VIP-ellipticine derivatives inhibit the growth of breast cancer cells.
The effects of vasoactive intestinal peptide (VIP)-ellipticine (E) derivatives were investigated on breast cancer cells. VIP-ALALA-E and VIP-LALA-E inhibited 125I-VIP binding to MCF-7 cells with an IC(50) values of 1 and 0.2 microM respectively. VIP-ALALA-E and VIP-LALA-E caused elevation of cAMP in MCF-7 cells with ED(50) values of 1 and 0.1 microM. VIP-LALA-E caused increased c-fos mRNA in MCF-7 cells. Radiolabeled VIP-LALA-E was internalized at 37 degrees C and delivered the cytotoxic E into MCF-7 cells. VIP-LALA-E inhibited the clonal growth of MCF-7 cells, decreased cell viability based on trypan blue exclusion and reduced 35S-methionine uptake. These results indicate that VIP-E derivatives function as breast cancer VPAC(1) receptor agonists which inhibit MCF-7 cellular viability.
Moody
T W
TW
Cell and Cancer Biology Branch, Center for Cancer Research, National Cancer Institute, Rockville, MD 20850, USA. moodyt@mail.nih.gov
Czerwinski
G
G
Tarasova
N I
NI
Michejda
C J
CJ
D000595:Amino Acid Sequence; D001943:Breast Neoplasms / Q000235:genetics / Q000473:pathology*; D002455:Cell Division / Q000187:drug effects*; D004611:Ellipticines / Q000494:pharmacology*; D006801:Humans; D008969:Molecular Sequence Data; D016760:Proto-Oncogene Proteins c-fos / Q000235:genetics; D012333:RNA, Messenger / Q000235:genetics; D018005:Receptors, Vasoactive Intestinal Peptide / Q000819:agonists; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I; D014660:Vasoactive Intestinal Peptide / Q000494:pharmacology*
D004611:Ellipticines; D016760:Proto-Oncogene Proteins c-fos; D012333:RNA, Messenger; D018005:Receptors, Vasoactive Intestinal Peptide; D051238:Receptors, Vasoactive Intestinal Polypeptide, Type I; C034192:ellipticine; D014660:Vasoactive Intestinal Peptide