Decreased susceptibility of the cytochrome P450 2B6 variant K262R to inhibition by several clinically important drugs.

@article{Talakad2009DecreasedSO,
  title={Decreased susceptibility of the cytochrome P450 2B6 variant K262R to inhibition by several clinically important drugs.},
  author={Jyothi C. Talakad and Santosh Kumar and James R. Halpert},
  journal={Drug metabolism and disposition: the biological fate of chemicals},
  year={2009},
  volume={37 3},
  pages={
          644-50
        }
}
Cytochrome P450 (P450) 2B6 metabolizes a number of clinically relevant drugs and is one of the most highly polymorphic human P450 enzymes, with the Lys(262)-->Arg substitution being especially common in several genetic variants. Therefore, K262R (2B6*4) was created in the CYP2B6dH background (N-terminal-modified and C-terminal His-tagged) and expressed in Escherichia coli. The recombinant CYP2B6dH and K262R were purified and studied to investigate the effect of the Lys(262)-->Arg substitution… CONTINUE READING

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