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Bombesin marine toxin conjugates inhibit the growth of lung cancer cells

  1. Author:
    Moody, T. W.
    Pradhan, T.
    Mantey, S. A.
    Jensen, R. T.
    Dyba, M.
    Moody, D.
    Tarasova, N. I.
    Michejda, C. J.

  2. Author Address

    Moody, Terry W.] NCI Off, CCR, Dept Hlth & Human Serv, Bethesda, MD 20892 USA. [Pradhan, Tapas, Mantey, Samuel A.; Jensen, Robert T.] NIDDK, NIH, Digest Dis Branch, Bethesda, MD 20892 USA. [Moody, Deborah, Tarasova, Nadya I.; Michejda, Christopher J.] NCI, Struct Biophys Lab, Mol Aspects Drug Design Sect, Frederick, MD 21702 USA.
    1. Year: 2008
  2. Journal: Life Sciences
    1. 82
    2. 15-16
    3. Pages: 855-861
  4. Type of Article: Article
  1. Abstract:

    Hemiasterlin (Hem) and dolastatin (Dol) are marine natural products which are cytotoxic for cancer cells. Hem, a tripeptide, and Dol, a hexapeptide, were conjugated with linkers (L) to the universal BB agonist DPhe-Gln-Trp-Ala-Val-beta Ala-His-Phe-Nle-NH2(BA1) and the effects of the Hem-BB and Dol-BB conjugates investigated on NCI-H1299 lung cancer cells. Hem-LA-BA1 and Hem-LB-BA1 inhibited specific (I-125-Tyr(4)) BB binding to NCI-H1299 cells, which have 13132 receptors (R), with IC50 values of 15 and 25 nM, respectively. Addition of Hem-LA-BA1 and Hem-LB-BA1 to Fura-2 AM loaded cells containing BB2R, caused elevated cytosolic Ca2+. In a growth assay, Hem-LA-BA1 and Hem-LB-BA1 inhibited the proliferation of NCI-H1299 cells. Dol-succinamide (Dols)-LD-BA1 and Dols-LE-BA1 bound with high affinity to NCI-H1299 cells and elevated cytosolic Ca2+, but did not inhibit the proliferation of NCI-H1299 cells. Also, Hem-LA-BA1 inhibited I-125-DTyr-Gln-Trp-Ala-Val-beta Ala-His-Phe-Nle-NH2 (BA2) binding to Balb/3T3 cells transfected with BB1R BB2R as well as with BRS-3 with IC50 values of 130, 8, and 540 nM, respectively. These results show that Hem-BB conjugates are cytotoxic for cancer cells containing BB2R. Published by Elsevier Inc.

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External Sources

  1. PMID: 18336841

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