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Inhibition of Human Immunodeficiency Virus integrase by beta-conidendrol.


Natl Conf Hum Retroviruses Relat Infect (1st). 1993 Dec 12-16;:147.

The Human Immunodeficiency Virus type 1 (HIV-1) integrase protein is required for productive virus spread in infected T-lymphoid cells. This suggests that inhibitors of integrase may be useful in controlling the spread of HIV-1 in infected individuals. Integrase protein expressed in E. Coli displays three functions in vitro, when oligonucleotides modelled on the viral termini are used as substrates. These functions are a specific dinucleotide cleavage, a non-specific endonuclease activity, and a strand-transfer activity. We have observed that beta-conidendrol inhibits the specific endonucleolytic function of integrase in vitro with an IC50 of 500 nM. Parallel inhibition of the non-specific cleavage function was also observed, and in the absence of non- specific cleavage, integration products were not detected. Beta-conidendrol also inhibits a modified integrase (C43S) which is notably reduced in its ability to specifically cleave a dinucleotide from the substrate terminus. Beta- conidendrol was modelled as a nucleotide (AMP), and may resemble either the A residue that contributes to the specific cleavage reaction, or an adenylate interacting at a putative allosteric site.

Adult Female Herpes Zoster/*COMPLICATIONS Human HIV Infections/*COMPLICATIONS/EPIDEMIOLOGY HIV Seroprevalence Male Middle Age Prevalence Prospective Studies Retrospective Studies Risk Factors United States/EPIDEMIOLOGY ABSTRACT


Information in this article was accurate in December 30, 1995. The state of the art may have changed since the publication date. This material is designed to support, not replace, the relationship that exists between you and your doctor. Always discuss treatment options with a doctor who specializes in treating HIV.