Fusion Inhibitors Mechanism of Action

Fusion inhibitors are antiretroviral drugs that interfere with the fusion of viral and cellular membranes, preventing HIV entry into human cells. They are used in HIV treatment.

Fusion Inhibitors FAQ

Image credit: clinicalinfo.hiv.gov

What are fusion inhibitors?

Fusion inhibitorsblock fusion of the HIV virus to the human cell and thereby reduce entry of the virus into the CD4 cell. They are also called entry inhibitors. Prototype and common drugs Prototype: enfuvirtide Others: PRO 140, ibalizumab MOA (Mechanism of Action) (Figure 18-25) Several steps are involved in the replication of HIV.

How do fusion inhibitors work?

Fusion inhibitors bind to the gp41 protein on the outside of the virus. Gp41 is involved in the physical merging of the outsides of the virus and CD4 cells, allowing HIV to get inside the host cell. This blending and absorption of the virus is called fusion.

What are HIV fusion inhibitors?

Fusion inhibitors are a class of molecules designed to disrupts the HIV-1 fusion protein equipment at the final stage of fusion with the host cell. HIV binds to the host CD4 + cell receptor via the viral protein gp120 and gp41, and then undergoes a conformational change that assists in the fusion of the viral membrane with the host cell membrane.

What is fusion inhibitor resistance?

Fusion Inhibitor Resistance to the entry inhibitors targeting the CCR5 receptor (e.g. maraviroc) is unusual and more complex, resulting from mutations that promote gp120 binding of the virus to the CCR5 receptor which is bound to the drug. From:Infectious Diseases (Third Edition), 2010 Related terms: Virus Reverse-Transcriptase Inhibitor

What is a gp120 fusion inhibitor?

Inhibitors of the fusion of HIV to host cells, preventing viral entry. This includes compounds that block attachment of HIV ENVELOPE PROTEIN GP120 to CD4 RECEPTORS. An HIV-1 gp41 fusion inhibitor used in patients experiencing HIV-1 replication who are already being treated with other anti-retrovirals.