Journal of Biological Chemistry, ISSN 0021-9258, 09/2005, Volume 280, Issue 35, pp. 30949 - 30955
Phosphodiesterase (PDE) inhibitors have been widely studied as therapeutics for treatment of human diseases. However, the mechanism by which each PDE family...
COMPLEX | MESSENGER-RNA | MECHANISM | AMP | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CATALYTIC DOMAIN | PDE7A | IDENTIFICATION | CAMP | LYMPHOCYTES | Protein Structure, Tertiary | 3',5'-Cyclic-AMP Phosphodiesterases - metabolism | Amino Acid Sequence | Cyclic Nucleotide Phosphodiesterases, Type 4 | Humans | Models, Molecular | Molecular Sequence Data | Crystallography, X-Ray | 3',5'-Cyclic-AMP Phosphodiesterases - genetics | Sequence Alignment | 3',5'-Cyclic-AMP Phosphodiesterases - chemistry | 1-Methyl-3-isobutylxanthine - chemistry | Phosphodiesterase Inhibitors - metabolism | 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors | Molecular Structure | Cyclic Nucleotide Phosphodiesterases, Type 7 | Phosphodiesterase Inhibitors - chemistry | 1-Methyl-3-isobutylxanthine - metabolism | Cyclic AMP - metabolism
COMPLEX | MESSENGER-RNA | MECHANISM | AMP | CRYSTAL-STRUCTURE | BIOCHEMISTRY & MOLECULAR BIOLOGY | CATALYTIC DOMAIN | PDE7A | IDENTIFICATION | CAMP | LYMPHOCYTES | Protein Structure, Tertiary | 3',5'-Cyclic-AMP Phosphodiesterases - metabolism | Amino Acid Sequence | Cyclic Nucleotide Phosphodiesterases, Type 4 | Humans | Models, Molecular | Molecular Sequence Data | Crystallography, X-Ray | 3',5'-Cyclic-AMP Phosphodiesterases - genetics | Sequence Alignment | 3',5'-Cyclic-AMP Phosphodiesterases - chemistry | 1-Methyl-3-isobutylxanthine - chemistry | Phosphodiesterase Inhibitors - metabolism | 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors | Molecular Structure | Cyclic Nucleotide Phosphodiesterases, Type 7 | Phosphodiesterase Inhibitors - chemistry | 1-Methyl-3-isobutylxanthine - metabolism | Cyclic AMP - metabolism
Journal Article
Analytical Biochemistry, ISSN 0003-2697, 2011, Volume 409, Issue 1, pp. 144 - 149
The classical malachite green (MLG) assay of phosphate, which added MLG after molybdate to the acidified reaction solutions of phosphate, tolerated...
Aggregates | Papaverine | Phosphate | Interference | Malachite green | Cyclic nucleotide phosphodiesterase | CHEMISTRY, ANALYTICAL | PROTEIN | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES | COLORIMETRIC ASSAY | BIOCHEMISTRY & MOLECULAR BIOLOGY | BIOCHEMICAL RESEARCH METHODS | INORGANIC-PHOSPHATE | INHIBITION | DRUG DEVELOPMENT | TARGETS | AGENTS | SCATTERING | Amines - chemistry | Molybdenum - chemistry | Rabbits | Rosaniline Dyes - chemistry | Humans | Phosphates - chemistry | Phosphoric Acids - chemistry | Phosphodiesterase Inhibitors - pharmacology | Papaverine - pharmacology | Cyclic Nucleotide Phosphodiesterases, Type 4 - genetics | Recombinant Fusion Proteins - metabolism | Brain - metabolism | Recombinant Fusion Proteins - antagonists & inhibitors | Animals | Spectrophotometry, Ultraviolet - methods | Hydrophobic and Hydrophilic Interactions | Recombinant Fusion Proteins - genetics | Papaverine - chemistry | Phosphodiesterase Inhibitors - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Phosphates | Phosphatases | Isoenzymes | Rain and rainfall
Aggregates | Papaverine | Phosphate | Interference | Malachite green | Cyclic nucleotide phosphodiesterase | CHEMISTRY, ANALYTICAL | PROTEIN | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES | COLORIMETRIC ASSAY | BIOCHEMISTRY & MOLECULAR BIOLOGY | BIOCHEMICAL RESEARCH METHODS | INORGANIC-PHOSPHATE | INHIBITION | DRUG DEVELOPMENT | TARGETS | AGENTS | SCATTERING | Amines - chemistry | Molybdenum - chemistry | Rabbits | Rosaniline Dyes - chemistry | Humans | Phosphates - chemistry | Phosphoric Acids - chemistry | Phosphodiesterase Inhibitors - pharmacology | Papaverine - pharmacology | Cyclic Nucleotide Phosphodiesterases, Type 4 - genetics | Recombinant Fusion Proteins - metabolism | Brain - metabolism | Recombinant Fusion Proteins - antagonists & inhibitors | Animals | Spectrophotometry, Ultraviolet - methods | Hydrophobic and Hydrophilic Interactions | Recombinant Fusion Proteins - genetics | Papaverine - chemistry | Phosphodiesterase Inhibitors - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Phosphates | Phosphatases | Isoenzymes | Rain and rainfall
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 07/2016, Volume 291, Issue 31, pp. 16282 - 16291
Phosphodiesterase 6 (PDE6) is the effector enzyme in the phototransduction cascade and is critical for the health of both rod and cone photoreceptors. Its...
RETINAL DEGENERATION | LEBER CONGENITAL AMAUROSIS | DOMAIN | GENE | BIOCHEMISTRY & MOLECULAR BIOLOGY | MOUSE | ROD CGMP-PHOSPHODIESTERASE | AIPL1 | BETA-SUBUNIT | NONSENSE MUTATION | CYCLIC-GMP PHOSPHODIESTERASE | Retinal Diseases - genetics | Cyclic Nucleotide Phosphodiesterases, Type 6 - metabolism | Molecular Chaperones - metabolism | Humans | Molecular Chaperones - genetics | Cercopithecus aethiops | Retinal Diseases - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 6 - genetics | Animals | Adaptor Proteins, Signal Transducing - genetics | HEK293 Cells | Mice | Adaptor Proteins, Signal Transducing - metabolism | COS Cells | phosphodiesterases | protein folding | Signal Transduction | chaperone | phototransduction | photoreceptor
RETINAL DEGENERATION | LEBER CONGENITAL AMAUROSIS | DOMAIN | GENE | BIOCHEMISTRY & MOLECULAR BIOLOGY | MOUSE | ROD CGMP-PHOSPHODIESTERASE | AIPL1 | BETA-SUBUNIT | NONSENSE MUTATION | CYCLIC-GMP PHOSPHODIESTERASE | Retinal Diseases - genetics | Cyclic Nucleotide Phosphodiesterases, Type 6 - metabolism | Molecular Chaperones - metabolism | Humans | Molecular Chaperones - genetics | Cercopithecus aethiops | Retinal Diseases - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 6 - genetics | Animals | Adaptor Proteins, Signal Transducing - genetics | HEK293 Cells | Mice | Adaptor Proteins, Signal Transducing - metabolism | COS Cells | phosphodiesterases | protein folding | Signal Transduction | chaperone | phototransduction | photoreceptor
Journal Article
Human Molecular Genetics, ISSN 0964-6906, 02/2011, Volume 20, Issue 4, pp. 719 - 730
Mutations in the gene encoding the catalytic subunit of the cone photoreceptor phosphodiesterase (PDE6C) have been recently reported in patients with autosomal...
TRANSDUCIN | ROD CGMP PHOSPHODIESTERASE | GENETIC-BASIS | INHIBITORY GAMMA-SUBUNIT | ALPHA-SUBUNIT | BIOCHEMISTRY & MOLECULAR BIOLOGY | GAFA DOMAINS | GENETICS & HEREDITY | MUTATIONS | IDENTIFICATION | BINDING | TOTAL COLOURBLINDNESS | Cyclic Nucleotide Phosphodiesterases, Type 6 - metabolism | Color Vision Defects - enzymology | Humans | Cercopithecus aethiops | Cyclic Nucleotide Phosphodiesterases, Type 6 - antagonists & inhibitors | Substrate Specificity | Cyclic Nucleotide Phosphodiesterases, Type 6 - chemistry | Male | Cyclic Nucleotide Phosphodiesterases, Type 6 - genetics | Color Vision Defects - genetics | Microsatellite Repeats - genetics | Phenotype | RNA Splicing | Animals | Pedigree | Adolescent | Cyclic Nucleotide Phosphodiesterases, Type 5 - genetics | Adult | Female | Mutation | COS Cells | Child | Cyclic Nucleotide Phosphodiesterases, Type 5 - metabolism | Medicinsk genetik | Basic Medicine | Medical Genetics | Medical and Health Sciences | Medicin och hälsovetenskap | Medicinska och farmaceutiska grundvetenskaper
TRANSDUCIN | ROD CGMP PHOSPHODIESTERASE | GENETIC-BASIS | INHIBITORY GAMMA-SUBUNIT | ALPHA-SUBUNIT | BIOCHEMISTRY & MOLECULAR BIOLOGY | GAFA DOMAINS | GENETICS & HEREDITY | MUTATIONS | IDENTIFICATION | BINDING | TOTAL COLOURBLINDNESS | Cyclic Nucleotide Phosphodiesterases, Type 6 - metabolism | Color Vision Defects - enzymology | Humans | Cercopithecus aethiops | Cyclic Nucleotide Phosphodiesterases, Type 6 - antagonists & inhibitors | Substrate Specificity | Cyclic Nucleotide Phosphodiesterases, Type 6 - chemistry | Male | Cyclic Nucleotide Phosphodiesterases, Type 6 - genetics | Color Vision Defects - genetics | Microsatellite Repeats - genetics | Phenotype | RNA Splicing | Animals | Pedigree | Adolescent | Cyclic Nucleotide Phosphodiesterases, Type 5 - genetics | Adult | Female | Mutation | COS Cells | Child | Cyclic Nucleotide Phosphodiesterases, Type 5 - metabolism | Medicinsk genetik | Basic Medicine | Medical Genetics | Medical and Health Sciences | Medicin och hälsovetenskap | Medicinska och farmaceutiska grundvetenskaper
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 09/2017, Volume 60, Issue 18, pp. 7658 - 7676
Herein, we describe the discovery of a potent, selective, brain-penetrating, in vivo active phosphodiesterase (PDE) 2A inhibitor lead series. To identify...
HIPPOCAMPUS | OBSTRUCTIVE PULMONARY-DISEASE | CHEMISTRY, MEDICINAL | PERSPECTIVE | MILRINONE | EFFICACY | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES | CGMP | SYNAPTIC PLASTICITY | ROFLUMILAST | SELECTIVITY | Cyclic Nucleotide Phosphodiesterases, Type 2 - antagonists & inhibitors | Humans | Cognition Disorders - metabolism | Male | Pyrimidines - chemistry | Brain - metabolism | Phosphodiesterase Inhibitors - chemistry | Cognition Disorders - enzymology | Phosphodiesterase Inhibitors - pharmacokinetics | Administration, Oral | Pyrimidines - administration & dosage | Cyclic Nucleotide Phosphodiesterases, Type 2 - metabolism | Phosphodiesterase Inhibitors - pharmacology | Rats | Pyrimidines - pharmacology | Cognition Disorders - drug therapy | Drug Discovery | Mice, Inbred ICR | Brain - drug effects | Phosphodiesterase Inhibitors - administration & dosage | Animals | Cyclic GMP - metabolism | Pyrimidines - pharmacokinetics | Mice | Molecular Docking Simulation
HIPPOCAMPUS | OBSTRUCTIVE PULMONARY-DISEASE | CHEMISTRY, MEDICINAL | PERSPECTIVE | MILRINONE | EFFICACY | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASES | CGMP | SYNAPTIC PLASTICITY | ROFLUMILAST | SELECTIVITY | Cyclic Nucleotide Phosphodiesterases, Type 2 - antagonists & inhibitors | Humans | Cognition Disorders - metabolism | Male | Pyrimidines - chemistry | Brain - metabolism | Phosphodiesterase Inhibitors - chemistry | Cognition Disorders - enzymology | Phosphodiesterase Inhibitors - pharmacokinetics | Administration, Oral | Pyrimidines - administration & dosage | Cyclic Nucleotide Phosphodiesterases, Type 2 - metabolism | Phosphodiesterase Inhibitors - pharmacology | Rats | Pyrimidines - pharmacology | Cognition Disorders - drug therapy | Drug Discovery | Mice, Inbred ICR | Brain - drug effects | Phosphodiesterase Inhibitors - administration & dosage | Animals | Cyclic GMP - metabolism | Pyrimidines - pharmacokinetics | Mice | Molecular Docking Simulation
Journal Article
Circulation, ISSN 0009-7322, 2006, Volume 113, Issue 18, pp. 2221 - 2228
Background - Cyclic guanosine monophosphate (cGMP) is the common second messenger for the cardiovascular effects of nitric oxide (NO) and natriuretic peptides,...
Sildenafil | Phosphodiesterases | Cyclic GMP | Nitric oxide | Natriuretic peptides | nitric oxide | CARDIAC & CARDIOVASCULAR SYSTEMS | cyclic GMP | CALCIUM CURRENT | DEPENDENT PROTEIN-KINASE | sildenafil | natriuretic peptides | SOLUBLE GUANYLYL CYCLASE | CGMP-SPECIFIC PHOSPHODIESTERASE | CA2+ CURRENT | phosphodiesterases | NITRIC-OXIDE | PERIPHERAL VASCULAR DISEASE | ADENOVIRUS-MEDIATED EXPRESSION | FROG VENTRICULAR MYOCYTES | NUCLEOTIDE-GATED CHANNELS | HEMATOLOGY | HUMAN ATRIAL MYOCYTES | Cyclic GMP - pharmacology | Heart Ventricles - cytology | Rats, Wistar | Cyclic Nucleotide Phosphodiesterases, Type 5 | Cyclic Nucleotide Phosphodiesterases, Type 2 | Humans | Recombinant Fusion Proteins - analysis | Recombinant Fusion Proteins - physiology | Male | Ion Channels - physiology | Natriuretic Peptide, Brain - pharmacology | Phosphoric Diester Hydrolases - physiology | Cell Compartmentation | Sildenafil Citrate | Purines | Biological Transport | Cell Membrane - metabolism | Atrial Natriuretic Factor - pharmacology | Nitric Oxide Donors - pharmacology | Sarcolemma - metabolism | Second Messenger Systems | Sulfones | Isoenzymes - physiology | Adenine - analogs & derivatives | 3',5'-Cyclic-GMP Phosphodiesterases - physiology | Solubility | Phosphodiesterase Inhibitors - pharmacology | Rats | Adenine - pharmacology | Myocytes, Cardiac - chemistry | Piperazines - pharmacology | 1-Methyl-3-isobutylxanthine - pharmacology | Ion Channels - antagonists & inhibitors | Cyclic AMP - pharmacology | Animals | Ion Channels - analysis | Myocytes, Cardiac - drug effects | Cyclic GMP - metabolism | Cyclic Nucleotide-Gated Cation Channels | Myocytes, Cardiac - ultrastructure | Isoenzymes - antagonists & inhibitors | Ion Channel Gating - drug effects | Life Sciences | Cellular Biology | Cell Membrane | cytology | Ion Channels | cGMP | Recombinant Fusion Proteins | Heart Ventricles | Nitric Oxide Donors | Natriuretic Peptide, Brain | Atrial Natriuretic Factor | pharmacology | 3',5'-Cyclic-GMP Phosphodiesterase | chemistry | Sarcolemma | Phosphodiesterase Inhibitors | Myocytes, Cardiac | Piperazines | Isoenzymes | physiology | Adenine | Cyclic AMP | 1-Methyl-3-isobutylxanthine | drug effects | analysis | ultrastructure | antagonists & inhibitors | Phosphoric Diester Hydrolases | analogs & derivatives | metabolism | Ion Channel Gating
Sildenafil | Phosphodiesterases | Cyclic GMP | Nitric oxide | Natriuretic peptides | nitric oxide | CARDIAC & CARDIOVASCULAR SYSTEMS | cyclic GMP | CALCIUM CURRENT | DEPENDENT PROTEIN-KINASE | sildenafil | natriuretic peptides | SOLUBLE GUANYLYL CYCLASE | CGMP-SPECIFIC PHOSPHODIESTERASE | CA2+ CURRENT | phosphodiesterases | NITRIC-OXIDE | PERIPHERAL VASCULAR DISEASE | ADENOVIRUS-MEDIATED EXPRESSION | FROG VENTRICULAR MYOCYTES | NUCLEOTIDE-GATED CHANNELS | HEMATOLOGY | HUMAN ATRIAL MYOCYTES | Cyclic GMP - pharmacology | Heart Ventricles - cytology | Rats, Wistar | Cyclic Nucleotide Phosphodiesterases, Type 5 | Cyclic Nucleotide Phosphodiesterases, Type 2 | Humans | Recombinant Fusion Proteins - analysis | Recombinant Fusion Proteins - physiology | Male | Ion Channels - physiology | Natriuretic Peptide, Brain - pharmacology | Phosphoric Diester Hydrolases - physiology | Cell Compartmentation | Sildenafil Citrate | Purines | Biological Transport | Cell Membrane - metabolism | Atrial Natriuretic Factor - pharmacology | Nitric Oxide Donors - pharmacology | Sarcolemma - metabolism | Second Messenger Systems | Sulfones | Isoenzymes - physiology | Adenine - analogs & derivatives | 3',5'-Cyclic-GMP Phosphodiesterases - physiology | Solubility | Phosphodiesterase Inhibitors - pharmacology | Rats | Adenine - pharmacology | Myocytes, Cardiac - chemistry | Piperazines - pharmacology | 1-Methyl-3-isobutylxanthine - pharmacology | Ion Channels - antagonists & inhibitors | Cyclic AMP - pharmacology | Animals | Ion Channels - analysis | Myocytes, Cardiac - drug effects | Cyclic GMP - metabolism | Cyclic Nucleotide-Gated Cation Channels | Myocytes, Cardiac - ultrastructure | Isoenzymes - antagonists & inhibitors | Ion Channel Gating - drug effects | Life Sciences | Cellular Biology | Cell Membrane | cytology | Ion Channels | cGMP | Recombinant Fusion Proteins | Heart Ventricles | Nitric Oxide Donors | Natriuretic Peptide, Brain | Atrial Natriuretic Factor | pharmacology | 3',5'-Cyclic-GMP Phosphodiesterase | chemistry | Sarcolemma | Phosphodiesterase Inhibitors | Myocytes, Cardiac | Piperazines | Isoenzymes | physiology | Adenine | Cyclic AMP | 1-Methyl-3-isobutylxanthine | drug effects | analysis | ultrastructure | antagonists & inhibitors | Phosphoric Diester Hydrolases | analogs & derivatives | metabolism | Ion Channel Gating
Journal Article
PLoS Neglected Tropical Diseases, ISSN 1935-2727, 07/2017, Volume 11, Issue 7, p. e0005680
Background Reliance on just one drug to treat the prevalent tropical disease, schistosomiasis, spurs the search for new drugs and drug targets. Inhibitors of...
CAENORHABDITIS-ELEGANS | PHARMACOLOGICAL VALIDATION | SCHISTOSOMA-MANSONI | PROTEIN-KINASE | ALZHEIMERS-DISEASE | 5 INHIBITOR ANALOGS | MIRACIDIAL TRANSFORMATION | TRYPANOSOMA-BRUCEI PHOSPHODIESTERASES | CONSERVED REGIONS UCRS | PARASITOLOGY | TROPICAL MEDICINE | CAMP-SPECIFIC PHOSPHODIESTERASES | Schistosoma mansoni - drug effects | Schistosoma mansoni - physiology | Catalytic Domain | Caenorhabditis elegans - genetics | Schistosoma mansoni - anatomy & histology | Cyclic Nucleotide Phosphodiesterases, Type 4 - genetics | Phosphodiesterase 4 Inhibitors - pharmacology | Animals | Caenorhabditis elegans - drug effects | Animals, Genetically Modified - genetics | Anthelmintics - pharmacology | Cloning, Molecular | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Locomotion - drug effects | Caenorhabditis elegans | Schistosomiasis | Care and treatment | Lung diseases, Obstructive | Genetic aspects | Research | Phosphodiesterases | Alzheimer's disease | Asthma | Drugs | Transgenic | Phosphodiesterase IV | Genomes | Parasites | Nucleotides | Drug development | Kinases | Gene sequencing | Parasitic diseases | Tropical environment | Degeneration | Chronic obstructive pulmonary disease | cDNA | Aquatic invertebrates | Catalysis | Phosphodiesterase | 3',5'-Cyclic-nucleotide phosphodiesterase | Lung diseases | Catechol | Gene expression | Diseases | Inhibitors | DNA | Obstructive lung disease | Nematodes | Hypothermia | Lines
CAENORHABDITIS-ELEGANS | PHARMACOLOGICAL VALIDATION | SCHISTOSOMA-MANSONI | PROTEIN-KINASE | ALZHEIMERS-DISEASE | 5 INHIBITOR ANALOGS | MIRACIDIAL TRANSFORMATION | TRYPANOSOMA-BRUCEI PHOSPHODIESTERASES | CONSERVED REGIONS UCRS | PARASITOLOGY | TROPICAL MEDICINE | CAMP-SPECIFIC PHOSPHODIESTERASES | Schistosoma mansoni - drug effects | Schistosoma mansoni - physiology | Catalytic Domain | Caenorhabditis elegans - genetics | Schistosoma mansoni - anatomy & histology | Cyclic Nucleotide Phosphodiesterases, Type 4 - genetics | Phosphodiesterase 4 Inhibitors - pharmacology | Animals | Caenorhabditis elegans - drug effects | Animals, Genetically Modified - genetics | Anthelmintics - pharmacology | Cloning, Molecular | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Locomotion - drug effects | Caenorhabditis elegans | Schistosomiasis | Care and treatment | Lung diseases, Obstructive | Genetic aspects | Research | Phosphodiesterases | Alzheimer's disease | Asthma | Drugs | Transgenic | Phosphodiesterase IV | Genomes | Parasites | Nucleotides | Drug development | Kinases | Gene sequencing | Parasitic diseases | Tropical environment | Degeneration | Chronic obstructive pulmonary disease | cDNA | Aquatic invertebrates | Catalysis | Phosphodiesterase | 3',5'-Cyclic-nucleotide phosphodiesterase | Lung diseases | Catechol | Gene expression | Diseases | Inhibitors | DNA | Obstructive lung disease | Nematodes | Hypothermia | Lines
Journal Article
British Journal of Pharmacology, ISSN 0007-1188, 06/2013, Volume 169, Issue 3, pp. 528 - 538
Background and Purpose PDE3 and/or PDE4 control ventricular effects of catecholamines in several species but their relative effects in failing human ventricle...
inotropism and lusitropism | human heart failure | phosphodiesterases 3 and 4 | noradrenaline and adrenaline | metoprolol | β1 and β2 adrenoceptors | and β | adrenoceptors | Adrenergic beta-1 Receptor Antagonists - adverse effects | Heart Failure - surgery | Cyclic Nucleotide Phosphodiesterases, Type 3 - chemistry | Norepinephrine - pharmacology | Adrenergic alpha-Agonists - chemistry | Phosphodiesterase 3 Inhibitors - pharmacology | Humans | Middle Aged | Adrenergic beta-1 Receptor Antagonists - pharmacology | Heart Failure - physiopathology | Myocardial Contraction - drug effects | Receptors, Adrenergic, beta-1 - chemistry | Adrenergic beta-1 Receptor Antagonists - therapeutic use | Adrenergic beta-Agonists - chemistry | Epinephrine - agonists | Receptors, Adrenergic, beta-2 - chemistry | Cardiotonic Agents - therapeutic use | Cyclic Nucleotide Phosphodiesterases, Type 3 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Adrenergic beta-2 Receptor Antagonists - pharmacology | Adrenergic beta-Agonists - pharmacology | Heart Transplantation | Metoprolol - therapeutic use | Receptors, Adrenergic, beta-1 - metabolism | Drug Resistance - drug effects | Heart Failure - metabolism | Anti-Arrhythmia Agents - therapeutic use | Cardiotonic Agents - pharmacology | Metoprolol - adverse effects | Norepinephrine - agonists | Phosphodiesterase 4 Inhibitors - pharmacology | Receptors, Adrenergic, beta-2 - metabolism | Heart Failure - drug therapy | Heart Ventricles - physiopathology | Anti-Arrhythmia Agents - adverse effects | Adrenergic alpha-Agonists - pharmacology | Heart Ventricles - metabolism | In Vitro Techniques | Epinephrine - pharmacology | Heart Ventricles - drug effects | Research Paper with
inotropism and lusitropism | human heart failure | phosphodiesterases 3 and 4 | noradrenaline and adrenaline | metoprolol | β1 and β2 adrenoceptors | and β | adrenoceptors | Adrenergic beta-1 Receptor Antagonists - adverse effects | Heart Failure - surgery | Cyclic Nucleotide Phosphodiesterases, Type 3 - chemistry | Norepinephrine - pharmacology | Adrenergic alpha-Agonists - chemistry | Phosphodiesterase 3 Inhibitors - pharmacology | Humans | Middle Aged | Adrenergic beta-1 Receptor Antagonists - pharmacology | Heart Failure - physiopathology | Myocardial Contraction - drug effects | Receptors, Adrenergic, beta-1 - chemistry | Adrenergic beta-1 Receptor Antagonists - therapeutic use | Adrenergic beta-Agonists - chemistry | Epinephrine - agonists | Receptors, Adrenergic, beta-2 - chemistry | Cardiotonic Agents - therapeutic use | Cyclic Nucleotide Phosphodiesterases, Type 3 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Adrenergic beta-2 Receptor Antagonists - pharmacology | Adrenergic beta-Agonists - pharmacology | Heart Transplantation | Metoprolol - therapeutic use | Receptors, Adrenergic, beta-1 - metabolism | Drug Resistance - drug effects | Heart Failure - metabolism | Anti-Arrhythmia Agents - therapeutic use | Cardiotonic Agents - pharmacology | Metoprolol - adverse effects | Norepinephrine - agonists | Phosphodiesterase 4 Inhibitors - pharmacology | Receptors, Adrenergic, beta-2 - metabolism | Heart Failure - drug therapy | Heart Ventricles - physiopathology | Anti-Arrhythmia Agents - adverse effects | Adrenergic alpha-Agonists - pharmacology | Heart Ventricles - metabolism | In Vitro Techniques | Epinephrine - pharmacology | Heart Ventricles - drug effects | Research Paper with
Journal Article
Journal of Biological Chemistry, ISSN 0021-9258, 11/2005, Volume 280, Issue 47, pp. 39168 - 39174
Three isoforms of PDE3 (cGMP-inhibited) cyclic nucleotide phosphodiesterase regulate cAMP content in different intracellular compartments of cardiac myocytes...
NATRIURETIC-PEPTIDE | CA2+ CURRENT | RAT CARDIAC MYOCYTES | BIOCHEMISTRY & MOLECULAR BIOLOGY | HEART-FAILURE | NITRIC-OXIDE | DEPENDENT PROTEIN-KINASE | HUMAN VENTRICULAR MYOCARDIUM | SARCOPLASMIC-RETICULUM | GUANYLYL CYCLASE-A | ROLIPRAM INHIBITION | Cyclic GMP - pharmacology | Cyclic Nucleotide Phosphodiesterases, Type 1 | Humans | Cyclic Nucleotide Phosphodiesterases, Type 3 | Isoenzymes - chemistry | Isoenzymes - metabolism | Myocardium - metabolism | Cyclic AMP - metabolism | Calcium Signaling | Recombinant Proteins - metabolism | 3',5'-Cyclic-AMP Phosphodiesterases - metabolism | Recombinant Proteins - antagonists & inhibitors | Signal Transduction | Isoenzymes - genetics | Enzyme Inhibitors - pharmacology | Recombinant Proteins - chemistry | Recombinant Proteins - genetics | 3',5'-Cyclic-AMP Phosphodiesterases - genetics | Subcellular Fractions - metabolism | Hydrolysis | 3',5'-Cyclic-AMP Phosphodiesterases - chemistry | Cyclic GMP - metabolism | 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors | Kinetics | In Vitro Techniques | Isoenzymes - antagonists & inhibitors
NATRIURETIC-PEPTIDE | CA2+ CURRENT | RAT CARDIAC MYOCYTES | BIOCHEMISTRY & MOLECULAR BIOLOGY | HEART-FAILURE | NITRIC-OXIDE | DEPENDENT PROTEIN-KINASE | HUMAN VENTRICULAR MYOCARDIUM | SARCOPLASMIC-RETICULUM | GUANYLYL CYCLASE-A | ROLIPRAM INHIBITION | Cyclic GMP - pharmacology | Cyclic Nucleotide Phosphodiesterases, Type 1 | Humans | Cyclic Nucleotide Phosphodiesterases, Type 3 | Isoenzymes - chemistry | Isoenzymes - metabolism | Myocardium - metabolism | Cyclic AMP - metabolism | Calcium Signaling | Recombinant Proteins - metabolism | 3',5'-Cyclic-AMP Phosphodiesterases - metabolism | Recombinant Proteins - antagonists & inhibitors | Signal Transduction | Isoenzymes - genetics | Enzyme Inhibitors - pharmacology | Recombinant Proteins - chemistry | Recombinant Proteins - genetics | 3',5'-Cyclic-AMP Phosphodiesterases - genetics | Subcellular Fractions - metabolism | Hydrolysis | 3',5'-Cyclic-AMP Phosphodiesterases - chemistry | Cyclic GMP - metabolism | 3',5'-Cyclic-AMP Phosphodiesterases - antagonists & inhibitors | Kinetics | In Vitro Techniques | Isoenzymes - antagonists & inhibitors
Journal Article
Cellular Signalling, ISSN 0898-6568, 09/2014, Volume 26, Issue 9, pp. 2016 - 2029
Apremilast, an oral small molecule inhibitor of phosphodiesterase 4 (PDE4), is in development for chronic inflammatory disorders, and has shown efficacy in...
Phosphodiesterase inhibitor | Apremilast | Spondyloarthropathies | Psoriasis | Preclinical drug evaluation | Psoriatic arthritis | PROTEIN-KINASE-A | CONTROLLED-TRIAL | CAMP-SPECIFIC PHOSPHODIESTERASE | NECROSIS-FACTOR-ALPHA | KAPPA-B | PSORIATIC-ARTHRITIS | CELL BIOLOGY | ORAL PHOSPHODIESTERASE-4 INHIBITOR | CYCLIC-AMP | THALIDOMIDE ANALOGS | B-MEDIATED TRANSCRIPTION | Thalidomide - metabolism | Humans | Male | Thalidomide - pharmacology | Lung Diseases - drug therapy | Thalidomide - analogs & derivatives | T-Lymphocytes - metabolism | T-Lymphocytes - drug effects | Female | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic AMP - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Vomiting - prevention & control | B-Lymphocytes - metabolism | Disease Models, Animal | Cell Line | Cytokines - metabolism | Immunity, Innate - drug effects | Jurkat Cells | Phosphodiesterase 4 Inhibitors - therapeutic use | Mice, Transgenic | Phosphodiesterase 4 Inhibitors - metabolism | Ferrets | Phosphodiesterase 4 Inhibitors - pharmacology | B-Lymphocytes - drug effects | Adaptive Immunity - drug effects | Animals | B-Lymphocytes - immunology | Protein Binding | T-Lymphocytes - immunology | Mice | Thalidomide - therapeutic use | Dendritic cells | Analysis | Development and progression | Genetic engineering | B cells | Biological response modifiers | T cells
Phosphodiesterase inhibitor | Apremilast | Spondyloarthropathies | Psoriasis | Preclinical drug evaluation | Psoriatic arthritis | PROTEIN-KINASE-A | CONTROLLED-TRIAL | CAMP-SPECIFIC PHOSPHODIESTERASE | NECROSIS-FACTOR-ALPHA | KAPPA-B | PSORIATIC-ARTHRITIS | CELL BIOLOGY | ORAL PHOSPHODIESTERASE-4 INHIBITOR | CYCLIC-AMP | THALIDOMIDE ANALOGS | B-MEDIATED TRANSCRIPTION | Thalidomide - metabolism | Humans | Male | Thalidomide - pharmacology | Lung Diseases - drug therapy | Thalidomide - analogs & derivatives | T-Lymphocytes - metabolism | T-Lymphocytes - drug effects | Female | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic AMP - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Vomiting - prevention & control | B-Lymphocytes - metabolism | Disease Models, Animal | Cell Line | Cytokines - metabolism | Immunity, Innate - drug effects | Jurkat Cells | Phosphodiesterase 4 Inhibitors - therapeutic use | Mice, Transgenic | Phosphodiesterase 4 Inhibitors - metabolism | Ferrets | Phosphodiesterase 4 Inhibitors - pharmacology | B-Lymphocytes - drug effects | Adaptive Immunity - drug effects | Animals | B-Lymphocytes - immunology | Protein Binding | T-Lymphocytes - immunology | Mice | Thalidomide - therapeutic use | Dendritic cells | Analysis | Development and progression | Genetic engineering | B cells | Biological response modifiers | T cells
Journal Article
Nature Communications, ISSN 2041-1723, 03/2016, Volume 7, Issue 1, p. 10856
Biguanides such as metformin have previously been shown to antagonize hepatic glucagon-stimulated cyclic AMP (cAMP) signalling independently of AMP-activated...
GLYCOGEN-METABOLISM | SKELETAL-MUSCLE | CULTURED RAT HEPATOCYTES | HORMONAL-CONTROL | PROTEIN-KINASE | MULTIDISCIPLINARY SCIENCES | MULTISITE PHOSPHORYLATION | BINDING-PROTEIN | GENE-EXPRESSION | MASS-SPECTROMETRY | GLUCOSE-PRODUCTION | AMP-Activated Protein Kinases - metabolism | Phosphorylation | Signal Transduction | Mice, Inbred C57BL | Cells, Cultured | Enzyme Activators - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - genetics | Hepatocytes - metabolism | Amino Acid Motifs | Mice, Knockout | Animals | Glucagon - metabolism | Mice | Enzyme Activation | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic AMP - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | AMP-Activated Protein Kinases - genetics | Hepatocytes - enzymology
GLYCOGEN-METABOLISM | SKELETAL-MUSCLE | CULTURED RAT HEPATOCYTES | HORMONAL-CONTROL | PROTEIN-KINASE | MULTIDISCIPLINARY SCIENCES | MULTISITE PHOSPHORYLATION | BINDING-PROTEIN | GENE-EXPRESSION | MASS-SPECTROMETRY | GLUCOSE-PRODUCTION | AMP-Activated Protein Kinases - metabolism | Phosphorylation | Signal Transduction | Mice, Inbred C57BL | Cells, Cultured | Enzyme Activators - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - genetics | Hepatocytes - metabolism | Amino Acid Motifs | Mice, Knockout | Animals | Glucagon - metabolism | Mice | Enzyme Activation | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Cyclic AMP - metabolism | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | AMP-Activated Protein Kinases - genetics | Hepatocytes - enzymology
Journal Article
Bioorganic & Medicinal Chemistry Letters, ISSN 0960-894X, 06/2013, Volume 23, Issue 11, pp. 3438 - 3442
We identified potent, selective PDE2 inhibitors by optimizing residual PDE2 activity in a series of PDE4 inhibitors, while simultaneously minimizing PDE4...
Phosphodiesterase 2 (PDE2)inhibition | Structure-based drug design | Osteoarthritis(OA)pain | ISOZYME | Osteoarthritis(OA) pain | CHEMISTRY, MEDICINAL | CGMP | CHEMISTRY, ORGANIC | Phosphodiesterase 2 (PDE2) inhibition | Cyclic Nucleotide Phosphodiesterases, Type 2 - antagonists & inhibitors | Phosphodiesterase Inhibitors - therapeutic use | Catalytic Domain | Phosphodiesterase 4 Inhibitors - chemistry | Dihydropyridines - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 2 - metabolism | Crystallography, X-Ray | Structure-Activity Relationship | Dihydropyridines - metabolism | Osteoarthritis - drug therapy | Dihydropyridines - therapeutic use | Azirines - chemistry | Animals | Phosphodiesterase Inhibitors - metabolism | Azirines - therapeutic use | Azirines - metabolism | Protein Binding | Phosphodiesterase Inhibitors - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Drug Evaluation, Preclinical | Binding Sites | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Disease Models, Animal | Osteoarthritis
Phosphodiesterase 2 (PDE2)inhibition | Structure-based drug design | Osteoarthritis(OA)pain | ISOZYME | Osteoarthritis(OA) pain | CHEMISTRY, MEDICINAL | CGMP | CHEMISTRY, ORGANIC | Phosphodiesterase 2 (PDE2) inhibition | Cyclic Nucleotide Phosphodiesterases, Type 2 - antagonists & inhibitors | Phosphodiesterase Inhibitors - therapeutic use | Catalytic Domain | Phosphodiesterase 4 Inhibitors - chemistry | Dihydropyridines - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 2 - metabolism | Crystallography, X-Ray | Structure-Activity Relationship | Dihydropyridines - metabolism | Osteoarthritis - drug therapy | Dihydropyridines - therapeutic use | Azirines - chemistry | Animals | Phosphodiesterase Inhibitors - metabolism | Azirines - therapeutic use | Azirines - metabolism | Protein Binding | Phosphodiesterase Inhibitors - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 4 - metabolism | Drug Evaluation, Preclinical | Binding Sites | Cyclic Nucleotide Phosphodiesterases, Type 4 - chemistry | Disease Models, Animal | Osteoarthritis
Journal Article
Biochemical Journal, ISSN 0264-6021, 02/2003, Volume 370, Issue 1, pp. 1 - 18
cAMP is a second messenger that controls many key cellular functions. The only way to inactivate cAMP is to degrade it through the action of cAMP...
Chronic obstructive pulmonary disease (COPD) | Phosphorylation | Arrestin | Rolipram | Targeting | Asthma | DROSOPHILA-MELANOGASTER | BIOCHEMISTRY & MOLECULAR BIOLOGY | LIVER PLASMA-MEMBRANES | rolipram | DEPENDENT PROTEIN-KINASE | asthma | AMP-SPECIFIC PHOSPHODIESTERASE | arrestin | targeting | chronic obstructive pulmonary disease (COPD) | N-TERMINAL DOMAIN | A-MEDIATED PHOSPHORYLATION | PHOSPHATIDIC-ACID | MOLECULAR-CLONING | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE | phosphorylation | SMOOTH-MUSCLE CELLS | Cell Compartmentation | 3',5'-Cyclic-AMP Phosphodiesterases - metabolism | Catalytic Domain | 3',5'-Cyclic-AMP Phosphodiesterases - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 4 | Signal Transduction | Humans | Models, Molecular | Protein Conformation | Pulmonary Disease, Chronic Obstructive - enzymology
Chronic obstructive pulmonary disease (COPD) | Phosphorylation | Arrestin | Rolipram | Targeting | Asthma | DROSOPHILA-MELANOGASTER | BIOCHEMISTRY & MOLECULAR BIOLOGY | LIVER PLASMA-MEMBRANES | rolipram | DEPENDENT PROTEIN-KINASE | asthma | AMP-SPECIFIC PHOSPHODIESTERASE | arrestin | targeting | chronic obstructive pulmonary disease (COPD) | N-TERMINAL DOMAIN | A-MEDIATED PHOSPHORYLATION | PHOSPHATIDIC-ACID | MOLECULAR-CLONING | CYCLIC-NUCLEOTIDE PHOSPHODIESTERASE | phosphorylation | SMOOTH-MUSCLE CELLS | Cell Compartmentation | 3',5'-Cyclic-AMP Phosphodiesterases - metabolism | Catalytic Domain | 3',5'-Cyclic-AMP Phosphodiesterases - chemistry | Cyclic Nucleotide Phosphodiesterases, Type 4 | Signal Transduction | Humans | Models, Molecular | Protein Conformation | Pulmonary Disease, Chronic Obstructive - enzymology
Journal Article