This invention identifies a novel class of HIV inhibitors targeting RNA-protein interactions.
The global market for HIV drugs is around $20 billion annually. To find new and more effective HIV antivirals, scientists at UCSF have recently focused on viral regulatory complexes that perform critical functions in HIV replication and are important targets for therapeutic intervention. In HIV-infected cells, the Tat and Rev proteins form regulatory complexes with multiple viral and cellular factors to direct transcription and export of the viral RNA. Scientists have identified novel lead compounds that may disrupt the interaction between Rev and the Rev Response Element (RRE) thus preventing HIV replication. These molecules have been tested extensively in HIV replication studies in cell culture and in primary cells and represent an important step towards the development of a new class of HIV therapeutics that could eventually find a place in future HIV combination therapies.
The current invention provides the following advantages:Through a screen for RNA-protein inhibitors, researchers at UCSF have identified a new class of HIV inhibitors. Following multiple rounds of medicinal chemistry and compound testing, the most advanced compounds have improved the efficacy more than two logs and are capable of inhibiting HIV replication with low-nanomolar IC50s and Therapeutic Indices >10,000. Interestingly, the pathway to drug resistance is unique with these inhibitors and we have discovered that resistant viruses are defective in an important viral gene. These findings raise the question of whether the compounds could be used to drive the viral populations towards attenuation and possibly one step closer to a functional cure.
To develop & commercialize the technology as a therapy for HIV and other viral infections
In vitro data available
Country | Type | Number | Dated | Case |
United States Of America | Issued Patent | 10,154,992 | 12/18/2018 | 2013-151 |
Antiviral, Inhibitors, Rev, HIV, RRE, RNA-protein interactions