A non-internalizing alpha(v)beta(3) integrin ligand was conjugated to the anticancer drug MMAE through a beta-glucuronidase-responsive linker. In the presence of beta-glucuronidase, only the conjugate bearing a PEG(4) spacer inhibited the proliferation of integrinexpressing cancer cells at low nanomolar concentrations, indicating important structural requirements for the efficacy of these therapeutics.
beta-Glucuronidase triggers extracellular MMAE release from an integrin-targeted conjugate
Arosio Daniela;
2019
Abstract
A non-internalizing alpha(v)beta(3) integrin ligand was conjugated to the anticancer drug MMAE through a beta-glucuronidase-responsive linker. In the presence of beta-glucuronidase, only the conjugate bearing a PEG(4) spacer inhibited the proliferation of integrinexpressing cancer cells at low nanomolar concentrations, indicating important structural requirements for the efficacy of these therapeutics.File in questo prodotto:
Non ci sono file associati a questo prodotto.
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
