Crystal structure of FMN-dependent nitroreductase from Escherichia coli B: A prodrug-activating enzyme

Journal of Medicinal Chemistry

Volumn 43, Issue 20, 2000, Pages 3624-3631

  Parkinson, G N ^a   Skelly, J V ^a   Neidle, S ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

5 (1 AZIRIDINYL) 2,4 DINITROBENZAMIDE; FLAVINE MONONUCLEOTIDE; NITROREDUCTASE; PRODRUG; SN 23862; UNCLASSIFIED DRUG;

ARTICLE; BINDING SITE; CANCER CHEMOTHERAPY; CRYSTAL STRUCTURE; CRYSTALLIZATION; DRUG ISOLATION; DRUG STRUCTURE; ENZYME ACTIVATION; ENZYME KINETICS; ENZYME SPECIFICITY; ESCHERICHIA COLI; MOLECULAR INTERACTION; MOLECULAR MODEL; OPTICAL RESOLUTION; STRUCTURE ANALYSIS;

AMINO ACID SEQUENCE; BINDING SITES; CRYSTALLOGRAPHY, X-RAY; ESCHERICHIA COLI; ESCHERICHIA COLI PROTEINS; MODELS, MOLECULAR; MOLECULAR SEQUENCE DATA; NITROREDUCTASES; PRODRUGS; PROTEIN STRUCTURE, TERTIARY;

EID: 0034609776     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm000159m     Document Type: Article

References (26)

1. A sensitive method for the detection of mutagenic nitroarenes: Construction of nitroreductase-overproducing derivatives of Salmonella typhimurium strains TA98 and TA100
2. Cloning, nucleotide sequence, and expression of the nitroreductase gene from enterobacter cloacae
3. The bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB1954) II. A comparison of an Escherichia coli nitroreductase and Walker DT diaphorase
4. The bioactivation of CB 1954 and its use as a prodrug in Antibody-directed Enzyme Prodrug Therapy (ADEPT)
5. Basic local alignment search tool
6. 1.8 Å crystal structure of the major NAD(P)H:FMN oxidoreductase of a bioluminescent bacterium, Vibrio fischeri: Overall structure, cofactor and substrate-analogue binding, and comparison with related flavoproteins
7. Crystal structure of NADH oxidase from thermus thermophilus
8. Flavin reductase P: Structure of a dimeric enzyme that reduces flavin
9. The bioactivation of 5-(aziridin-1-yl)-2,4-dinitrobenzamide (CB1954) I. Purification and properties of a nitroreductase enzyme from Escherichia coli - A potential enzyme for Antibody-directed Enzyme Prodrug Therapy (ADEPT)
10. Oxygen-sensitive and -Insensitive nitroreduction by Escherichia coli and rat hepatic microsomes
11. Mustard prodrugs for activation by Escherichia coli nitroreductase in gene-directed enzyme prodrug therapy
12. The three-dimensional structure of NAD(P)H:quinone reductase, a flavoprotein involved in cancer chemoprotection and chemotherapy: Mechanism of the two-electron reduction
13. Crystal structure of human DT-diaphorase: A model for interaction with the cytotoxic prodrug 5-(Aziridin-1-yl)-2,4-dinitrobenzamide (CB1954)
14. The differences in kinetics of rat and human DT diaphorase result in a differential sensitivity of derived cell lines to CB 1954 (5-(Aziridin-1-yl)-2,4-dinitrobenzamide)
15. Bioactivation of dinitrobenzamide mustards by an E. coli B nitroreductase
16. Gene cloning, purification, and characterization of NfsB, a minor oxygen-insensitive nitroreductase from Escherichia coli, similar in biochemical properties to FRase I, the major flavin reductase in Vibrio fischeri
17. Conversion of NfsB, a minor Escherichia coli nitroreductase, to a Flavin reductase similar in biochemical properties to FRase I, the major Flavin reductase in Vibrio fischeri, by a single amino acid substitution
18. Crystallization and preliminary crystallographic data for an FMN-dependent nitroreductase from Escherichia coli B
19. TURBO-FRODO
20. PROCHECK: A program to check the stereochemical quality of protein structures
21. The protein data bank
22. MOLSCRIPT: A program to produce both detailed and schematic plots of protein structures
23. Protein Folding and Association: Insights from the interfacial and thermodynamic properties of hydrocarbons