Design and synthesis of novel annulated thienopyrimidines as phosphodiesterase 5 (PDE5) inhibitors
Sign Up to like & getrecommendations! Published in 2018 at "Archiv der Pharmazie"
DOI: 10.1002/ardp.201800018
Abstract: Novel cycloalkene‐fused thienopyrimidine analogues with enhanced phosphodiesterase 5 (PDE5) inhibitory properties are presented. The structure of the reported scaffold was modulated through variation of the terminal cycloalkene ring size, as well as by varying the… read more here.
Keywords: design synthesis; synthesis novel; phosphodiesterase; phosphodiesterase pde5 ... See more keywords
Characterization and role of a 2′,3′-cyclic phosphodiesterase from Deinococcus radiodurans
Sign Up to like & getrecommendations! Published in 2017 at "Biotechnology Letters"
DOI: 10.1007/s10529-017-2349-7
Abstract: ObjectivesA 2′,3′-cyclic phosphodiesterase gene (drCPDase) has been characterized from Deinococcus radiodurans and is involved in the robust resistance of this organism.ResultsCells lacking 2′,3′-cyclic phosphodiesterase gene (drCPDase) showed modest growth defects and displayed increased sensitivities to… read more here.
Keywords: deinococcus radiodurans; drcpdase; characterization role; cyclic phosphodiesterase ... See more keywords
Expression and localization of phosphodiesterase 2A in the submandibular gland of mice.
Sign Up to like & getrecommendations! Published in 2018 at "Archives of oral biology"
DOI: 10.1016/j.archoralbio.2018.03.009
Abstract: OBJECTIVES Phosphodiesterases comprise a superfamily of enzymes that hydrolyze and inactivate cyclic AMP (cAMP) and/or cyclic GMP (cGMP), thereby regulating cellular signaling mechanisms. We herein investigated the production of phosphodiesterase 2A (PDE2A) in the mouse… read more here.
Keywords: submandibular gland; phosphodiesterase; gland; expression localization ... See more keywords
TAK-915, a phosphodiesterase 2A inhibitor, ameliorates the cognitive impairment associated with aging in rodent models
Sign Up to like & getrecommendations! Published in 2019 at "Behavioural Brain Research"
DOI: 10.1016/j.bbr.2019.112192
Abstract: Changes in the cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) signaling are implicated in older people with dementia. Drugs that modulate the cAMP/cGMP levels in the brain might therefore provide new therapeutic options… read more here.
Keywords: associated aging; phosphodiesterase; cognitive impairment; tak 915 ... See more keywords
Heme inhibits the activity of a c-di-GMP phosphodiesterase in Vibrio cholerae.
Sign Up to like & getrecommendations! Published in 2020 at "Biochemical and biophysical research communications"
DOI: 10.1016/j.bbrc.2020.06.048
Abstract: Heme, a complex of iron and protoporphyrin IX, plays an essential role in numerous biological processes including oxygen transport, oxygen storage, and electron transfer. The role of heme as a prosthetic group in bacterial hemoprotein… read more here.
Keywords: heme; vibrio cholerae; activity; phosphodiesterase ... See more keywords
Discovery of trisubstituted pyrazolines as a novel scaffold for the development of selective phosphodiesterase 5 inhibitors.
Sign Up to like & getrecommendations! Published in 2020 at "Bioorganic chemistry"
DOI: 10.1016/j.bioorg.2020.104322
Abstract: Celecoxib, is a selective cyclooxygenase-2 (COX2) inhibitor with a 1,5-diaryl pyrazole scaffold. Celecoxib has a better safety profile compared to other COX2 inhibitors having side effects of systemic hypertension and thromboembolic complications. This may be… read more here.
Keywords: pyrazolines novel; pde5 inhibitors; pde5; discovery trisubstituted ... See more keywords
Light-Activated Cyclic Nucleotide Phosphodiesterases
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DOI: 10.1016/j.bpj.2016.11.950
Abstract: The second messengers 3′,5′-cyclic adenosine monophosphate (cAMP) and cyclic 3′,5′-cyclic guanosine monophosphate (cGMP) mediate various biological responses like apoptosis, smooth muscle relaxation and vision. Cyclic-nucleotide-dependent processes have been analyzed with spatiotemporal resolution through optogenetics. In… read more here.
Keywords: cyclic nucleotide; light activated; phosphodiesterase; activated cyclic ... See more keywords
Phosphodiesterase-2 inhibitor reverses post-traumatic stress induced fear memory deficits and behavioral changes via cAMP/cGMP pathway.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2020.173768
Abstract: Phosphodiesterase 2 is one of the phosphodiesterase (PDEs) family members that regulate cyclic nucleotide (namely cAMP and cGMP) concentrations. The present study determined whether PDE2 inhibition could rescue post-traumatic stress disorder (PTSD)-like symptoms. Mice were… read more here.
Keywords: bay 7550; inhibitor; fear memory; phosphodiesterase ... See more keywords
Potent immunosuppressive activity of a phosphodiesterase‐4 inhibitor N‐acylhydrazone in models of lipopolysaccharide‐induced shock and delayed‐type hypersensitivity reaction
Sign Up to like & getrecommendations! Published in 2018 at "International Immunopharmacology"
DOI: 10.1016/j.intimp.2018.09.047
Abstract: &NA; Immunosuppressive drugs are widely used for the treatment of immune‐mediated diseases and inflammation, but the toxicity and side effects of the available immunosuppressors make the search of new agents of great relevance. Here, we… read more here.
Keywords: lassbio; activity; phosphodiesterase; lassbio 1386 ... See more keywords
Structural Analysis of the Regulatory GAF Domains of cGMP Phosphodiesterase Elucidates the Allosteric Communication Pathway.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of molecular biology"
DOI: 10.1016/j.jmb.2020.08.026
Abstract: Regulation of photoreceptor phosphodiesterase (PDE6) activity is responsible for the speed, sensitivity, and recovery of the photoresponse during visual signaling in vertebrate photoreceptor cells. It is hypothesized that physiological differences in the light responsiveness of… read more here.
Keywords: phosphodiesterase; allosteric communication; gaf domains; cone ... See more keywords
Brain cholesterol metabolite 24‐hydroxycholesterol modulates inotropic responses to &bgr;‐adrenoceptor stimulation: The role of NO and phosphodiesterase
Sign Up to like & getrecommendations! Published in 2019 at "Life Sciences"
DOI: 10.1016/j.lfs.2019.01.054
Abstract: Aims: 24‐Hydroxycholesterol (24HC) is the main brain cholesterol metabolite, which level in the circulation is significantly changed under physiological and pathological conditions. Here, we have studied the effect of 24HC on the inotropic responses to… read more here.
Keywords: bgr; phosphodiesterase; responses bgr; adrenoceptor stimulation ... See more keywords