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.
Titolo: | β-Glucuronidase triggers extracellular MMAE release from an integrin-targeted conjugate |
Autori: | LOPEZ RIVAS, PAULA (Primo) DAL CORSO, ALBERTO (Penultimo) GENNARI, CESARE MARIO ARTURO (Ultimo) (Corresponding) |
Settore Scientifico Disciplinare: | Settore CHIM/06 - Chimica Organica |
Progetto: | Peptide-Drug Conjugates for Targeted Delivery in Tumor Therapy Tumor-targeting peptidomimetics: synthesis and bio-medical applications |
Data di pubblicazione: | 25-apr-2019 |
Rivista: | |
Tipologia: | Article (author) |
Data ahead of print / Data di stampa: | 25-apr-2019 |
Digital Object Identifier (DOI): | http://dx.doi.org/10.1039/c9ob00617f |
Appare nelle tipologie: | 01 - Articolo su periodico |
File in questo prodotto:
File | Descrizione | Tipologia | Licenza | |
---|---|---|---|---|
Accepted manuscript_DETEMPLATED.pdf | Articolo principale | Post-print, accepted manuscript ecc. (versione accettata dall'editore) | Open Access Visualizza/Apri | |
Org. Biomol. Chem., 2019, 17, 4705–4710.pdf | Publisher's version/PDF | Administrator Richiedi una copia |