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Cyclic nucleotide phosphodiesterases: New targets in the metabolic syndrome?
Pharmacology & Therapeutics ( IF 13.5 ) Pub Date : 2020-01-09 , DOI: 10.1016/j.pharmthera.2020.107475
Claire Lugnier 1 , Alain Meyer 1 , Samy Talha 1 , Bernard Geny 1
Affiliation  

Metabolic diseases have a tremendous impact on human morbidity and mortality. Numerous targets regulating adenosine monophosphate kinase (AMPK) have been identified for treating the metabolic syndrome (MetS), and many compounds are being used or developed to increase AMPK activity. In parallel, the cyclic nucleotide phosphodiesterase families (PDEs) have emerged as new therapeutic targets in cardiovascular diseases, as well as in non-resolved pathologies. Since some PDE subfamilies inactivate cAMP into 5'-AMP, while the beneficial effects in MetS are related to 5'-AMP-dependent activation of AMPK, an analysis of the various controversial relationships between PDEs and AMPK in MetS appears interesting. The present review will describe the various PDE families, AMPK and molecular mechanisms in the MetS and discuss the PDEs/PDE modulators related to the tissues involved, thus supporting the discovery of original molecules and the design of new therapeutic approaches in MetS.

中文翻译:

环核苷酸磷酸二酯酶:代谢综合征的新目标?

代谢性疾病对人类的发病率和死亡率具有巨大影响。已经确定了许多调节单磷酸腺苷激酶(AMPK)的靶标用于治疗代谢综合征(MetS),并且正在使用或开发许多化合物来增加AMPK活性。同时,环状核苷酸磷酸二酯酶家族(PDE)已成为心血管疾病以及未解决的病理学中的新治疗靶标。由于一些PDE亚家族将cAMP灭活为5'-AMP,而MetS中的有益作用与AMPK的5'-AMP依赖性激活有关,因此对MetS中PDE和AMPK之间各种有争议关系的分析似乎很有趣。本评论将描述各种PDE系列,
更新日期:2020-01-09
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