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(+-)-2-(2-hydroxy-3-(octylsulfonamido)-cyclopentyl)acetic acid
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclohexanecarboxylic acid
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclopentane carboxylic acid
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97% inhibition at 40 microg/ml
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclopentanecarboxylic acid
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3% inhibition at 40 microg/ml
(1S,2R,3R)-2-hydroxy-3-[(octylsulfonyl)amino]cyclopentanecarboxylic acid
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(1S,2S,3S)-2-hydroxy-3-[(octylsulfonyl)amino]cyclopentanecarboxylic acid
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1-monooleoylglycerol
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mechanism
1-monooleoylglycerol 3-phosphate
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non-competitive, mitochondrial isozyme
1-monooleoylglycerol amide
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mechanism
1-monooleoylglycerol ester
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mechanism
1-palmitoyl-sn-glycerol 3-phosphate
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2,3-Butanedione
5 mM, 54% and 21% inhibition of microsomal and mitochondrial acyltransferase respectively
2-(2-phenylethylsulfonamido)benzoic acid
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2-(4-chlorophenylsulfonamido)benzoic acid
-
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2-(hexadecylsulfonamido)benzoic acid
-
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2-(methylsulfonamido)benzoic acid
-
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2-(nonylsulfonamido)benzoic acid
2-(nonylsulfonamido)benzylphosphonic acid
-
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2-(octylsulfonamido)phenylphosphonic acid
-
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2-(pentylsulfonamido)benzylphosphonic acid
-
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2-(phenylmethylsulfonamido)benzoic acid
-
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2-(phenylsulfonamido)benzoic acid
-
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2-(tetradecylsulfonamido)benzoic acid
-
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2-monooleoylglycerol
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mechanism
2-monooleoylglycerol amide
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mechanism
2-monooleoylglycerol ether
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mechanism
3-(2-phenylethylsulfonamido)benzoic acid
-
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3-(4-chlorophenylsulfonamido)benzoic acid
-
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3-(nonylsulfonamido)benzoic acid
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3-(nonylsulfonamido)benzylphosphonic acid
-
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3-(nonylsulfonamidomethyl)benzoic acid
-
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3-(octylsulfonamido)phenylphosphonic acid
-
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3-(pentylsulfonamido)benzylphosphonic acid
-
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3-(pentylsulfonamidomethyl)benzoic acid
-
-
3-(phenylmethylsulfonamido)benzoic acid
-
-
3-(phenylsulfonamido)benzoic acid
-
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3-[(3-cholamidopropyl)-dimethylammonio]-1-propanesulfonic acid
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trivial name CHAPS, complete inhibition
4-(2-phenylethylsulfonamido)benzoic acid
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4-(4-chlorophenylsulfonamido)benzoic acid
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4-(nonylsulfonamido)benzoic acid
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4-(nonylsulfonamido)benzylphosphonic acid
-
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4-(nonylsulfonamidomethyl)benzoic acid
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4-(octylsulfonamido)phenylphosphonic acid
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4-(pentylsulfonamido)benzylphosphonic acid
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4-(pentylsulfonamidomethyl)benzoic acid
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4-(phenylmethylsulfonamido)benzoic acid
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4-(phenylsulfonamido)benzoic acid
-
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5,5'-dithiobis(2-nitro-benzoate)
5-chloro-2-(nonylsulfonamido)benzoic acid
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5-fluoro-2-(octylsulfonamido)benzoic acid
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5-hydroxy-2-(octylsulfonamido)benzoic acid
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acetone
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inhibition of microsomal enzyme
acyl-CoA
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strong substrate inhibition
aminophenylboronate
mixed-type inhibition of microsomal and mitochondrial acyltransferase vs. glycerol 3-phosphate
AMP-activated protein kinase
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AMP-activated protein kinase reciprocally regulates GPAT1
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Antibodies to cocoa seed enzyme
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raised in rabbit
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bovine serum albumin
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above 6 mg/ml, at 0.01 mg palmitoyl-CoA depending on palmitoyl-CoA and phospholipid concentration
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Bromelain
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strong inhibition of microsomal enzyme
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CaCl2
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33% inhibition of isozyme mtGPAT1, 70% inhibition of isozyme mtGPAT2
cis-9,10-Methylenehexadecanoic acid
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0.15 mM, 50% inhibition, non-competitive to glycerol 3-phosphate, synergism with oleate, palmitoleate or cis-vaccenate
cis-vaccenate
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0.45 mM, 50% inhibition, synergism with cis-9,10-methylenehexadecanoic acid
cyclohexandione
50 mM, almost complete inhibition of mitochondrial acyltransferase
Detergents
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e.g. Brij 35, Brij 58, Lubrol 17A-10, phospholipids restore activity
diethyldicarbonate
0.3 mM, approx. 67% inhibition of microsomal acyltransferase, approx. 40% inhibition of mitochondrial acyltransferase, approx. 60% inhibition of recombinant mitochondrial acyltransferase, activity is restored to approx 50% by hydroxylamine
dihydroxyacetone phosphate
dihydroxyacetonephosphate
-
competitive inhibition of isozyme mtGPAT2, no inhibition of isozyme mtGPAT1
diisopropylfluorophosphate
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weak inhibition
dithiothreitol
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palmitoyl-CoA-specific isozyme
EDTA
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1 mM, 79% inhibition
lysophosphatidic acid
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product inhibition, all isozymes
MgCl2
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inhibition of microsomal enzyme
Mn2+
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2 mM, 82% residaul activity; slightly decreases activity, relative activity: 81.5% (2 mM)
NaCl
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100 mM, 30% inhibition
palmitoleate
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0.31 mM, 50% inhibition, synergism with cis-9,10-methylenehexadecanoic acid
palmitoleoyl-CoA
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shows substrate inhibition, therfore Km value is not determined
papain
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strong inhibition of microsomal enzyme
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phosphatidylethanolamine
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1,2-unsaturated species
phosphatidylglycerol
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above 1.5 mM, activation below
phosphatidylinositol
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inhibition of microsomal enzyme
phosphatidylserine
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inhibition of microsomal enzyme
Pronase
-
strong inhibition of microsomal enzyme
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sn-2-monooleoylglycerol
-
-
sn-2-monooleoylglycerol amide
-
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spermidine
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inhibits slightly in absence of bovine serum albumin
spermine
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inhibits slightly in absence of bovine serum albumin
(+-)-2-(2-hydroxy-3-(octylsulfonamido)-cyclopentyl)acetic acid
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(+-)-2-(2-hydroxy-3-(octylsulfonamido)-cyclopentyl)acetic acid
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8% inhibition at 40 microg/ml
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclohexanecarboxylic acid
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(+-)-2-hydroxy-3-(octylsulfonamido)-cyclohexanecarboxylic acid
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36% inhibition at 40 microg/ml
2-(nonylsulfonamido)benzoic acid
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2-(nonylsulfonamido)benzoic acid
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-
2-(nonylsulfonamido)benzoic acid
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97% inhibition at 40 microg/ml
2-(nonylsulfonamido)benzoic acid
i.e. FSG67a, GPAT inhibitor, has a broad spectrum inhibitory effect on GPAT activity; i.e. FSG67a, GPAT inhibitor, has a broad spectrum inhibitory effect on GPAT activity; i.e. FSG67a, GPAT inhibitor, has a broad spectrum inhibitory effect on GPAT activity
2-(nonylsulfonamido)benzoic acid
i.e. FSG67a, GPAT inhibitor, has a broad spectrum inhibitory effect on GPAT activity, metabolic effects in mice, overview; i.e. FSG67a, GPAT inhibitor, has a broad spectrum inhibitory effect on GPAT activity, metabolic effects in mice, overview; i.e. FSG67a, GPAT inhibitor, has a broad spectrum inhibitory effect on GPAT activity, metabolic effects in mice, overview; i.e. FSG67a, GPAT inhibitor, has a broad spectrum inhibitory effect on GPAT activity, metabolic effects in mice, overview. GPAT4 activity is significantly reduced in the liver, brown adipose tissue, and mammary gland as compared to the control group, but is normal in inguinal adipose tissue
5,5'-dithiobis(2-nitro-benzoate)
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1 mM, 20-30% inhibition of activity on palmitoyl-CoA, complete inhibition of activity on other acyl-CoAs
5,5'-dithiobis(2-nitro-benzoate)
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5,5'-dithiobis(2-nitro-benzoate)
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0.15mM, 90% inhibition in sonicated vesicles
5,5'-dithiobis(2-nitro-benzoate)
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inhibition of microsomal enzyme, mitochondrial enzyme is not inhibited
5,5'-dithiobis(2-nitro-benzoate)
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5,5'-dithiobis(2-nitro-benzoate)
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1 mM, 77% inhibition
Ca2+
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in the absence of NaCl
Ca2+
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higher concentration, small amounts of phospholipids protect
Ca2+
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5 mM, 70% inhibition
cardiolipin
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inhibition of mitochondrial enzyme
cholate
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phospholipids restore activity
cholate
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complete inhibition
deoxycholate
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phospholipids restore activity
deoxycholate
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complete inhibition
deoxycholate
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above 0.35 mg/ml
diacylglycerophosphate
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i.e. phosphatidic acid, inhibition of mitochondrial enzyme
diacylglycerophosphate
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dihydroxyacetone phosphate
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palmitoyl-CoA-specific isozyme
dihydroxyacetone phosphate
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microsomal isozyme
dihydroxyacetone phosphate
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iodoacetamide
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strong inhibition of microsomal enzyme, mitochondrial enzyme is not inhibited
Mg2+
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in the absence of NaCl
Mg2+
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2 mM, 87% residual activity; slightly decreases activity, relative activity: 87.5% (2 mM), 37% (5 mM)
Mg2+
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5 mM, 75% inhibition
Monoacylglycerophosphate
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Monoacylglycerophosphate
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i.e. lysophosphatidic acid, inhibition of mitochondrial enzyme
Monoacylglycerophosphate
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N-ethylmaleimide
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N-ethylmaleimide
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10 mM, 65% inhibition in sonicated vesicles, 2 mM, 93% inhibition in vesicles treated with 0.3% toluene
N-ethylmaleimide
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only N-ethylmaleimide sensitive isoform
N-ethylmaleimide
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strong inhibition of microsomal isozyme, mitochondrial enzyme is not inhibited
N-ethylmaleimide
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0.5-10 mM, 80-90% inhibition of microsomal acyltransferase, mitochondrial acyltransferase is not inhibited
N-ethylmaleimide
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4 mM, approx. 50% inhibition of the solubilized acyltransferase, membrane-bound enzyme is not inhibited
N-ethylmaleimide
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0.4 mM, 60% inhibition after 10 min
N-ethylmaleimide
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5 mM, 79% inhibition
NEM
microsomal GPAT3 activity is sensitive to NEM; mitochondrial GPAT2 is sensitive to NEM
NEM
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inactivation of isozyme mtGPAT2 and the microsomal isozyme
NEM
GPAT3 is a NEM-sensitive GPAT; GPAT4 is a NEM-sensitive GPAT
oleate
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0.31 mM, 50% inhibition, synergism with cis-9,10-methylenehexadecanoic acid
p-chloromercuribenzoate
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p-chloromercuribenzoate
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10 mM, 88% inhibition in sonicated vesicles, 1 mM, 98% inhibition in vesicles treated with 0.3% toluene, 2-mercaptoethanol partially restores activity, not inhibited by p-chloromercuriphenylsulfonic acid
p-chloromercuribenzoate
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1 mM, 64% inhibition
palmitoyl-CoA
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bovine serum albumin attenuates
palmitoyl-CoA
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microsomal enzyme, above 0.1 mM
Phenylglyoxal
50 mM, approx. 70% inhibition of mitochondrial acyltransferase
Phenylglyoxal
1 mM, 88% and 59% inhibition of microsomal and mitochondrial acyltransferase, respectively; 1 mM, 88% and 59% inhibition of microsomal and mitochondrial acyltransferase, respectively
Polymyxin B
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inhibitis isozyme mtGPAT2 and the microsomal isozyme
Polymyxin B
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0.5 mg/ml, approx. 75% inhibition of microsomal enzyme, slight stimulation of mitochondrial enzyme
Polymyxin B
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in absence of BSA the antibiotic is slightly inhibitory
Triton X-100
-
-
Triton X-100
-
phospholipids restore activity
Triton X-100
-
strong, above 0.15 mg/ml
Trypsin
-
-
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Trypsin
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0.04 mg/ml, approx. 80% inhibition of microsomal enzyme within 3 min at 37°C, inhibition of the mitochondrial enzyme only in the presence of 0.05% deoxycholate or 0.1% Triton X-100
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Trypsin
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0.06 mg/ml, 80% inhibition after 10 min
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additional information
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not inhibited by palmitate, elaidate, trans-vaccenate
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additional information
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cyclopentyl and cyclohexyl scaffolds may be occluded from the enzyme active site by two protein loops that sterically guard the phosphate binding region
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additional information
mitochondrial GPAT1 is resistant to inactivation induced by sulfhydryl-group modifying reagents like N-ethylmaleimide (NEM)
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additional information
mitochondrial GPAT1 is resistant to inactivation induced by sulfhydryl-group modifying reagents like N-ethylmaleimide (NEM)
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additional information
mitochondrial GPAT1 is resistant to inactivation induced by sulfhydryl-group modifying reagents like N-ethylmaleimide (NEM)
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additional information
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recombinant mitochondrial acyl transferase, not inhibited by N-ethylmaleimide
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additional information
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no inhibition by malonyl-CoA, substrate inhibition by acyl-CoAs at concentrations above 0.075 mM
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additional information
mitochondrial GPAT1 is resistant to inactivation induced by sulfhydryl-group modifying reagents like N-ethylmaleimide (NEM)
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additional information
mitochondrial GPAT1 is resistant to inactivation induced by sulfhydryl-group modifying reagents like N-ethylmaleimide (NEM)
-
additional information
mitochondrial GPAT1 is resistant to inactivation induced by sulfhydryl-group modifying reagents like N-ethylmaleimide (NEM)
-
additional information
mitochondrial GPAT1 is resistant to inactivation induced by sulfhydryl-group modifying reagents like N-ethylmaleimide (NEM)
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additional information
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liver microsomal enzyme is inhibited by all proteases; liver mitochondrial enzyme, not inhibited by trypsin and chymotrypsin
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additional information
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mitochondrial enzyme, not inhibited by N-ethylmaleimide
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additional information
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mitochondrial enzyme, not inhibited by bromelain, papain, pronase and trypsin
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additional information
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microsomal isozyme, not inhibited by sn-1,2-diolein, 1,2-dioleoylglycerol ether, dioleoylphosphatidic acid
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additional information
antisense LeGPAT is introduced to inhibit the expression of LeGPAT
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2.3.1.15 glycerol-3-phosphate 1-O-acyltransferase
results (
results (
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