Environmentally sensitive fluorescent probes with improved properties for detecting and imaging PDEδ in live cells and tumor slices

Kirsten rat sarcoma viral oncogene homolog (KRAS)–phosphodiesterase-delta (PDEδ) is a promising target for antitumor drug discovery. Herein, highly efficient and environmentally sensitive fluorescent probes of PDEδ (DS-Probes) were rationally designed. As compared with the reported PDEδ probes, DS-Probes showed higher binding affinity and selectivity, which were able to conveniently and efficiently label PDEδ in live cells as well as tumor tissues. Therefore, these fluorescent probes are expected to facilitate PDEδ-based mechanism elucidation, drug discovery and pathologic diagnosis.