Twenty-five years of Research on Cytochromes P450 2B: To ...

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Approaches to EnableCrystallization <strong>of</strong> Human P450 2B6• N-terminal modification and use <strong>of</strong>chaperones• Internal mutations to improve stability(Y226H) and solubility (K262R)• Different CM-resin• Replacement <strong>of</strong> glycerol by sucrose afterchromatography• Inclusion <strong>of</strong> facial amphiphiles during trials
P450 2B6:4-CPI Complex Structure (2 Å)
Page 3 and 4: Goals of Predictiv
Page 5 and 6: Species, Strain, and IndividualDiff
Page 7 and 8: 14 C (cpm)Halpert, J. (1981). Coval
Page 9 and 10: Halpert, J., Jaw, J.-Y., Balfour, C
Page 11: 245-HCB Metabolism(% of</st
Page 15 and 16: % P450 ExtractedScott, E.E., Spatze
Page 17 and 18: • protein engineering:highly conc
Page 19 and 20: Location of Active
Page 21 and 22: Comparison of 2B4
Page 23 and 24: P450 PlasticityDefinition• Involv
Page 25 and 26: Comparison of Five
Page 27 and 28: DX-MS Setup (Exchange)• Remove al
Page 29 and 30: B’-C RegionF-G Cassette2B4dH Exch
Page 31 and 32: CYP2B4:Ticlopidine Complex Ribbon D
Page 33 and 34: Structure of Ticlo
Page 36 and 37: Molecular ReplacementE301T302• Ma
Page 38 and 39: Properties of Huma
Page 42 and 43: Structural Alignment of</st
Page 44 and 45: Summary1. P450 2B4 exhibits remarka
Page 46 and 47: Multiplicity of P4
Page 48 and 49: Halpert, J.R. (1988). Multiplicity
Page 50 and 51: Complications Presented by CYP3A4
Page 52 and 53: Multiple Conformers as an Alternati
Page 54 and 55: • Lack of Substr
Page 56 and 57: Lessons Learned from Colleagues•

Twenty-five years of Research on Cytochromes P450 2B: To ...

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