Folate stimulation is known to enhance Dictyostelium discoideum differentiation. During early differentiation, D. discoideum cells possess two classes of folate receptors which can be distinguished by their difference in specificity (R. J. W. de Wit, FEBS Lett. 150, 445-448, 1982). We investigated the type of receptor by which folate affects cell differentiation. Two independently regulated dev...

Adenosine 3',5'-cyclic monophosphate (cAMP) phosphodiesterase inhibition testing provides a useful means for the screening of biologically active compounds contained in medicinal plants. We have identified cAMP phosphodiesterase inhibitors contained in various medicinal plants.2a-k) The present paper deals with the identification of cAMP phosphodiesterase inhibitors contained in the flowers and...

The phosphodiesterase inhibitor tetrahydrophthalazinone NPD-008 was explored by phenotypic in vitro screening, target validation, and ultrastructural approaches against Trypanosoma cruzi . displayed activity different forms strains of T. (50% effective concentration [EC 50 ], 6.6 to 39.5 μM). Increased cAMP levels its combination with benznidazole gave synergistic interaction.

The binding of [3H]cGMP (guanosine 3',5'-monophosphate) to purified bovine adrenal cGMP-stimulated phosphodiesterase was measured by Millipore filtration on cellulose ester filter. [3H]cGMP-binding activity was enhanced when the assay was terminated in buffer containing 70% of saturated ammonium sulfate to dilute the enzyme and wash the filters. The cGMP-binding activity was co-purified with th...

Purification of cyclic 3’,5’-nucleotide phosphodiesterase of bovine brain cerebrum resulted in partial loss of activity, due to dissociation of an activator (or cofactor) from the enzyme. A systematic study showed that as purification proceeded, the activator was removed from phosphodiesterase in a stepwise fashion. Fractions representing phosphodiesterase at different stages of purification co...

Neonates cannot concentrate their urine to the same degree as adults. One of the key factors in concentrating the urine is the renal collecting duct osmotic water permeability (Pf) response to antidiuretic hormone (ADH). Neonatal cortical collecting ducts have a blunted Pf response to ADH compared with adult tubules (Pf: 119.0 +/- 12.5 vs. 260.1 +/- 29.5 microm/s, P < 0.05). We found that the p...

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 ...

in this paper a general discussion of the available data on the role of prostaglandin (pg) and phosphodiesterase is discussed. functional studies would be a next step to understand the functional meaning of the data described in this paper. the data presented are a basis for further research on selective modulation of the ep1 and ep2 receptor which could be a therapeutic target in functional bl...

The exo-enzyme autotaxin/NPP2 (ATX/NPP2) is a potent stimulator of cell migration, invasion, metastasis, and angiogenesis. Recently, ATX/NPP2 was found to possess lysophospholipase D (lyso-LPD) activity, generating the bioactive mediator lysophosphatidic acid from precursors. In the present study, we used site-directed mutagenesis to delineate the active domain of lysophospholipid catalytic act...

Daily variations in cGMP, guanylate cyclase and phosphodiesterase activity in golden hamster retina were studied. Cyclic GMP content exhibited significant variations throughout the 24-hr cycle with maximal values during the dark phase. In order to establish the relative participation of nucleotide synthesis and breakdown during a 24-hr cycle, guanylate cyclase and phosphodiesterase activity wer...