CES2

CES2

A gene on chromosome 16q22.1 that encodes a carboxylesterase which plays a role in detoxifying xenobiotics (e.g., cocaine and heroin) and in activating ester and amide prodrugs. It is primarily expressed in the intestine, and less so in the liver. CES2 is also a less preferred gene symbol for what is now designated as CES1, see there.
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Irinotecan is a prodrug, and its conversion to the active compound 7-ethyl-10-hydroxycamptothesin (SN-38) requires its hydrolysis by the carboxylesterase CES2. This enzyme exhibits a 60-fold higher hydrolytic efficiency against irinotecan than CES1, another human carboxylesterase isozyme [1], and the ability of colorectal tumors to hydrolyze irinotecan correlates with their expression of CES2, but not CES1 [2].
Indeed, the colon may also serve as a major site for irinotecan activation since CES2 is highly expressed in this tissue, while the expression of the other carboxylesterase isozymes is relatively low [2].
Recent studies suggest that CES2 expression is regulated by p53 in colorectal cancer cell lines [6, 7].
With these possibilities in mind, we investigated the relationship between TP53 gene status and CES2 expression in colorectal cancer.
The sequences of the primers used were as follows: CES2 forward 5'-GTAGCACATTTTCAGTGTTCC-3' and reverse 5'-GTAGTTGCCCCCAAAGAA-3', p21 forward 5'-GATT TCTACCACTCCAAACGCC-3' and reverse 5'-AGAAGA TGTAGAGCGGGC-3', Noxa forward 5'-GCTGGAAGTC GAGTGTGCTA-3' and reverse 5'-CCTGAGCAGAAGAG TTTGGA-3', GAPDH forward 5'-TGCCCTCAACGACC ACTTTG-3' and reverse 5'-CTCTTCCTCTTGTGCTCTT GCTG-3', and 18S rRNA forward 5'-GTAACCCGTTG AACCCCATT-3' and reverse 5'-CCATCCAATCGGTA GTAGCG-3'.
Recognized dystocia scores were CES1 = no problem, CES2 = slight problem, CES3 = needed assistance, CES4 = considerable force, CES5 = extreme difficulty.
Por outro lado, na segunda avaliacao (destrutiva), foram tambem avaliados: comprimento (cm) de estolao secundario (CES2) e terciario (CES3), numero de ramificacoes por estolao (rami/est), numero de inflorescencias (NI) por contagem; producao de massa seca de folha (MSF), de estolao (MSE) e de raiz (MSR), atraves do corte das plantas com auxilio de tesouras, e secagem em estufa a 60[degrees]C ate massa constante; taxa fotossintetica liquida (A), condutancia estomatica (g), transpiracao (Tr), atraves de um medidor de fotossintese modelo LICOR 6400, e eficiencia do uso da agua (EUA), atraves da razao entre fotossintese e transpiracao.
O numero de ramificacoes por estolao esta correlacionado com os CES1, CES2 e CES3, com o NFV (r=0,65) e negativamente correlacionado com a AF (r=-0,45), indicando que quanto maior o CES, maior o NFV e menor a AF dessa planta.
Primary Insecticide class Mode of Vulnerable neurological action genetic target subpopulations AChE OP Inhibition PON1 polymorphisms CB Inhibition Voltage-gated OC Modified SCN1A, SCN1B sodium gating channel kinetics pyrethrin/pyrethriod Modified HCE1 (CES1) gating kinetics GABA-gated Cyclodienes (a form Antagonism HCE2 (CES2) GABA chloride of OC) receptor channel polymorphisms Phenylpyrazole Antagonism nAChR(a) Neonicotinoid Agonism Haploinsufficiency of [alpha]7 nAChR Adapted from Scharf (2003).
Assay characteristics Assay S/B (a) S/N (a) Enzyme sEH 4.0 [+ or -] 0.1 38 [+ or -] 8 CES1 11 [+ or -] 3 19 [+ or -] 2 CES2 9.2 [+ or -] 0.9 106 [+ or -] 33 CES3 6.1 [+ or -] 0.7 28 [+ or -] 7 FAAH 150 [+ or -] 10 35 [+ or -] 5 P0N2 18 [+ or -] 2 134 [+ or -] 31 GSTs 2.4 [+ or -] 0.5 28 [+ or -] 9 CYP450 1A2 and 2C6 13 [+ or -] 5 48 [+ or -] 10 CYP450 2C9 19 [+ or -] 4 79 [+ or -] 18 Receptor AhR 32 [+ or -] 1 410 [+ or -] 30 ER 18 [+ or -] 2 180 [+ or -] 70 ER 5 [+ or -] 1 80 [+ or -] 40 RyR1 170 [+ or -] 30 500 [+ or -] 90 RyR2 100 [+ or -] 10 310 [+ or -] 40 Assay No.
Interestingly, we found that, in addition to CES1 and CES2, TPP can also significantly reduce PON2 activity.
For example, the inhibition of CES1 and CES2 by triclosan was totally unexpected, as was the inhibition of the RyRs by chloranil and dichlone.