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Literature summary extracted from

  • Arenz, C.
    Small molecule inhibitors of acid sphingomyelinase (2010), Cell. Physiol. Biochem., 26, 1-8.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.1.4.12 (1-aminodecane-1,1-diyl)bis(phosphonic acid) a substrate analogue inhibitor of aSMase Homo sapiens
3.1.4.12 AD2765 a substrate analogue inhibitor of aSMase Homo sapiens
3.1.4.12 alpha-mangostin a xanthone from the bark of Garcinia speciosa Homo sapiens
3.1.4.12 amitriptyline performs indirect inhibition of aSMase Homo sapiens
3.1.4.12 cowanin a xanthone from the bark of Garcinia speciosa Homo sapiens
3.1.4.12 cowanol a xanthone from the bark of Garcinia speciosa Homo sapiens
3.1.4.12 desipramine performs indirect inhibition of aSMase Homo sapiens
3.1.4.12 imipramine performs indirect inhibition of aSMase Homo sapiens
3.1.4.12 phosphatidyl inositol-3,5-bisphosphate
-
Homo sapiens
3.1.4.12 phosphatidylinositol-4,5-bisphosphate
-
Homo sapiens
3.1.4.12 SR33557 the calcium channel inhibitor performs indirect inhibition of aSMase Homo sapiens

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
3.1.4.12 lysosome
-
Homo sapiens 5764
-
3.1.4.12 additional information the processed mature enzyme one portion of this enzyme is transported to the lysosomes and a second portion is secreted to extracytosolic side of the plasma membrane Homo sapiens
-
-
3.1.4.12 plasma membrane extracytosolic side Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
3.1.4.12 a sphingomyelin + H2O Homo sapiens
-
a ceramide + choline phosphate
-
?

Organism

EC Number Organism UniProt Comment Textmining
3.1.4.12 Homo sapiens
-
-
-

Posttranslational Modification

EC Number Posttranslational Modification Comment Organism
3.1.4.12 glycoprotein synthesis of a 78 kDA preproform of the enzyme which is glycosylated and proteolytically cleaved to a 72 kDa pre-form and subsequently to a 70 kDA mature enzyme Homo sapiens
3.1.4.12 proteolytic modification synthesis of a 78 kDA preproform of the enzyme which is glycosylated and proteolytically cleaved to a 72 kDa pre-form and subsequently to a 70 kDA mature enzyme Homo sapiens

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.1.4.12 a sphingomyelin + H2O
-
Homo sapiens a ceramide + choline phosphate
-
?

Synonyms

EC Number Synonyms Comment Organism
3.1.4.12 acid sphingomyelinase
-
Homo sapiens
3.1.4.12 aSMase
-
Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.1.4.12 0.0109
-
pH and temperature not specified in the publication Homo sapiens cowanol
3.1.4.12 0.014
-
pH and temperature not specified in the publication Homo sapiens alpha-mangostin
3.1.4.12 0.0192
-
pH and temperature not specified in the publication Homo sapiens cowanin
3.1.4.12 0.07
-
pH and temperature not specified in the publication Homo sapiens AD2765

General Information

EC Number General Information Comment Organism
3.1.4.12 malfunction an inborn deficiency in aSMase activity leads to a lysosomal storage of sphingomyelin and a fatal pathology that has been designated as the type A and type B of Niemann-Pick-disease Homo sapiens
3.1.4.12 additional information besides the aSMase, an alkaline sphingomyelinase and two neutral sphingomyelinases 1 and 2, nSMase1 and nSMase2, exist Homo sapiens
3.1.4.12 physiological function aSMase is known to induce apoptosis in a variety of cell lines and is emerging as an important mediator of inflammation in various pathological backgrounds Homo sapiens