human-MGLL

 
Homo sapiens (Human) Monoglyceride lipase (MAGL) lysophospholipase homolog

Comment
Human monoacylglycerol lipase (hMAGL Monoglyceride lipase MGLL) converts monoacylglycerides to free fatty acids and glycerol. Hydrolyzes the endocannabinoid 2-arachidonoylglycerol, and thereby contributes to the regulation of endocannabinoid signaling, nociperception and perception of pain. Regulates the levels of fatty acids that serve as signaling molecules and promote cancer cell migration, invasion and tumor growth


Relationship
Block X
Homo sapiens position in NCBI Life Tree :
N link to NCBI taxonomic web page and E link to ESTHER gene locus found in this strain.
> cellular organisms: N E > Eukaryota: N E > Opisthokonta: N E > Metazoa: N E > Eumetazoa: N E > Bilateria: N E > Deuterostomia: N E > Chordata: N E > Craniata: N E > Vertebrata: N E > Gnathostomata: N E > Teleostomi: N E > Euteleostomi: N E > Sarcopterygii: N E > Dipnotetrapodomorpha: N E > Tetrapoda: N E > Amniota: N E > Mammalia: N E > Theria: N E > Eutheria: N E > Boreoeutheria: N E > Euarchontoglires: N E > Primates: N E > Haplorrhini: N E > Simiiformes: N E > Catarrhini: N E > Hominoidea: N E > Hominidae: N E > Homininae: N E > Homo: N E > Homo sapiens: N E

Molecular evidence
Database
No mutation
15 structures (e.g. : 8AQF, 7L4W, 7L50... more)
No kinetic

Substrate: PGE2-glyceryl-ester , AHMMCE , 2-Arachidonylglycerol , Arachidonoyl-1-thioglycerol ,
Inhibitor: NSD1819 , MAGL17b , YH149 , ZYH-deriv-F , XP7-7L4U , SCHEMBL19421119 , SCHEMBL19421059 , SCHEMBL19834081 , Cpd37-Fluoroindol-carbamate , Octhilinone , Octyl-Benzisothiazolinone , Benzisothiazolinone-13 , T-401 , ZINC12863377 , ZINC24092691 , (R)-3t , 5ZUN-3l , PF-06795071 , 2-methyl-pentane-2,4-diol , 1-(2-Morpholine-acetamido)-tanshinone-IIA , UCM-03025 , JJKK-048 , 6AX1-cp3 , Pristimerin , URB602 , AM9928 , AM6580 , N-Arachidonylmaleimide , SA-57 , MJN110 , MGL-Inhibitor-26 , MGL-Inhibitor-21 , CAY10499 , JW651 , JZL195 , JZL184 , F4P , 64D , ABX-1431 , ZYH , KML29 , AM6701 , LY2183240 , URB597 ,
>3 Genbank links 12 more: U67963, CR456835, AJ270950
>3 UniProt links 1 more: Q99685, Q2VYF8, B2ZGL7
>3 Structure links 12 more: 8AQF, 7L4W, 7L50
>3 UniProtTrembl links 4 more: Q99685, Q2VYF8, B2ZGL7
>3 Interpro links 4 more: Q99685, Q2VYF8, B2ZGL7
>3 Prodom links 4 more: Q99685, Q2VYF8, B2ZGL7
>3 Pfam links 4 more: Q99685, Q2VYF8, B2ZGL7
>3 PIRSF links 4 more: Q99685, Q2VYF8, B2ZGL7
>3 SUPERFAM links 4 more: Q99685, Q2VYF8, B2ZGL7
>3 QuickSwissBlast links 4 more: Q99685, Q2VYF8, B2ZGL7
1 EntrezGene : 11343
1 SNP : 11343
1 UniGene : 277035
1 HUGO HGNC : 17038
1 IUPHAR : 1399
1 OMIM : 609699
1 Ensembl : ENSG00000074416
 
Sequence
Graphical view for this peptide sequence: human-MGLL
Colored MSA for Monoglyceridelipase_lysophospholip (raw)
MPEESSPRRTPQSIPYQDLPHLVNADGQYLFCRYWKPTGTPKALIFVSHG
AGEHSGRYEELARMLMGLDLLVFAHDHVGHGQSEGERMVVSDFHVFVRDV
LQHVDSMQKDYPGLPVFLLGHSMGGAIAILTAAERPGHFAGMVLISPLVL
ANPESATTFKVLAAKVLNLVLPNLSLGPIDSSVLSRNKTEVDIYNSDPLI
CRAGLKVCFGIQLLNAVSRVERALPKLTVPFLLLQGSADRLCDSKGAYLL
MELAKSQDKTLKIYEGAYHVLHKELPEVTNSVFHEINMWVSQRTATAGTA
SPP
Legend This sequence has been compared to family alignement (MSA)
red => minority aminoacid
blue => majority aminoacid
color intensity => conservation rate
title => sequence position(MSA position)aminoacid rate
Catalytic site
Catalytic site in the MSA

MPEESSPRRTPQSIPYQDLPHLVNADGQYLFCRYWKPTGTPKALIFVSHG
AGEHSGRYEELARMLMGLDLLVFAHDHVGHGQSEGERMVVSDFHVFVRDV
LQHVDSMQKDYPGLPVFLLGHSMGGAIAILTAAERPGHFAGMVLISPLVL
ANPESATTFKVLAAKVLNLVLPNLSLGPIDSSVLSRNKTEVDIYNSDPLI
CRAGLKVCFGIQLLNAVSRVERALPKLTVPFLLLQGSADRLCDSKGAYLL
MELAKSQDKTLKIYEGAYHVLHKELPEVTNSVFHEINMWVSQRTATAGTA
SPP

no DNA




References
59 more
    Title: Inhibition of triple negative breast cancer-associated inflammation, tumor growth and brain colonization by targeting monoacylglycerol lipase
    Benchama O, Tyukhtenko S, Malamas MS, Williams MK, Makriyannis A, Avraham HK
    Ref: Sci Rep, 12:5328, 2022 : PubMed

            

    Title: MAGL inhibitor NanoMicellar formulation (MAGL-NanoMicellar) for the development of an antiglaucoma eye drop
    Chetoni P, Burgalassi S, Zucchetti E, Granchi C, Minutolo F, Tampucci S, Monti D
    Ref: Int J Pharm, :122078, 2022 : PubMed

            

    Title: Mechanistic Modeling of Monoglyceride Lipase Covalent Modification Elucidates the Role of Leaving Group Expulsion and Discriminates Inhibitors with High and Low Potency
    Galvani F, Scalvini L, Rivara S, Lodola A, Mor M
    Ref: J Chem Inf Model, :, 2022 : PubMed

            


Other Papers


Send your questions or comments to :
Mail to: Nicolas Lenfant, Thierry Hotelier, Yves Bourne, Pascale Marchot and Arnaud Chatonnet.
Please cite: Lenfant 2013 Nucleic.Acids.Res. or Marchot Chatonnet 2012 Prot.Pept Lett.
For technical information about these pages see:
ESTHER Home Page and ACEDB Home Page
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