Influenza & HIV

What do neuraminidase inhibitors do in influenza?

They block the release of the virus from the outside of the cell by inhibiting neuraminidase.

What viral process does hemagglutinin (H) mediate?

Hemagglutinin mediates binding of the infleunza virus to the cell surface.

What viral process does neuraminidase (N) mediate?

Neuraminidase mediates release of the virus from the cell surface after replication.

How are influenza viruses classified?

Influenza viruses are named based on their hemagglutinin (H) and neuraminidase (N) subtypes, e.g., H1N1.

three inhibitors of neuramindase

Zanamivir, peramivir, and oseltamivir.

The inhibitors block release of a mature viron from the cell and mimic the transition state of sialic acid cleavage. (note: all end in “ivir.”)

Baloxavir MOA

inhibits a cap-dependent endonuclease thereby blocking influenza replication

Some antivirals must be ________ to be active

Phosphorylated

Why do phosphonate drugs have advantages

No need for viral kinases (bypass resistance in TK-deficient strains).

Stable C-P bond (resistant to esterase cleavage, increasing stability).

Broad-spectrum against a variety of DNA viruses.

Direct inhibition of viral DNA polymerase.

ask tenzin kunsel DOB 1996

Ritonavir and cobicistat in HIV therapy MOA

used as pharmacokinetic enhancers in combo with other HIV therapies.

reverse transcriptase inhibitors - nucleotide/nucleoside HIV-1 RT inhibitors binding site

Nucleoside/Nucleotide Reverse Transcriptase Inhibitors (NRTIs) target the HIV-1 reverse transcriptase enzyme and interfere with viral replication by binding to the enzyme’s active site.

reverse transcriptase inhibitors- non nucleoside RT inhibitors binding site

Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs) inhibit the HIV-1 reverse transcriptase enzyme by binding to a specific, non-active site (allosteric site) on the enzyme.

HIV protease inhibitors MOA

block the cleavage of the Gag and Gag-pol polypeptides blocking maturation.

Integrase inhibitors MOA

block integration of the pro-viral DNA into the host chromosome.