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Literature summary for 2.3.1.26 extracted from

  • Ohshiro, T.; Rudel, L.L.; Omura, S.; Tomoda, H.
    Selectivity of microbial acyl-CoA: cholesterol acyltransferase inhibitors toward isozymes (2007), J. Antibiot., 60, 43-51.
    View publication on PubMed
Search for more literature for 2.3.1.26

Inhibitors

Inhibitors Comment Organism Structure
beauvericin IC50: 0.00035 mM, ACAT1; IC50: 0.00035 mM, ACAT2 Chlorocebus aethiops
beauvericin
-
 Cricetulus griseus
beauvericin
-
 Rattus norvegicus
beauveriolide I IC50: 0.0019 mM, ACAT2; IC50: 0.0022 mM, ACAT1 Chlorocebus aethiops
beauveriolide I
-
 Cricetulus griseus
beauveriolide I
-
 Mus musculus
beauveriolide III IC50: 0.003 mM, ACAT1; IC50: 0.003 mM, ACAT2 Chlorocebus aethiops
beauveriolide III
-
 Cricetulus griseus
beauveriolide III
-
 Mus musculus
CL-283,546 IC50: 0.00006 mM, ACAT2; IC50: 0.00012 mM, ACAT1 Chlorocebus aethiops
CL-283,546
-
 Cricetulus griseus
glisoprenin A IC50: 0.0004 mM, ACAT1; IC50: 0.0013 mM, ACAT2 Chlorocebus aethiops
glisoprenin A
-
 Cricetulus griseus
glisoprenin A
-
 Rattus norvegicus
K97-0239A IC50: 0.038 mM, ACAT2; IC50: 0.04 mM, ACAT1 Chlorocebus aethiops
K97-0239A
-
 Cricetulus griseus
K97-0239A
-
 Mus musculus
K97-0239B IC50: above 0.07 mM, ACAT1; IC50: above 0.7 mM, ACAT2 Chlorocebus aethiops
K97-0239B
-
 Cricetulus griseus
K97-0239B
-
 Mus musculus
phenochalasin A IC50: above 0.1 mM, ACAT1; IC50: above 0.1 mM, ACAT2 Chlorocebus aethiops
phenochalasin A
-
 Cricetulus griseus
phenochalasin A
-
 Mus musculus
purpactin A IC50: 0.0009 mM, ACAT1; IC50: 0.0018 mM, ACAT2 Chlorocebus aethiops
purpactin A
-
 Cricetulus griseus
purpactin A
-
 Rattus norvegicus
purpactin B IC50: 0.012 mM, ACAT2; IC50: 0.022 mM, ACAT1 Chlorocebus aethiops
purpactin B
-
 Cricetulus griseus
purpactin B
-
 Rattus norvegicus
purpactin C IC50: 0.028 mM, ACAT1; IC50: 0.03 mM, ACAT2 Chlorocebus aethiops
purpactin C
-
 Cricetulus griseus
purpactin C
-
 Rattus norvegicus
pyripyropene A IC50: 0.00006 mM, ACAT2; IC50: above 0.03 mM, ACAT1 Chlorocebus aethiops
pyripyropene A
-
 Cricetulus griseus
pyripyropene A
-
 Rattus norvegicus
pyripyropene B IC50: 0.0008 mM, ACAT2; IC50: 0.03 mM, ACAT1 Chlorocebus aethiops
pyripyropene B
-
 Cricetulus griseus
pyripyropene B
-
 Rattus norvegicus
pyripyropene C IC50: 0.00035 mM, ACAT2; IC50: 0.015 mM, ACAT1 Chlorocebus aethiops
pyripyropene C
-
 Cricetulus griseus
pyripyropene C
-
 Rattus norvegicus
pyripyropene D IC50: 0.0012 mM, ACAT2; IC50: 0.015 mM, ACAT1 Chlorocebus aethiops
pyripyropene D
-
 Cricetulus griseus
pyripyropene D
-
 Rattus norvegicus
sespendole IC50: 0.012 mM, ACAT2; IC50: 0.02 mM, ACAT1 Chlorocebus aethiops
sespendole
-
 Cricetulus griseus
sespendole
-
 Mus musculus
spylidone IC50: 0.003 mM, ACAT2; IC50: 0.007 mM, ACAT1 Chlorocebus aethiops
spylidone
-
 Cricetulus griseus
spylidone
-
 Mus musculus
terpendole C IC50: 0.0005 mM, ACAT2; IC50: 0.008 mM, ACAT1 Chlorocebus aethiops
terpendole C
-
 Cricetulus griseus
terpendole C
-
 Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
endoplasmic reticulum
-
 Cricetulus griseus 5783
-
endoplasmic reticulum
-
 Mus musculus 5783
-
endoplasmic reticulum
-
 Rattus norvegicus 5783
-
membrane
-
 Cricetulus griseus 16020
-
membrane
-
 Mus musculus 16020
-
membrane
-
 Rattus norvegicus 16020
-
microsome
-
 Rattus norvegicus
-
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
acyl-CoA + cholesterol Cricetulus griseus
-
 CoA + cholesterol ester
-
 ?
acyl-CoA + cholesterol Mus musculus
-
 CoA + cholesterol ester
-
 ?
acyl-CoA + cholesterol Rattus norvegicus
-
 CoA + cholesterol ester
-
 ?

Organism

Organism UniProt Comment Textmining
Chlorocebus aethiops
-
 ACAT1 expressed by CHO cells
-
Chlorocebus aethiops
-
 ACAT2 expressed by CHO cells
-
Cricetulus griseus
-
-
-
Mus musculus
-
-
-
Rattus norvegicus
-
-
-

Purification (Commentary)

Purification (Comment) Organism
microsomes are prepared Cricetulus griseus
microsomes are prepared Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
CHO cell
-
 Cricetulus griseus
-
liver
-
 Rattus norvegicus
-
peritoneal macrophage
-
 Mus musculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
acyl-CoA + cholesterol
-
 Cricetulus griseus CoA + cholesterol ester
-
 ?
acyl-CoA + cholesterol
-
 Mus musculus CoA + cholesterol ester
-
 ?
acyl-CoA + cholesterol
-
 Rattus norvegicus CoA + cholesterol ester
-
 ?

Synonyms

Synonyms Comment Organism
ACAT
-
 Cricetulus griseus
ACAT
-
 Mus musculus
ACAT
-
 Rattus norvegicus
ACAT-1
-
 Cricetulus griseus
ACAT-2
-
 Cricetulus griseus
ACAT1
-
 Chlorocebus aethiops
ACAT2
-
 Rattus norvegicus
ACAT2
-
 Chlorocebus aethiops
acyl-CoA: cholesterol acyltransferase
-
 Cricetulus griseus
acyl-CoA: cholesterol acyltransferase
-
 Mus musculus
acyl-CoA: cholesterol acyltransferase
-
 Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 activity assay Cricetulus griseus
37
-
 activity assay Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00006
-
 IC50: 0.00006 mM, ACAT2 Chlorocebus aethiops pyripyropene A
0.00006
-
 IC50: 0.00006 mM, ACAT2 Chlorocebus aethiops CL-283,546
0.00006
-
 enzyme assay Cricetulus griseus pyripyropene A
0.00006
-
 enzyme assay Cricetulus griseus CL-283,546
0.00007
-
 cell-based assay Cricetulus griseus pyripyropene A
0.00009
-
 cell-based assay Cricetulus griseus CL-283,546
0.0001
-
 cell-based assay Cricetulus griseus CL-283,546
0.00012
-
 IC50: 0.00012 mM, ACAT1 Chlorocebus aethiops CL-283,546
0.00012
-
 enzyme assay Cricetulus griseus CL-283,546
0.00013
-
-
 Rattus norvegicus beauvericin
0.00035
-
 IC50: 0.00035 mM, ACAT1 Chlorocebus aethiops beauvericin
0.00035
-
 IC50: 0.00035 mM, ACAT2 Chlorocebus aethiops pyripyropene C
0.00035
-
 IC50: 0.00035 mM, ACAT2 Chlorocebus aethiops beauvericin
0.00035
-
 enzyme assay Cricetulus griseus pyripyropene C
0.00035
-
 enzyme assay Cricetulus griseus beauvericin
0.00036
-
 cell-based assay Cricetulus griseus pyripyropene C
0.0004
-
 IC50: 0.0004 mM, ACAT1 Chlorocebus aethiops glisoprenin A
0.0004
-
 enzyme assay Cricetulus griseus glisoprenin A
0.00041
-
-
 Mus musculus beauveriolide III
0.0005
-
 IC50: 0.0005 mM, ACAT2 Chlorocebus aethiops terpendole C
0.0005
-
 enzyme assay Cricetulus griseus terpendole C
0.0006
-
-
 Mus musculus phenochalasin A
0.0006
-
 cell-based assay Cricetulus griseus beauveriolide I
0.0007
-
 cell-based assay Cricetulus griseus beauvericin
0.00078
-
-
 Mus musculus beauveriolide I
0.0008
-
 IC50: 0.0008 mM, ACAT2 Chlorocebus aethiops pyripyropene B
0.0008
-
 enzyme assay Cricetulus griseus pyripyropene B
0.0009
-
 IC50: 0.0009 mM, ACAT1 Chlorocebus aethiops purpactin A
0.0009
-
 cell-based assay Cricetulus griseus beauveriolide III
0.0009
-
 enzyme assay Cricetulus griseus purpactin A
0.0012
-
 IC50: 0.0012 mM, ACAT2 Chlorocebus aethiops pyripyropene D
0.0012
-
 enzyme assay Cricetulus griseus pyripyropene D
0.0013
-
 IC50: 0.0013 mM, ACAT2 Chlorocebus aethiops glisoprenin A
0.0013
-
 enzyme assay Cricetulus griseus glisoprenin A
0.0015
-
-
 Mus musculus K97-0239A
0.0015
-
 cell-based assay Cricetulus griseus pyripyropene D
0.0015
-
 cell-based assay Cricetulus griseus purpactin A
0.0017
-
-
 Mus musculus K97-0239B
0.0018
-
 IC50: 0.0018 mM, ACAT2 Chlorocebus aethiops purpactin A
0.0018
-
 enzyme assay Cricetulus griseus purpactin A
0.0019
-
 IC50: 0.0019 mM, ACAT2 Chlorocebus aethiops beauveriolide I
0.0019
-
 enzyme assay Cricetulus griseus beauveriolide I
0.002
-
 cell-based assay Cricetulus griseus pyripyropene B
0.002
-
 cell-based assay Cricetulus griseus beauvericin
0.0022
-
 IC50: 0.0022 mM, ACAT1 Chlorocebus aethiops beauveriolide I
0.0022
-
 enzyme assay Cricetulus griseus purpactin B
0.0022
-
 enzyme assay Cricetulus griseus beauveriolide I
0.0025
-
-
 Rattus norvegicus terpendole C
0.0025
-
 cell-based assay Cricetulus griseus purpactin A
0.0028
-
 enzyme assay Cricetulus griseus purpactin C
0.003
-
 IC50: 0.003 mM, ACAT1 Chlorocebus aethiops beauveriolide III
0.003
-
 IC50: 0.003 mM, ACAT2 Chlorocebus aethiops spylidone
0.003
-
 IC50: 0.003 mM, ACAT2 Chlorocebus aethiops beauveriolide III
0.003
-
 enzyme assay Cricetulus griseus spylidone
0.003
-
 enzyme assay Cricetulus griseus beauveriolide III
0.004
-
-
 Mus musculus sespendole
0.0043
-
 cell-based assay Cricetulus griseus glisoprenin A
0.0045
-
-
 Rattus norvegicus purpactin A
0.005
-
 cell-based assay Cricetulus griseus spylidone
0.0057
-
 cell-based assay Cricetulus griseus purpactin B
0.0065
-
 cell-based assay Cricetulus griseus sespendole
0.007
-
 IC50: 0.007 mM, ACAT1 Chlorocebus aethiops spylidone
0.007
-
 enzyme assay Cricetulus griseus spylidone
0.008
-
 IC50: 0.008 mM, ACAT1 Chlorocebus aethiops terpendole C
0.008
-
 enzyme assay Cricetulus griseus terpendole C
0.009
-
 cell-based assay Cricetulus griseus K97-0239A
0.01
-
 cell-based assay Cricetulus griseus purpactin B
0.01
-
 cell-based assay Cricetulus griseus glisoprenin A
0.01
-
 cell-based assay Cricetulus griseus purpactin C
0.01
-
 cell-based assay Cricetulus griseus terpendole C
0.012
-
-
 Rattus norvegicus glisoprenin A
0.012
-
 IC50: 0.012 mM, ACAT2 Chlorocebus aethiops purpactin B
0.012
-
 IC50: 0.012 mM, ACAT2 Chlorocebus aethiops sespendole
0.012
-
 cell-based assay Cricetulus griseus sespendole
0.012
-
 enzyme assay Cricetulus griseus purpactin B
0.012
-
 enzyme assay Cricetulus griseus sespendole
0.013
-
 cell-based assay Cricetulus griseus K97-0239A
0.013
-
 cell-based assay Cricetulus griseus K97-0239B
0.015
-
 IC50: 0.015 mM, ACAT1 Chlorocebus aethiops pyripyropene C
0.015
-
 IC50: 0.015 mM, ACAT1 Chlorocebus aethiops pyripyropene D
0.015
-
 enzyme assay Cricetulus griseus pyripyropene C
0.015
-
 enzyme assay Cricetulus griseus pyripyropene D
0.018
-
-
 Rattus norvegicus purpactin C
0.02
-
-
 Rattus norvegicus purpactin B
0.02
-
 IC50: 0.02 mM, ACAT1 Chlorocebus aethiops sespendole
0.02
-
 cell-based assay Cricetulus griseus beauveriolide I
0.02
-
 cell-based assay Cricetulus griseus beauveriolide III
0.02
-
 cell-based assay Cricetulus griseus phenochalasin A
0.02
-
 enzyme assay Cricetulus griseus sespendole
0.022
-
 IC50: 0.022 mM, ACAT1 Chlorocebus aethiops purpactin B
0.025
-
 cell-based assay Cricetulus griseus spylidone
0.028
-
 IC50: 0.028 mM, ACAT1 Chlorocebus aethiops purpactin C
0.03
-
 IC50: 0.03 mM, ACAT1 Chlorocebus aethiops pyripyropene B
0.03
-
 IC50: 0.03 mM, ACAT2 Chlorocebus aethiops purpactin C
0.03
-
 IC50: above 0.03 mM, ACAT1 Chlorocebus aethiops pyripyropene A
0.03
-
 enzyme assay Cricetulus griseus pyripyropene A
0.03
-
 enzyme assay Cricetulus griseus pyripyropene B
0.03
-
 enzyme assay Cricetulus griseus purpactin C
0.032
-
 cell-based assay Cricetulus griseus pyripyropene C
0.035
-
-
 Rattus norvegicus pyripyropene D
0.038
-
-
 Rattus norvegicus pyripyropene B
0.038
-
 IC50: 0.038 mM, ACAT2 Chlorocebus aethiops K97-0239A
0.038
-
 cell-based assay Cricetulus griseus pyripyropene D
0.038
-
 enzyme assay Cricetulus griseus K97-0239A
0.04
-
-
 Rattus norvegicus pyripyropene C
0.04
-
 IC50: 0.04 mM, ACAT1 Chlorocebus aethiops K97-0239A
0.04
-
 enzyme assay Cricetulus griseus K97-0239A
0.042
-
-
 Mus musculus spylidone
0.048
-
 cell-based assay Cricetulus griseus pyripyropene B
0.07
-
 IC50: above 0.07 mM, ACAT1 Chlorocebus aethiops K97-0239B
0.07
-
 enzyme assay Cricetulus griseus K97-0239B
0.08
-
-
 Rattus norvegicus pyripyropene A
0.08
-
 cell-based assay Cricetulus griseus pyripyropene A
0.1
-
 IC50: above 0.1 mM, ACAT1 Chlorocebus aethiops phenochalasin A
0.1
-
 IC50: above 0.1 mM, ACAT2 Chlorocebus aethiops phenochalasin A
0.1
-
 enzyme assay Cricetulus griseus phenochalasin A
0.7
-
 IC50: above 0.7 mM, ACAT2 Chlorocebus aethiops K97-0239B