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===Inhibition of MGL=== | ===Inhibition of MGL=== | ||
The importance of inhibiting Monoglyceride lipase is to keep it from breaking down 2-arachidonoyl glycerol. When 2-Ag is broken down it is not able to suppress pain and depression brain functions that human beings experience. N-arachidonyl maleimide (NAM) is one inhibitor of MGL that reacts with the amino acid <scene name='58/580298/Cys252/1'>Cys252</scene>. This Cysteine is buried in the active site near the catalytic serine | The importance of inhibiting Monoglyceride lipase is to keep it from breaking down 2-arachidonoyl glycerol. When 2-Ag is broken down it is not able to suppress pain and depression brain functions that human beings experience. N-arachidonyl maleimide (NAM) is one inhibitor of MGL that reacts with the amino acid <scene name='58/580298/Cys252/1'>Cys252</scene>. [[Image:NAM.png]] | ||
This Cysteine is buried in the active site near the catalytic serine and functions by sterically clashing with the natural ligand. A possible conformational change to Cys252 upon the binding of NAM could also lead to an inactive form of MGL. | |||
MGL is also inhibited by being in complex with SAR629 that is covalently bound to the catalytic Ser132. SAR629 adopts a Y shape and interacts with the MGL by hydrophobic interactions, with a few polar interactions as well. With SAR629 interacting with the catalytic triad it inhibits the triad from breaking down 2-AG and it interacting with MGL makes it inactive <ref name="Bertrand" /> | MGL is also inhibited by being in complex with SAR629 that is covalently bound to the catalytic Ser132. SAR629 adopts a Y shape and interacts with the MGL by hydrophobic interactions, with a few polar interactions as well. With SAR629 interacting with the catalytic triad it inhibits the triad from breaking down 2-AG and it interacting with MGL makes it inactive <ref name="Bertrand" /> | ||