The folate receptor (FR) has emerged as an attractive target for both in vitro and in vivo imaging applications. Specifically, FR levels are elevated in numerous malignant tissues and diseases associated with inflammation (e.g. atherosclerosis, infection) and thus FA serves as a useful targeting moiety for the diagnosis and detection of these diseases. We describe the synthesis and assessment of a folate conjugate developed using the acid sensitive dye pHRhodo. The conjugate was readily taken up by FR+ L1210 leukemia cells as demonstrated via fluorescence microscopy. More importantly, uptake was blocked by excess folic acid and only observed during endocytosis. Given that the dye only fluoresces bright red in an acidic environment, this imaging agent should prove advantageous for assessing cells/tissues undergoing FR mediated endocytosis.

Synthesis and evaluation of a folate targeted, acid activated dye

245th National Meeting (2013)

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