CHARACTERIZATION AND INHIBITION OF A CHOLECYSTOKININ-INACTIVATING SERINE PEPTIDASE

Authors
ROSE C VARGAS F FACCHINETTI P BOURGEAT P BAMBAL RB BISHOP PB CHAN SMT MOORE ANJ GANELLIN CR SCHWARTZ JC
Citation
C. Rose et al., CHARACTERIZATION AND INHIBITION OF A CHOLECYSTOKININ-INACTIVATING SERINE PEPTIDASE, Nature, 380(6573), 1996, pp. 403-409
Citations number
50
Categorie Soggetti
Multidisciplinary Sciences
Journal title
Nature → ACNP
ISSN journal
00280836
Volume
380
Issue
6573
Year of publication
1996
Pages
403 - 409
Database
ISI
SICI code
0028-0836(1996)380:6573<403:CAIOAC>2.0.ZU;2-6
Abstract
A cholecystokinin (CCK)-inactivating peptidase was purified and identi fied as a membrane-bound isoform of tripeptidyl peptidase II (EC 3.4. 14. 10), a cytosolic subtilisin-like peptidase of previously unknown f unctions. The peptidase was found in neurons responding to cholecystok inin, as well as in non-neuronal cells. Butabindide, a potent and spec ific inhibitor, was designed and shown to protect endogenous cholecyst okinin from inactivation and to display pro-satiating effects mediated by the CCKA receptor.