BMS-192548, A TETRACYCLIC BINDING INHIBITOR OF NEUROPEPTIDE-Y RECEPTORS, FROM ASPERGILLUS-NIGER WB2346 .1. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL-ACTIVITY

Authors
KODUKULA K ARCURI M CUTRONE JQ HUGILL RM LOWE SE PIRNIK DM SHU YZ FERNANDES PB SEETHALA R
Citation
K. Kodukula et al., BMS-192548, A TETRACYCLIC BINDING INHIBITOR OF NEUROPEPTIDE-Y RECEPTORS, FROM ASPERGILLUS-NIGER WB2346 .1. TAXONOMY, FERMENTATION, ISOLATION AND BIOLOGICAL-ACTIVITY, Journal of antibiotics, 48(10), 1995, pp. 1055-1059
Citations number
19
Categorie Soggetti
Pharmacology & Pharmacy",Immunology,"Biothechnology & Applied Migrobiology
Journal title
Journal of antibiotics → ACNP
ISSN journal
00218820
Volume
48
Issue
10
Year of publication
1995
Pages
1055 - 1059
Database
ISI
SICI code
0021-8820(1995)48:10<1055:BATBIO>2.0.ZU;2-R
Abstract
During the screening of microbial fermentation extracts for their abil ity to inhibit the binding of I-125-peptid YY (PYY) to the neuropeptid e Y (NPY) receptor using the scintillation proximity assay (SPA), BMS- 192548 was isolated from the extract of Aspergillus niger WB2346 by bi oassay-guided fractionation. BMS-192548 showed the inhibitory activity against I-125-PYY binding to SK-N-MC and SMS-KAN cells, which express NPY, and NPY, receptors, respectively, with IC50 values of 24 mu M in Y-1 and 27 mu M in Y-2 receptor binding. BMS-192548 demonstrated weak cytotoxicity against murine tumor cell line M-109 with an IC50 value of 240 mu M.