A research team led by Dr. Pin-Fang Lin at Bristol-Myers Squibb, Wallingford, CT has discovered a small molecule compound that can block HIV-1’s entrance into cells (Lin, P.-F. et al., PNAS 100:11013-11018, Sep. 16, 2003). Most of the drugs currently available for treating HIV infection affect replication of viral nucleic acids or the synthesis of viral proteins.
The compound, BMS-378806, binds to the envelope protein, gp120, of HIV-1 and inhibits interactions between gp120 and the CD4 receptor molecule on CD4+ T cells, a necessary step for HIV-1 to infect host cells.
The inhibitory effect of compound BMS-378806 is selective for HIV-1. It is inactive against HIV-2 (a less virulent, primarily West African virus similar to HIV-1), simian immunodeficiency virus, and other viruses tested. The compound exhibits other encouraging pharmacokinetic amenities such as low protein binding and minimal impairment of the compound by human serum. Tests in animals showed that the compound is safe, with acceptable toxicity profiles.
The compound targets a specific HIV-1 protein that does not exist in human cells. It is a novel approach for HIV-1 therapies. It represents a hope that HIV-1 can be stopped before it infects cells. This class of drugs can be used in combination with other drugs to achieve maximum deterrence of HIV-1 infection.
The compound, BMS-378806, binds to the envelope protein, gp120, of HIV-1 and inhibits interactions between gp120 and the CD4 receptor molecule on CD4+ T cells, a necessary step for HIV-1 to infect host cells.
The inhibitory effect of compound BMS-378806 is selective for HIV-1. It is inactive against HIV-2 (a less virulent, primarily West African virus similar to HIV-1), simian immunodeficiency virus, and other viruses tested. The compound exhibits other encouraging pharmacokinetic amenities such as low protein binding and minimal impairment of the compound by human serum. Tests in animals showed that the compound is safe, with acceptable toxicity profiles.
The compound targets a specific HIV-1 protein that does not exist in human cells. It is a novel approach for HIV-1 therapies. It represents a hope that HIV-1 can be stopped before it infects cells. This class of drugs can be used in combination with other drugs to achieve maximum deterrence of HIV-1 infection.
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