(Q44237349)

English

Substrate selectivity of human cytochrome P450 2C9: importance of residues 476, 365, and 114 in recognition of diclofenac and sulfaphenazole and in mechanism-based inactivation by tienilic acid

scientific article published in January 2003

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scholarly article

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Europe PubMed Central

1 December 2017

Substrate selectivity of human cytochrome P450 2C9: importance of residues 476, 365, and 114 in recognition of diclofenac and sulfaphenazole and in mechanism-based inactivation by tienilic acid (English)

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Europe PubMed Central

1 December 2017

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Nadine Assrir

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Europe PubMed Central

1 December 2017

author name string

Armelle Melet

1

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Europe PubMed Central

1 December 2017

Pascale Jean

3

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Europe PubMed Central

1 December 2017

Maria Pilar Lopez-Garcia

4

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Europe PubMed Central

1 December 2017

Cristina Marques-Soares

5

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Europe PubMed Central

1 December 2017

Maryse Jaouen

6

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Europe PubMed Central

1 December 2017

Patrick M Dansette

7

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Europe PubMed Central

1 December 2017

Marie Agnès Sari

8

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Europe PubMed Central

1 December 2017

Daniel Mansuy

9

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Europe PubMed Central

1 December 2017

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publication date

1 January 2003

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1 December 2017

Archives of Biochemistry and Biophysics

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1 December 2017

409

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1 December 2017

80-91

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1 December 2017

1

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1 December 2017

Characterization of cDNAs, mRNAs, and proteins related to human liver microsomal cytochrome P-450 (S)-mephenytoin 4'-hydroxylase

1 reference

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Cloning and expression of complementary DNAs for multiple members of the human cytochrome P450IIC subfamily

1 reference

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Cytochrome P4502C9: an enzyme of major importance in human drug metabolism

1 reference

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Diclofenac and Its Derivatives As Tools for Studying Human Cytochromes P450 Active Sites: Particular Efficiency and Regioselectivity of P450 2Cs

1 reference

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7 January 2021

Speculations on the substrate structure-activity relationship (SSAR) of cytochrome P450 enzymes

1 reference

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The Substrate Binding Site of Human Liver Cytochrome P450 2C9: An Approach Using Designed Tienilic Acid Derivatives and Molecular Modeling

1 reference

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The Substrate Binding Site of Human Liver Cytochrome P450 2C9: An NMR Study†

1 reference

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Structural forms of phenprocoumon and warfarin that are metabolized at the active site of CYP2C9.

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Development of a combined protein and pharmacophore model for cytochrome P450 2C9.

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Molecular modelling of human CYP2C subfamily enzymes CYP2C9 and CYP2C19: rationalization of substrate specificity and site-directed mutagenesis experiments in the CYP2C subfamily

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Homology modeling and substrate binding study of human CYP2C9 enzyme

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A refined 3-dimensional QSAR of cytochrome P450 2C9: computational predictions of drug interactions

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Competitive CYP2C9 inhibitors: enzyme inhibition studies, protein homology modeling, and three-dimensional quantitative structure-activity relationship analysis

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Analysis of selective regions in the active sites of human cytochromes P450, 2C8, 2C9, 2C18, and 2C19 homology models using GRID/CPCA.

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Identification of human CYP2C19 residues that confer S-mephenytoin 4'-hydroxylation activity to CYP2C9.

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Identification of residues 99, 220, and 221 of human cytochrome P450 2C19 as key determinants of omeprazole activity

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Identification of residues 286 and 289 as critical for conferring substrate specificity of human CYP2C9 for diclofenac and ibuprofen

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7 January 2021

Identification of amino acid substitutions that confer a high affinity for sulfaphenazole binding and a high catalytic efficiency for warfarin metabolism to P450 2C19.

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Evidence that CYP2C19 is the major (S)-mephenytoin 4'-hydroxylase in humans

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Mammalian microsomal cytochrome P450 monooxygenase: structural adaptations for membrane binding and functional diversity

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7 January 2021

Enzymatic determinants of the substrate specificity of CYP2C9: role of B'-C loop residues in providing the pi-stacking anchor site for warfarin binding

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Arginines 97 and 108 in CYP2C9 are important determinants of the catalytic function

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7 January 2021

Thiophene derivatives as new mechanism-based inhibitors of cytochromes P-450: inactivation of yeast-expressed human liver cytochrome P-450 2C9 by tienilic acid

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7 January 2021

Tolbutamide hydroxylation by human liver microsomes. Kinetic characterisation and relationship to other cytochrome P-450 dependent xenobiotic oxidations

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Validation of the tolbutamide metabolic ratio for population screening with use of sulfaphenazole to produce model phenotypic poor metabolizers

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7 January 2021

Ketoconazole and sulphaphenazole as the respective selective inhibitors of P4503A and 2C9

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7 January 2021

Interaction of sulfaphenazole derivatives with human liver cytochromes P450 2C: molecular origin of the specific inhibitory effects of sulfaphenazole on CYP 2C9 and consequences for the substrate binding site topology of CYP 2C9

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7 January 2021

Interaction of new sulfaphenazole derivatives with human liver cytochrome p450 2Cs: structural determinants required for selective recognition by CYP 2C9 and for inhibition of human CYP 2Cs.

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Synthesis of sulfaphenazole derivatives and their use as inhibitors and tools for comparing the active sites of human liver cytochromes P450 of the 2C subfamily.

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Rearrangement of N-(alkylamino)azoles in acid media: a new entry to C-amino-N-substituted azoles

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Elevated recombination rates in transcriptionally active DNA

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Enhanced in vivo monooxygenase activities of mammalian P450s in engineered yeast cells producing high levels of NADPH-P450 reductase and human cytochrome b5.

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Xenobiotic metabolism in humanized yeast: engineered yeast cells producing human NADPH-cytochrome P-450 reductase, cytochrome b5, epoxide hydrolase and P-450s.

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Maximizing the expression of mammalian cytochrome P-450 monooxygenase activities in yeast cells

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Plasmid construction by homologous recombination in yeast.

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Protein engineering by cDNA recombination in yeasts: shuffling of mammalian cytochrome P-450 functions

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Cleavage of Structural Proteins during the Assembly of the Head of Bacteriophage T4

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10.1016/S0003-9861(02)00548-9

1 reference

Europe PubMed Central

1 December 2017

1 reference

Europe PubMed Central

1 December 2017

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