A single amino acid change makes a rat neuronal sodium channel highly sensitive to pyrethroid insecticides

FEBS Letters

Eldursi, N.²  Devonshire, A.L.¹  Williamson, M.S.¹  Usherwood, P.N.R.²  Vais, H.²  Atkinson, S.¹ 

[1] IACR-Rothamsted, Harpenden, Herts AL5 2JQ, UK;Molecular Toxicology Group, School of Biological Sciences, University of Nottingham, University Park, Nottingham NG7 2RD, UK

关键词: Sodium channel;    Rat brain α-subunit;    Housefly;    ‘Knockdown’ resistance (kdr;    super-kdr);    Pyrethroid;    Deltamethrin;    Drosophila para-subunit;    Xenopus laevis oocyte;   

DOI  :  10.1016/S0014-5793(00)01305-3

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Two amino acid substitutions in a housefly sodium channel, L1014F in domain IIS6 and M918T in the IIS4–S5 linker, have been identified in kdr and super-kdr pyrethroid-resistant phenotypes, respectively. Unlike their native insect counterparts, mammalian sodium channels are only weakly sensitive to pyrethroids. Do the sodium channels of mammal and pyrethroid-resistant housefly share similar structural characteristics that account for their low pyrethroid sensitivities? We report here that substitution of isoleucine for methionine at position 874 (equivalent to the super-kdr site 918 in the housefly) in the rat IIA α-subunit causes a 100-fold increase in sensitivity.

【 授权许可】

Unknown