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Literature summary for 3.1.4.12 extracted from

  • Arenz, C.
    Small molecule inhibitors of acid sphingomyelinase (2010), Cell. Physiol. Biochem., 26, 1-8.
    View publication on PubMed
Search for more literature for 3.1.4.12

Inhibitors

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

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Homo sapiens 5764
-
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
-
-
plasma membrane extracytosolic side Homo sapiens 5886
-

Natural Substrates/ Products (Substrates)

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
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
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)

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

Synonyms

Synonyms Comment Organism
acid sphingomyelinase
-
 Homo sapiens
aSMase
-
 Homo sapiens

IC50 Value

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

General Information

General Information Comment Organism
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
additional information besides the aSMase, an alkaline sphingomyelinase and two neutral sphingomyelinases 1 and 2, nSMase1 and nSMase2, exist Homo sapiens
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