Phosphodiesterase-5 (PDE5) specifically hydrolyzes cGMP, thereby contributing to modulation of intracellular levels of this nucleotide. In the present study, preincubation with cGMP increased PDE5 catalytic activity for cGMP degradation, and it converted the PDE5 catalytic site to a form that was more potently inhibited by each of the three PDE5 catalytic site-specific inhibitors: sildenafil, v...

In thick ascending limbs (THALs), nitric oxide (NO) decreases NaCl reabsorption via cGMP-mediated inhibition of Na-K-2Cl cotransporter (NKCC2). In angiotensin (ANG II)-induced hypertension, endothelin-1 (ET-1)-induced NO production by THALs is impaired. However, whether this alters NO's natriuretic effects and the mechanisms involved are unknown. In other cell types, ANG II augments phosphodies...

INTRODUCTION Medulloblastoma (MB) is the most common malignant paediatric brain tumour. Recurrence and progression of disease occurs in 15-20% of standard risk and 30-40% of high risk patients. We analysed whether circumvention of chemoresistance pathways (drug export, DNA repair and apoptotic inhibition) can restore chemotherapeutic efficacy in a panel of MB cell lines. RESULTS We demonstrat...

The title coordination polymer, {[Nd(2)(C(4)H(2)O(4))(3)(H(2)O)(4)]·3H(2)O}, was synthesized by the reaction of neodymium(III) nitrate hexa-hydrate with fumaric acid in a water-methanol (7:3) solution. The asymmetric unit comprises two Nd(3+) cations, three fumarate dianions (L(2-)), four aqua ligands and three uncoordinated water mol-ecules. The carboxyl-ate groups of the fumarate dianions exh...

The title dinuclear copper complex, [Cu(2)Cl(4)(C(28)H(32)N(6))]·3H(2)O, is located on a crystallographic inversion center. The unique Cu(II) ion is coordinated in a slightly distorted square-pyramidal environment in which the N atoms of the dipicolyl-amine group and a chloride ligand form the basal plane. The apical position is occupied by a second chloride atom. While the Cu-N distances of th...

In the crystal structure of the title compound, {[Eu(C(8)H(3)O(7)S)(H(2)O)(5)]·0.5C(10)H(8)N(2)O(2)·3H(2)O}(n), the Eu(III) coordination polymer displays a ribbon motif as the 5-sulfoisopthalate anion uses one of carboxyl -CO(2) units to chelate to a Eu atom and the other to bind to other two Eu atoms; the sulfonyl -SO(3) unit is not involved in coordination. Adjacent ribbons are linked by O-H⋯...

Phosphodiesterase type 5 (PDE5) inhibitors are arguably the gold standard for treatment of erectile dysfunction in men. While all three PDE5 inhibitors approved for use in the U.S. are effective in treating ED, they possess different characteristics. Tadalafil differs from both sildenafil and vardenafil in its long half-life, which makes it ideal for daily dosing. This regimen has been shown to...

In the title compound, [Mo(2)(C(2)O(4))O(4)(C(6)H(6)N(4))(H(2)O)(2)]·3H(2)O, the coordination polyhedra for both Mo(V) atoms consist of two bridging O atoms, two atoms of the chelating ligand (oxalate or diimidazole), a terminal O atom and one H(2)O mol-ecule. The two distorted octa-hedrally coordinated Mo(V) atoms are linked together via O-O edge-sharing and Mo-Mo inter-actions with a Mo-Mo bo...