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Literature summary for 3.2.1.45 extracted from

  • Patnaik, S.; Zheng, W.; Choi, J.H.; Motabar, O.; Southall, N.; Westbroek, W.; Lea, W.A.; Velayati, A.; Goldin, E.; Sidransky, E.; Leister, W.; Marugan, J.J.
    Discovery, structure-activity relationship, and biological evaluation of non-inhibitory small molecule chaperones of glucocerebrosidase (2012), J. Med. Chem., 55, 5734-5748.
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.2.1.45

Protein Variants

Protein Variants Comment Organism
L444P the mutant shows strongly reduced activity Homo sapiens
N370S the mutant shows reduced activity Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-[3-[(5-bromopyridin-2-yl)(3,4-dichlorobenzyl)amino]propyl]-3-[3-(1H-imidazol-4-yl)propyl]thiourea
-
 Homo sapiens
2-([4-[(5-chloro-2-methoxyphenyl)amino]-6-(pyrrolidin-1-yl)-1,3,5-triazin-2-yl]amino)ethanol
-
 Homo sapiens
4-[4-(naphthalen-2-ylsulfonyl)piperazin-1-yl]-2-(thiophen-2-yl)quinazoline
-
 Homo sapiens
isofagomine
-
 Homo sapiens
miglustat
-
 Homo sapiens
N-(5-ethyl-1,3,4-thiadiazol-2-yl)-4-[(phenylsulfonyl)amino]benzamide
-
 Homo sapiens
N-nonyldeoxynojirimycin
-
 Homo sapiens
N-[2-(3,6-dihydropyridin-1(2H)-yl)-4-methylquinolin-6-yl]cyclohexanecarboxamide
-
 Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
glucosylceramide + H2O Homo sapiens
-
 beta-D-glucose + ceramide
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-methylumbelliferyl beta-D-glucopyranoside + H2O
-
 Homo sapiens 4-methylumbelliferone + beta-D-glucopyranose
-
 ?
glucosylceramide + H2O
-
 Homo sapiens beta-D-glucose + ceramide
-
 ?

Synonyms

Synonyms Comment Organism
Cerezyme
-
 Homo sapiens
Gcase
-
 Homo sapiens
glucocerebrosidase
-
 Homo sapiens
Imiglucerase
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00003
-
 pH 5.9, at 22°C Homo sapiens N-[2-(3,6-dihydropyridin-1(2H)-yl)-4-methylquinolin-6-yl]cyclohexanecarboxamide
0.0001
-
 pH 5.9, at 22°C Homo sapiens N-(5-ethyl-1,3,4-thiadiazol-2-yl)-4-[(phenylsulfonyl)amino]benzamide
0.0004
-
 pH 5.9, at 22°C Homo sapiens 2-([4-[(5-chloro-2-methoxyphenyl)amino]-6-(pyrrolidin-1-yl)-1,3,5-triazin-2-yl]amino)ethanol
0.00071
-
 pH 5.9, at 22°C Homo sapiens 1-[3-[(5-bromopyridin-2-yl)(3,4-dichlorobenzyl)amino]propyl]-3-[3-(1H-imidazol-4-yl)propyl]thiourea
0.0089
-
 pH 5.9, at 22°C Homo sapiens 4-[4-(naphthalen-2-ylsulfonyl)piperazin-1-yl]-2-(thiophen-2-yl)quinazoline