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    Effect of conjugates of all-trans-retinoic acid and shorter polyene chain analogues with amino acids on prostate cancer cell growth

    Sadikoglou, E. and Magoulas, George D. and Theodoropoulou, C. and Athanassopoulos, C.M. and Giannopoulou, E. and Theodorakopoulou, O. and Drainas, D. and Papaioannou, D. and Papadimitriou, E. (2009) Effect of conjugates of all-trans-retinoic acid and shorter polyene chain analogues with amino acids on prostate cancer cell growth. European Journal of Medicinal Chemistry 44 (8), pp. 3175-3187. ISSN 0223-5234.

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    Abstract

    In the present work, a series of conjugates of amino acids with all-trans-retinoic acid (ATRA) and shorter polyene chain analogues were rationally designed, synthesized by coupling the succinimidyl active esters of the acidic retinoids with appropriately protected amino acids or peptides followed by deprotection, and examined for their possible effect on viability of human prostate cancer LNCaP cells. In contrast to ATRA, all conjugates bearing amino acids with polar side chains showed no inhibitory effect on LNCaP cell proliferation, while conjugates with α-amino acids with lipophilic side chain, such as 7, or linear amino acids, such as 9, significantly decreased prostate cancer LNCaP cell number. Interestingly, while the effect of ATRA was RARα-dependent, the effect of its active analogues was not inhibited by a selective RARα antagonist. Cell cycle analysis showed no effect on cell cycle, while quantitative analysis by annexin V-propidium iodide staining revealed that neither ATRA nor its analogues affected LNCaP cell apoptosis or necrosis. These results demonstrate that compounds 7 and 9 are potentially useful agents that warrant further preclinical development for treatment of prostate cancer.

    Metadata

    Item Type: Article
    Keyword(s) / Subject(s): Retinoid, amino acid, conjugate, prostate cancer cells, retinoid receptors
    School: Birkbeck Schools and Departments > School of Business, Economics & Informatics > Computer Science and Information Systems
    Research Centre: Birkbeck Knowledge Lab
    Depositing User: Administrator
    Date Deposited: 04 Feb 2011 15:53
    Last Modified: 02 Dec 2016 13:23
    URI: http://eprints.bbk.ac.uk/id/eprint/1874

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