RT INHIBITORS STRUCTURES

Question 1

Answer 1

ZIDOVUDINE

Thymidine Analog

Phosphorylated by TK

REsistance by Point Mutations in RT

Question 2

Answer 2

DIDANOSINE (DDI)

Inosine drug

Converted to 2’,3’’ di-deoxyadenosine triphosphate

Question 3

Answer 3

ZALCITABINE

Cytidine Analog

Works by Competitive Inhibition of dCTP

Question 4

Answer 4

STAVUDINE

D4T

Unsaturated Pyrimidine analog

Competes with TTP

Question 5

Answer 5

ABACAVIR

Penetrable to the Blood Brain Barrier

Question 6

Answer 6

TENOFOVIR

Cellular sterases cleaves phosphate to release it

Question 7

Answer 7

LAMIVUDINE

YOU HAVE A SULFUR HERE

Question 8

Answer 8

EMTRICITABINE

Cytidine Analog

RT inhibitor

Specific Point Mutation Resistance: MI84 V/I

Resistance is lower when pts take Emtricitabine and Tenofovir together

Question 9

Answer 9

NEVIRAPINE : “BUTTERFLY SHAPE”

DELAVIRDINE

Completely Innefective

Question 10

Answer 10

EFAVIRENZ

2nd Generation of Non-nucleoside Inhibitors

Not effective against K103N mutation

Question 11

Answer 11

CAPRAVIRINE

3rd Generation Inhibitor

Key: 1) Interacts with Backbone, not with the side chains of aa

2) Flexible Molecule

Resistance requires 2 mutations!

ALso inhibits HIV-2

3) Retains activity against mutant K103N