BINDING OF THE IMMUNOSUPPRESSANT PEPTIDE CYCLOSPORINE-A TO CALCIUM, ZINC AND COPPER - IS CYCLOSPORINE-A AN IONOPHORE

被引：17

作者：

DANCER, RJ ^{[1
]}

JONES, A ^{[1
]}

FAIRLIE, DP ^{[1
]}

机构：

[1] UNIV QUEENSLAND,CTR DRUG DESIGN & DEV,BRISBANE,QLD 4072,AUSTRALIA

来源：

AUSTRALIAN JOURNAL OF CHEMISTRY | 1995年 / 48卷 / 11期

关键词：

D O I：

10.1071/CH9951835

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Cyclosporin A is an immunosuppressant drug that has made organ transplantation possible during the past decade. This conformationally flexible peptide, which interferes in an unknown way with calcium-dependent intracellular signalling events, has now been examined in aqueous and acetone solutions containing metal ions. By using electrospray mass spectrometry and nuclear magnetic resonance spectroscopy, cyclosporin A was found to bind directly to endogenous metal ions Ca2+, Zn2+ and Cu2+, With the highest affinity being for Ca2+. These observations raise the possibility that cyclosporins might directly regulate local concentrations of metal ions associated with intracellular signal transduction. This may be an important clue to the mechanism of immunoregulation by this and structurally related drugs.

引用

页码：1835 / 1841

页数：7

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