Target Information

Target General Infomation
Target ID
T76369
Former ID
TTDR00274
Target Name
Liver carboxylesterase
Gene Name
CES1
Synonyms
ACAT; Acyl coenzyme A:cholesterol acyltransferase; Brain carboxylesterase hBr1; HCE1; HMSE; Human carboxylesterase 1; Monocyte/macrophage serine esterase; Serine esterase 1; CES1
Target Type
Clinical Trial
Disease Arteriosclerosis [ICD9: 440; ICD10: I70]
Atherosclerosis [ICD9: 414.0, 440; ICD10: I70]
Acute lymphoblastic leukemia [ICD9: 204.0, 556; ICD10: C91.0]
Hypercholesterolemia [ICD10: E78]
Hyperlipidaemia [ICD9: 272.0-272.4; 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.
BioChemical Class
Carboxylic ester hydrolase
Target Validation
T76369
UniProt ID
P23141
EC Number
EC 3.1.1.56
Sequence
MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPL
GPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLN
IYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFST
GDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLF
HRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLK
MKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIP
MQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDL
IADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPF
LKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLK
DKEVAFWTNLFAKKAVEKPPQTEHIEL
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 521676ClinicalTrials.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 522595ClinicalTrials.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 544811Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001196)
Ref 544948Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800001648)
Ref 545135Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002257)
Ref 545142Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002283)
Ref 545150Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002301)
Ref 545258Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002618)
Ref 545279Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002679)
Ref 545283Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002683)
Ref 545333Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002876)
Ref 545390Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003090)
Ref 545396Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003109)
Ref 545519Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003587)
Ref 545520Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003588)
Ref 545522Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003592)
Ref 545733Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004427)
Ref 545745Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004501)
Ref 545762Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004604)
Ref 546129Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800006465)
Ref 546451Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008195)
Ref 546526Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008778)
Ref 546745Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010079)
Ref 546902Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010990)
Ref 546909Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011031)
Ref 549199Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033616)
Ref 526020ACAT inhibitor F-1394 prevents intimal hyperplasia induced by balloon injury in rabbits. J Lipid Res. 2001 Apr;42(4):480-8.
Ref 527138Bioorg 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 527510J 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 527692J 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 528217J Nat Prod. 2006 May;69(5):853-5.Phenolic compounds from the roots of Lindera fruticosa.
Ref 528287A 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 528749J Med Chem. 2007 Apr 19;50(8):1876-85. Epub 2007 Mar 23.Selective inhibition of carboxylesterases by isatins, indole-2,3-diones.
Ref 528766Bioorg 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 529103J 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 529157Bioorg 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 529169Effects 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 529589J 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 530348Bioorg 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 531635Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
Ref 533344CL 277,082: a novel inhibitor of ACAT-catalyzed cholesterol esterification and cholesterol absorption. J Lipid Res. 1989 May;30(5):681-90.
Ref 533663Prospects for drug therapy for hyperlipoproteinaemia. Diabete Metab. 1995 Apr;21(2):139-46.
Ref 533670Potent 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 533685ACAT 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.
Ref 533828Effect of the acyl-CoA:cholesterol acyltransferase inhibitor, E5324, on experimental atherosclerosis in rabbits. Atherosclerosis. 1994 Jun;107(2):187-201.
Ref 533851J Med Chem. 1994 Jun 10;37(12):1733-6.2-Azetidinones as inhibitors of cholesterol absorption.
Ref 533861Effect of the acyl-CoA:cholesterol acyltransferase inhibitor DuP 128 on cholesterol absorption and serum cholesterol in humans. Clin Pharmacol Ther. 1994 Jul;56(1):65-74.
Ref 533950Divergent pharmacologic activities of PD 132301-2 and CL 277,082, urea inhibitors of acyl-CoA:cholesterol acyltransferase. J Pharmacol Exp Ther. 1993 Nov;267(2):734-43.
Ref 534076Effect of FR145237, a novel ACAT inhibitor, on atherogenesis in cholesterol-fed and WHHL rabbits. Evidence for a direct effect on the arterial wall. Biochim Biophys Acta. 1995 Dec 7;1259(3):254-60.
Ref 534116RP 64477: a potent inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase with low systemic bioavailability. Biochem Pharmacol. 1996 Feb 23;51(4):413-21.
Ref 534137The tolerability, pharmacokinetics and lack of effect on plasma cholesterol of 447C88, an AcylCoA: Cholesterol Acyl Transferase (ACAT) inhibitor with low bioavailability, in healthy volunteers. Eur JClin Pharmacol. 1995;49(3):243-9.
Ref 534219Plasma cholesterol reducing effect of FR129169, a novel acyl-CoA:cholesterol acyltransferase inhibitor, in the rat. Jpn J Pharmacol. 1996 Jan;70(1):35-41.
Ref 534282Hypolipidaemic properties of a potent and bioavailable alkylsulphinyl-diphenylimidazole ACAT inhibitor (RP 73163) in animals fed diets low in cholesterol. Biochem Pharmacol. 1996 Oct 25;52(8):1177-86.
Ref 534326Pharmacological properties of YM17E, an acyl-CoA:cholesterol acyltransferase inhibitor, and diarrheal effect in beagle dogs. Jpn J Pharmacol. 1997 Jan;73(1):41-50.
Ref 534440ACAT inhibitor HL-004 accelerates the regression of hypercholesterolemia in stroke-prone spontaneously hypertensive rats (SHRSP): stimulation of bile acid production by HL-004. Atherosclerosis. 1997 Aug;133(1):97-104.
Ref 534779Cholesterol-lowering effects of NTE-122, a novel acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor, on cholesterol diet-fed rats and rabbits. Jpn J Pharmacol. 1998 Nov;78(3):355-64.
Ref 534786Inhibitors of acyl-CoA:cholesterol O-acyltransferase (ACAT) as hypocholesterolemic agents: synthesis and structure-activity relationships of novel series of sulfonamides, acylphosphonamides and acylphosphoramidates. Bioorg Med Chem Lett. 1998 Feb 3;8(3):289-94.
Ref 535439New advances in lipid-modifying therapies for reducing cardiovascular risk. Cardiology. 2002;97(2):59-66.
Ref 537864Acyl-coenzyme A:cholesterol-acyltransferase (ACAT) inhibitors modulate monocyte adhesion to aortic endothelial cells. Atherosclerosis. 1995 Jan 6;112(1):7-17.
Ref 543651(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. (Target id: 2592).
Ref 545334Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002876)
Ref 546746Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800010079)
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
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