Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates.

Anselmi M, Borbély AN, Figueras Agustí E, Michalek C, Kemker I, Gentilucci L, Sewald N (2021)
Chemistry - A European Journal 27(3): 1015-1022.

Zeitschriftenaufsatz | Veröffentlicht | Englisch
 
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Abstract / Bemerkung
Most anticancer agents are hydrophobic and can easily penetrate the tumor cell membrane by passive diffusion. This may impede the development of highly effective and tumor-selective treatment options. A hydrophilic beta-glucuronidase-cleavable linker was used to connect the highly potent antimitotic agent cryptophycin-55 glycinate with the alphavbeta3 integrin ligand c(RGDfK). Incorporation of the self-immolative linker containing glucuronic acid results in decreased cytotoxicity compared to the free payload, suggesting that hydrophilic sugar linkers can preclude passive cellular uptake. In vitro drug-release studies and cytotoxicity assays demonstrated the potential of this small molecule-drug conjugate, providing guidance for the development of therapeutics containing hydrophobic anticancer drugs. © 2020 Wiley-VCH GmbH.
Erscheinungsjahr
2021
Zeitschriftentitel
Chemistry - A European Journal
Band
27
Ausgabe
3
Seite(n)
1015-1022
eISSN
1521-3765
Finanzierungs-Informationen
Open-Access-Publikationskosten wurden durch die Universität Bielefeld im Rahmen des DEAL-Vertrags gefördert.
Page URI
https://pub.uni-bielefeld.de/record/2946327

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Anselmi M, Borbély AN, Figueras Agustí E, et al. Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal . 2021;27(3):1015-1022.
Anselmi, M., Borbély, A. N., Figueras Agustí, E., Michalek, C., Kemker, I., Gentilucci, L., & Sewald, N. (2021). Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal , 27(3), 1015-1022. doi:10.1002/chem.202003471
Anselmi, M., Borbély, A. N., Figueras Agustí, E., Michalek, C., Kemker, I., Gentilucci, L., and Sewald, N. (2021). Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal 27, 1015-1022.
Anselmi, M., et al., 2021. Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal , 27(3), p 1015-1022.
M. Anselmi, et al., “Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates.”, Chemistry - A European Journal , vol. 27, 2021, pp. 1015-1022.
Anselmi, M., Borbély, A.N., Figueras Agustí, E., Michalek, C., Kemker, I., Gentilucci, L., Sewald, N.: Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal . 27, 1015-1022 (2021).
Anselmi, Michele, Borbély, Adina Noémi, Figueras Agustí, Eduard, Michalek, Carmela, Kemker, Isabell, Gentilucci, Luca, and Sewald, Norbert. “Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates.”. Chemistry - A European Journal 27.3 (2021): 1015-1022.
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2021-02-05T12:19:35Z
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