NeoMProbe: a new class of fluorescent cellular and tissue membrane probe.

The development of long-lasting plasma membrane (PM) and basement membrane (BM) probes is in high demand to advance our understanding of membrane dynamics during differentiation and disease conditions. Herein, we report that the microheterogeneity of heparan sulfate (HS) on fluorescent neo-proteoglycans backbone offers a facile platform for designing membrane probes. Confocal live-cell imaging studies of cancer and normal cell lines with a panel of Cy5 fluorescently tagged neo-proteoglycans confirmed that highly sulfated HS ligands with an l-iduronic acid component (PG@ID-6) induce a prolonged and brighter expression on the PM compared to low-sulfated and uronic acid counterparts.

Rational designing of glyco-nanovehicles to target cellular heterogeneity.

The aberrant expression of endocytic epidermal growth factor receptors (EGFRs) in cancer cells has emerged as a key target for therapeutic intervention. Here, we describe for the first time a state-of-the-art design for a heparan sulfate (HS) oligosaccharide-based nanovehicle to target EGFR-overexpressed cancer cells in cellular heterogeneity. An ELISA plate IC inhibition assay and surface plasma resonance (SPR) binding assay of structurally well-defined HS oligosaccharides showed that 6--sulfation (6--S) and 6--phosphorylation (6--P) of HS tetrasaccharides significantly enhanced EGFR cognate growth factor binding.