closo-borane conjugated regulatory peptides retain high biological affinity: synthesis of closo-borane conjugated Tyr(3)-octreotate derivatives for BNCT

Bioconjugate Chemistry
Thomas BetzelFrank Roesch

Abstract

Despite the improvements in cancer therapy during the past years, high-grade gliomas and many other types of cancer are still extremely resistant to current forms of therapy. Boron neutron capture therapy (BNCT) provides a promising way to destroy cancer cells without damaging healthy tissue. However, BNCT in practice is still limited due to the lack of boron-containing compounds that selectively deliver boron to cancer cells. Since many neuroendocrine tumors show an overexpression of the somatostatin receptor, it was our aim to synthesize compounds that contain a large number of boron atoms and still show high affinity toward this transmembrane receptor. The synthetic peptide Tyr (3)-octreotate (TATE) was chosen as a high-affinity and internalizing tumor targeting vector (TTV). Novel boron cluster compounds, containing 10 or 20 boron atoms, were coupled to the N-terminus of TATE. The obtained affinity data demonstrate that the use of a spacer between TATE and the closo-borane moiety is the option to avoid a loss of biological affinity of closo-borane conjugated TATE. For the first time, it was shown that closo-borane conjugated regulatory peptides retain high biological affinity and selectivity toward their transmembrane tumor...Continue Reading

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Citations

Mar 15, 2011·Journal of Medicinal Chemistry·Verena M AhrensEvamarie Hey-Hawkins
Dec 2, 2009·Expert Opinion on Drug Delivery·Gábor Mezo, Marilena Manea
Jul 23, 2013·Frontiers in Neuroendocrinology·Marily Theodoropoulou, Günter K Stalla
Aug 1, 2018·Expert Opinion on Biological Therapy·Tomasz M GoszczyńskiJanusz Boratyński
Oct 24, 2014·ChemMedChem·Verena M AhrensAnnette G Beck-Sickinger
Sep 1, 2018·Journal of Peptide Science : an Official Publication of the European Peptide Society·Dennis J WormAnnette G Beck-Sickinger
Aug 1, 2020·Frontiers in Chemistry·Paul HoppenzAnnette G Beck-Sickinger
Oct 27, 2018·Bioconjugate Chemistry·Krzysztof FinkTomasz M Goszczyński

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