Immunophilins: Receptor Protein For Immunosuppressant Drugs
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چکیده
منابع مشابه
Neural actions of immunophilin ligands.
Immunophilins, protein receptors for immunosuppressant drugs such as cyclosporin A and FK506, are enriched far more in the brain than in the immune system. Drug-immunophilin complexes bind to calcineurin, inhibiting its phosphatase activity and leading to immunosuppressant effects. The immunophilin FKBP-12 (FK506 binding protein, 12 kDa) forms a complex with the ryanodine and inositol (1,4,5) t...
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The search for immunosuppressant drugs to increase the success of organ transplantation led to the discovery of the immunophilins, proteins that interface with a range of signal transduction systems inside cells, especially in the nervous and immune systems. Here we review how these interesting molecules work and consider their therapeutic potential.
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Despite immunophilins being abundant in the brain,their functional role there remains unclear. Using rat models of transient focal cerebral ischemia,I investigated the effect of ischemic stress on the rotamase activity of immunophilins in the brain and examined the possible role of immunophilins in postischemic neuroprotection. I found that the rotamase activity of the FK506 binding protein cla...
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FKBP52 (FKBP59, FKBP4) is a "macro" immunophilin that, although sharing high structural and functional homologies in its amino-terminal domain with FKBP12 (FKBP1), does not have immunosuppressant activity when complexed with FK506, unlike FKBP12. To investigate the physiological function of FKBP52, we used the yeast two-hybrid system as an approach to find its potential protein partners and, fr...
متن کاملImmunophilin regulation of neurotransmitter release.
BACKGROUND The immunophilins are proteins that mediate actions of immunosuppressant drugs such as FK506 and cyclosporin A by binding to calcineurin, inhibiting its phosphatase activity, and increasing the phosphorylation level of transcription factors required for interleukin 2 formation. Though concentrations in the brain greatly exceed levels in immune tissues, no function has been previously...
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