NEW SELECTIVE AND POTENT INHIBITORS OF HUMAN CYTOCHROM P450 1A FAMILY ENZYMES

  • F. Peter Guengerich (Department of Biochemistry and Center in Molecular Toxicology, Vanderbilt University) ;
  • Chun, Young-Jin (College of Pharmacy, Chungang University) ;
  • Kim, Sanghee (Natural Product Research Institute, Seoul National University) ;
  • Kim, Donghak (Natural Product Research Institute, Seoul National University) ;
  • Lee, Sang-Kwang (Department of Biochemistry and Center in Molecular Toxicology, Vanderbilt University) ;
  • Dong, Mi-Sook (Korea Graduate School of Biotechnology, Korea University) ;
  • Ueng, Yune-Fang (National Research Institute of Chinese Medicine)
  • Published : 2001.10.01

Abstract

The cytochrome P450 (P450) 1 family (1A1, 1A2, 1B1) is involved in the activation of many pro-carcinogens. Previously we characterized a number of synthetic bi- and polycyclic hydrocarbon acetylenes as selective-mechanism-based inhibitors of recombinent P450s 1A1, 1A2, 1B1 (Shimada et al., Chem. Res. Toxicol., 11, 1048-1056, 1998). We reported that the drug oltipraz is a mechanism-based indicator of P450 1A2 (Lagouet et al. Chem. Res. Toxicol., 13, 245-252, 2000).(omitted)

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