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15 Cards in this Set

  • Front
  • Back

B cell

- Antibody mediated immunity


- Bone marrow


- Stored in spleen



T Cell

- Cell mediated immunity


- Thymus




Normal Funct;


1. Receptor binding & signalling APC + HLA complex


2. Cell-cell signalling: surface interaction + secreted proteins


3. Autocrine signalling: IL-2


4. Proliferation

T Cell Receptor

- Binds HLA-antigen complex


- Activates PLC gamma


- Phosphatidyl inositol -> IP3


- Release Ca2+, activate calcineurin


- Calcineurin dephos NF-AT& recruit Oct


- NF-AT + Oct transcription factor for IL-2 with Rel-A and NF-kB

Calcineurin

Phosphatase that removes phosphate from NF-AT & Oct

Cyclosporin

- Calcineurin inhibitor


- Binds cyclophilin- inhibits


- Fungal peptide


- AUC predicts response and toxicity, but variable absorption


- C2 better predictor than trough





Tacrolimus

- Calcineurin inhibitor


- Binds immunophilin (FKBP)


- Fungal macrolide


- Long t1/2: trough C0 good measure

Glucocorticoids

1. Inhibits AP-1 directly


2. Increases transcription of I-kB, indirectly increases inhibition of NF-kB and Rel-A


3. Increases mRNA degradation

mTOR

- Mammalian target of rapamycin


- Increase translation of mRNA for cell cycle proteins


- Increase p27 degradation


- Binds EIF-4E and 40-S subunit needed for translation

p27

- Inhibits cyclin E, CDK2 complex


- Inhibits during G0 and G1

Sirolimus

- mTOR inhibitor


- fungal macrolide


- binds immunophilin


- Long t1/2: trough C0 good measure

Everolimus

- mTOR inhibitor


- fungal macrolide


- binds immunophilin


- Long t1/2: trough C0 good measure

Mycophenolate

- Funal


- Inhbits IMP dehydrogenase


- Inhibits de novo synthesis of guanosine monophosphate


- G-MP needed in B and T cells for DNA & RNA synth and signalling


- Glucuronidated in liver


- Conc increases after 4 hours- recycle, more variable relationship b/w C0 and AUC



Anti-CD3 antibody

- Binds CD2 on T cell receptor


- Prevents T cell from binding to APC


- Apoptose?

Eliminated by CYP3A4

Everolimus, tacrolimus, cyclosporin & sirolimus

Substrates for p-gp

Everolimus, tacrolimus, cyclosporin & sirolimus