منابع مشابه
Phosphodiesterase 4 isoenzyme inhibitory activity of 3-phenylxanthines and 4-pheny.
On the basis of our study on the structure-activity relationships of 1,3,7-alkylxanthines and condensed-purines on cAMP-phosphodiesterase 4 (PDE 4) isoenzyme inhibitor, we investigated the synthesis and the inhibitory activity of 3-phenylxanthine and 4-phenyl[i]condensed-purine derivatives. Xanthines and condensed-purines with the phenyl group exhibited potent and selective PDE 4 inhibitory act...
متن کاملPhosphodiesterase 4-targeted treatments for autoimmune diseases
Advancements in phosphodiesterase (PDE)-targeted therapies have shown promise in recent years for treating patients with a variety of autoimmune diseases. This review summarizes the development of PDE4 inhibitors and the associated literature with a focus on treatments for autoimmune diseases. After the initial investigations of the prototypic PDE inhibitor, rolipram, more selective inhibitors ...
متن کاملPhosphodiesterase-4 inhibition and brain tumor growth.
To the Editor: We read with great interest the December 1, 2008, article by Goldhoff et al. (1) on the role of cyclic AMP phosphodiesterase-4 (PDE4) in brain tumor growth. The authors found that PDE4 is expressed in human brain tumors of glial and neuronal lineage (glioblastoma, medulloblastoma, ependymoma, and meningioma). In addition, overexpression of PDE4A1, a brain-specific isoform of PDE4...
متن کاملRoflumilast, a phosphodiesterase-4 inhibitor, induces phagocytic activity in Greek COPD patients
BACKGROUND A new approach to the treatment of COPD includes controlling inflammation because of its important role in exacerbation of the disease. Recently, roflumilast has been added as a therapeutic option for COPD. Roflumilast is an oral phosphodiesterase-4 inhibitor that targets inflammatory cells involved in triggering exacerbations of COPD. The objective of the current study was to evalua...
متن کاملAnalysis of a mutation in phosphodiesterase type 4 that alters both inhibitor activity and nucleotide selectivity.
Cyclic nucleotide phosphodiesterase type 4 (PDE4) is a cAMP-specific phosphodiesterase that is found as four distinct genes in the mammalian genome (PDE4A, 4B, 4C, and 4D). Mutation analysis was done to identify the amino acids involved in activity and inhibitor selectivity. Mutations at Asp333 were made in HSPDE4D3 based on mutations that affect rolipram sensitivity in RNPDE4B1. The PDE4D3 Asp...
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ژورنال
عنوان ژورنال: Journal of the American College of Cardiology
سال: 2012
ISSN: 0735-1097
DOI: 10.1016/j.jacc.2012.03.027