Display Settings:

Items per page
We are sorry, but NCBI web applications do not support your browser and may not function properly. More information

Results: 6

1.
Fig. 1.

Fig. 1. From: Crystal Structure of a Cytochrome P450 2B6 Genetic Variant in Complex with the Inhibitor 4-(4-Chlorophenyl)imidazole at 2.0-? Resolution.

Divergent stereo view of the 2B6-4-CPI complex. The sequence is colored from the N terminus (blue) to the C terminus (red). The heme and partial Cymal-5 detergents are shown as red sticks. The 4-CPI inhibitor is shown as cyan sticks.

Sean C. Gay, et al. Mol Pharmacol. 2010 April;77(4):529-538.
2.
Fig. 4.

Fig. 4. From: Crystal Structure of a Cytochrome P450 2B6 Genetic Variant in Complex with the Inhibitor 4-(4-Chlorophenyl)imidazole at 2.0-? Resolution.

Ribbon-and-stick depiction of a typical pose for ticlopidine docking into the active site of a model of P450 2B6 based on the crystal structure of the 4-CPI complex. This and other similar poses are consistent with data that show ticlopidine to be oxidized on the thiophene ring and cause mechanism-based inactivation of P450 2B6.

Sean C. Gay, et al. Mol Pharmacol. 2010 April;77(4):529-538.
3.
Fig. 5.

Fig. 5. From: Crystal Structure of a Cytochrome P450 2B6 Genetic Variant in Complex with the Inhibitor 4-(4-Chlorophenyl)imidazole at 2.0-? Resolution.

Ribbon diagram showing the location of known SNPs (yellow sticks) in 2B6. Residues 99 and 476 (both glycine) are not shown as sticks, but locations are identified. The heme is shown as red sticks; 4-CPI, cyan sticks. The majority of the known 2B6 coding sequence variants contain substitutions that occur relatively far from the active site, and none of them actually lies within the active site.

Sean C. Gay, et al. Mol Pharmacol. 2010 April;77(4):529-538.
4.
Fig. 2.

Fig. 2. From: Crystal Structure of a Cytochrome P450 2B6 Genetic Variant in Complex with the Inhibitor 4-(4-Chlorophenyl)imidazole at 2.0-? Resolution.

Protein sequence alignment of 2B4dH and 2B6dH(Y226H, K262R). The alignment also includes the N terminus of wild-type 2B6 to indicate changes made to the construct for expression and purification. Secondary structure of the 4-CPI complexes is indicated by boxes (α-helices) and underlined regions (β-strands). Mutations are marked in bold type. Diamonds indicate residues interacting with 4-CPI. The locations of known 2B6 SNPs are denoted by squares.

Sean C. Gay, et al. Mol Pharmacol. 2010 April;77(4):529-538.
5.
Fig. 3.

Fig. 3. From: Crystal Structure of a Cytochrome P450 2B6 Genetic Variant in Complex with the Inhibitor 4-(4-Chlorophenyl)imidazole at 2.0-? Resolution.

Divergent stereo view of an overlay of both 2B4 (purple) and 2B6 (green) 4-CPI complexes. The 2B6 heme and 4-CPI are shown in red, whereas the corresponding molecules in 2B4 are shown in blue. a, the overall structure of the human and rabbit enzymes, with an RMSD of 0.65 Å, are almost indistinguishable from one another. b, the active sites of 2B4 and 2B6 are shown. Residues found within a 5-Å radius of 4-CPI are depicted as sticks. An FoFc simulated annealing omit map contoured at 3-σ clearly shows the 2B6 4-CPI and heme.

Sean C. Gay, et al. Mol Pharmacol. 2010 April;77(4):529-538.
6.
Fig. 6.

Fig. 6. From: Crystal Structure of a Cytochrome P450 2B6 Genetic Variant in Complex with the Inhibitor 4-(4-Chlorophenyl)imidazole at 2.0-? Resolution.

Ribbon-and-stick diagram depicting the G and H helices region in the 2B4 bifonazole (orange; 2bdm), 1-(4-phenyl)benzylimidazole (1-PBI) (blue; 3g5n), and 4-CPI (green; 1suo) structures. Aligning the G and H helices in the absence of the remaining protein shows that this region maintains a consistent local structure despite larger movements in the overall protein (inset). The hydrogen-bonding network among His 252, Thr 255, Arg 262, Asp 263, and Asp 266 seems to link the G and H helices together throughout these shifts in secondary structure placement. These same interactions are also seen in the present 2B6 structure.

Sean C. Gay, et al. Mol Pharmacol. 2010 April;77(4):529-538.

Display Settings:

Items per page

Supplemental Content

Recent activity

Your browsing activity is empty.

Activity recording is turned off.

Turn recording back on

See more...
Write to the Help Desk