Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates.
Borbély AN, Thoreau F, Figueras Agustí E, Kadri M, Coll J-L, Boturyn D, Sewald N (2020)
Chemistry - A European Journal 26(12): 2602-2605.
Zeitschriftenaufsatz
| Veröffentlicht | Englisch
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Autor*in
Borbély, Adina NoémiUniBi;
Thoreau, Fabien;
Figueras Agustí, EduardUniBi;
Kadri, Malika;
Coll, Jean-Luc;
Boturyn, Didier;
Sewald, NorbertUniBi 
Einrichtung
Abstract / Bemerkung
The effective delivery of cytotoxic agents to the tumor cells is a key challenge in anticancer therapy. Multivalent integrinspecific ligands are considered a promising tool to increase the binding affinity, selectivity, and internalization efficiency of small molecule-drug conjugates. Here we report the synthesis and biological evaluation of a multimeric conjugate containing the high-affinity integrin alpha v beta 3 binding ligand RAFT- c (RGDfK) 4 , a lysosomally cleavable Val-Cit linker and cryptophycin-55 glycinate, a potent inhibitor of tubulin polymerization. In vitro cytotoxicity assays verified that the multimeric RGD-cryptophycin conjugate displays improved potency compared to the monomeric analogue in integrin alpha v beta 3 overexpressing tumor cell lines, while significantly reduced activity was observed in the integrin-negative cell line. © 2020 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
Erscheinungsjahr
2020
Zeitschriftentitel
Chemistry - A European Journal
Band
26
Ausgabe
12
Seite(n)
2602-2605
Urheberrecht / Lizenzen
ISSN
0947-6539
eISSN
1521-3765
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Open-Access-Publikationskosten wurden durch die Universität Bielefeld im Rahmen des DEAL-Vertrags gefördert.
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https://pub.uni-bielefeld.de/record/2940382
Zitieren
Borbély AN, Thoreau F, Figueras Agustí E, et al. Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates. Chemistry - A European Journal. 2020;26(12):2602-2605.
Borbély, A. N., Thoreau, F., Figueras Agustí, E., Kadri, M., Coll, J. - L., Boturyn, D., & Sewald, N. (2020). Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates. Chemistry - A European Journal, 26(12), 2602-2605. https://doi.org/10.1002/chem.201905437
Borbély, Adina Noémi, Thoreau, Fabien, Figueras Agustí, Eduard, Kadri, Malika, Coll, Jean-Luc, Boturyn, Didier, and Sewald, Norbert. 2020. “Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates.”. Chemistry - A European Journal 26 (12): 2602-2605.
Borbély, A. N., Thoreau, F., Figueras Agustí, E., Kadri, M., Coll, J. - L., Boturyn, D., and Sewald, N. (2020). Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates. Chemistry - A European Journal 26, 2602-2605.
Borbély, A.N., et al., 2020. Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates. Chemistry - A European Journal, 26(12), p 2602-2605.
A.N. Borbély, et al., “Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates.”, Chemistry - A European Journal, vol. 26, 2020, pp. 2602-2605.
Borbély, A.N., Thoreau, F., Figueras Agustí, E., Kadri, M., Coll, J.-L., Boturyn, D., Sewald, N.: Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates. Chemistry - A European Journal. 26, 2602-2605 (2020).
Borbély, Adina Noémi, Thoreau, Fabien, Figueras Agustí, Eduard, Kadri, Malika, Coll, Jean-Luc, Boturyn, Didier, and Sewald, Norbert. “Synthesis and Biological Characterization of Monomeric and Tetrameric RGD-Cryptophycin Conjugates.”. Chemistry - A European Journal 26.12 (2020): 2602-2605.
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