BIOMAT Database Logo BIOMAT Database Logo

In vitro selection and analysis of human immunodeficiency virus type 1 resistant to derivatives of beta-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine. 2005

Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Department of Medicine, Division of Infectious Diseases, University of Pittsburgh School of Medicine, 3550 Terrace Street, Pittsburgh, PA 15261, USA.

Serial passage of human immunodeficiency virus type 1 in MT-2 cells in increasing concentrations of the d- and l-enantiomers of beta-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine (d4FC) resulted in the selection of viral variants with reverse transcriptase substitutions M184I or M184V for l-d4FC and I63L, K65R, K70N, K70E, or R172K for d-d4FC. Phenotypic analysis of site-directed mutants defined the role of these mutations in reducing susceptibility to l- or d-d4FC.

UI MeSH Term Description Entries
D009154 Mutation Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations. Mutations
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D003570 Cytidine Triphosphate Cytidine 5'-(tetrahydrogen triphosphate). A cytosine nucleotide containing three phosphate groups esterified to the sugar moiety. CTP,CRPPP,Magnesium CTP,Mg CTP,Triphosphate, Cytidine
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013237 Stereoisomerism The phenomenon whereby compounds whose molecules have the same number and kind of atoms and the same atomic arrangement, but differ in their spatial relationships. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed) Molecular Stereochemistry,Stereoisomers,Stereochemistry, Molecular,Stereoisomer
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D015497 HIV-1 The type species of LENTIVIRUS and the etiologic agent of AIDS. It is characterized by its cytopathic effect and affinity for the T4-lymphocyte. Human immunodeficiency virus 1,HIV-I,Human Immunodeficiency Virus Type 1,Immunodeficiency Virus Type 1, Human
D016047 Zalcitabine A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen. This modification prevents the formation of phosphodiester linkages which are needed for the completion of nucleic acid chains. The compound is a potent inhibitor of HIV replication at low concentrations, acting as a chain-terminator of viral DNA by binding to reverse transcriptase. Its principal toxic side effect is axonal degeneration resulting in peripheral neuropathy. 2',3'-Dideoxycytidine,Dideoxycytidine,ddC (Antiviral),HIVID Roche,Hivid,NSC-606170,2',3' Dideoxycytidine,NSC 606170,NSC606170
D016297 Mutagenesis, Site-Directed Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion. Mutagenesis, Oligonucleotide-Directed,Mutagenesis, Site-Specific,Oligonucleotide-Directed Mutagenesis,Site-Directed Mutagenesis,Site-Specific Mutagenesis,Mutageneses, Oligonucleotide-Directed,Mutageneses, Site-Directed,Mutageneses, Site-Specific,Mutagenesis, Oligonucleotide Directed,Mutagenesis, Site Directed,Mutagenesis, Site Specific,Oligonucleotide Directed Mutagenesis,Oligonucleotide-Directed Mutageneses,Site Directed Mutagenesis,Site Specific Mutagenesis,Site-Directed Mutageneses,Site-Specific Mutageneses
D054303 HIV Reverse Transcriptase A reverse transcriptase encoded by the POL GENE of HIV. It is a heterodimer of 66 kDa and 51 kDa subunits that are derived from a common precursor protein. The heterodimer also includes an RNAse H activity (RIBONUCLEASE H, HUMAN IMMUNODEFICIENCY VIRUS) that plays an essential role the viral replication process. Reverse Transcriptase, HIV,Reverse Transcriptase, Human Immunodeficiency Virus,Transcriptase, HIV Reverse

Related Publications

Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Anti-hepatitis B virus activity and metabolism of 2',3'-dideoxy-2',3'-didehydro-beta-L(-)-5-fluorocytidine.
July 1998, Antimicrobial agents and chemotherapy,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Antiviral activity of 2',3'-dideoxy-beta-L-5-fluorocytidine (beta-L-FddC) and 2',3'-dideoxy-beta-L-cytidine (beta-L-ddC) against hepatitis B virus and human immunodeficiency virus type 1 in vitro.
January 1994, Biochemical pharmacology,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Metabolism of 2',3'-dideoxy-2',3'-didehydro-beta-L(-)-5-fluorocytidine and its activity in combination with clinically approved anti-human immunodeficiency virus beta-D(+) nucleoside analogs in vitro.
July 1998, Antimicrobial agents and chemotherapy,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Design and synthesis of 2',3'-dideoxy-2',3'-didehydro-beta-L-cytidine (beta-L-d4C) and 2',3'-dideoxy 2',3'-didehydro-beta-L-5-fluorocytidine (beta-L-Fd4C), two exceptionally potent inhibitors of human hepatitis B virus (HBV) and potent inhibitors of human immunodeficiency virus (HIV) in vitro.
April 1996, Journal of medicinal chemistry,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Pharmacokinetics of the antiviral agent beta-D-2',3'-didehydro-2',3'-dideoxy-5-fluorocytidine in rhesus monkeys.
February 1999, Antimicrobial agents and chemotherapy,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Antiviral activity of beta-L-2',3'-dideoxy-2',3'-didehydro-5-fluorocytidine in woodchucks chronically infected with woodchuck hepatitis virus.
April 2001, Antimicrobial agents and chemotherapy,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
HIV-1 resistance profile of the novel nucleoside reverse transcriptase inhibitor beta-D-2',3'-dideoxy-2',3'-didehydro-5-fluorocytidine (Reverset).
January 2003, Antiviral chemistry & chemotherapy,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Selection and characterization of human immunodeficiency virus type 1 variants resistant to the (+) and (-) enantiomers of 2'-deoxy-3'-oxa-4'-thio-5-fluorocytidine.
May 2000, Antimicrobial agents and chemotherapy,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Characterization of the antiviral effect of 2',3'-dideoxy-2', 3'-didehydro-beta-L-5-fluorocytidine in the duck hepatitis B virus infection model.
January 2000, Antimicrobial agents and chemotherapy,
Jennifer L Hammond, and Urvi M Parikh, and Dianna L Koontz, and Susan Schlueter-Wirtz, and Chung K Chu, and Hengameh Z Bazmi, and Raymond F Schinazi, and John W Mellors
Interaction of beta-L-2',3'-dideoxy-2',3'-didehydro-5-fluoro-CTP with human immunodeficiency virus-1 reverse transcriptase and human DNA polymerases: implications for human immunodeficiency virus drug design.
May 1998, Molecular pharmacology,
Copied contents to your clipboard!