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- Title
The Construction and Application of a New Screening Method for Phosphodiesterase Inhibitors.
- Authors
Gao, Chunhua; Wang, Zhe; Liu, Xiaojing; Sun, Rongzhen; Ma, Shengyao; Ma, Zongchen; Wang, Qi; Li, Guoqiang; Zhang, Han-Ting
- Abstract
Phosphodiesterases (PDEs), a superfamily of enzymes that hydrolyze cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), are recognized as a therapeutic target for various diseases. However, the current screening methods for PDE inhibitors usually experience problems due to complex operations and/or high costs, which are not conducive to drug development in respect of this target. In this study, a new method for screening PDE inhibitors based on GloSensor technology was successfully established and applied, resulting in the discovery of several novel compounds of different structural types with PDE inhibitory activity. Compared with traditional screening methods, this method is low-cost, capable of dynamically detecting changes in substrate concentration in live cells, and can be used to preliminarily determine the type of PDEs affected by the detected active compounds, making it more suitable for high-throughput screening for PDE inhibitors.
- Subjects
PHOSPHODIESTERASE inhibitors; CYCLIC adenylic acid; CYCLIC guanylic acid; HIGH throughput screening (Drug development); PHOSPHODIESTERASES; KINASE inhibitors
- Publication
Biosensors (2079-6374), 2024, Vol 14, Issue 5, p252
- ISSN
2079-6374
- Publication type
Article
- DOI
10.3390/bios14050252