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International Journal of Medical Sciences

.: Home > International Journal of Medical Sciences > 2010 > Volume 7 Number 6 > Klaus Braun, Manfred Wiessler, Rüdiger Pipkorn, Volker Ehemann, Tobias Bäuerle, Heinz Fleischhacker, Gabriele Müller, Peter Lorenz, Waldemar Waldeck

A cyclic-RGD-BioShuttle functionalized with TMZ by DARinv “Click Chemistry” targeted to αvβ3 integrin for therapy

Klaus Braun, Manfred Wiessler, Rüdiger Pipkorn, Volker Ehemann, Tobias Bäuerle, Heinz Fleischhacker, Gabriele Müller, Peter Lorenz, Waldemar Waldeck
Abstract :

Clinical experiences often document, that a successful tumor control requires high doses of drug applications. It is widely believed that unavoidable adverse reactions could be minimized by using gene-therapeutic strategies protecting the tumor-surrounding healthy tissue as well as the bone-marrow. One new approach in this direction is the use of “Targeted Therapies” realizing a selective drug targeting to gain effectual amounts at the target site, even with drastically reduced application doses. MCF-7 breast cancer cells expressing the αvβ3 [alpha(v)beta(3)] integrin receptor are considered as appropriate candidates for such a targeted therapy. The modularly composed BioShuttle carrier consisting of different units designed to facilitate the passage across the cell membranes and for subcellular addressing of diagnostic and/or therapeutic molecules could be considered as an eligible delivery platform. Here we used the cyclic RGD-BioShuttle as a carrier for temozolomide (TMZ) at the αvβ3 integrin receptor realizing local TMZ concentrations sufficient for cell killing. The IC50 values are 12 µMol/L in the case of cRGD-BioShuttle-TMZ and 100 µMol/L for underivatized TMZ, which confirms the advantage of TMZ reformulation to realize local concentrations sufficient for cell killing.

Keywords :

Date Deposited : 12 Jan 2011 12:59

Last Modified : 12 Jan 2011 12:59

Official URL: http://www.medsci.org/v07p0326.htm

Volume 7, Number 6, - 2010

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