OCTAPEPTIDE ANALOGS OF SOMATOSTATIN INHIBIT THE CLONAL GROWTH AND VASOACTIVE INTESTINAL PEPTIDE-STIMULATED CYCLIC-AMP FORMATION IN HUMAN SMALL-CELL LUNG-CANCER CELLS

被引:27
作者
TAYLOR, JE [1 ]
MOREAU, JP [1 ]
BAPTISTE, L [1 ]
MOODY, TW [1 ]
机构
[1] GEORGE WASHINGTON UNIV,SCH MED & HLTH SCI,DEPT BIOCHEM & MOLEC BIOL,WASHINGTON,DC 20037
关键词
SOMATOSTATIN; SRIF; SMALL CELL LUNG CANCER; SOMATOSTATIN RECEPTORS; VASOACTIVE INTESTINAL PEPTIDE; CYCLIC AMP;
D O I
10.1016/0196-9781(91)90143-D
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Two endocrinologically active octapeptide analogues (BIM-23014 C and BIM-23034) of somatostatin (SRIF) containing either an N- or C-terminal 3-(2-naphthyl)-D-Ala residue were examined for their ability to inhibit the in vitro receptor binding, clonal growth, and vasoactive intestinal peptide (VIP)-stimulated cyclic AMP formation in human small cell lung cancer cell (SCLC) line NCI-H345. Both SRIF peptides inhibited [I-125]SRIF(Tyr11)-14 binding with IC50 values in the low nM range. Colony formation in the in vitro SCLC growth assay was also inhibited in the same concentration range, as was VIP-stimulated cyclic AMP formation. Therefore, octapeptide analogues of SRIF function as SCLC SRIF receptor agonists.
引用
收藏
页码:839 / 843
页数:5
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