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Details on Person UniProt:P23141 CES1
| Class:Id | ReferenceGeneProduct:54474 |
|---|---|
| _chainChangeLog | signal peptide:1-17 added on Sat February 7 2015;chain:18-567 added on Sat February 7 2015 |
| _displayName | UniProt:P23141 CES1 |
| _timestamp | 2026-02-20 22:09:28 |
| chain | signal peptide:1-17 chain:18-567 |
| checksum | D3A00BDCDC7E5DFF |
| comment | FUNCTION Involved in the detoxification of xenobiotics and in the activation of ester and amide prodrugs (PubMed:18762277, PubMed:7980644, PubMed:9169443, PubMed:9490062). Hydrolyzes aromatic and aliphatic esters, but has no catalytic activity toward amides or a fatty acyl-CoA ester (PubMed:18762277, PubMed:7980644, PubMed:9169443, PubMed:9490062). Hydrolyzes the methyl ester group of cocaine to form benzoylecgonine (PubMed:7980644). Catalyzes the transesterification of cocaine to form cocaethylene (PubMed:7980644). Displays fatty acid ethyl ester synthase activity, catalyzing the ethyl esterification of oleic acid to ethyloleate (PubMed:7980644). Converts monoacylglycerides to free fatty acids and glycerol. Hydrolyzes of 2-arachidonoylglycerol and prostaglandins (PubMed:21049984). Hydrolyzes cellular cholesteryl esters to free cholesterols and promotes reverse cholesterol transport (RCT) by facilitating both the initial and final steps in the process (PubMed:11015575, PubMed:16024911, PubMed:16971496, PubMed:18762277). First of all, allows free cholesterol efflux from macrophages to extracellular cholesterol acceptors and secondly, releases free cholesterol from lipoprotein-delivered cholesteryl esters in the liver for bile acid synthesis or direct secretion into the bile (PubMed:16971496, PubMed:18599737, PubMed:18762277).CATALYTIC ACTIVITY a carboxylic ester + H2O = an alcohol + a carboxylate + H(+)CATALYTIC ACTIVITY 4-methylumbelliferyl acetate + H2O = 4-methylumbelliferone + acetate + H(+)CATALYTIC ACTIVITY a cholesterol ester + H2O = cholesterol + a fatty acid + H(+)CATALYTIC ACTIVITY cholesteryl (9Z-octadecenoate) + H2O = cholesterol + (9Z)-octadecenoate + H(+)CATALYTIC ACTIVITY 2-(5Z,8Z,11Z,14Z-eicosatetraenoyl)-glycerol + H2O = glycerol + (5Z,8Z,11Z,14Z)-eicosatetraenoate + H(+)CATALYTIC ACTIVITY prostaglandin E2 1-glyceryl ester + H2O = prostaglandin E2 + glycerol + H(+)CATALYTIC ACTIVITY prostaglandin F2alpha 1-glyceryl ester + H2O = prostaglandin F2alpha + glycerol + H(+)ACTIVITY REGULATION Activated by CHAPS (PubMed:9490062). Inhibited by chlorpyrifos oxon (IC(50)=0.21 nM), paraoxon (IC(50)=0.29 nM), or methyl paraoxon (IC(50)=49 nM) (PubMed:18762277).BIOPHYSICOCHEMICAL PROPERTIES kcat is 59 min(-1), 29 min(-1), 90 min(-1) with 2-arachidonoylglycerol, prostaglandin F2alpha 1-glyceryl ester and prostaglandin E2 1-glyceryl ester as substrates, respectively.SUBUNIT Homotrimer and homohexamer. Binds to beta-glucuronidase.INTERACTION Moves from cytoplasm to lipid droplets upon lipid loading. Associates with lipid droplets independently of triglycerides (TG) content of the droplets and hydrolyzes cholesteryl esters more efficiently from mixed droplets.ALTERNATIVE PRODUCTS Expressed predominantly in liver with lower levels in heart and lung (PubMed:10562416). Expressed in macrophages (PubMed:11015575, PubMed:18762277, PubMed:21049984).PTM Contains sialic acid.PTM Cleavage of the signal sequence can occur at 2 positions, either between Trp-17 and Gly-18 or between Gly-18 and His-19.POLYMORPHISM Genetic variants in CES1 are associated with clinically significant alterations in pharmacokinetics and drug response of carboxylesterase 1 substrates [MIM:618057].MISCELLANEOUS Involved in the activation pathway of bemnifosbuvir (AT-527) and its epimer, AT-752 (PubMed:39190717). AT-527 and AT-752 are two guanosine analogs tested in clinical trials against several RNA viruses, which are activated into their common 5'-triphosphate AT-9010 in human cells (PubMed:39190717). Mediates the first activation step by catalyzing transformation of AT-527 and AT-75 into AT-551 (PubMed:39190717).SIMILARITY Belongs to the type-B carboxylesterase/lipase family. |
| description | recommendedName: fullName evidence="22"Liver carboxylesterase 1 alternativeName: Acyl-coenzyme A:cholesterol acyltransferase shortName: ACAT alternativeName: Brain carboxylesterase hBr1 alternativeName: Carboxylesterase 1 shortName: CE-1 shortName: hCE-1 ecNumber evidence="14 16 17"3.1.1.1 alternativeName: fullName evidence="18"Cholesteryl ester hydrolase shortName evidence="18"CEH ecNumber evidence="3 7 8 11"3.1.1.13 alternativeName: Cocaine carboxylesterase alternativeName: Egasyn alternativeName: HMSE alternativeName: Methylumbelliferyl-acetate deacetylase 1 ecNumber evidence="11 16"3.1.1.56 alternativeName: Monocyte/macrophage serine esterase alternativeName: Retinyl ester hydrolase shortName: REH alternativeName: Serine esterase 1 alternativeName: Triacylglycerol hydrolase shortName: TGH |
| geneName | CES1 CES2 SES1 |
| identifier | P23141 |
| isSequenceChanged | FALSE |
| keyword | 3D-structure Alternative splicing Cytoplasm Direct protein sequencing Disulfide bond Endoplasmic reticulum Glycoprotein Hydrolase Lipid droplet Lipid metabolism Phosphoprotein Proteomics identification Reference proteome Serine esterase Signal |
| modified | [InstanceEdit:84067] Schmidt, EE, 2003-12-18 04:29:09 [InstanceEdit:143527] Schmidt, EE, 2004-11-12 07:45:10 [InstanceEdit:217385] Schmidt, EE, 2008-03-27 06:23:53 [InstanceEdit:354386] Schmidt, EE, 2008-06-18 04:45:12 [InstanceEdit:384350] Kanapin, AA, 2008-11-26 14:00:39 [InstanceEdit:392885] Kanapin, AA, 2009-03-09 12:07:18 [InstanceEdit:400710] Schmidt, EE, 2009-03-25 05:33:35 [InstanceEdit:423310] Kanapin, AA [InstanceEdit:435478] Kanapin, AA [InstanceEdit:435871] Kanapin, AA [InstanceEdit:447347] Kanapin, AA [InstanceEdit:525883] Kanapin, AA [InstanceEdit:613449] Kanapin, AA [InstanceEdit:797602] Kanapin, AA [InstanceEdit:937368] Yung, CK [InstanceEdit:1042053] Yung, CK [InstanceEdit:1220657] Yung, CK [InstanceEdit:1300696] Yung, CK [InstanceEdit:1301627] Yung, CK [InstanceEdit:1551960] Weiser, JD [InstanceEdit:1995863] Weiser, JD [InstanceEdit:2132304] Weiser, JD [InstanceEdit:2265580] Weiser, JD [InstanceEdit:2455454] Weiser, JD [InstanceEdit:4341137] Weiser, JD [InstanceEdit:5433710] Weiser, JD [InstanceEdit:5618415] Weiser, JD [InstanceEdit:5634237] Weiser, JD [InstanceEdit:5673015] Weiser, JD [InstanceEdit:5691543] Weiser, JD [InstanceEdit:8856987] Weiser, JD [InstanceEdit:8869714] Weiser, JD [InstanceEdit:8987656] Weiser, JD [InstanceEdit:9037114] Weiser, JD [InstanceEdit:9627708] Weiser, JD [InstanceEdit:9637257] Weiser, JD [InstanceEdit:9676415] Weiser, JD [InstanceEdit:9698430] Weiser, JD [InstanceEdit:9715482] Weiser, JD [InstanceEdit:9730071] Weiser, JD [InstanceEdit:9767224] Weiser, Joel [InstanceEdit:9852000] Weiser, Joel, 2023-11-03 [InstanceEdit:9917590] Weiser, Joel, 2024-08-09 [InstanceEdit:9926675] Weiser, Joel, 2024-11-03 [InstanceEdit:9939033] Weiser, Joel, 2025-02-21 [InstanceEdit:9983091] Weiser, Joel, 2026-02-20 |
| name | CES1 |
| referenceDatabase | [ReferenceDatabase:2] UniProt |
| referenceGene | [ReferenceDNASequence:8989503] ENSEMBL:ENSG00000198848 CES1 [Homo sapiens] |
| secondaryIdentifier | EST1_HUMAN A6NIM1 A8K3K8 A8K844 E9PAU8 P82127 Q00015 Q13657 Q14062 Q16737 Q16788 Q549X7 Q549X8 Q86UK2 Q96EE8 Q9UC52 Q9UDG8 Q9UK77 Q9ULY2 |
| sequenceLength | 567 |
| species | [Species:48887] Homo sapiens |
| (isoformParent) | [ReferenceIsoform:228538] UniProt:P23141-2 CES1 [Homo sapiens] [ReferenceIsoform:403361] UniProt:P23141-1 CES1 [Homo sapiens] [ReferenceIsoform:8968276] UniProt:P23141-3 CES1 [Homo sapiens] |
| (referenceEntity) | [EntityWithAccessionedSequence:2429659] CES1 [endoplasmic reticulum lumen] [Homo sapiens] [EntityWithAccessionedSequence:9727618] CES1 [lipid droplet] [Homo sapiens] |
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No pathways have been reviewed or authored by UniProt:P23141 CES1 (54474)
