Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 61, Issue 13, Pages 5467-5483Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.jmedchem.7b01370
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Funding
- National Key R&D Program of China [2017YFB0202600]
- Natural Science Foundation of China [21402243, 21572279, 81522041, 81373258, 81602968]
- Science Foundation of Guangdong Province [2014A020210009, 2016A030310144]
- Guangdong Province Higher Vocational Colleges & Schools Pearl River Scholar Funded Scheme
- Foundation of Traditional Chinese Medicine, Bureau of Guangdong Province [20171049]
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Alzheimer's disease (AD) is one of the greatest public health challenges. Phosphodiesterases (PDEs) are a superenzyme family responsible for the hydrolysis of two second messengers: cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). Since several PDE subfamilies are highly expressed in the human brain, the inhibition of PDEs is involved in neurodegenerative processes by regulating the concentration of cAMP and/or cGMP. Currently, PDEs are considered as promising targets for the treatment of AD since many PDE inhibitors have exhibited remarkable cognitive improvement effects in preclinical studies and over 15 of them have been subjected to clinical trials. The aim of this review is to summarize the outstanding progress that has been made by PDE inhibitors as anti-AD agents with encouraging results in preclinical studies and clinical trials. The binding affinity, pharmacokinetics, underlying mechanisms, and limitations of these PDE inhibitors in the treatment of AD are also reviewed and discussed.
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