- A new compound has showed strong anti-viral activity against HIV, including some drug-resistant variants
- The HIV virus that causes AIDS remains a major global health challenge
- The team used MX2 beamline to determine how the compound IC-2i bound to the HIV protein shell
A large international team has developed a new compound that showed strong anti-viral activity against HIV, including some drug-resistant variants.
Despite major advances in HIV treatment, lifelong therapy is still required because the virus cannot be completely eradicated, creating a need for safer and more effective drugs that can overcome drug resistance.
In research reported in the journal MedComm earlier this year, investigators combined and refined useful parts of previously studied HIV inhibitors to create smaller, more stable compounds that bind an additional, less mutation-prone region of the HIV capsid, or protein shell.
The HIV-1 capsid (CA) has been validated as an antiviral target that plays critical roles in both the early and late stages of the viral life cycle.
To understand why the new compound IC-2i was effective, they used the Microfocus crystallography (MX2) beamline at the Australian Synchrotron. MX2 can reveal the structure of biological molecules at atomic resolution.
Using MX2, the team determined how IC-2i bound to the HIV capsid. The data revealed the interactions that help the drug bind to its target and provided insights into how future HIV medicines could be designed to address resistance.
Read more on the ANSTO website
Image: 2D view of binding mode for IC-2i and distance between residues, water and ligand. Water were shown in light blue round without hydrogen
Credit: Reprinted under Creative Commons license https://creativecommons.org/licenses/by/4.0/
