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The Sound of Evolution
Enfuvirtide
Mechanism of action:
Enfuvirtide is a fusion inhibitor. When HIV enters CD4+ T cells, the viral surface protein gp120 first binds to the CD4 receptor and the co-receptors CCR5 or CXCR4. Then gp41 undergoes a conformational change that brings the viral envelope and host cell membrane close enough to fuse, allowing infection to proceed. Enfuvirtide binds to the HR1 (heptad repeat 1) region of gp41, preventing fusion between the viral envelope and the host cell membrane.
Reference(s):
Greenberg ML et al. (2004). Resistance to enfuvirtide, the first HIV fusion inhibitor. J Antimicrob Chemother.
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