Sandbox Reserved 1160: Difference between revisions
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The mGlu5 TMD contains 7 <scene name='72/721531/Protien_7_helices/4'> alpha helices</scene> that spans the membrane. The protein was crystallized with <scene name='72/721531/Protien_clean_sce/5'>Oleic acid</scene>. On the top portion of the protein several critical extracellular loops connect the TMD to the CRD. The binding pocket can be found near the middle of the protein, and is mainly comprised of hydrophobic amino acids with more polar amino acids found in the upper and lower portions of the binding site. Inserted into the biding pocket is the negative allosteric modulator [http://www.en.wikipedia.org/wiki/Mavoglurant mavoglurant]. The TMD is in an inactive conformation, since mavoglurant is bound. Also, the deletion of the flexible domains leaves the mGlu5 receptor unable to bind to its [[GPCR]]. The inactive state is maintained by multiple ionic locks whose positions determine the active versus inactive conformation. | The mGlu5 TMD contains 7 <scene name='72/721531/Protien_7_helices/4'> alpha helices</scene> that spans the membrane. The protein was crystallized with <scene name='72/721531/Protien_clean_sce/5'>Oleic acid</scene>. On the top portion of the protein several critical extracellular loops connect the TMD to the CRD. The binding pocket can be found near the middle of the protein, and is mainly comprised of hydrophobic amino acids with more polar amino acids found in the upper and lower portions of the binding site. Inserted into the biding pocket is the negative allosteric modulator [http://www.en.wikipedia.org/wiki/Mavoglurant mavoglurant]. The TMD is in an inactive conformation, since mavoglurant is bound. Also, the deletion of the flexible domains leaves the mGlu5 receptor unable to bind to its [[GPCR]]. The inactive state is maintained by multiple ionic locks whose positions determine the active versus inactive conformation. | ||
=== Extracellular Domain === | === Extracellular Domain === | ||
These are the <scene name='72/721532/ | These are the <scene name='72/721532/Ecl_trail_7/2'>Extracellular Loops</scene> with extracellular loops (ECLs) 1, 2, and 3 highlighted in purple. Additionally in the ECL domain, a <scene name='72/721532/Ecl_trail_1/6'>disulfide bond</scene> is attached to both Helix 3 and the amino acid chain between Helix 5 and the N terminus. The disulfide bond is highlighted in yellow, and it is conserved in all classes of glutamate receptor 5 transmembrane domains<ref name="Wu" />. | ||
=== Binding Pocket === | === Binding Pocket === | ||
[[Image: Organic with clipped surface.png|200 px|left|thumb|Cross section view of mavoglurant in the binding pocket]] | [[Image: Organic with clipped surface.png|200 px|left|thumb|Cross section view of mavoglurant in the binding pocket]] | ||
