Immunosuppressants Mechanism of Action

Question 1

Cyclosporine

Answer 1

Calcineurin inhibitor; binds cyclophilin. Blocks T cell activation by preventing IL-2 transcription.

Question 2

Tacrolimus

Answer 2

Calcineurin inhibitor; binds FK506 binding protein (FKBP). Blocks T cell activation by preventing IL-2 transcription.

Question 3

Sirolimus (Rapamycin)

Answer 3

mTOR inhibitor; binds FKBP. Blocks T cell activationa nd B cell differentiation by preventing IL-2 signal transduction.

Question 4

Basiliximab

Answer 4

Monoclonal antibody; blocks IL-2R

Question 5

Azathioprine

Answer 5

Antimetabolite precursor of 5-mercaptopurine. Inhibits lymphocyte proliferation by blocking nucleotide synthesis.

Question 6

Glucocorticoids

Answer 6

Inhibit NF-kappaB. Suppress both B and T cell function by decreasing transcription of many cytokines.

Question 7

Immunosuppresants do what

Answer 7

Block lymphocyte activation and proliferation. Reduce acute transplant rejection by suppressing cellular immunity. Frequently combined to achieve greater efficacy with dec. toxicity. Chronic suppression increases risk of infection and malignancy.

Question 8

Draw out the target map

Answer 8

………………

Question 9

What does Azathioprine inhibit

Answer 9

Blocks PPRP Amidotransferase