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Potency of stampidine against multi-nucleoside reverse transcriptase inhibitor resistant human immunodeficiency viruses. 2006

Fatih M Uckun, and Taracad K Venkatachalam, and Sanjive Qazi
Parker Hughes Institute, Roseville, Minnesota, USA. fatih_uckun@ih.org

The in vitro potency of stampidine (STAMP, DDE-113, HI-113, N-[p-(4-bromophenyl)-2',3'-didehydro-3'-deoxy-5'-thymidylyl]-L-alanine methyl ester, CAS 217178-62-6) was examined against 8 clinical non-B subtype HIV-1 isolates with resistance to stavudine (STV, d4T), adefovir and tenofovir, 19 clinical zidovudine-resistant HIV-1 isolates, and 6 recombinant HIV-1 clones with multi-resistance against nucleoside reverse transcriptase inhibitors. Stampidine exhibited potent anti-HIV activity against each one of these 33 HIV-1 isolates with subnanomolar to nanomolar IC50 values.

UI MeSH Term Description Entries
D008958 Models, Molecular Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures. Molecular Models,Model, Molecular,Molecular Model
D009000 Monocytes Large, phagocytic mononuclear leukocytes produced in the vertebrate BONE MARROW and released into the BLOOD; contain a large, oval or somewhat indented nucleus surrounded by voluminous cytoplasm and numerous organelles. Monocyte
D004797 Enzyme-Linked Immunosorbent Assay An immunoassay utilizing an antibody labeled with an enzyme marker such as horseradish peroxidase. While either the enzyme or the antibody is bound to an immunosorbent substrate, they both retain their biologic activity; the change in enzyme activity as a result of the enzyme-antibody-antigen reaction is proportional to the concentration of the antigen and can be measured spectrophotometrically or with the naked eye. Many variations of the method have been developed. ELISA,Assay, Enzyme-Linked Immunosorbent,Assays, Enzyme-Linked Immunosorbent,Enzyme Linked Immunosorbent Assay,Enzyme-Linked Immunosorbent Assays,Immunosorbent Assay, Enzyme-Linked,Immunosorbent Assays, Enzyme-Linked
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D013938 Thymidine Monophosphate 5-Thymidylic acid. A thymine nucleotide containing one phosphate group esterified to the deoxyribose moiety. DTMP,TMP,Thymidylic Acid,Deoxythymidylate,Thymidylic Acids,Acid, Thymidylic,Acids, Thymidylic,Monophosphate, Thymidine
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
D016655 HIV Core Protein p24 A major core protein of the human immunodeficiency virus encoded by the HIV gag gene. HIV-seropositive individuals mount a significant immune response to p24 and thus detection of antibodies to p24 is one basis for determining HIV infection by ELISA and Western blot assays. The protein is also being investigated as a potential HIV immunogen in vaccines. HIV Major Core Protein p24,HIV gag Gene Product p24,HIV p24 Antigen,gag Protein p24, HIV,p24(HIV),HIV Protein p24,HTLV-III p24,p24 protein, Human Immunodeficiency Virus,HTLV III p24,p24 Antigen, HIV,p24, HIV Protein,p24, HTLV-III
D054306 Dideoxynucleotides The phosphate esters of DIDEOXYNUCLEOSIDES. Dideoxynucleotide Triphosphates,ddNTPs,Triphosphates, Dideoxynucleotide
D018119 Stavudine A dideoxynucleoside analog that inhibits reverse transcriptase and has in vitro activity against HIV. 2',3'-Didehydro-3'-deoxythymidine,D4T,2',3'-Didehydro-2',3'-dideoxythmidine,BMY-27857,Stavudine, Monosodium Salt,Zerit,2',3' Didehydro 3' deoxythymidine,BMY 27857,BMY27857
D018894 Reverse Transcriptase Inhibitors Inhibitors of reverse transcriptase (RNA-DIRECTED DNA POLYMERASE), an enzyme that synthesizes DNA on an RNA template. Reverse Transcriptase Inhibitor,Inhibitors, Reverse Transcriptase,Inhibitor, Reverse Transcriptase,Transcriptase Inhibitor, Reverse

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