Journal
CHEMICAL SCIENCE
Volume 8, Issue 5, Pages 3427-3433Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/c7sc00472a
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Funding
- CNRS
- La Ligue Nationale contre le Cancer (Comites Vienne and Deux-Sevres), Sport et Collection, Therapeutic Impact
- Agence Nationale de la Recherche (ARN) [Blanc-SIMI 7]
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The development of novel therapeutic strategies allowing the destruction of tumour cells while sparing healthy tissues is one of the main challenges of cancer chemotherapy. Here, we report on the design and antitumour activity of a low-molecular-weight drug delivery system programmed for the selective release of the potent monomethylauristatin E in the tumour microenvironment of solid tumours. After intravenous administration, this compound binds covalently to plasmatic albumin through Michael addition, thereby enabling its passive accumulation in tumours where extracellular beta-glucuronidase initiates the selective release of the drug. This targeting device produces outstanding therapeutic efficacy on orthotopic triple-negative mammary and pancreatic tumours in mice (50% and 33% of mice with the respective tumours cured), leading to impressive reduction or even disappearance of tumours without inducing side effects.
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