Liver carboxylesterase 1
Details
- Name
- Liver carboxylesterase 1
- Kind
- protein
- Synonyms
- ACAT
- Acyl-coenzyme A:cholesterol acyltransferase
- Brain carboxylesterase hBr1
- Carboxylesterase 1
- CE-1
- CEH
- CES2
- Cholesteryl ester hydrolase
- Cocaine carboxylesterase
- Egasyn
- hCE-1
- HMSE
- Methylumbelliferyl-acetate deacetylase 1
- Monocyte/macrophage serine esterase
- REH
- Retinyl ester hydrolase
- Serine esterase 1
- SES1
- TGH
- Triacylglycerol hydrolase
- Gene Name
- CES1
- UniProtKB Entry
- P23141Swiss-Prot
- Organism
- Humans
- NCBI Taxonomy ID
- 9606
- Amino acid sequence
>lcl|BSEQ0005305|Liver carboxylesterase 1 MWLRAFILATLSASAAWGHPSSPPVVDTVHGKVLGKFVSLEGFAQPVAIFLGIPFAKPPL GPLRFTPPQPAEPWSFVKNATSYPPMCTQDPKAGQLLSELFTNRKENIPLKLSEDCLYLN IYTPADLTKKNRLPVMVWIHGGGLMVGAASTYDGLALAAHENVVVVTIQYRLGIWGFFST GDEHSRGNWGHLDQVAALRWVQDNIASFGGNPGSVTIFGESAGGESVSVLVLSPLAKNLF HRAISESGVALTSVLVKKGDVKPLAEQIAITAGCKTTTSAVMVHCLRQKTEEELLETTLK MKFLSLDLQGDPRESQPLLGTVIDGMLLLKTPEELQAERNFHTVPYMVGINKQEFGWLIP MQLMSYPLSEGQLDQKTAMSLLWKSYPLVCIAKELIPEATEKYLGGTDDTVKKKDLFLDL IADVMFGVPSVIVARNHRDAGAPTYMYEFQYRPSFSSDMKPKTVIGDHGDELFSVFGAPF LKEGASEEEIRLSKMVMKFWANFARNGNPNGEGLPHWPEYNQKEGYLQIGANTQAAQKLK DKEVAFWTNLFAKKAVEKPPQTEHIEL
- Number of residues
- 567
- Molecular Weight
- 62520.62
- Theoretical pI
- 6.58
- GO Classification
- Functionscarboxylesterase activityProcessescellular response to cholesterol / cellular response to low-density lipoprotein particle stimulus / cholesterol biosynthetic process / cholesterol ester hydrolysis involved in cholesterol transport / cholesterol homeostasis / cholesterol metabolic process / medium-chain fatty acid metabolic process / negative regulation of cholesterol storage / positive regulation of cholesterol efflux / positive regulation of cholesterol metabolic process / regulation of bile acid biosynthetic process / regulation of bile acid secretion / reverse cholesterol transportComponentscytoplasm / cytosol / endoplasmic reticulum / lipid droplet
- General 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)
- Specific Function
- carboxylesterase activity
- Pfam Domain Function
- COesterase (PF00135)
- Signal Regions
- 1-17
- Transmembrane Regions
- Not Available
- Cellular Location
- Endoplasmic reticulum lumen
- Gene sequence
>lcl|BSEQ0021334|Liver carboxylesterase 1 (CES1) ATGTGGCTCCGTGCCTTTATCCTGGCCACTCTCTCTGCTTCCGCGGCTTGGGGGCATCCG TCCTCGCCACCTGTGGTGGACACCGTGCATGGCAAAGTGCTGGGGAAGTTCGTCAGCTTA GAAGGATTTGCACAGCCTGTGGCCATTTTCCTGGGAATCCCTTTTGCCAAGCCGCCTCTT GGACCCCTGAGGTTTACTCCACCGCAGCCTGCAGAACCATGGAGCTTTGTGAAGAATGCC ACCTCGTACCCTCCTATGTGCACCCAAGATCCCAAGGCGGGGCAGTTACTCTCAGAGCTA TTTACAAACCGAAAGGAGAACATTCCTCTCAAGCTTTCTGAAGACTGTCTTTACCTCAAT ATTTACACTCCTGCTGACTTGACCAAGAAAAACAGGCTGCCGGTGATGGTGTGGATCCAC GGAGGGGGGCTGATGGTGGGTGCGGCATCAACCTATGATGGGCTGGCCCTTGCTGCCCAT GAAAACGTGGTGGTGGTGACCATTCAATATCGCCTGGGCATCTGGGGATTCTTCAGCACA GGGGATGAACACAGCCGGGGGAACTGGGGTCACCTGGACCAGGTGGCTGCCCTGCGCTGG GTCCAGGACAACATTGCCAGCTTTGGAGGGAACCCAGGCTCTGTGACCATCTTTGGAGAG TCAGCGGGAGGAGAAAGTGTCTCTGTTCTTGTTTTGTCTCCATTGGCCAAGAACCTCTTC CACCGGGCCATTTCTGAGAGTGGCGTGGCCCTCACTTCTGTTCTGGTGAAGAAAGGTGAT GTCAAGCCCTTGGCTGAGCAAATTGCTATCACTGCTGGGTGCAAAACCACCACCTCTGCT GTCATGGTTCACTGCCTGCGACAGAAGACGGAAGAGGAGCTCTTGGAGACGACATTGAAA ATGAAATTCTTATCTCTGGACTTACAGGGAGACCCCAGAGAGAGTCAACCCCTTCTGGGC ACTGTGATTGATGGGATGCTGCTGCTGAAAACACCTGAAGAGCTTCAAGCTGAAAGGAAT TTCCACACTGTCCCCTACATGGTCGGAATTAACAAGCAGGAGTTTGGCTGGTTGATTCCA ATGCAGTTGATGAGCTATCCACTCTCCGAAGGGCAACTGGACCAGAAGACAGCCATGTCA CTCCTGTGGAAGTCCTATCCCCTTGTTTGCATTGCTAAGGAACTGATTCCAGAAGCCACT GAGAAATACTTAGGAGGAACAGACGACACTGTCAAAAAGAAAGACCTGTTCCTGGACTTG ATAGCAGATGTGATGTTTGGTGTCCCATCTGTGATTGTGGCCCGGAACCACAGAGATGCT GGAGCACCCACCTACATGTATGAGTTTCAGTACCGTCCAAGCTTCTCATCAGACATGAAA CCCAAGACGGTGATAGGAGACCACGGGGATGAGCTCTTCTCCGTCTTTGGGGCCCCATTT TTAAAAGAGGGTGCCTCAGAAGAGGAGATCAGACTTAGCAAGATGGTGATGAAATTCTGG GCCAACTTTGCTCGCAATGGAAACCCCAATGGGGAAGGGCTGCCCCACTGGCCAGAGTAC AACCAGAAGGAAGGGTATCTGCAGATTGGTGCCAACACCCAGGCGGCCCAGAAGCTGAAG GACAAAGAAGTAGCTTTCTGGACCAACCTCTTTGCCAAGAAGGCAGTGGAGAAGCCACCC CAGACAGAACACATAGAGCTGTGA
- Chromosome Location
- 16
- Locus
- 16q12.2
- External Identifiers
Resource Link UniProtKB ID P23141 UniProtKB Entry Name EST1_HUMAN GenBank Gene ID M73499 GeneCard ID CES1 GenAtlas ID CES1 HGNC ID HGNC:1863 PDB ID(s) 1MX1, 1MX5, 1MX9, 1YA4, 1YA8, 1YAH, 1YAJ, 2DQY, 2DQZ, 2DR0, 2H7C, 2HRQ, 2HRR, 3K9B, 4AB1, 5A7F, 5A7G, 5A7H, 8EOR KEGG ID hsa:1066 IUPHAR/Guide To Pharmacology ID 2592 NCBI Gene ID 1066 - General References
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Associated Data
- Drug Relations
Drug Drug group Pharmacological action? Type Actions Details Thenoyltrifluoroacetone experimental yes target inhibitor Details Hydroxy-Phenyl-Acetic Acid 8-Methyl-8-Aza-Bicyclo[3.2.1]Oct-3-Yl Ester experimental unknown target Details N-acetyl-alpha-neuraminic acid experimental yes target inhibitor Details Avasimibe investigational yes target inhibitor Details Capecitabine approved, investigational no enzyme substrate Details Tamoxifen approved unknown enzyme inhibitor Details Indomethacin approved, investigational unknown enzyme substrate Details Mevastatin experimental unknown enzyme inhibitor Details 4-Piperidino-Piperidine experimental yes target inhibitor Details Cholic Acid approved yes target inhibitor Details (1R)-1,2,2-trimethylpropyl (R)-methylphosphinate experimental unknown target Details (1S,7S,8S,8AR)-1,2,3,7,8,8A-HEXAHYDRO-7-METHYL-8-[2-[(2R,4R)-TETRAHYDRO-4-HY DROXY-6-OXO-2H-PYRAN-2-YL]ETHYL]-1-NAPHTHALENOL experimental unknown target Details Ciclesonide approved, investigational unknown enzyme substrate Details Levocarnitine approved, investigational unknown target Details Cyclandelate approved unknown target Details Probucol approved, investigational unknown target Details Benzocaine approved, investigational unknown enzyme inhibitor Details Trandolapril approved unknown enzyme substrate Details Rufinamide approved unknown enzyme substrate Details Dabigatran etexilate approved unknown enzyme substrate Details Clopidogrel approved no enzyme substrate Details Mycophenolate mofetil approved, investigational unknown enzyme substrate Details Selexipag approved no enzyme substrate Details Phenylacetic acid approved unknown enzyme substrate Details Meperidine approved unknown target Details Dextropropoxyphene approved, illicit, investigational, withdrawn unknown target Details Naloxone approved, vet_approved unknown target binder Details Tacrine approved, investigational, withdrawn unknown target Details Cocaine approved, illicit unknown target binder Details Diamorphine approved, illicit, investigational unknown target Details Propoxycaine approved unknown enzyme substrate Details Homatropine approved unknown enzyme substrate Details Tenofovir alafenamide approved no enzyme substrate Details Oseltamivir approved yes enzyme substrate Details Quinapril approved, investigational unknown enzyme substrate Details Fenofibrate approved unknown enzyme substrate Details Cocaine approved, illicit unknown enzyme substrate Details Remimazolam approved, investigational unknown enzyme substrate Details Filgotinib approved, investigational unknown enzyme metabolizer Details Remdesivir approved, investigational yes enzyme substrate Details Flupentixol approved, investigational, withdrawn no enzyme inhibitor Details Vicagrel investigational unknown enzyme substrate Details Cannabidiol approved, investigational no enzyme inhibitor Details Dronabinol approved, illicit no enzyme inhibitor Details Cannabinol experimental, investigational unknown enzyme inhibitor Details Medical Cannabis experimental, investigational unknown enzyme inhibitor Details Simvastatin approved unknown enzyme inhibitor Details Telotristat ethyl approved, investigational no enzyme substrate Details N-Methylnaloxonium experimental yes target inhibitor Details Benzoin approved, experimental yes target inhibitor Details 1,1,1-TRIFLUORO-3-(OCTYLTHIO)ACETONE experimental yes target inhibitor Details Pactimibe investigational yes target inhibitor Details