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

被引:18
作者
KODUKULA, K [1 ]
ARCURI, M [1 ]
CUTRONE, JQ [1 ]
HUGILL, RM [1 ]
LOWE, SE [1 ]
PIRNIK, DM [1 ]
SHU, YZ [1 ]
FERNANDES, PB [1 ]
SEETHALA, R [1 ]
机构
[1] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,PRINCETON,NJ 08543
关键词
D O I
10.7164/antibiotics.48.1055
中图分类号
Q81 [生物工程学(生物技术)]; Q93 [微生物学];
学科分类号
071005 ; 0836 ; 090102 ; 100705 ;
摘要
During the screening of microbial fermentation extracts for their ability to inhibit the binding of I-125-peptid YY (PYY) to the neuropeptide Y (NPY) receptor using the scintillation proximity assay (SPA), BMS-192548 was isolated from the extract of Aspergillus niger WB2346 by bioassay-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.
引用
收藏
页码:1055 / 1059
页数:5
相关论文
共 19 条