A non-internalizing αvβ3 integrin ligand was conjugated to the anticancer drug MMAE through a β-glucuronidase-responsive linker. In the presence of β-glucuronidase, only the conjugate bearing a PEG4 spacer inhibited the proliferation of integrin-expressing cancer cells at low nanomolar concentrations, indicating important structural requirements for the efficacy of these therapeutics.
β-Glucuronidase triggers extracellular MMAE release from an integrin-targeted conjugate / P. López Rivas, C. Müller, C. Breunig, T. Hechler, A. Pahl, D. Arosio, L. Belvisi, L. Pignataro, A. Dal Corso, C. Gennari. - In: ORGANIC & BIOMOLECULAR CHEMISTRY. - ISSN 1477-0520. - 17:19(2019 Apr 25), pp. 4705-4710.
β-Glucuronidase triggers extracellular MMAE release from an integrin-targeted conjugate
P. López RivasPrimo
;L. Belvisi;L. Pignataro;A. Dal CorsoPenultimo
;C. Gennari
Ultimo
2019
Abstract
A non-internalizing αvβ3 integrin ligand was conjugated to the anticancer drug MMAE through a β-glucuronidase-responsive linker. In the presence of β-glucuronidase, only the conjugate bearing a PEG4 spacer inhibited the proliferation of integrin-expressing cancer cells at low nanomolar concentrations, indicating important structural requirements for the efficacy of these therapeutics.
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Org. Biomol. Chem., 2019, 17, 4705–4710.pdf
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