Abstract
This chapter describes crystal structures of phosphodiesterases (PDEs) that are involved in CNS diseases and their interactions with family selective inhibitors. The structural comparison identifies a small hydrophobic pocket next to the active site, which may be valuable for improvement of selectivity of PDE inhibitors.
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Abbreviations
- cAMP:
-
cyclic adenosine monophosphate
- cGMP:
-
cyclic guanosine monophosphate
- IBMX:
-
3-isobutyl-1-methylxanthine
- PDE:
-
phosphodiesterase
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Acknowledgment
We thank for supports of NIH GM59791 to HK and the National Natural Science Foundation of China (31271944, 31471626).
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The authors declare that they have no conflicts of interest.
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Wang, Y., Ke, H. (2017). A Unique Sub-Pocket for Improvement of Selectivity of Phosphodiesterase Inhibitors in CNS. In: Zhang, HT., Xu, Y., O'Donnell, J. (eds) Phosphodiesterases: CNS Functions and Diseases. Advances in Neurobiology, vol 17. Springer, Cham. https://doi.org/10.1007/978-3-319-58811-7_17
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DOI: https://doi.org/10.1007/978-3-319-58811-7_17
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