Su: Anti-HIV Fusion Inhibitors and CCR5 Antagonists

lecture 1

what is the anti-HIV fusion inhibitor

enfuvirtide

enfuvirtide is a _____ drug

polypeptide

Enfuvirtide binds to ____ to prevent the creation of an entry pore for the capsid of the virus, keeping it out of the cell.

gp41

Enfuvirtide binds to gp41 to….

prevent the creation of an entry pore for the capsid of the virus, keeping it out of the cell.

what are the key proteins involved in the HIV entry process

CD4

gp120

CCR5

CXCR4

gp41

what is CD4

a protein receptor found on the surface of helper T cells in the human immune system

what is gp120

a protein on HIV surface that binds to the CD4 receptor

what is CCR5

a second receptor found on the surface of CD4+ cells

what is CXCR4

chemokine co-receptor found on CD4+ cells

what is gp41

a HIV protein, closely associated with gp120, that penetrates the cell membrane

what drug is this (biggest bitch wtf)

enfuvirtide

what is the CCR5 antagonist

maraviroc

CCR5 is a member of the ____ family

beta-chemokine receptor

maraviroc is an ____ inhibitor

entry

maraviroc is a _____ of the CCR5

negative allosteric modulator

maraviroc does not compete with CCR5 (directly or indirectly)

directly

MOA of maraviroc

alters the structure of CCR5 receptor, makes it less likely to bind to the HIV virus (which inhibits it from entering the cell)