June 3, 2015
Inhibition of HIV-1 protease has been documented as an effective strategy for the treatment of HIV/AIDS. However, most peptidomimetic inhibitors do not cross the blood-brain barrier. Early on during infection, HIV infects the brain cells and becomes a latent reservoir for the virus, making it difficult to completely clear it from the system. Typically, most HIV-1 protease inhibitors and other antiretroviral agents, including Darunavir, show significantly lower levels of the drug in the brain than other parts of the body. It is very important to develop antiretroviral agents that have much higher levels of brain penetration.
Researchers at Purdue University have developed three novel HIV-1 protease inhibitors that contain bis-THF and a difluoride moiety that show marked enzyme inhibitory and antiviral potency. These inhibitors demonstrated a five-fold improvement in blood-brain barrier penetration and were highly potent against many current multidrug-resistant strains of HIV-1. Cytotoxicity and other side effects of the inhibitors are also very low and infrequent, which is critical for those patients who require treatment for extended periods.
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technology summary researchers
current multidrug-resistant strains
develop antiretroviral agents
blood-brain barrier penetration
hiv-1 protease inhibitors
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