Typical class A GPCRs contain the conserved ‘toggle switch’ Trp336. In MRGPRX2, this residue is replaced by <scene name='90/904324/Toggle_switch/7'>Gly236</scene>.<ref name="Can"/> By substituting the larger Trp residue with a smaller Gly residue, TM6 is shifted closer to TM3 on the extracellular side of the membrane and contributes to the more tightly packed and shallow binding pocket as compared to other canonical structures. The occluded binding pocket contributes the surface level binding depicted in '''Figure 5''', and allows for a greater variety of ligands interactions with MRGPRX2 as compared to other class A GPCRs, such as [https://proteopedia.org/wiki/index.php/5-hydroxytryptamine_receptor 5-HT<sub>2A</sub>R], [https://proteopedia.org/wiki/index.php/Adrenergic_receptor A<sub>2A</sub>R], and [https://proteopedia.org/wiki/index.php/Beta-2_Adrenergic_Receptor β<sub>2</sub>AR].<ref name="Can"/> | ||
=== PIF/LLF motif === | === PIF/LLF motif === | ||
