Target General Infomation
Target ID
T76369 (Former ID: TTDR00274)
Target Name
Liver carboxylesterase (CES1)
Synonyms
Serine esterase 1; Monocyte/macrophage serine esterase; Human carboxylesterase 1; HMSE; HCE1; CES1; Brain carboxylesterase hBr1; Acyl coenzyme A:cholesterol acyltransferase
Gene Name
CES1
Target Type
Successful target
[1]
Disease [+] 2 Target-related Diseases +
1 Peroxisomal disease [ICD-11: 5C57]
2 Synthesis disorder [ICD-11: 5C52-5C59]
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
UniProt ID
EST1_HUMAN
EC Number
EC 3.1.1.1
Sequence
MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPL
GPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLN
IYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFST
GDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLF
HRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLK
MKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIP
MQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDL
IADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPF
LKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLK
DKEVAFWTNLFAKKAVEKPPQTEHIEL
Drugs and Modes of Action
Approved Drug(s) [+] 1 Approved Drugs +
1 Cholic Acid Drug Info Approved Synthesis disorder [2]
Clinical Trial Drug(s) [+] 4 Clinical Trial Drugs +
1 PACTIMIBE Drug Info Phase 2/3 Arteriosclerosis [3]
2 Eldacimibe Drug Info Phase 2 Hyperlipidaemia [4]
3 K-604 Drug Info Phase 2 Arteriosclerosis [5]
4 GR148672X Drug Info Clinical trial Acute lymphoblastic leukaemia [6]
Discontinued Drug(s) [+] 22 Discontinued Drugs +
1 Avasimibe Drug Info Discontinued in Phase 3 Peripheral vascular disease [7]
2 CI-976 Drug Info Discontinued in Phase 2 Hyperlipidaemia [8]
3 CL-283796 Drug Info Discontinued in Phase 2 Hyperlipidaemia [9]
4 E-5324 Drug Info Discontinued in Phase 2 Hyperlipidaemia [10]
5 Eflucimibe Drug Info Discontinued in Phase 2 Hyperlipidaemia [11]
6 RP-64477 Drug Info Discontinued in Phase 2 Hyperlipidaemia [12]
7 447C88 Drug Info Discontinued in Phase 1 Hyperlipidaemia [13]
8 CL-277082 Drug Info Discontinued in Phase 1 Arteriosclerosis [14]
9 F-1394 Drug Info Discontinued in Phase 1 Arteriosclerosis [15]
10 YM-17E Drug Info Discontinued in Phase 1 Hyperlipidaemia [16]
11 YM-750 Drug Info Discontinued in Phase 1 Hyperlipidaemia [17]
12 CEB-925 Drug Info Terminated Hypercholesterolaemia [19]
13 CI-999 Drug Info Terminated Arteriosclerosis [20]
14 DuP-129 Drug Info Terminated Hypercholesterolaemia [21]
15 FR-129169 Drug Info Terminated Arteriosclerosis [22]
16 FR-145237 Drug Info Terminated Arteriosclerosis [23]
17 Lecimibide Drug Info Terminated Hyperlipidaemia [24]
18 NTE-122 Drug Info Terminated Arteriosclerosis [25]
19 PD-132301-2 Drug Info Terminated Arteriosclerosis [26]
20 RP-70676 Drug Info Terminated Hyperlipidaemia [27]
21 RP-73163 Drug Info Terminated Arteriosclerosis [28]
22 TEI-6522 Drug Info Terminated Arteriosclerosis [29]
Preclinical Drug(s) [+] 1 Preclinical Drugs +
1 HL-004 Drug Info Preclinical Arteriosclerosis [18]
Mode of Action [+] 2 Modes of Action +
Inhibitor [+] 123 Inhibitor drugs +
1 Cholic Acid Drug Info [1]
2 PACTIMIBE Drug Info [30]
3 K-604 Drug Info [32]
4 GR148672X Drug Info [33]
5 Avasimibe Drug Info [34]
6 CI-976 Drug Info [35]
7 Eflucimibe Drug Info [31]
8 YM-750 Drug Info [44]
9 CEB-925 Drug Info [46]
10 CI-999 Drug Info [47]
11 DuP-129 Drug Info [33]
12 NTE-122 Drug Info [51]
13 (1R)-1,2,2-TRIMETHYLPROPYL (R)-METHYLPHOSPHINATE Drug Info [56]
14 (E)-Octadec-9-enoic acid phenylamide Drug Info [57]
15 1,1,1-trifluoro-3-(hexylsulfinyl)propan-2-one Drug Info [58]
16 1,1,1-trifluoro-3-(hexylsulfonyl)propan-2-one Drug Info [58]
17 1,1,1-trifluoro-3-(hexylthio)propan-2-one Drug Info [58]
18 1,1,1-trifluoro-3-(octylsulfinyl)propan-2-one Drug Info [58]
19 1,1,1-trifluoro-3-(octylsulfonyl)propan-2-one Drug Info [58]
20 1,1,1-trifluoro-3-(octylthio)propan-2-one Drug Info [58]
21 1,1,1-trifluorododecan-2-one Drug Info [58]
22 1,10-phenanthroline-5,6-dione Drug Info [59]
23 1,2-bis(2,3,4-trifluorophenyl)-2-hydroxyethanone Drug Info [60]
24 1,2-bis(2,3,4-trifluorophenyl)ethane-1,2-dione Drug Info [60]
25 1,2-bis(2,3,5-trifluorophenyl)-2-hydroxyethanone Drug Info [60]
26 1,2-bis(2,3,5-trifluorophenyl)ethane-1,2-dione Drug Info [60]
27 1,2-bis(2,3,6-trifluorophenyl)ethane-1,2-dione Drug Info [60]
28 1,2-bis(2,3-difluorophenyl)-2-hydroxyethanone Drug Info [60]
29 1,2-bis(2,3-fluorophenyl)ethane-1,2-dione Drug Info [60]
30 1,2-bis(2,4-difluorophenyl)-2-hydroxyethanone Drug Info [60]
31 1,2-bis(2,4-difluorophenyl)ethane-1,2-dione Drug Info [60]
32 1,2-bis(2,5-difluorophenyl)-2-hydroxyethanone Drug Info [60]
33 1,2-bis(2,5-difluorophenyl)ethane-1,2-dione Drug Info [60]
34 1,2-bis(2,6-difluorophenyl)-2-hydroxyethanone Drug Info [60]
35 1,2-bis(2,6-difluorophenyl)ethane-1,2-dione Drug Info [60]
36 1,2-bis(2-fluorophenyl)-2-hydroxyethanone Drug Info [60]
37 1,2-bis(2-fluorophenyl)ethane-1,2-dione Drug Info [60]
38 1,2-bis(3,4,5-trifluorophenyl)-2-hydroxyethanone Drug Info [60]
39 1,2-bis(3,4,5-trifluorophenyl)ethane-1,2-dione Drug Info [60]
40 1,2-bis(3,4-difluorophenyl)-2-hydroxyethanone Drug Info [60]
41 1,2-bis(3,4-difluorophenyl)ethane-1,2-dione Drug Info [60]
42 1,2-bis(3,5-difluorophenyl)-2-hydroxyethanone Drug Info [60]
43 1,2-bis(3,5-difluorophenyl)ethane-1,2-dione Drug Info [60]
44 1,2-bis(3-fluorophenyl)-2-hydroxyethanon Drug Info [60]
45 1,2-bis(3-fluorophenyl)ethane-1,2-dione Drug Info [60]
46 1,2-bis(4-fluorophenyl)ethane-1,2-dione Drug Info [60]
47 1,2-Bis-(2-chloro-phenyl)-ethane-1,2-dione Drug Info [61]
48 1,2-Bis-(3-methoxy-phenyl)-ethane-1,2-dione Drug Info [61]
49 1,2-Bis-(3-nitro-phenyl)-ethane-1,2-dione Drug Info [61]
50 1,2-Bis-(4-bromo-phenyl)-ethane-1,2-dione Drug Info [61]
51 1,2-Bis-(4-chloro-phenyl)-ethane-1,2-dione Drug Info [61]
52 1,2-Bis-(4-methoxy-phenyl)-ethane-1,2-dione Drug Info [61]
53 1,2-Di-naphthalen-2-yl-ethane-1,2-dione Drug Info [62]
54 1,2-Di-p-tolyl-ethane-1,2-dione Drug Info [61]
55 1,2-dicyclohexylethane-1,2-dione Drug Info [59]
56 1,2-indanedione Drug Info [59]
57 1,2-NAPHTHOQUINONE Drug Info [59]
58 1-(2-bromoethyl)-1H-indole-2,3-dione Drug Info [63]
59 1-(2-iodoethyl)-1H-indole-2,3-dione Drug Info [63]
60 1-(3,4-dichlorobenzyl)-1H-indole-2,3-dione Drug Info [63]
61 1-(3,4-Dimethyl-phenyl)-2-phenyl-ethane-1,2-dione Drug Info [61]
62 1-(4-Chloro-phenyl)-2-p-tolyl-ethane-1,2-dione Drug Info [61]
63 1-(4-Chloro-phenyl)-2-phenyl-ethane-1,2-dione Drug Info [61]
64 1-(4-chlorobenzyl)-1H-indole-2,3-dione Drug Info [63]
65 1-(4-Methoxy-phenyl)-2-phenyl-ethane-1,2-dione Drug Info [61]
66 1-(4-Nitro-phenyl)-2-phenyl-ethane-1,2-dione Drug Info [61]
67 1-benzyl-1H-indole-2,3-dione Drug Info [63]
68 1-butyryl-1H-indole-2,3-dione Drug Info [63]
69 1-dodecyl-1H-indole-2,3-dione Drug Info [63]
70 1-hexadecyl-1H-indole-2,3-dione Drug Info [63]
71 1-methyl-1H-indole-2,3-dione Drug Info [63]
72 1-phenyl-1H-indole-2,3-dione Drug Info [63]
73 1-Phenyl-2-p-tolyl-ethane-1,2-dione Drug Info [61]
74 1-Phenyl-propane-1,2-dione Drug Info [61]
75 1-propionyl-1H-indole-2,3-dione Drug Info [63]
76 11,12-dihydro-dibenzo[a,e]cyclooctene-5,6-dione Drug Info [59]
77 2,2-Dimethoxy-1,2-diphenyl-ethanone Drug Info [61]
78 2,2-dimethyl-3-methyleneheptadecane Drug Info [58]
79 2-methoxy-3,4-methylenedioxybenzophenone Drug Info [64]
80 3,4,5,6-Tetrachloro-[1,2]benzoquinone Drug Info [61]
81 3,5-Di-tert-butyl-[1,2]benzoquinone Drug Info [61]
82 3-(butylsulfinyl)-1,1,1-trifluoropropan-2-one Drug Info [58]
83 3-(butylthio)-1,1,1-trifluoropropan-2-one Drug Info [58]
84 3-(decylsulfinyl)-1,1,1-trifluoropropan-2-one Drug Info [58]
85 3-(decylsulfonyl)-1,1,1-trifluoropropan-2-one Drug Info [58]
86 3-(decylthio)-1,1,1-trifluoropropan-2-one Drug Info [58]
87 3-(dodecylsulfinyl)-1,1,1-trifluoropropan-2-one Drug Info [58]
88 3-(dodecylsulfonyl)-1,1,1-trifluoropropan-2-one Drug Info [58]
89 4,5-dichloro-1H-indole-2,3-dione Drug Info [63]
90 4,6-dichloro-1H-indole-2,3-dione Drug Info [63]
91 4,7-dichloro-1H-indole-2,3-dione Drug Info [63]
92 4-(2-Oxo-2-phenyl-acetyl)-benzoic acid Drug Info [61]
93 4-chloro-1H-indole-2,3-dione Drug Info [63]
94 4-chloro-7-methyl-1H-indole-2,3-dione Drug Info [63]
95 4-Piperidino-Piperidine Drug Info [56]
96 5,6-dinitroacenaphthoquinone Drug Info [59]
97 5,7-dichloro-1H-indole-2,3-dione Drug Info [63]
98 5-(trifluoromethoxy)-1H-indole-2,3-dione Drug Info [63]
99 5-chloro-1H-indole-2,3-dione Drug Info [63]
100 6,7-dichloro-1H-indole-2,3-dione Drug Info [63]
101 6-bromo-5-methyl-1H-indole-2,3-dione Drug Info [63]
102 7-(trifluoromethyl)-1H-indole-2,3-dione Drug Info [63]
103 7-chloro-1H-indole-2,3-dione Drug Info [63]
104 Acenanthrene-9,10-dione Drug Info [59]
105 ACENAPHTHOQUINONE Drug Info [59]
106 Alpha-D-Mannose Drug Info [1]
107 BENZIL Drug Info [58]
108 BENZOIN Drug Info [60]
109 CHLORANIL Drug Info [61]
110 Dibutyl 2,2,2-trifluoro-1-phenylethyl phosphate Drug Info [65]
111 Diethyl 2,2,2-trifluoro-1-phenylethyl phosphate Drug Info [65]
112 Dimethyl 2,2,2-trifluoro-1-phenylethyl phosphate Drug Info [65]
113 Heptane-2,3-dione Drug Info [61]
114 N-Methylnaloxonium Drug Info [66]
115 NSC-23180 Drug Info [59]
116 O-Sialic Acid Drug Info [56]
117 Oleic acid anilide Drug Info [64]
118 Phenanthrene-9,10-dione Drug Info [59]
119 PYRIPYROPENE A Drug Info [57]
120 SCH-48375 Drug Info [67]
121 Thenoyltrifluoroacetone Drug Info [69]
122 Thieno[3,2-e][1]benzothiophene-4,5-dione Drug Info [59]
123 VULM-1457 Drug Info [33]
Modulator [+] 18 Modulator drugs +
1 Eldacimibe Drug Info [31]
2 CL-283796 Drug Info [36], [37]
3 E-5324 Drug Info [38]
4 RP-64477 Drug Info [39]
5 447C88 Drug Info [40]
6 CL-277082 Drug Info [41]
7 F-1394 Drug Info [42]
8 YM-17E Drug Info [43]
9 HL-004 Drug Info [45]
10 FR-129169 Drug Info [48]
11 FR-145237 Drug Info [49]
12 Lecimibide Drug Info [50]
13 PD-132301-2 Drug Info [52]
14 RP-70676 Drug Info [53]
15 RP-73163 Drug Info [54]
16 TEI-6522 Drug Info [55]
17 KY-382 Drug Info [33]
18 SMP-797 Drug Info [68]
Target Profiles in Patients
Target Expression
 Profile (TEP)
Target Affiliated Biological Pathways
KEGG Pathway [+] 2 KEGG Pathways +
1 Drug metabolism - other enzymes
2 Metabolic pathways
PID Pathway [+] 1 PID Pathways +
1 E2F transcription factor network
WikiPathways [+] 6 WikiPathways +
1 NRF2 pathway
2 Nuclear Receptors Meta-Pathway
3 Heroin metabolism
4 Irinotecan Pathway
5 Fluoropyrimidine Activity
6 Phase I biotransformations, non P450
Target-Related Models and Studies
Target Validation
References
REF 1 How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 2 URL: 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 3 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 4 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 5 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 6 URL: 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 7 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 8 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 9 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 10 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 11 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800011031)
REF 12 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 13 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 14 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 15 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 16 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 17 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 18 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033616)
REF 19 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 20 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 21 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 22 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 23 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 24 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 25 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 26 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 27 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 28 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 29 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 30 Novel indoline-based acyl-CoA:cholesterol acyltransferase inhibitor with antiperoxidative activity: improvement of physicochemical properties and b... J Med Chem. 2008 Aug 14;51(15):4823-33.
REF 31 Prospects for drug therapy for hyperlipoproteinaemia. Diabete Metab. 1995 Apr;21(2):139-46.
REF 32 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.
REF 33 URL: 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 34 New advances in lipid-modifying therapies for reducing cardiovascular risk. Cardiology. 2002;97(2):59-66.
REF 35 Acyl-coenzyme A:cholesterol-acyltransferase (ACAT) inhibitors modulate monocyte adhesion to aortic endothelial cells. Atherosclerosis. 1995 Jan 6;112(1):7-17.
REF 36 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.
REF 37 Therapeutic target database update 2012: a resource for facilitating target-oriented drug discovery. Nucleic Acids Res. 2012 Jan;40(Database issue):D1128-36.
REF 38 Effect of the acyl-CoA:cholesterol acyltransferase inhibitor, E5324, on experimental atherosclerosis in rabbits. Atherosclerosis. 1994 Jun;107(2):187-201.
REF 39 RP 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 40 The 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 41 CL 277,082: a novel inhibitor of ACAT-catalyzed cholesterol esterification and cholesterol absorption. J Lipid Res. 1989 May;30(5):681-90.
REF 42 ACAT inhibitor F-1394 prevents intimal hyperplasia induced by balloon injury in rabbits. J Lipid Res. 2001 Apr;42(4):480-8.
REF 43 Pharmacological 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 44 Effects of an anti-oxidative ACAT inhibitor on apoptosis/necrosis and cholesterol accumulation under oxidative stress in THP-1 cell-derived foam ce... Life Sci. 2008 Jan 2;82(1-2):79-84.
REF 45 ACAT 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 46 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 47 Inhibitors 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 48 Plasma 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 49 Effect 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 50 Effect 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 51 Cholesterol-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 52 Divergent 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 53 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 54 Hypolipidaemic 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 55 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 56 The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 57 Acyl-CoA: cholesterol acyltransferase inhibitory activities of fatty acid amides isolated from Mylabris phalerate Pallas. Bioorg Med Chem Lett. 2004 Aug 16;14(16):4277-80.
REF 58 Influence of sulfur oxidation state and steric bulk upon trifluoromethyl ketone (TFK) binding kinetics to carboxylesterases and fatty acid amide hy... Bioorg Med Chem. 2008 Feb 15;16(4):2114-30.
REF 59 Planarity and constraint of the carbonyl groups in 1,2-diones are determinants for selective inhibition of human carboxylesterase 1. J Med Chem. 2007 Nov 15;50(23):5727-34.
REF 60 Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils. Bioorg Med Chem. 2007 Jun 1;15(11):3801-17.
REF 61 Identification and characterization of novel benzil (diphenylethane-1,2-dione) analogues as inhibitors of mammalian carboxylesterases. J Med Chem. 2005 Apr 21;48(8):2906-15.
REF 62 Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and t... J Med Chem. 2005 Aug 25;48(17):5543-50.
REF 63 Selective inhibition of carboxylesterases by isatins, indole-2,3-diones. J Med Chem. 2007 Apr 19;50(8):1876-85.
REF 64 Phenolic compounds from the roots of Lindera fruticosa. J Nat Prod. 2006 May;69(5):853-5.
REF 65 Synthesis of organophosphates with fluorine-containing leaving groups as serine esterase inhibitors with potential for Alzheimer disease therapeutics. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5528-30.
REF 66 DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-41.
REF 67 2-Azetidinones as inhibitors of cholesterol absorption. J Med Chem. 1994 Jun 10;37(12):1733-6.
REF 68 Company report (Dainippon Sumitomo Pharma)
REF 69 Zhang JG, Fariss MW: Thenoyltrifluoroacetone, a potent inhibitor of carboxylesterase activity. Biochem Pharmacol. 2002 Feb 15;63(4):751-4.

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