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Here we describe a compound, BC54, that is a selective inhibitor of enzymes from the cAMP-specific PDE4 and PDE7 families. Consistent with the biological effect of other PDE4 and PDE7 inhibitors, BC54 displays potent anti-inflammatory properties and is superior to a combination of rolipram (a PDE4 inhibitor) and BRL50481 (a PDE7A inhibitor) for inducing apoptosis in chronic lymphocytic leukemia (CLL) cells
Low PDE7A expression is associated with sepsis.
PDE7A is a high-speed and low-affinity phosphodiesterase for cCMP.
PDE7 has roles in regulating oligodendrocyte precursor survival and differentiation during brain development and in adulthood
PDE7 has the potential to regulate human T cell function including cytokine production, proliferation and expression of activation markers.
Ubiquitous expression of phosphodiesterase 7A in human proinflammatory and immune cells; PDE7A was expressed in neutrophils and alveolar macrophages
crystal structure of PDE7A1 catalytic domain complexed with the inhibitor 3-isobutyl-1-methylxanthine & kinetic analysis on mutant PDE7A1 and PDE4D2; results show several residues must work together to switch inhibitor selectivity between PDE4 & PDE7
results show that specific gene silencing with the RNAi method is a useful tool for inhibiting the gene expression of specific PDEs and that PDE7 silencing upregulates several osteogenic genes and increases mineralization
PDE7A is not essential for activation of T lymphocytes; its inactivation by targeted gene disruption appears to enhance in vivo humoral immune responses.
The roles PDE7A1 and its regulatory region play in cAMP signaling were examined by studying interactions with PKA subunits.
results demonstrate that PDE7A might regulate TNF-alpha production in keratinocytes in a cAMP-dependent fashion
PDE7A is involved in regulation of cell proliferation and cytokine production of NKT cells.
The protein encoded by this gene belongs to the cyclic nucleotide phosphodiesterase (PDE) family, and PDE7 subfamily. This PDE hydrolyzes the second messenger, cAMP, which is a regulator and mediator of a number of cellular responses to extracellular signals. Thus, by regulating the cellular concentration of cAMP, this protein plays a key role in many important physiological processes. Alternatively spliced transcript variants encoding different isoforms have been described for this gene.
, high affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A
, phosphodiesterase isozyme 7
, rolipram-insensitive phosphodiesterase type 7
, high-affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A
, phosphodiesterase 7A
, high affinity cAMP-specific 3',5'-cyclic phosphodiesterase 7A-like