Title : Assessment of the inhibitory effects of pyrethroids against human carboxylesterases.

Pub. Date : 2017 Apr 15

PMID : 28242322






8 Functional Relationships(s)
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1 The results demonstrated that most of the tested pyrethroids showed moderate to weak inhibitory effects against both CES1 and CES2, but deltamethrin displayed strong inhibition towards CES1. decamethrin carboxylesterase 1 Homo sapiens
2 The IC50 values of deltamethrin against CES1-mediated BMBT, DME, and DMCB hydrolysis were determined as 1.58muM, 2.39muM, and 3.3muM, respectively. decamethrin carboxylesterase 1 Homo sapiens
3 Moreover, deltamethrin was cell membrane permeable and capable of inhibition endogenous CES1 in living cells. decamethrin carboxylesterase 1 Homo sapiens
4 Further investigation revealed that deltamethrin inhibited CES1-mediated BMBT hydrolysis via competitive manner but noncompetitively inhibited DME or DMCB hydrolysis. decamethrin carboxylesterase 1 Homo sapiens
5 The inhibition behaviors of deltamethrin against CES1 were also studied by molecular docking simulation. decamethrin carboxylesterase 1 Homo sapiens
6 The results demonstrated that CES1 had at least two different ligand-binding sites, one was the DME site and another was the BMBT site which was identical to the binding site of deltamethrin. decamethrin carboxylesterase 1 Homo sapiens
7 In summary, deltamethrin was a strong reversible inhibitor against CES1 and it could tightly bind on CES1 at the same ligand-binding site as BMBT. decamethrin carboxylesterase 1 Homo sapiens
8 In summary, deltamethrin was a strong reversible inhibitor against CES1 and it could tightly bind on CES1 at the same ligand-binding site as BMBT. decamethrin carboxylesterase 1 Homo sapiens