CALCISEPTINE, A PEPTIDE ISOLATED FROM BLACK MAMBA VENOM, IS A SPECIFIC BLOCKER OF THE L-TYPE CALCIUM-CHANNEL

被引:221
作者
DEWEILLE, JR
SCHWEITZ, H
MAES, P
TARTAR, A
LAZDUNSKI, M
机构
[1] INST PHARMACOL MOLEC & CELLULAIRE, CNRS,UNITE RECH 411,660 ROUTE LUCIOLES, SOPHIA ANTIPOLIS, F-06560 VALBONNE, FRANCE
[2] INST PASTEUR, SERV CHIM MOLEC, CNRS, UNITE RECH 1309, F-59019 LILLE, FRANCE
关键词
TOXINS; CONTRACTION; CARDIAC CELLS; VASCULAR RELAXANT;
D O I
10.1073/pnas.88.6.2437
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 venom of the black mamba contains a 60-amino acid peptide called calciseptine. The peptide has been fully sequenced. It is a smooth muscle relaxant and an inhibitor of cardiac contractions. Its physiological action resembles that of drugs, such as the 1,4-dihydropyridines, which are important in the treatment of cardiovascular diseases. Calciseptine, like the 1,4-dihydropyridines, selectively blocks L-type Ca2+ channels and is totally inactive on other voltage-dependent Ca2+ channels such as N-type and T-type channels. To our knowledge, it is the only natural polypeptide that has been shown to be a specific inhibitor of L-type Ca2+ channels.
引用
收藏
页码:2437 / 2440
页数:4
相关论文
共 53 条
[1]   PROPERTIES OF STRUCTURE AND INTERACTION OF THE RECEPTOR FOR RHO-CONOTOXIN, A POLYPEPTIDE ACTIVE ON CA-2+ CHANNELS [J].
BARHANIN, J ;
SCHMID, A ;
LAZDUNSKI, M .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1988, 150 (03) :1051-1062
[2]  
BROWN AM, 1987, CIRC RES, V61, P6
[3]   MODULATION OF CALCIUM CHANNELS IN CARDIAC AND NEURONAL CELLS BY AN ENDOGENOUS PEPTIDE [J].
CALLEWAERT, G ;
HANBAUER, I ;
MORAD, M .
SCIENCE, 1989, 243 (4891) :663-666
[4]  
CARBONE E, 1989, ANN NY ACAD SCI, V560, P346, DOI 10.1111/j.1749-6632.1989.tb24114.x
[5]   A LOW VOLTAGE-ACTIVATED, FULLY INACTIVATING CA-CHANNEL IN VERTEBRATE SENSORY NEURONS [J].
CARBONE, E ;
LUX, HD .
NATURE, 1984, 310 (5977) :501-502
[6]   LONG-TERM POTENTIATION OF SYNAPTIC TRANSMISSION IN THE HIPPOCAMPUS INDUCED BY A BEE VENOM PEPTIDE [J].
CHERUBINI, E ;
BENARI, Y ;
GHO, M ;
BIDARD, JN ;
LAZDUNSKI, M .
NATURE, 1987, 328 (6125) :70-73
[7]   TRANSPLANTABLE INSULINOMA IN RAT [J].
CHICK, WL ;
WARREN, S ;
CHUTE, RN ;
LIKE, AA ;
LAURIS, V ;
KITCHEN, KC .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1977, 74 (02) :628-632
[8]  
COGNARD C, 1986, P NATL ACAD SCI USA, V83, P1518, DOI 10.1073/pnas.83.5.1518
[9]   NEUROTRANSMITTERS DECREASE THE CALCIUM CONDUCTANCE ACTIVATED BY DEPOLARIZATION OF EMBRYONIC CHICK SENSORY NEURONS [J].
DUNLAP, K ;
FISCHBACH, GD .
JOURNAL OF PHYSIOLOGY-LONDON, 1981, 317 (AUG) :519-535
[10]   SEQUENCE AND EXPRESSION OF MESSENGER-RNAS ENCODING THE ALPHA-1-SUBUNIT AND ALPHA-2-SUBUNIT OF A DHP-SENSITIVE CALCIUM-CHANNEL [J].
ELLIS, SB ;
WILLIAMS, ME ;
WAYS, NR ;
BRENNER, R ;
SHARP, AH ;
LEUNG, AT ;
CAMPBELL, KP ;
MCKENNA, E ;
KOCH, WJ ;
HUI, A ;
SCHWARTZ, A ;
HARPOLD, MM .
SCIENCE, 1988, 241 (4873) :1661-1664