Characterization and Inhibition of a cholecystokinin-inactivating serine peptidase

被引:140
作者
Rose, C
Vargas, F
Facchinetti, P
Bourgeat, P
Bambal, RB
Bishop, PB
Chan, SMT
Moore, ANJ
Ganellin, CR
Schwartz, JC
机构
[1] UNIV LONDON UNIV COLL, CHRISTOPHER INGOLD LABS, DEPT CHEM, LONDON WC1H 0AJ, ENGLAND
[2] UNIV PARIS 05, FAC PHARM, F-75006 PARIS, FRANCE
关键词
D O I
10.1038/380403a0
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 cholecystokinin (CCK)-inactivating peptidase was purified and identified as a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4. 14. 10), a cytosolic subtilisin-like peptidase of previously unknown functions. The peptidase was found in neurons responding to cholecystokinin, as well as in non-neuronal cells. Butabindide, a potent and specific inhibitor, was designed and shown to protect endogenous cholecystokinin from inactivation and to display pro-satiating effects mediated by the CCKA receptor.
引用
收藏
页码:403 / 409
页数:7
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