Suzuki et al., "Structural basis for the activity of drugs that inhibit phosphodiesterases
, " Structure, vol.
This study also indicated Pd(II) compounds as far more superior inhibitors of urease and phosphodiesterase-I than parent ligands; many of them exhibited inhibitions equivalent or even >the standard inhibitors (thiourea, urease; EDTA, phosphodiesterase
), which shows their potential use in future in the control of peptic ulcer and arthritis, respectively.
Vascular cyclic nucleotide phosphodiesterases
(PDE1, PDE3, PDE4 and PDE5) were purified from smooth muscle of bovine aorta (Lugnier et al., 1986).
4 (PDE4) inhibitors negatively modulate many inflammatory responses, and some of these pharmacological effects are mediated by inhibition of PDE4B in inflammatory cells.
Goettingen, Germany, October 02, 2014 --(PR.com)-- In a paper published in 2009, researchers led by Paul Marker at UW-Madison, identified Phosphodiesterase
4D (PDE4D) as a novel proliferation-promoting factor in prostate cancer.
(PDE) superfamily participates in the only cellular pathways for degradation of the ubiquitous intracellular second messengers.
type-5 (PDE-5) inhibitors are approved as the first line of therapy for the treatment of erectile dysfunction.
(PDEs), especially PDE4, may also modulate fibroblast-mediated tissue remodeling by increasing intracellular cAMP levels.
However, this new insight into the phosphodiesterases
might prove an interesting avenue to pursue."
of Glasgow, UK) present the first major compendium on the science of cyclic nucleotide phosphodiesterases
(PDEs) and their therapeutic and biomedical applications in some 15 years, a period during which new mammalian PDE families have been discovered and characterized and PDE-selective inhibitors have been successively marketed (including Viagra, Levitra, and Cialis).
IBMX, theophylline, and papaverine are not selective for any of the cyclic nucleotide phosphodiesterase
isozymes (Thompson, 1993); they inhibit phosphodiesterases
that hydrolyze cGMP as well as those that hydrolyze cAMP.
According to the company, MN-001 (tipelukast) is a novel, orally bioavailable small molecule compound thought to exert its effects through several mechanisms to produce its anti-inflammatory and anti-fibrotic activity in preclinical models, including leukotriene (LT) receptor antagonism, inhibition of phosphodiesterases
(PDE) and inhibition of 5-lipoxygenase (5-LO).