Molecular View on the iRGD Peptide Binding Mechanism: Implications for Integrin Activity and Selectivity Profiles
Vincenzo Maria D’Amore,
Greta Donati,
Elena Lenci
et al.
Abstract:Receptor-selective peptides are widely used as smart
carriers for
specific tumor-targeted delivery. A remarkable example is the cyclic
nonapeptide iRGD (CRGDKPGDC, 1) that
couples intrinsic cytotoxic effects with striking tumor-homing properties.
These peculiar features are based on a rather complex multistep mechanism
of action, where the primary event is the recognition of RGD integrins.
Despite the high number of preclinical studies and the recent success
of a phase I trial for the treatment of pancreatic d… Show more
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