Sandbox Reserved 1160: Difference between revisions
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=== Binding Pocket === | === Binding Pocket === | ||
[[Image: Organic with clipped surface.png|200 px|left|thumb|'''Figure 2.''' Mavolugarent in its binding pocket of the 7TM region of mGLu5 Class C receptor. The binding pocket's surface is clipped in black with the substrate, mavolugarent, in red. The rest of the protein is colored in green. The binding pocket is present in the 7 Helix Transmembrane Domain that would be present in the phosolipid bilayer appearing as an intergral protein. The presence of mavolugarent inhibits the function of the metabotropic glutamate receptor.]] | [[Image: Organic with clipped surface.png|200 px|left|thumb|'''Figure 2.''' Mavolugarent in its binding pocket of the 7TM region of mGLu5 Class C receptor. The binding pocket's surface is clipped in black with the substrate, mavolugarent, in red. The rest of the protein is colored in green. The binding pocket is present in the 7 Helix Transmembrane Domain that would be present in the phosolipid bilayer appearing as an intergral protein. The presence of mavolugarent inhibits the function of the metabotropic glutamate receptor.]] | ||
The binding pocket, not to be confused with the glutamate binding site, represents an useful source of regulatory control. The binding pocket is only accessible by a relatively narrow (7 Å) <scene name='72/721531/Protien_sur/4'>entrance</scene><ref name="Dore" />. This small entrance severely restricts the access of both positive and negative allosteric regulators. | The binding pocket, not to be confused with the glutamate binding site, represents an useful source of regulatory control. The binding pocket is only accessible by a relatively narrow (7 Å) <scene name='72/721531/Protien_sur/4'>entrance</scene><ref name="Dore" />. This small entrance severely restricts the access of both positive and negative allosteric regulators. One such regulator, <scene name='72/721531/Mavo/2'>mavoglurant</scene>, is a relatively small molecule that can travel through the entrance and fit between the helices of the mGlu5 receptor. Mavoglurant acts as a negative allosteric modulator of the mGlu5 receptor. Mavoglurant is a relatively hydrophobic molecule, which compliments the largely hydrophobic nature of the interior of mGlu5. The carbamate tail and hydroxyl group of mavoglurant will also interact with several key amino acids in the binding site of mGlu5. | ||
One such regulator, <scene name='72/721531/Mavo/2'>mavoglurant</scene>, is a | |||
Important Amino Acids<ref name="Dore" />: | Important Amino Acids<ref name="Dore" />: | ||
