ArticleRSC advances2021
Discovery of catalytic-site-fluorescent probes for tracing phosphodiesterase 5 in living cells.
Article in RSC advances, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Authors and funding
9 authors at 1 institution in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
Small molecule fluorescent probes provide a powerful labelling technology to enhance our understanding of particular proteins. However, the discovery of a proper fluorescent probe for detecting PDE5 is still a challenge due to the highly conservative structure of the catalytic domain in the phosphodiesterase (PDE) families. Herein, we identified probes based on the key amino residues in the ligand binding pocket of PDE5 and catalytic-site-fluorescent probes PCO2001-PCO2003 were well designed and synthesized. Among them, PCO2003 exhibited extraordinary fluorescence properties and the ability to be applied to PDE5 visualization in live cells as well as in pulmonary tissue slices, demonstrating the location and expression level of PDE5 proteins. Overall, the environment-sensitive "turn-on" probe is economical, convenient and rapid for PDE5 imaging, implying that the catalytic-site-fluorescent probe will have a variety of future applications in pathological diagnosis as well as drug screening.
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Registered trials
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