A MOLECULAR BLUEPRINT FOR THE PORE-FORMING STRUCTURE OF VOLTAGE-GATED CALCIUM CHANNELS

被引：74
作者：
GROVE, A
TOMICH, JM
MONTAL, M
机构：
[1] UNIV CALIF SAN DIEGO,DEPT BIOL,LA JOLLA,CA 92093
[2] UNIV CALIF SAN DIEGO,DEPT PHYS,LA JOLLA,CA 92093
[3] UNIV SO CALIF,SCH MED,DEPT BIOCHEM,LOS ANGELES,CA 90033
[4] CHILDRENS HOSP,LOS ANGELES,CA 90054
来源：
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 1991年 / 88卷 / 15期
关键词：
DRUG; LIPID BILAYERS; MOLECULAR MODELING; 4-HELIX BUNDLE;
D O I：
10.1073/pnas.88.15.6418
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：
A protein that imitates the sequence of a highly conserved segment predicted to line the pore of dihydropyridine-sensitive L-type calcium channels was designed and synthesized. Single-channel conductance properties were studied in planar lipid bilayers. The synthetic protein emulates the ionic conductance, ionic selectivity, and pharmacological properties of the authentic calcium channel, including the stereospecific action of agonist and antagonist enantiomers of the dihydropyridine BayK 8644. The identified sequence is identical in L-type calcium channels from skeletal muscle and isoforms of cardiac muscle, brain, and aorta. It is plausible that this structural motif represents the molecular blueprint for the pore-forming structure of voltage-gated calcium channels.
引用
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页码：6418 / 6422
页数：5
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