SINGLE-CHANNEL ACTIVITY OF THE RYANODINE RECEPTOR CALCIUM-RELEASE CHANNEL IS MODULATED BY FK-506

被引:128
作者
AHERN, GP [1 ]
JUNANKAR, PR [1 ]
DULHUNTY, AF [1 ]
机构
[1] AUSTRALIAN NATL UNIV,JOHN CURTIN SCH MED RES,DIV NEUROSCI,CANBERRA,ACT 2601,AUSTRALIA
关键词
FK-506; SKELETAL MUSCLE; SARCOPLASMIC RETICULUM; EXCITATION-CONTRACTION COUPLING; RYANODINE RECEPTOR CALCIUM RELEASE CHANNEL;
D O I
10.1016/0014-5793(94)01001-3
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
The immunosuppressant drug FK-506 (3-20 mu M) increased the open probability of ryanodine receptor calcium release channels, formed by incorporation of terminal cisternae vesicles from rabbit skeletal muscle into lipid bilayers, with cis (cytoplasmic) calcium concentrations between 10(-7) M and 10(-3) M. FK-506 increased mean current and channel open time and induced long sojourns at subconductance levels that were between 28% and 38% of the maximum conductance and were distinct from the ryanodine-induced subconductance level at about 45% of the maximum conductance. FK-506 relieved the Ca2+ inactivation of the ryanodine receptor seen at 10(-3) M Ca2+. The results are consistent with FK-506 removal of FK-506 binding protein from the ryanodine receptor [15].
引用
收藏
页码:369 / 374
页数:6
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