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VIP-ellipticine derivatives inhibit the growth of breast cancer cells

  1. Author:
    Moody, T. W.
    Czerwinski, G.
    Tarasova, N. I.
    Michejda, C. J.

  2. Author Address

    NCI, Cell & Canc Biol Branch, Ctr Canc Res, Rockville, MD 20850 USA NCI, Cell & Canc Biol Branch, Ctr Canc Res, Rockville, MD 20850 USA NCI, Mol Aspects Drug Design Sect, Macromol Struct Lab, Adv BioSci Labs, Frederick, MD 21702 USA Moody TW NCI, Cell & Canc Biol Branch, Ctr Canc Res, Rockville, MD 20850 USA
    1. Year: 2002
  2. Journal: Life Sciences
    1. 71
    2. 9
    3. Pages: 1005-1014
  4. Type of Article: Article
  1. Abstract:

    The effects of vasoactive intestinal peptide (VIP)-ellipticine (E) derivatives were investigated on breast cancer cells. VIP- ALALA-E and VIP-LALA-E inhibited I-125-VIP binding to MCF-7 cells with an IC50 values of 1 and 0.2 muM respectively. VIP- ALALA-E and VIP-LALA-E caused elevation of cAMP in MCF-7 cells with ED50 values of 1 and 0.1 muM. VIP-LALA-E caused increased c-fos mRNA in MCF-7 cells. Radiolabeled VIP-LALA-E was internalized at 37 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 S-35-methionine uptake. These results indicate that VIP-E derivatives function as breast cancer VPAC(1) receptor agonists which inhibit MCF-7 cellular viability. (C) 2002 Elsevier Science Inc. All rights reserved.

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