β-Galactosidase fluorescence probe with improved cellular accumulation based on a spirocyclized rhodol scaffold

M Kamiya, D Asanuma, E Kuranaga… - Journal of the …, 2011 - ACS Publications
M Kamiya, D Asanuma, E Kuranaga, A Takeishi, M Sakabe, M Miura, T Nagano, Y Urano
Journal of the American Chemical Society, 2011ACS Publications
We identified a rhodol bearing a hydroxymethyl group (HMDER) as a suitable scaffold for
designing fluorescence probes for various hydrolases. HMDER shows strong fluorescence
at physiological pH, but phenolic O-alkylation of HMDER results in a strong preference for
the spirocyclic form, which has weak fluorescence. As a proof of concept, we utilized this
finding to develop a new fluorescence probe for β-galactosidase. This probe has favorable
characteristics for imaging in biological samples: it has good cellular permeability, and its …
We identified a rhodol bearing a hydroxymethyl group (HMDER) as a suitable scaffold for designing fluorescence probes for various hydrolases. HMDER shows strong fluorescence at physiological pH, but phenolic O-alkylation of HMDER results in a strong preference for the spirocyclic form, which has weak fluorescence. As a proof of concept, we utilized this finding to develop a new fluorescence probe for β-galactosidase. This probe has favorable characteristics for imaging in biological samples: it has good cellular permeability, and its hydrolysis product is well-retained intracellularly. It could rapidly and clearly visualize β-galactosidase activity in cultured cells and in Drosophila melanogaster tissue, which has rarely been achieved with previously reported fluorescence probes.
ACS Publications