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 (Accepted)
Chemistry - A European Journal .

Zeitschriftenaufsatz | Angenommen | 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
2020
Zeitschriftentitel
Chemistry - A European Journal
eISSN
1521-3765
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 . Accepted.
Anselmi, M., Borbély, A. N., Figueras Agustí, E., Michalek, C., Kemker, I., Gentilucci, L., & Sewald, N. (Accepted). Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal . doi:10.1002/chem.202003471
Anselmi, M., Borbély, A. N., Figueras Agustí, E., Michalek, C., Kemker, I., Gentilucci, L., and Sewald, N. (Accepted). Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal .
Anselmi, M., et al., Accepted. Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates. Chemistry - A European Journal .
M. Anselmi, et al., “Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates.”, Chemistry - A European Journal , Accepted.
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 . (Accepted).
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 (Accepted).

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