ACCELERATION OF ACTIVATION AND INACTIVATION BY THE BETA SUBUNIT OF THE SKELETAL-MUSCLE CALCIUM-CHANNEL

被引:267
作者
VARADI, G [1 ]
LORY, P [1 ]
SCHULTZ, D [1 ]
VARADI, M [1 ]
SCHWARTZ, A [1 ]
机构
[1] UNIV CINCINNATI,DEPT PHARMACOL & CELL BIOPHYS,231 BETHESDA AVE,CINCINNATI,OH 45267
关键词
D O I
10.1038/352159a0
中图分类号
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号
07 ; 0710 ; 09 ;
摘要
THE L-type voltage-dependent calcium channel is an important link in excitation-contraction coupling of muscle cells 1 (reviewed in refs 2 and 3). The channel has two functional characteristics: calcium permeation and receptor sites for calcium antagonists. In skeletal muscle the channel is a complex of five subunits, alpha-1, alpha-2, beta, gamma and delta (ref. 4). Complementary DNAs to these subunits have been cloned and their amino-acid sequences deduced 5-8. The skeletal muscle alpha-1 subunit cDNA expressed in L cells manifests as specific calcium-ion permeation, as well as sensitivity to the three classes of organic calcium-channel blockers 9,10. We report here that coexpression of the alpha-1 subunit with other subunits results in significant changes in dihydropyridine binding and gating properties. The available number of drug receptor sites increases 10-fold with an alpha-1-beta combination, whereas the affinity of the dihydropyridine binding site remains unchanged. Also, the presence of the beta-subunit accelerates activation and inactivation kinetics of the calcium-channel current.
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页码:159 / 162
页数:4
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