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12 Cards in this Set

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Transplant Rejection Mech.

1. Direct Pathway: 수여자의 T cell이 공여자의 APC의 표면에 있는 allogenic MHC 인지.

2. Indirect pathway: 공여자의 MHC를 수여자의 APC가 가공처리하여 수여자의 T cell이 인지.


a. Glucocorticoids

b. Selective inhibitors of cytokine production an d function

c. Anti-metabolic & anti-prolif. drug: azathioprine, methotrexate (MTX)

d. Biologicals


a. Bind to receptors inside cells and regulate the transcription of proinflammatory cytokines (such as IL-1 and IL-6).

b. T cells are inhibited from making IL-2.

c. The activation of cytotoxic T cells is inhibited.

d. Neutrophils and monocytes display poor chemotaxis.

e. IL1 생성 억제/ NFkB, AP1에 의한 작용 억제.


-이것도 스테로이드

-감염 증가/고혈압 및 고혈당증 유발.

Selective Inhibitor

1. Calcineurin Inhibitors:

-cyclosporine, tacrolimus (FK506).

-blocks calcineurin's phosphatase activity.

2. mTOR Inhibitors:

-sirolimus, everolimus.

-blocks mTOR kinase activity.


-Inhibits T-cell activation by inhibiting calcineurin

-Forms a complex with cyclophilin. This complex binds to calcineurin, inhibiting Ca stimulated dephosphorylation of NFAT.

-Prevents the nuclear translocation of NFAT and inhibits T-cell activation

-Also increases expression of TGF-beta, a potent inhibitor of IL-2-stimulated T-cell proliferation.




-Elevates LDL cholesterol lv

피해야될 음식: 자몽 주스.

Tacrolimus (FK506)

-binds to an intracellular ptn FK506-BP12 (FKBP-12)

-calcineurin phosphatase activity is inhibited.


-Neurotoxicty: 구분되는 부작용. 두통, 경련, 손이나 발의 감각이상.


-복용방법: cyclosporine 먼저 복용 후 다음으로 sirolimus 복용.

-forms complex with FKBP12, but the complex does not affect calcineurin activity.

-binds and inhibits a protein kinase mTOR (이를 통해 CDK2 activity inhibition)

-usually used in combination with a reduced dose of calcineurin inhibitor & glucocorticoids.

Toxicities: Increase in serum cholesterol and TG/ not recommended in lung transplants

Anti-metabolic drugs: Azathioprine

-Cleaved to 6 mercaptopurine (6MP)

-inhibits de novo purine synthesis.

-made allogenic kidney transplantation possible

toxicity: BM suppression (leukopenia)

-CBC (Complete blood count) & liver function should be monitored (부작용: 백혈구 감소증)


-TIMP -> 6TGN (incorporated into DNA)

-TIMP-> 6MeMPN (inhibition of de novo purine synthesis: TPMT에 의해 이 과정 촉진)

Mycophenolate Mofetil (MMF)

-hydrolyzed to the active form MPA

-inhibits IMPDH (inosine monophosphate DH)

-inhibits de novo pathway of guanine nucleotide synthesis

Therapeutic Use: Typically used in combination with glucocorticoids and a calcineurin inhibitor but not with azathioprien

Toxicity: 위장장애


제1세대: Polyclonal antisera (ATG, ALG)

제2세대: OKT3 (monoclonal reagents): TCR complex block.

제 3세대: Daclizumab, Basiliximab

:binds to IL2R on the surface of activated T cell. used in the prophylaxis of acute organ rejection in adults.

Drug/Site of Action