The Construction and Application of a New Screening Method for Phosphodiesterase Inhibitors
Chunhua Gao, Zhe Wang, Xiaojing Liu, Rongzhen Sun, Shengyao Ma, Zongchen Ma, Qi Wang, Guoqiang Li, Han-Ting Zhang
TL;DR
This paper introduces a new, cost-effective method for screening PDE inhibitors using GloSensor technology, enabling efficient drug discovery for diseases targeting PDE enzymes.
Contribution
A novel, low-cost screening method for PDE inhibitors using GloSensor technology is developed and applied for high-throughput drug discovery.
Findings
The new method successfully identified novel compounds with PDE inhibitory activity.
The method allows dynamic detection of substrate concentration changes in live cells.
It can preliminarily determine the PDE type affected by active compounds.
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…
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Taxonomy
TopicsPhosphodiesterase function and regulation · Receptor Mechanisms and Signaling · Cholinesterase and Neurodegenerative Diseases