4 ms·
by preventing viral capsid assembly, as noted in the article. Once bound to the P24 capsid protein, the drug also interferes with other stages of the virus’ li
by mrtesthah 2y ago
by preventing viral capsid assembly, as noted in the article.
Once bound to the P24 capsid protein, the drug also interferes with other stages of the virus’ lifecycle[1]:
>Lenacapavir is a multistage, selective inhibitor of HIV-1 capsid function that directly binds to the interface between capsid protein (p24) subunits in hexamers. Surface plasmon resonance sensorgrams showed dose-dependent and saturable binding of lenacapavir to cross-linked wild-type capsid hexamer with an equilibrium binding constant (KD) of 1.4 nM. Lenacapavir inhibits HIV-1 replication by interfering with multiple essential steps of the viral lifecycle, including capsid-mediated nuclear uptake of HIV-1 proviral DNA (by blocking nuclear import proteins binding to capsid), virus assembly and release (by interfering with Gag/Gag-Pol functioning, reducing production of capsid protein subunits), and capsid core formation (by disrupting the rate of capsid subunit association, leading to malformed capsids).
1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e5652804-29c4-40d7-aeb2-0142ed2a7b5b#S12.4 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e56...
- deleted 2y ago[deleted]