Sandbox reserved 915: Difference between revisions
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Representation of the <scene name='58/580298/Overall_structure/3'>Overall Structure</scene> of MGL. | Representation of the <scene name='58/580298/Overall_structure/3'>Overall Structure</scene> of MGL. | ||
MGL has eight-stranded β-sheet protein fold with seven parallel and one <scene name='58/580299/Beta_sheets/1'> antiparallel strand </scene> (Bertrand et al. 2010). | MGL has eight-stranded β-sheet protein fold with seven parallel and one <scene name='58/580299/Beta_sheets/1'> antiparallel strand </scene> (Bertrand et al. 2010). The β-sheets are surrounded by α-helices. The combination of the α-helices and β-sheets are able to provide a stable scaffold for the active sites within MGL (Bertrand et al. 2010). Within the main domain of MGL is the conserved catalytic triad (Bertrand et al. 2010). | ||
== Catalytic triad == | == Catalytic triad == | ||
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==Ligand Binding Site== | ==Ligand Binding Site== | ||
[[Image:Overall_ligand.png|left|200px|thumb|Ligand within the Overall Structure of MGL]] | [[Image:Overall_ligand.png|left|200px|thumb|Ligand within the Overall Structure of MGL]] | ||
The ligand binding pocket of MGL has a large hydrophobic region with a polar bottom (Bertrand et al. 2010). Bertrand found that in MGL the binding pocket is not adjusted to the ligands shape. 2-archidonylglycerol are ligands for cannabinoid receptors (Clemente et al. 2012). Inhibition of MGL leads to increase in 2-AG levels since AG is broken down by MGL (Clemente et al. 2012). Through covalent interactions with a Cys residue, NAM, one of the many possible inhibitors, is able to inhibit MGL (Bertrand et al. 2010). <scene name='58/580298/Ligand/1'>Lignad binding site</scene> | The ligand binding pocket of MGL has a large hydrophobic region with a polar bottom (Bertrand et al. 2010). The entrance of the binding pocket for MGL contains a lid, which is very flexible (Bertrand et al. 2010). Bertrand found that in MGL the binding pocket is not adjusted to the ligands shape. 2-archidonylglycerol are ligands for cannabinoid receptors (Clemente et al. 2012). Inhibition of MGL leads to increase in 2-AG levels since AG is broken down by MGL (Clemente et al. 2012). Through covalent interactions with a Cys residue, NAM, one of the many possible inhibitors, is able to inhibit MGL (Bertrand et al. 2010). <scene name='58/580298/Ligand/1'>Lignad binding site</scene> | ||
==Overall Reaction== | ==Overall Reaction== | ||
[[Image:Reaction.PNG|350px|thumb|Overall reaction representing the hydrolysis of 2-AG by MGL]] | [[Image:Reaction.PNG|350px|thumb|Overall reaction representing the hydrolysis of 2-AG by MGL]] | ||
