Related Experiment Video
Updated: Jan 25, 2026

Author Spotlight: Exploring the Mechanisms of MicroRNA Loading into Extracellular Vesicles in Cancer Progression
Published on: October 6, 2023
β-Glucuronidase triggers extracellular MMAE release from an integrin-targeted conjugate
Paula López Rivas1, Christoph Müller, Christian Breunig
1Università degli Studi di Milano, Dipartimento di Chimica, Via C. Golgi, 19 I-20133, Milan, Italy. cesare.gennari@unimi.it.
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.
Related Concept Videos
Integrins
Some ECM proteins assemble into a basement membrane to which the remaining components adhere. Proteoglycans typically form the bulk of the ECM while fibrous proteins, like collagen,...
Conjugate Addition to α,β-Unsaturated Carbonyl Compounds
Activation of Integrins
In "outside-in signaling," external factors in the extracellular space bind to exposed ligand binding sites on integrins. This causes the inactive protein to undergo a conformational change to become active. Integrins are often clustered on the cell membrane. Repetitive and regularly spaced ligand binding...
Conjugated Proteins
Nucleoproteins are protein complexes that contain nucleic acids, categorized as deoxyribonucleoproteins (DNPs) or ribonucleoproteins (RNPs) respectively. The nucleosome is a typical example of a DNP where nuclear DNA is associated with histone proteins. The major antigen for the Covid-19 virus SARS-CoV is an RNP that is critical...
Conjugated Proteins
The Extracellular Matrix

