TY  - JOUR
AB  - 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.
DA  - 2021
DO  - 10.1002/chem.202003471
LA  - eng
IS  - 3
M2  - 1015
PY  - 2021
SP  - 1015-1022
T2  - Chemistry - A European Journal
TI  - Linker Hydrophilicity Modulates the Anticancer Activity of RGD-Cryptophycin Conjugates.
UR  - https://nbn-resolving.org/urn:nbn:de:0070-pub-29463279
Y2  - 2024-11-21T20:57:50
ER  -