| Tchem | Cocaine esterase |
This gene encodes a member of the carboxylesterase large family. The family members are responsible for the hydrolysis or transesterification of various xenobiotics, such as cocaine and heroin, and endogenous substrates with ester, thioester, or amide bonds. They may participate in fatty acyl and cholesterol ester metabolism, and may play a role in the blood-brain barrier system. The protein encoded by this gene is the major intestinal enzyme and functions in intestine drug clearance. Alternatively spliced transcript variants have been found for this gene.[provided by RefSeq, Oct 2010]
Comments
Property Summary
| NCBI Gene PubMed Count | 56 |
| Grant Count | 69 |
| R01 Count | 35 |
| Funding | $12,463,205.25 |
| PubMed Score | 251.92 |
| PubTator Score | 318.29 |
| Disease | log2 FC | p |
|---|---|---|
| osteosarcoma | -1.580 | 0.008 |
| Becker muscular dystrophy | 1.065 | 0.000 |
| acute quadriplegic myopathy | 1.461 | 0.000 |
| pancreatic ductal adenocarcinoma liver m... | -1.235 | 0.040 |
| intraductal papillary-mucinous neoplasm ... | 2.300 | 0.002 |
| colon cancer | -1.700 | 0.008 |
| active Crohn's disease | -1.330 | 0.020 |
| ulcerative colitis | -2.000 | 0.000 |
| ovarian cancer | 1.300 | 0.000 |
CHEMBL117447
pKi 6.02
CHEMBL364729
pKi 6.06
CHEMBL242288
pKi 6.08
CHEMBL2151605
pIC50 6.18
CHEMBL396977
pKi 6.19
CHEMBL190672
pKi 6.24
CHEMBL242506
pKi 6.26
CHEMBL1812861
pKi 6.31
CHEMBL394807
pKi 6.40
CHEMBL191796
pKi 6.40
CHEMBL244425
pKi 6.41
CHEMBL195713
pKi 6.42
CHEMBL193180
pKi 6.44
CHEMBL365392
pKi 6.45
CHEMBL1812851
pKi 6.48
CHEMBL155396
pIC50 6.51
CHEMBL187460
pKi 6.54
CHEMBL1812852
pKi 6.57
CHEMBL1812857
pKi 6.57
CHEMBL242287
pKi 6.57
| PMID | Text |
|---|---|
| 26025324 | Findings suggest that CES2 expression and activity, by mediating the intratumoral activation of irinotecan, is a contributor to FOLFIRINOX sensitivity in pancreatic cancer. |
| 25724353 | In the liver and duodenum, CES2 mRNA expression increased and exhibited a postnatal surge. |
| 24212379 | After oral administration of dabigatran etexilate to humans, DABE is hydrolyzed by intestinal CES2 to the intermediate M2 metabolite followed by hydrolysis of M2 to DAB in the liver by CES1. |
| 24195516 | expression of CES2, UGTA1A1, and GUSB varies in colorectal pathology tissues and that the expression of CES2 is somewhat related to tumor staging. |
| 23480903 | CES2 RNA expression was observed in neuroblastoma cells, and its expression in neuroblastoma cell lines was positively correlated with sensitivity to CPT-11 and apoptosis after CPT-11 exposure in vitro |
| 23471941 | Variations in CES2 in the promoter region, may alter rifampicin metabolism by affecting expression of the gene |
| 22525521 | tested the hypothesis that an individual's CES phenotype can be characterized by reporter substrates/probes that interrogate native CES1 and CES2 activities in liver and immunoblotting methods |
| 20649590 | Report CES2 mediated hydrolysis of heroin, cocaine and CPT-11. |
| 20628086 | Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator) |
| 20529763 | Observational study of gene-disease association. (HuGE Navigator) |
| More... |
MRLHRLRARLSAVACGLLLLLVRGQGQDSASPIRTTHTGQVLGSLVHVKGANAGVQTFLGIPFAKPPLGP 1 - 70 LRFAPPEPPESWSGVRDGTTHPAMCLQDLTAVESEFLSQFNMTFPSDSMSEDCLYLSIYTPAHSHEGSNL 71 - 140 PVMVWIHGGALVFGMASLYDGSMLAALENVVVVIIQYRLGVLGFFSTGDKHATGNWGYLDQVAALRWVQQ 141 - 210 NIAHFGGNPDRVTIFGESAGGTSVSSLVVSPISQGLFHGAIMESGVALLPGLIASSADVISTVVANLSAC 211 - 280 DQVDSEALVGCLRGKSKEEILAINKPFKMIPGVVDGVFLPRHPQELLASADFQPVPSIVGVNNNEFGWLI 281 - 350 PKVMRIYDTQKEMDREASQAALQKMLTLLMLPPTFGDLLREEYIGDNGDPQTLQAQFQEMMADSMFVIPA 351 - 420 LQVAHFQCSRAPVYFYEFQHQPSWLKNIRPPHMKADHGDELPFVFRSFFGGNYIKFTEEEEQLSRKMMKY 421 - 490 WANFARNGNPNGEGLPHWPLFDQEEQYLQLNLQPAVGRALKAHRLQFWKKALPQKIQELEEPEERHTEL 491 - 559 //
| PMID | Year | Title |
|---|---|---|
| 26025324 | 2015 | Carboxylesterase 2 as a Determinant of Response to Irinotecan and Neoadjuvant FOLFIRINOX Therapy in Pancreatic Ductal Adenocarcinoma. |
| 25724353 | 2015 | Ontogenic expression of human carboxylesterase-2 and cytochrome P450 3A4 in liver and duodenum: postnatal surge and organ-dependent regulation. |
| 24275569 | 2014 | An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome. |
| 24212379 | 2014 | Identification of carboxylesterase-dependent dabigatran etexilate hydrolysis. |
| 24195516 | 2014 | Relationship between the expression of CES2, UGT1A1, and GUSB in colorectal cancer tissues and aberrant methylation. |
| 23480903 | 2013 | Clinical implications of CES2 RNA expression in neuroblastoma. |
| 23471941 | 2013 | Relationship between CES2 genetic variations and rifampicin metabolism. |
| 22525521 | 2012 | Examination of the carboxylesterase phenotype in human liver. |
| 21269460 | 2011 | Initial characterization of the human central proteome. |
| 20931200 | 2010 | Recommended nomenclature for five mammalian carboxylesterase gene families: human, mouse, and rat genes and proteins. |
| More... |
