Sandbox Reserved 919
From Proteopedia
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==Introduction== | ==Introduction== | ||
[[Image:MGLProt.jpg|300 px|right|thumb|Monomer of MGL created in PYMOL (PDB:3PE6)]] | [[Image:MGLProt.jpg|300 px|right|thumb|Monomer of MGL created in PYMOL (PDB:3PE6)]] | ||
| - | '''Monoglyceride Lipase''' ('''MGL''', '''MAGL''', '''MGLL''') is a 33 kDa [http://en.wikipedia.org/wiki/Protein protein] found mostly in the cell membrane. It is a [http://en.wikipedia.org/wiki/Serine_hydrolase serine hydrolase] enzyme that exhibits an [http://en.wikipedia.org/wiki/Alpha/beta_hydrolase_fold α/β hydrolase fold]. In addition, MGL possesses amphitropic character, where the area around the active site of MGL is polar while the site itself is non-polar. This characteristic allows the protein to be present both in the membrane and in the cytosol. MGL plays a key role in the hydrolysis of 2-arachidonoylglycerol (2-AG), an endocannabinoid produced by the the central nervous system. The α/β fold allows 2-AG to selectively bind to the active site and be broken down into arachidonic acid and glycerol. Upon breakdown, glycerol leaves via an "exit tunnel" found perpendicular to the α/β fold. 2-AG itself has been found to possess anti-nociceptive, immunomodulatory, anti-inflammatory and tumor-reductive character when it binds to cannabinoid receptors. Due to the vast medical and therapeutic utility of 2-AG, the inhibition of MGL is a high interest target in pharmaceutical research. <ref> PMID:19962385 </ref> | + | '''Monoglyceride Lipase''' ('''MGL''', '''MAGL''', '''MGLL''') is a 33 kDa [http://en.wikipedia.org/wiki/Protein protein] found mostly in the cell membrane. It is a [http://en.wikipedia.org/wiki/Serine_hydrolase serine hydrolase] enzyme that exhibits an [http://en.wikipedia.org/wiki/Alpha/beta_hydrolase_fold α/β hydrolase fold]. In addition, MGL possesses amphitropic character, where the area around the active site of MGL is polar while the site itself is non-polar. This characteristic allows the protein to be present both in the membrane and in the cytosol. MGL plays a key role in the hydrolysis of 2-arachidonoylglycerol (2-AG), an endocannabinoid produced by the the central nervous system. The α/β fold allows 2-AG to selectively bind to the active site and be broken down into arachidonic acid and glycerol. Upon breakdown, glycerol leaves via an "exit tunnel" found perpendicular to the α/β fold. 2-AG itself has been found to possess anti-nociceptive, immunomodulatory, anti-inflammatory and tumor-reductive character when it binds to cannabinoid receptors. Due to the vast medical and therapeutic utility of 2-AG, the inhibition of MGL is a high interest target in pharmaceutical research. <ref name="bert"> PMID:19962385 </ref> |
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==Structure== | ==Structure== | ||
| - | <scene name='57/573133/Generic_monomer/3'> | + | Bertrand, et al, created the first crystal structure of MGL in its <scene name='57/573133/Generic_monomer/3'>apo form</scene>. MGL is a part of the α-β hydrolase family of enzymes. This category of proteins contains an eight-stranded [http://en.wikipedia.org/wiki/Beta_sheet beta sheet], specifically containing seven parallel and one antiparallel constituent strand (<scene name='57/573134/Beta_sheet/1'>beta sheets</scene>), surrounded by [http://en.wikipedia.org/wiki/Alpha_helix alpha-helices]. <ref name="bert" /> |
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===Active Site=== | ===Active Site=== | ||
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Monoglyceride Lipase
Introduction
Image:MGLProt.jpg
Monomer of MGL created in PYMOL (PDB:3PE6)
Monoglyceride Lipase (MGL, MAGL, MGLL) is a 33 kDa protein found mostly in the cell membrane. It is a serine hydrolase enzyme that exhibits an α/β hydrolase fold. In addition, MGL possesses amphitropic character, where the area around the active site of MGL is polar while the site itself is non-polar. This characteristic allows the protein to be present both in the membrane and in the cytosol. MGL plays a key role in the hydrolysis of 2-arachidonoylglycerol (2-AG), an endocannabinoid produced by the the central nervous system. The α/β fold allows 2-AG to selectively bind to the active site and be broken down into arachidonic acid and glycerol. Upon breakdown, glycerol leaves via an "exit tunnel" found perpendicular to the α/β fold. 2-AG itself has been found to possess anti-nociceptive, immunomodulatory, anti-inflammatory and tumor-reductive character when it binds to cannabinoid receptors. Due to the vast medical and therapeutic utility of 2-AG, the inhibition of MGL is a high interest target in pharmaceutical research. [1]
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References
- ↑ 1.0 1.1 Bertrand T, Auge F, Houtmann J, Rak A, Vallee F, Mikol V, Berne PF, Michot N, Cheuret D, Hoornaert C, Mathieu M. Structural basis for human monoglyceride lipase inhibition. J Mol Biol. 2010 Feb 26;396(3):663-73. Epub 2009 Dec 3. PMID:19962385 doi:10.1016/j.jmb.2009.11.060
