Biochemical and Biophysical Research Communications
Regular ArticleMolecular Cloning and Characterization of Human PDE8B, a Novel Thyroid-Specific Isozyme of 3′,5′-Cyclic Nucleotide Phosphodiesterase☆,☆☆
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The synthesis and biological evaluation of nucleobases/tetrazole hybrid compounds: A new class of phosphodiesterase type 3 (PDE3) inhibitors
2020, Bioorganic and Medicinal ChemistryCitation Excerpt :The most important interactions between the synthesized compounds and the PDE3A are the purine-2NH interaction with Asp26, carbonyl ‘O’ of purine ring with His58 and tetrazole-H with Gln190. Moreover, purine-7NH interacts with His29 and purine-2NH interacts with Asp139. There are a few greasy amino acids, like Ile157, Pro143, Phe193, Phe161, Phe178, Leu189 and Trp153 at the binding site, so this can provide an opportunity for hydrophobic interactions with synthesized compounds.
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2020, Molecular and Cellular EndocrinologyCitation Excerpt :The rise of intracellular Ca2+ levels activates calmodulin, which initiates the transport and membrane fusion of GH storage vesicles (Anderson and Scanes, 2012; Frohman et al., 1999). One of the ways PKA's activation is terminated is by PDEs decreasing endogenous cAMP levels; the pituitary expresses PDE isoforms PDE2, PDE4, PDE8B, and PDE11A, of which PDE4 and PDE8B are cAMP-selective, whereas PDE2 and PDE11A hydrolyze both cAMP and cGMP (Peverelli et al., 2009a; Persani et al., 2001; Loughney et al., 2005; Hayashi et al., 1998). Intracellular cAMP levels are also lowered by the MRP family of cyclic nucleotide transporters.
Phosphodiesterase inhibitors say NO to Alzheimer's disease
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2019, Pharmacology and TherapeuticsCitation Excerpt :As another cAMP-specific hydrolyzing PDE, PDE8, consisting of PDE8A and PDE8B, exhibits a higher-affinity and lower Km (≈0.04 - 0.15 μM) for cAMP compared to other PDE isoforms, thus acting as a potential drug target to shape low-level intracellular cAMP signals (Fisher, Smith, Pillar, St Denis, & Cheng, 1998; Hayashi et al., 1998; Soderling, Bayuga, & Beavo, 1998; Vang et al., 2010; Yan, Wang, Cai, & Ke, 2009). PDE8A is highly expressed in the testis, liver and heart (Fisher et al., 1998; Soderling et al., 1998), whereas PDE8B is richly found in the thyroid and brain (Hayashi et al., 1998). In the lung, both PDE8 isoforms have been detected, albeit the relevant expression levels are low.
Distribution and function of 3',5'-Cyclic-AMP phosphodiesterases in the human ovary
2015, Molecular and Cellular Endocrinology
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The nucleotide and deduced amino acid sequences reported in this paper have been deposited with the GenBank/EMBL Data Bank under Accession No. AF079529.
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Abbreviations used: PDE, 3′, 5′ cyclic nucleotide phosphodiesterase; cAMP, adenosine 3′, 5′-cyclic monophosphate; cGMP, guanosine 3′, 5′-cyclic monophosphate; EST, expressed sequence tag; PCR, polymerase chain reaction; RACE, rapid amplification of cDNA ends; nt, nucleotide; bp, base pair; kb, kilobase; DMSO, dimethyl sulfoxide; IBMX, 3-isobutyl-1-methylxanthine; IC50, 50% inhibitory concentration
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