Target Information
Target General Infomation | |||||
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Target ID |
T76369
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Former ID |
TTDR00274
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Target Name |
Liver carboxylesterase
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Gene Name |
CES1
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Synonyms |
ACAT; Acyl coenzyme A:cholesterol acyltransferase; Brain carboxylesterase hBr1; HCE1; HMSE; Human carboxylesterase 1; Monocyte/macrophage serine esterase; Serine esterase 1; CES1
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Target Type |
Clinical Trial
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Disease | Arteriosclerosis [ICD9: 440; ICD10: I70] | ||||
Atherosclerosis [ICD9: 414.0, 440; ICD10: I70] | |||||
Acute lymphoblastic leukemia [ICD9: 204.0, 556; ICD10: C91.0] | |||||
Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78] | |||||
Hypercholesterolemia [ICD10: E78] | |||||
Peripheral vascular disease [ICD9: 443.9; ICD10: I73.9] | |||||
Function |
Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs. Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl coa ester.
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BioChemical Class |
Carboxylic ester hydrolase
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Target Validation |
T76369
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UniProt ID | |||||
EC Number |
EC 3.1.1.56
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Sequence |
MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPL
GPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLN IYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFST GDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLF HRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLK MKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIP MQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDL IADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPF LKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLK DKEVAFWTNLFAKKAVEKPPQTEHIEL |
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Drugs and Mode of Action | |||||
Drug(s) | Cholic Acid | Drug Info | Approved | Peroxisomal disorders; Synthesis disorders | [541327] |
PACTIMIBE | Drug Info | Phase 2/3 | Arteriosclerosis | [521676] | |
Eldacimibe | Drug Info | Phase 2 | Hyperlipidaemia | [545522] | |
K-604 | Drug Info | Phase 2 | Arteriosclerosis | [522595] | |
GR148672X | Drug Info | Clinical trial | Acute lymphoblastic leukemia | [541808] | |
HL-004 | Drug Info | Preclinical | Arteriosclerosis | [549199] | |
Avasimibe | Drug Info | Discontinued in Phase 3 | Peripheral vascular disease | [546526] | |
CI-976 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [544811] | |
CL-283796 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [545762] | |
E-5324 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [545733] | |
Eflucimibe | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [546909] | |
RP-64477 | Drug Info | Discontinued in Phase 2 | Hyperlipidaemia | [545150] | |
447C88 | Drug Info | Discontinued in Phase 1 | Hyperlipidaemia | [545135] | |
CL-277082 | Drug Info | Discontinued in Phase 1 | Arteriosclerosis | [544948] | |
F-1394 | Drug Info | Discontinued in Phase 1 | Arteriosclerosis | [545396] | |
YM-17E | Drug Info | Discontinued in Phase 1 | Hyperlipidaemia | [545258] | |
YM-750 | Drug Info | Discontinued in Phase 1 | Hyperlipidaemia | [545390] | |
CEB-925 | Drug Info | Terminated | Hypercholesterolemia | [546745] | |
CI-999 | Drug Info | Terminated | Arteriosclerosis | [546902] | |
DuP-129 | Drug Info | Terminated | Hypercholesterolemia | [545519] | |
FR-129169 | Drug Info | Terminated | Arteriosclerosis | [545283] | |
FR-145237 | Drug Info | Terminated | Arteriosclerosis | [546129] | |
Lecimibide | Drug Info | Terminated | Hyperlipidaemia | [545142] | |
NTE-122 | Drug Info | Terminated | Atherosclerosis | [546451] | |
PD-132301-2 | Drug Info | Terminated | Arteriosclerosis | [545279] | |
RP-70676 | Drug Info | Terminated | Hyperlipidaemia | [545333] | |
RP-73163 | Drug Info | Terminated | Arteriosclerosis | [545520] | |
TEI-6522 | Drug Info | Terminated | Arteriosclerosis | [545745] | |
Inhibitor | (1R)-1,2,2-TRIMETHYLPROPYL (R)-METHYLPHOSPHINATE | Drug Info | [551374] | ||
(E)-Octadec-9-enoic acid phenylamide | Drug Info | [527138] | |||
1,1,1-trifluoro-3-(hexylsulfinyl)propan-2-one | Drug Info | [529157] | |||
1,1,1-trifluoro-3-(hexylsulfonyl)propan-2-one | Drug Info | [529157] | |||
1,1,1-trifluoro-3-(hexylthio)propan-2-one | Drug Info | [529157] | |||
1,1,1-trifluoro-3-(octylsulfinyl)propan-2-one | Drug Info | [529157] | |||
1,1,1-trifluoro-3-(octylsulfonyl)propan-2-one | Drug Info | [529157] | |||
1,1,1-trifluoro-3-(octylthio)propan-2-one | Drug Info | [529157] | |||
1,1,1-trifluorododecan-2-one | Drug Info | [529157] | |||
1,10-phenanthroline-5,6-dione | Drug Info | [529103] | |||
1,2-bis(2,3,4-trifluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(2,3,4-trifluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(2,3,5-trifluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(2,3,5-trifluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(2,3,6-trifluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(2,3-difluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(2,3-fluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(2,4-difluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(2,4-difluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(2,5-difluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(2,5-difluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(2,6-difluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(2,6-difluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(2-fluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(2-fluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(3,4,5-trifluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(3,4,5-trifluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(3,4-difluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(3,4-difluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(3,5-difluorophenyl)-2-hydroxyethanone | Drug Info | [528766] | |||
1,2-bis(3,5-difluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(3-fluorophenyl)-2-hydroxyethanon | Drug Info | [528766] | |||
1,2-bis(3-fluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-bis(4-fluorophenyl)ethane-1,2-dione | Drug Info | [528766] | |||
1,2-Bis-(2-chloro-phenyl)-ethane-1,2-dione | Drug Info | [527510] | |||
1,2-Bis-(3-methoxy-phenyl)-ethane-1,2-dione | Drug Info | [527510] | |||
1,2-Bis-(3-nitro-phenyl)-ethane-1,2-dione | Drug Info | [527510] | |||
1,2-Bis-(4-bromo-phenyl)-ethane-1,2-dione | Drug Info | [527510] | |||
1,2-Bis-(4-chloro-phenyl)-ethane-1,2-dione | Drug Info | [527510] | |||
1,2-Bis-(4-methoxy-phenyl)-ethane-1,2-dione | Drug Info | [527510] | |||
1,2-Di-naphthalen-2-yl-ethane-1,2-dione | Drug Info | [527692] | |||
1,2-Di-p-tolyl-ethane-1,2-dione | Drug Info | [527510] | |||
1,2-dicyclohexylethane-1,2-dione | Drug Info | [529103] | |||
1,2-indanedione | Drug Info | [529103] | |||
1,2-NAPHTHOQUINONE | Drug Info | [529103] | |||
1-(2-bromoethyl)-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-(2-iodoethyl)-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-(3,4-Dimethyl-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [527510] | |||
1-(4-Chloro-phenyl)-2-p-tolyl-ethane-1,2-dione | Drug Info | [527510] | |||
1-(4-Chloro-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [527510] | |||
1-(4-chlorobenzyl)-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-(4-Methoxy-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [527510] | |||
1-(4-Nitro-phenyl)-2-phenyl-ethane-1,2-dione | Drug Info | [527510] | |||
1-benzyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-butyryl-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-dodecyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-hexadecyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-methyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-phenyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
1-Phenyl-2-p-tolyl-ethane-1,2-dione | Drug Info | [527510] | |||
1-Phenyl-propane-1,2-dione | Drug Info | [527510] | |||
1-propionyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
11,12-dihydro-dibenzo[a,e]cyclooctene-5,6-dione | Drug Info | [529103] | |||
2,2-Dimethoxy-1,2-diphenyl-ethanone | Drug Info | [527510] | |||
2,2-dimethyl-3-methyleneheptadecane | Drug Info | [529157] | |||
2-methoxy-3,4-methylenedioxybenzophenone | Drug Info | [528217] | |||
3,4,5,6-Tetrachloro-[1,2]benzoquinone | Drug Info | [527510] | |||
3,5-Di-tert-butyl-[1,2]benzoquinone | Drug Info | [527510] | |||
3-(butylsulfinyl)-1,1,1-trifluoropropan-2-one | Drug Info | [529157] | |||
3-(butylthio)-1,1,1-trifluoropropan-2-one | Drug Info | [529157] | |||
3-(decylsulfinyl)-1,1,1-trifluoropropan-2-one | Drug Info | [529157] | |||
3-(decylsulfonyl)-1,1,1-trifluoropropan-2-one | Drug Info | [529157] | |||
3-(decylthio)-1,1,1-trifluoropropan-2-one | Drug Info | [529157] | |||
3-(dodecylsulfinyl)-1,1,1-trifluoropropan-2-one | Drug Info | [529157] | |||
3-(dodecylsulfonyl)-1,1,1-trifluoropropan-2-one | Drug Info | [529157] | |||
4,5-dichloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
4,6-dichloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
4,7-dichloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
4-(2-Oxo-2-phenyl-acetyl)-benzoic acid | Drug Info | [527510] | |||
4-chloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
4-chloro-7-methyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
4-Piperidino-Piperidine | Drug Info | [551374] | |||
5,6-dinitroacenaphthoquinone | Drug Info | [529103] | |||
5,7-dichloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
5-(trifluoromethoxy)-1H-indole-2,3-dione | Drug Info | [528749] | |||
5-chloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
6,7-dichloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
6-bromo-5-methyl-1H-indole-2,3-dione | Drug Info | [528749] | |||
7-(trifluoromethyl)-1H-indole-2,3-dione | Drug Info | [528749] | |||
7-chloro-1H-indole-2,3-dione | Drug Info | [528749] | |||
Acenanthrene-9,10-dione | Drug Info | [529103] | |||
ACENAPHTHOQUINONE | Drug Info | [529103] | |||
Alpha-D-Mannose | Drug Info | [551393] | |||
Avasimibe | Drug Info | [535439] | |||
BENZIL | Drug Info | [529157] | |||
BENZOIN | Drug Info | [528766] | |||
CEB-925 | Drug Info | [546746] | |||
CHLORANIL | Drug Info | [527510] | |||
Cholic Acid | Drug Info | [551393] | |||
CI-976 | Drug Info | [537864] | |||
CI-999 | Drug Info | [534786] | |||
Dibutyl 2,2,2-trifluoro-1-phenylethyl phosphate | Drug Info | [530348] | |||
Diethyl 2,2,2-trifluoro-1-phenylethyl phosphate | Drug Info | [530348] | |||
Dimethyl 2,2,2-trifluoro-1-phenylethyl phosphate | Drug Info | [530348] | |||
DuP-129 | Drug Info | [543651] | |||
Eflucimibe | Drug Info | [533663] | |||
GR148672X | Drug Info | [543651] | |||
Heptane-2,3-dione | Drug Info | [527510] | |||
K-604 | Drug Info | [528287] | |||
N-Methylnaloxonium | Drug Info | [551391] | |||
NSC-23180 | Drug Info | [529103] | |||
NTE-122 | Drug Info | [534779] | |||
O-Sialic Acid | Drug Info | [551374] | |||
Oleic acid anilide | Drug Info | [528217] | |||
PACTIMIBE | Drug Info | [529589] | |||
Phenanthrene-9,10-dione | Drug Info | [529103] | |||
PYRIPYROPENE A | Drug Info | [527138] | |||
SCH-48375 | Drug Info | [533851] | |||
Thenoyltrifluoroacetone | Drug Info | [551409] | |||
Thieno[3,2-e][1]benzothiophene-4,5-dione | Drug Info | [529103] | |||
VULM-1457 | Drug Info | [543651] | |||
YM-750 | Drug Info | [529169] | |||
Modulator | 447C88 | Drug Info | [534137] | ||
CL-277082 | Drug Info | [533344] | |||
CL-283796 | Drug Info | [531635], [533685] | |||
E-5324 | Drug Info | [533828] | |||
Eldacimibe | Drug Info | [533663] | |||
F-1394 | Drug Info | [526020] | |||
FR-129169 | Drug Info | [534219] | |||
FR-145237 | Drug Info | [534076] | |||
HL-004 | Drug Info | [534440] | |||
KY-382 | Drug Info | [543651] | |||
Lecimibide | Drug Info | [533861] | |||
PD-132301-2 | Drug Info | [533950] | |||
RP-64477 | Drug Info | [534116] | |||
RP-70676 | Drug Info | [545334] | |||
RP-73163 | Drug Info | [534282] | |||
SMP-797 | Drug Info | ||||
TEI-6522 | Drug Info | [533670] | |||
YM-17E | Drug Info | [534326] | |||
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM) | |||||
TEP | EXP Info | ||||
Pathways | |||||
KEGG Pathway | Drug metabolism - other enzymes | ||||
Metabolic pathways | |||||
Pathway Interaction Database | E2F transcription factor network | ||||
WikiPathways | NRF2 pathway | ||||
Nuclear Receptors Meta-Pathway | |||||
Heroin metabolism | |||||
Irinotecan Pathway | |||||
Fluoropyrimidine Activity | |||||
Phase I biotransformations, non P450 | |||||
References | |||||
Ref 521676 | ClinicalTrials.gov (NCT00151788) Efficacy and Safety of the ACAT Inhibitor CS-505 (Pactimibe) for Reducing the Progression of Carotid Artery Disease. This Study is Also Known as CAPTIVATE.. U.S. National Institutes of Health. | ||||
Ref 522595 | ClinicalTrials.gov (NCT00851500) A Trial of the Safety and Efficacy of K-604 for the Treatment of Atherosclerosis. U.S. National Institutes of Health. | ||||
Ref 541327 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 609). | ||||
Ref 541808 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6701). | ||||
Ref 544811 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001196) | ||||
Ref 544948 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001648) | ||||
Ref 545135 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002257) | ||||
Ref 545142 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002283) | ||||
Ref 545150 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002301) | ||||
Ref 545258 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002618) | ||||
Ref 545279 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002679) | ||||
Ref 545283 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002683) | ||||
Ref 545333 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002876) | ||||
Ref 545390 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003090) | ||||
Ref 545396 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003109) | ||||
Ref 545519 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003587) | ||||
Ref 545520 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003588) | ||||
Ref 545522 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003592) | ||||
Ref 545733 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004427) | ||||
Ref 545745 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004501) | ||||
Ref 545762 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004604) | ||||
Ref 546129 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006465) | ||||
Ref 546451 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008195) | ||||
Ref 546526 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008778) | ||||
Ref 546745 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010079) | ||||
Ref 546902 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010990) | ||||
Ref 526020 | ACAT inhibitor F-1394 prevents intimal hyperplasia induced by balloon injury in rabbits. J Lipid Res. 2001 Apr;42(4):480-8. | ||||
Ref 527138 | Bioorg Med Chem Lett. 2004 Aug 16;14(16):4277-80.Acyl-CoA: cholesterol acyltransferase inhibitory activities of fatty acid amides isolated from Mylabris phalerate Pallas. | ||||
Ref 527510 | J Med Chem. 2005 Apr 21;48(8):2906-15.Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. | ||||
Ref 527692 | J Med Chem. 2005 Aug 25;48(17):5543-50.Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and the flexibility of the dione moiety. | ||||
Ref 528287 | A selective ACAT-1 inhibitor, K-604, suppresses fatty streak lesions in fat-fed hamsters without affecting plasma cholesterol levels. Atherosclerosis. 2007 Apr;191(2):290-7. Epub 2006 Jul 3. | ||||
Ref 528749 | J Med Chem. 2007 Apr 19;50(8):1876-85. Epub 2007 Mar 23.Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. | ||||
Ref 528766 | Bioorg Med Chem. 2007 Jun 1;15(11):3801-17. Epub 2007 Mar 12.Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils. | ||||
Ref 529103 | J Med Chem. 2007 Nov 15;50(23):5727-34. Epub 2007 Oct 17.Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1. | ||||
Ref 529157 | Bioorg Med Chem. 2008 Feb 15;16(4):2114-30. Epub 2007 Nov 26.Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hydrolase (FAAH). | ||||
Ref 529169 | Effects of an anti-oxidative ACAT inhibitor on apoptosis/necrosis and cholesterol accumulation under oxidative stress in THP-1 cell-derived foam cells. Life Sci. 2008 Jan 2;82(1-2):79-84. Epub 2007 Nov 26. | ||||
Ref 529589 | J Med Chem. 2008 Aug 14;51(15):4823-33. Epub 2008 Jul 12.Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical propertiesand biological activities by introduction of carboxylic acid. | ||||
Ref 530348 | Bioorg Med Chem Lett. 2009 Oct 1;19(19):5528-30. Epub 2009 Aug 21.Synthesis of organophosphates with fluorine-containing leaving groups as serine esterase inhibitors with potential for Alzheimer disease therapeutics. | ||||
Ref 531635 | Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36. | ||||
Ref 533344 | CL 277,082: a novel inhibitor of ACAT-catalyzed cholesterol esterification and cholesterol absorption. J Lipid Res. 1989 May;30(5):681-90. | ||||
Ref 533663 | Prospects for drug therapy for hyperlipoproteinaemia. Diabete Metab. 1995 Apr;21(2):139-46. | ||||
Ref 533670 | Potent inhibitors of acyl-CoA:cholesterol acyltransferase. Structure-activity relationships of novel N-(4-oxochroman-8-yl)amides. J Med Chem. 1995 Aug 4;38(16):3174-86. | ||||
Ref 533685 | ACAT inhibitors CL 283,546 and CL 283,796 reduce LDL cholesterol without affecting cholesterol absorption in African green monkeys. J Lipid Res. 1995 Jun;36(6):1199-210. | ||||
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