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

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

Automated summary

Kirsten rat sarcoma viral oncogene homolog (KRAS)-phosphodiesterase-delta (PDEd) is a promising target for antitumor drug discovery. Highly efficient and environmentally sensitive fluorescent probes of PDEd (DS-Probes) were designed and showed higher binding affinity and selectivity. These probes can conveniently and efficiently label PDEd in live cells and tumor tissues, facilitating PDEd-based mechanism elucidation, drug discovery, and pathologic diagnosis.