This technology presents a series of novel small molecule compounds that target a key regulatory protein implicated in HIV progression. The compounds were discovered through a high-throughput screening assay linking viral accessory protein activity with a specific kinase activation. They exhibit low micromolar potency in inhibiting the related kinase activity induced by the viral protein while exerting minimal impact on the kinase itself. Additionally, they demonstrate submicromolar effectiveness against HIV replication in primary human macrophages, with confirmed direct binding via surface plasmon resonance and low toxicity across tested models.
Description
This approach is differentiated by its focus on directly inhibiting a viral accessory factor rather than conventional targets like viral enzymes. By intervening at the level of the viral protein that modulates host kinase activity, it potentially restores immune recognition and reduces the risk of drug resistance when combined with standard therapies. The unique chemical scaffolds and specific substituent modifications further enhance its selectivity and pharmacological profile, paving the way for a synergistic treatment strategy that could significantly improve therapeutic outcomes in HIV management.
Applications
- Targeted Nef inhibition drugs
- Novel antiretroviral agents development
- HIV combination therapy enhancer
- Drug resistance mitigation solutions
- Immunorecognition restoration treatments
Advantages
- Directly targets HIV-1 Nef to disrupt viral replication and immune evasion.
- Demonstrates high potency at low micromolar to nanomolar concentrations with minimal toxicity.
- Offers synergistic benefits when combined with existing antiretroviral therapies, potentially reducing required dosages and side effects.
- Minimizes the risk of developing drug resistance while restoring immune recognition of infected cells.
- Exhibits favorable pharmacological profiles and water solubility, supporting both in vitro and in vivo applications.
IP Status
https://patents.google.com/patent/US10603321B2
