Folate receptor (FR) levels are overexpressed on cells associated with numerous diseases including cancers (e.g. ovarian, lung) and inflammatory conditions (e.g. atherosclerosis, arthritis). Folic acid binds with its cognate FR with high affinity and thus serves as a useful targeting moiety for both diagnosis and treatment of diseases. This report describes the synthesis and evaluation of a pH sensitive folate conjugate that increases in fluorescence upon endocytosis, which facilitates its use for fluorescence imaging and fluorescence based analytical detection systems. As evidenced during fluorescence microscopy, the folate based probe was readily taken up via endocytosis by FR+ L1210 leukemia cells. Uptake in controls was readily blocked by excess folic acid indicating folate specific targeting. Given that small-molecule targeted imaging agents constitute a new type of diagnostic strategy, this probe, with its pH sensitive nature, may prove useful in both in vivo and in vitro diagnostic applications.

Synthesis and evaluation of pH sensitive folate targeted probes

246th National Meeting (2013)

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