Future Articles ISSUE 6/98
- Publisher
- Wiley (John Wiley & Sons)
- Year
- 1998
- Tongue
- English
- Weight
- 53 KB
- Volume
- 17
- Category
- Article
- ISSN
- 1868-1743
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โฆ Synopsis
and C, respectively. The E term is the degree of the electrostatic potential: E 0 for ร25e52, E 1 for ร65e5ร2 or 25e56, E 2 for ร105e5ร6 or 65e, E 3 for e5ร10. E was determined from the highest values of the regions in Figure . The coefยฎcient for E ร I A was higher than those for E ร I B and E ร I C , suggesting that afยฎnity of substrate to P-450 was mainly inยฏuenced by the negative electrostatic potential of the region A. To evaluate the effect of electrostatic potential, however, more compounds with hetero atomic substituents which have electrostatic potential in the regions B and C would be required. The three dimensional conformation of rabbit P-450 is not determined. From the results of the present study, however, the pocket of this enzyme is assumed to have one negative electrostatic potential region and two positive electrostatic potential regions. The afยฎnity of substrates to these regions would decrease with the decrease of the electrostatic potential of substituent. When the degree of the potential decreases to the level of alkyl substituent ranging from ร2 kcalymol to 2, substituent is assumed to lose the binding function and play a role of steric hindrance, resulting in the increase of K m with the increase of V w .
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