Important note: Information in this article was accurate in 1994. The state of the art may have changed since the publication date.
Molecular targets for HIV therapy.
Annu Conf Australas Soc HIV Med. 1993 Oct 28-30;5:25 (abstract no. SPI-3). Unique Identifier : AIDSLINE ASHM5/94348944 Rosenberg M; SmithKline Beecham Pharmaceutical, King of Prussia, Pennsylvania; 19406-0939.
Abstract:
There continues to be an urgent need for the discovery and design of better drugs with antiviral activities against the HIV viruses. The various stages of the HIV life cycle provide specific molecular targets for which novel assays and mechanistic approaches can be developed to search for and identify new inhibitory agents. For example, viral replication, integration, gene expression, and maturation are dependent on the presence and function of specific virally encoded gene products such as the reverse transcriptase, required for RNA-dependent DNA synthesis prior to integration of the pro-viral DNA into the host genome; integrase, the enzyme responsible for the integration event; the TAT and REV regulatory proteins involved in transactivating viral gene expression within the host; and protease, the enzyme responsible for proteolytic maturation of the viral precursor polyproteins. In addition, viral recognition and entry into human cells also provides certain molecular targets for potential intervention. For example, the interaction of the viral envelope with the CD4 receptor found on human lymphocytes and other cells is utilized by free virus as a route of cell entry and also is involved in the direct cell-to-cell spread of the virus. A variety of recombinant molecular technologies have been used to isolate and characterise the various proteins which function as these key molecular targets of viral growth and development. Specific assays have been developed utilizing these proteins in order to 1) Screen synthetic and natural products and identify potential anti-viral compounds, and 2) Test drugs designed to be inhibitory based on either a) the characterisation and elucidation of mechanism of action of the target or b) on the structure of compounds discovered by screen. The results obtained to date and the future perspectives for using these molecular targeted approaches will be described and discussed.
Keywords: Antiviral Agents/*THERAPEUTIC USE DNA Nucleotidyltransferases/ANTAGONISTS & INHIB Gene Expression Regulation, Viral/DRUG EFFECTS/GENETICS Gene Products, rev/ANTAGONISTS & INHIB/GENETICS Gene Products, tat/ANTAGONISTS & INHIB/GENETICS Human HIV/*DRUG EFFECTS/GENETICS HIV Infections/*DRUG THERAPY/MICROBIOLOGY HIV Protease Inhibitors/THERAPEUTIC USE RNA-Directed DNA Polymerase/ANTAGONISTS & INHIB Virus Replication/DRUG EFFECTS/GENETICS ABSTRACT 941230
M94C4283
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Important note: Information in this article was accurate in 1994. The state of the art may have changed since the publication date.
