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 Rivas
Primo
;
L. Belvisi;L. Pignataro;A. Dal Corso
Penultimo
;
C. Gennari
Ultimo
2019-04-25

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.
Settore CHIM/06 - Chimica Organica
Peptide-Drug Conjugates for Targeted Delivery in Tumor Therapy
Tumor-targeting peptidomimetics: synthesis and bio-medical applications
25-apr-2019
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Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/640803
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