AZIDOBUTYRYL CLENTIAZEM, A NEW PHOTOACTIVATABLE DILTIAZEM ANALOG, LABELS BENZOTHIAZEPINE BINDING-SITES IN THE ALPHA(1) SUBUNIT OF THE SKELETAL-MUSCLE CALCIUM-CHANNEL

被引：35

作者：

WATANABE, T

KALASZ, H

YABANA, H

KUNIYASU, A

MERSHON, J

ITAGAKI, K

VAGHY, PL

NAITO, K

NAKAYAMA, H

SCHWARTZ, A

机构：

[1] UNIV CINCINNATI,COLL MED,DEPT PHARMACOL & CELL BIOPHYS,CINCINNATI,OH 45267

[2] HOKKAIDO UNIV,FAC PHARMACEUT SCI,SAPPORO,HOKKAIDO 060,JAPAN

来源：

FEBS LETTERS | 1993年 / 334卷 / 03期

关键词：

H-3]AZIDOBUTYRYL CLENTIAZEM; DILTIAZEM-BINDING SITE; PHOTOAFFINITY LABELING; CALCIUM CHANNEL; SEQUENCE-DIRECTED ANTIBODY;

D O I：

10.1016/0014-5793(93)80690-V

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：

[H-3]Azidobutyryl clentiazem, a new photoactivatable diltiazem derivative, has a higher binding affinity than azidobutyryl diltiazem. It can be covalently incorporated into the alpha1 subunit of the skeletal muscle calcium channel by UV irradiation, which allows the benzothiazepine binding site to be determined. The photolabeled alpha1 subunit and its proteolytic fragments were analyzed with a panel of sequence-directed antibodies. The results suggest that the linker region between segment S5 and S6 of domain IV is involved in benzothiazepine binding. This site is different from the dihydropyridine and verapamil binding sites.

引用

页码：261 / 264

页数：4

共 19 条

[1] QUATERNARY DILTIAZEM CAN ACT FROM BOTH SIDES OF THE MEMBRANE IN VENTRICULAR MYOCYTES [J].