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11 Cards in this Set
- Front
- Back
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Calcium and calcinuleurin have ability to do what and what does CsA and FK506 inhibit |
Dephosphorylate NFAT The phosphatase activity of calcineurin is Whats inhibited |
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What do you need to do to FK506 and CsA to be immunosuppressive |
Have to be on their binding protein to have activity Must bend the molecule in a specific way and must allosterically change the structure slightly so it fits on active site |
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What inhibits calcineurin |
FK506+FKBP Cyclosporin A and cyclophillin |
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What does rap inhibit |
On its FKBP it inhibits mtor |
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Before rapamycin what did we not know |
That cells had mTOR |
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What usually happens in mtor pathway |
IL-2 receptor with alpha beta and gamma subunits activates mTOR then activates P70 56K which activates S6(ribosomal protein) for protein synthesis |
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What does rapamycin inhibit |
Stops the mtor pathway to S6- so no protein synthesis Inhibits cyclin E- which gives the go ahead for cell cycle to continue Protein translation is controlled by eif-4F - doesn’t get the signal so stopes protein translation |
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What does rapamycin on FKBP bind to |
Mammalian target of rapamycin mTOR |
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mTOR (mTORC1) binding inhibits what |
S6 kinase Cyclins eIF4 |
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What can rapamycin said to be and how could this be used |
Not just immunisuppression but stops cell proliferation Can he tried in disease states with over proliferative cells |
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Why cant CsA FK506 or rapamycin not bind to targets |
Only drug and binding protein complexes suppress |
