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Description: A dideoxynucleoside compound in which the 3'-hydroxy group on the sugar moiety has been replaced by a hydrogen.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. [PubChem]
Drug Type: Small Molecule; Approved
Pharmacology: Zalcitabine inhibits the activity of HIV-1 reverse transcriptase (RT) both by competing with the natural substrate dGTP and by its incorporation into viral DNA.
Mechanism of Action: Zalcitabine is a nucleoside reverse transcriptase inhibitor (NRTI) with activity against Human Immunodeficiency Virus Type 1 (HIV-1). Zalcitabine is phosphorylated to active metabolites that compete for incorporation into viral DNA. They inhibit the HIV reverse transcriptase enzyme competitively and act as a chain terminator of DNA synthesis. The lack of a 3'-OH group in the incorporated nucleoside analogue prevents the formation of the 5' to 3' phosphodiester linkage essential for DNA chain elongation, and therefore, the viral DNA growth is terminated.
Indication: For the treatment of Human immunovirus (HIV) infections.
Half Life: 2 hours
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Data Correlations | 3 studies

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Genes category icon Genes
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SLC22A8 100 100
NR0B2 99 99
CA3 99 99
RGD1561637_predicted 90 90
27306 90 90
57469 89 89
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Biogroups category icon Biogroups
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IQ calmodulin-binding region 100 100
Myosin head, motor region 100 100
Axon Guidance 99 99
Immunoglobulin I-set 99 99
Immunoglobulin subtype 2 98 98
Zinc finger, CCCH-type 98 98
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Individual Studies

  • Liver Pharmacology and Xenobiotic Response Repertoire

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    A definition of RNA expression changes that correlate with liver response programs and an understanding of the similarities and differences in responses to different classes of chemicals would aid in new chemical or drug characterization and add to our understanding of liver biology.

    Authors: Natsoulis G, Pearson CI, Gollub J et al.

    Organization: Iconix Biosciences 325 E. Middlefield Rd…
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Associated Researchers

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Thought leaders and organizations working on research involving Zalcitabine.

View All Author iconAuthors
  • Ulrich A Walker
  • Dirk Lebrecht
  • Bernhard Setzer
  • Georg M N Behrens
  • Metodi V Stankov
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • National Institute of Allergy and Infectious Diseases (NIAID)
  • Hoffmann-La Roche
  • Glaxo Wellcome
  • Bristol-Myers Squibb
  • Parexel
View All Affiliations icon Organizations
  • Medizinische Universitätsklinik
  • Hannover Medical School
  • Chosun University
  • Chelsea and Westminster Hospital
  • Katholieke Universiteit Leuven

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