Cyclic Nucleotide Phosphodiesterases, Type 1
Cyclic Nucleotide Phosphodiesterases, Type 4
Cyclic Nucleotide Phosphodiesterases, Type 3
Cyclic Nucleotide Phosphodiesterases, Type 2
Phosphoric Diester Hydrolases
Cyclic Nucleotide Phosphodiesterases, Type 5
Cyclic Nucleotide Phosphodiesterases, Type 7
Molecular Sequence Data
Amino Acid Sequence
Cyclic Nucleotide Phosphodiesterases, Type 6
Dibutyryl Cyclic GMP
Cyclic Nucleotide-Gated Cation Channels
Cyclic AMP-Dependent Protein Kinases
Cyclic GMP-Dependent Protein Kinases
Second Messenger Systems
Polymorphism, Single Nucleotide
8-Bromo Cyclic Adenosine Monophosphate
Cloning and characterization of PDE7B, a cAMP-specific phosphodiesterase. (1/27)A member of the phosphodiesterase (PDE)7 family with high affinity and specificity for cAMP has been identified. Based on sequence homologies, we designate this PDE as PDE7B. The full-length cDNA of PDE7B is 2399 bp, and its ORF sequence predicts a protein of 446 amino acids with a molecular mass of 50.1 kDa. Comparison of the predicted protein sequences of PDE7A and PDE7B reveals an identity of 70% in the catalytic domain. Northern blotting indicates that the mRNA of PDE7B is 5.6 kb. It is most highly expressed in pancreas followed by brain, heart, thyroid, skeletal muscle, eye, ovary, submaxillary gland, epididymus, and liver. Recombinant PDE7B protein expressed in a Baculovirus expression system is specific for cAMP with a K(m) of 0.03 microM. Within a series of common PDE inhibitors, it is most potently inhibited by 3-isobutyl-1-methylxanthine with an IC(50) of 2.1 microM. It is also inhibited by papaverine, dipyridamole, and SCH51866 at higher doses. PDE7A and PDE7B exhibit the same general pattern of inhibitor specificity among the several drugs tested. However, differences in IC(50) for some of the drugs suggest that isozyme selective inhibitors can be developed. (+info)
Novel alternative splice variants of rat phosphodiesterase 7B showing unique tissue-specific expression and phosphorylation. (2/27)cDNA species coding for novel variants of cyclic-AMP-specific phosphodiesterases (PDEs), namely the PDE7B family, were isolated from rats and characterized. Rat PDE7B1 (RNPDE7B1) was composed of 446 amino acid residues. Rat PDE7B2 (RNPDE7B2) and PDE7B3 (RNPDE7B3), which possessed unique N-terminal sequences, consisted of 359 and 459 residues respectively. Northern hybridization analysis showed that rat PDE7B transcripts were particularly abundant in the striatum and testis. PCR analyses revealed that rat PDE7B2 transcripts were restricted to the testis and that low levels of PDE7B3 transcripts were expressed in the heart, lung and skeletal muscle. In situ hybridization analysis demonstrated that rat PDE7B transcripts were expressed in striatal neurons and spermatocytes. In spermatocytes, rat PDE7B transcripts were expressed in a stage-specific manner during spermatogenesis. The K(m) values of recombinant rat PDE7B1, PDE7B2 and PDE7B3 for cAMP were 0.05, 0.07 and 0.05 microM respectively. Each rat PDE7B variant was the most sensitive to 3-isobutyl-1-methylxanthine (IC(50) 1.5-2.1 microM). Two phosphorylation sites for cAMP-dependent protein kinase (PKA) were found in rat PDE7B1 and PDE7B3, whereas rat PDE7B2 possessed one site. PKA-dependent phosphorylation was observed in C-terminal phosphorylation sites of three rat PDE7B variants, in addition to unique N-terminal regions of rat PDE7B1 and PDE7B3. Unique tissue distribution and PKA-dependent phosphorylation of PDE7B variants suggested that each variant has a specific role for cellular functions via cAMP signalling in various tissues. (+info)
Inhibition of PDE3B augments PDE4 inhibitor-induced apoptosis in a subset of patients with chronic lymphocytic leukemia. (3/27)PURPOSE: cAMP phosphodiesterase (PDE) 4 is a family of enzymes the inhibition of which induces chronic lymphocytic leukemia (CLL) apoptosis. However, leukemic cells from a subset of CLL patients are relatively resistant to treatment with the PDE4 inhibitor rolipram, particularly when this drug is used in the absence of an adenylate cyclase stimulus such as forskolin. Elevated cAMP levels induce compensatory up-regulation of several cyclic nucleotide PDE families in other model systems. We here examine the hypothesis that CLL cells that survive treatment with rolipram do so as a result of residual PDE activity that is not inhibited by this drug. EXPERIMENTAL DESIGN: We examined by Western analysis the effect of rolipram treatment on CLL expression of PDE3B, PDE4A, PDE4B, PDE4D, and PDE7A. We also examined the ability of rolipram (PDE4 inhibitor) or cilostamide (PDE3 inhibitor), alone or together, to induce apoptosis or elevate cyclic AMP in leukemic cells from patients with CLL. RESULTS: Rolipram increased levels of PDE4B and, to a variable extent, PDE4D. When combined with forskolin, rolipram also increased levels of a second family of PDEs, PDE3B. Addition of the specific PDE3 inhibitor, cilostamide, modestly augmented rolipram-induced apoptosis in five of seven "rolipram-resistant" CLL samples. CONCLUSIONS: Although this work confirms that PDE4 appears to be the most important PDE target for induction of apoptosis in CLL, combination therapy with PDE3 and PDE4 inhibitors or use of dual-selective drugs may be of benefit in a subset of relatively PDE4-inhibitor resistant CLL patients. (+info)
Potential role of phosphodiesterase 7 in human T cell function: comparative effects of two phosphodiesterase inhibitors. (4/27)Even though the existence of phosphodiesterase (PDE) 7 in T cells has been proved, the lack of a selective PDE7 inhibitor has confounded an accurate assessment of PDE7 function in such cells. In order to elucidate the role of PDE7 in human T cell function, the effects of two PDE inhibitors on PDE7A activity, cytokine synthesis, proliferation and CD25 expression of human peripheral blood mononuclear cells (PBMC) were determined. Recombinant human PDE7A was obtained and subjected to cyclic AMP-hydrolysis assay. PBMC of Dermatophagoides farinae mite extract (Df)-sensitive donors were stimulated with the relevant antigen or an anti-CD3 monoclonal antibody (MoAb). PBMC produced IL-5 and proliferated in response to stimulation with Df, while stimulation with anti-CD3 MoAb induced CD25 expression and messenger RNA (mRNA) synthesis of IL-2, IL-4 and IL-5 in peripheral T cells. A PDE inhibitor, T-2585, which suppressed PDE4 isoenzyme with high potency (IC50 = 0.00013 microM) and PDE7A with low potency (IC50 = 1.7 microM) inhibited cytokine synthesis, proliferation and CD25 expression in the dose range at which the drug suppressed PDE7A activity. A potent selective inhibitor of PDE4 (IC50 = 0.00031 microM), RP 73401, which did not effectively suppress PDE7A (IC50 > 10 microM), inhibited the Df- and anti-CD3 MoAb-stimulated responses only weakly, even at 10 microM. PDE7 may play a critical role in the regulation of human T cell function, and thereby selective PDE7 inhibitors have the potential to be used to treat immunological and inflammatory disorders. (+info)
Ubiquitous expression of phosphodiesterase 7A in human proinflammatory and immune cells. (5/27)We have determined the expression of phosphodiesterase (PDE) 7A1 and PDE7A2 in human cells that have been implicated in the pathogenesis of chronic obstructive pulmonary disease and asthma. Messenger RNA transcripts were detected by RT-PCR in T lymphocytes, monocytes, neutrophils, airway and vascular smooth muscle cells, lung fibroblasts, epithelial cells, and cardiac myocytes. Human epithelial, T cell, eosinophil, and lung fibroblast cell lines were also positive for PDE7A1 and PDE7A2 mRNA transcripts. By Western immunoblot analyses the amount of PDE7A1 was greatest in T cell lines, peripheral blood T lymphocytes, epithelial cell lines, airway and vascular smooth muscle cells, lung fibroblasts, and eosinophils but was not detected in neutrophils. In contrast, PDE7A2 protein, which was identified in human cardiac myocytes, was not found in any of the other cell types investigated. Immunoconfocal analyses showed that PDE7A was expressed in neutrophils and alveolar macrophages. As the expression of PDE7A mirrors the distribution of PDE4 we speculate that this enzyme could be a target for novel anti-inflammatory drugs. (+info)
Functional characterization of the human phosphodiesterase 7A1 promoter. (6/27)In this paper, the human phosphodiesterase 7A1 (h PDE7A1 ) promoter region was identified and functionally characterized. Transient transfection experiments indicated that a 2.9 kb fragment of the h PDE7A1 5'-flanking region, to position -2907, has strong promoter activity in Jurkat T-cells. Deletion analysis showed that the proximal region, up to position -988, contains major cis -regulatory elements of the h PDE7A1 promoter. This minimal promoter region contains a regulatory CpG island which is essential for promoter activity. The CpG island contains three potential cAMP-response-element-binding protein (CREB)-binding sites that, as judged by in vivo dimethyl sulphate (DMS) footprinting, are occupied in Jurkat T-cells. Moreover, over-expression of CREB results in increased promoter activity, but, on the other hand, promoter activity decreases when a dominant-negative form of CREB (KCREB) is over-expressed. In vivo DMS footprinting strongly indicates that other transcription factors, such Ets-2, nuclear factor of activated T-cells 1 (NFAT-1) and nuclear factor kappaB (NF-kappaB), might also contribute to the regulation of h PDE7A1 promoter. Finally, h PDE7A1 promoter was found to be induced by treatment with PMA, but not by treatment with dibutyryl cAMP or forskolin. These results provide insights into the factors and mechanisms that regulate expression of the h PDE7A gene. (+info)
Phosphodiesterase 7A-deficient mice have functional T cells. (7/27)Phosphodiesterases (PDEs) are enzymes which hydrolyze the cyclic nucleotide second messengers, cAMP and cGMP. In leukocytes, PDEs are responsible for depletion of cAMP which broadly suppresses cell functions and cellular responses to many activation stimuli. PDE7A has been proposed to be essential for T lymphocyte activation based on its induction during cell activation and the suppression of proliferation and IL-2 production observed following inhibition of PDE7A expression using a PDE7A antisense oligonucleotide. These observations have led to the suggestion that selective PDE7 inhibitors could be useful in the treatment of T cell-mediated autoimmune diseases. In the present report, we have used targeted gene disruption to examine the role PDE7A plays in T cell activation. In our studies, PDE7A knockout mice (PDE7A(-/-)) showed no deficiencies in T cell proliferation or Th1- and Th2-cytokine production driven by CD3 and CD28 costimulation. Unexpectedly, the Ab response to the T cell-dependent Ag, keyhole limpet hemocyanin, in the PDE7A(-/-) mice was found to be significantly elevated. The results from our studies strongly support the notion that PDE7A is not essential for T cell activation. (+info)
Genome annotation of a 1.5 Mb region of human chromosome 6q23 encompassing a quantitative trait locus for fetal hemoglobin expression in adults. (8/27)BACKGROUND: Heterocellular hereditary persistence of fetal hemoglobin (HPFH) is a common multifactorial trait characterized by a modest increase of fetal hemoglobin levels in adults. We previously localized a Quantitative Trait Locus for HPFH in an extensive Asian-Indian kindred to chromosome 6q23. As part of the strategy of positional cloning and a means towards identification of the specific genetic alteration in this family, a thorough annotation of the candidate interval based on a strategy of in silico / wet biology approach with comparative genomics was conducted. RESULTS: The ~1.5 Mb candidate region was shown to contain five protein-coding genes. We discovered a very large uncharacterized gene containing WD40 and SH3 domains (AHI1), and extended the annotation of four previously characterized genes (MYB, ALDH8A1, HBS1L and PDE7B). We also identified several genes that do not appear to be protein coding, and generated 17 kb of novel transcript sequence data from re-sequencing 97 EST clones. CONCLUSION: Detailed and thorough annotation of this 1.5 Mb interval in 6q confirms a high level of aberrant transcripts in testicular tissue. The candidate interval was shown to exhibit an extraordinary level of alternate splicing - 19 transcripts were identified for the 5 protein coding genes, but it appears that a significant portion (14/19) of these alternate transcripts did not have an open reading frame, hence their functional role is questionable. These transcripts may result from aberrant rather than regulated splicing. (+info)
Cyclic Nucleotide Phosphodiesterases, Type 1 (PDE1) are a family of enzymes that break down cyclic nucleotides, such as cyclic AMP (cAMP) and cyclic GMP (cGMP), into their corresponding monophosphates. These enzymes play a crucial role in regulating various cellular processes, including muscle contraction, neurotransmission, and immune function. In the medical field, PDE1 inhibitors are being investigated as potential treatments for a variety of conditions, including heart failure, erectile dysfunction, and neurological disorders. These inhibitors work by increasing the levels of cAMP or cGMP in the cell, leading to the activation of downstream signaling pathways that promote beneficial effects. However, PDE1 inhibitors can also have side effects, such as headache, flushing, and gastrointestinal symptoms, and their use may be limited by potential drug interactions and other safety concerns. Therefore, further research is needed to fully understand the therapeutic potential and safety profile of PDE1 inhibitors in the medical field.
3',5'-Cyclic-AMP phosphodiesterases (PDEs) are a family of enzymes that play a crucial role in regulating the levels of cyclic AMP (cAMP) in the body. cAMP is a signaling molecule that is involved in a wide range of cellular processes, including cell growth, differentiation, and metabolism. PDEs are responsible for breaking down cAMP into inactive products, thereby regulating the levels of this signaling molecule in the body. There are 11 different subtypes of PDEs, each with its own specific substrate specificity and tissue distribution. In the medical field, PDEs are of particular interest because they are involved in the regulation of many different physiological processes, including the cardiovascular system, the nervous system, and the immune system. In addition, PDEs are the targets of many drugs, including some used to treat conditions such as erectile dysfunction, asthma, and heart failure.
Cyclic Nucleotide Phosphodiesterases, Type 4 (PDE4) are a family of enzymes that break down cyclic AMP (cAMP) and cyclic GMP (cGMP) in the body. These enzymes play a crucial role in regulating various cellular processes, including inflammation, immune response, and muscle contraction. PDE4 enzymes are found in a variety of tissues, including the lungs, heart, and immune cells. They are also present in the brain, where they play a role in regulating mood and cognition. In the medical field, PDE4 inhibitors are used to treat a variety of conditions, including asthma, chronic obstructive pulmonary disease (COPD), psoriasis, and depression. These drugs work by inhibiting the activity of PDE4 enzymes, leading to an accumulation of cAMP and cGMP in the cell. This, in turn, can result in a range of therapeutic effects, depending on the tissue and condition being treated.
Cyclic Nucleotide Phosphodiesterases, Type 3 (PDE3) are a family of enzymes that play a crucial role in regulating the levels of cyclic AMP (cAMP) and cyclic GMP (cGMP) in the body. These enzymes are found in a variety of tissues, including the heart, blood vessels, and immune system. PDE3 enzymes are responsible for breaking down cAMP and cGMP, which are important signaling molecules that regulate a wide range of cellular processes, including muscle contraction, blood vessel dilation, and immune cell activation. By breaking down these molecules, PDE3 enzymes help to maintain the appropriate balance of cAMP and cGMP in the body. In the medical field, PDE3 inhibitors are often used to treat conditions such as heart failure, high blood pressure, and asthma. These drugs work by blocking the activity of PDE3 enzymes, which leads to increased levels of cAMP and cGMP in the body. This, in turn, can help to improve blood flow, relax blood vessels, and reduce inflammation, among other effects. Overall, PDE3 enzymes play a critical role in regulating the levels of cAMP and cGMP in the body, and PDE3 inhibitors are an important class of drugs used to treat a variety of medical conditions.
Cyclic Nucleotide Phosphodiesterases, Type 2 (PDE2) are a family of enzymes that break down cyclic nucleotides, such as cyclic AMP (cAMP) and cyclic GMP (cGMP), into their corresponding monophosphates. These enzymes play a crucial role in regulating various cellular processes, including signal transduction, gene expression, and metabolism. In the medical field, PDE2 inhibitors are being investigated as potential therapeutic agents for a variety of diseases, including Parkinson's disease, Alzheimer's disease, and schizophrenia. These inhibitors work by increasing the levels of cAMP and cGMP in the cell, which can lead to the activation of downstream signaling pathways and the modulation of various cellular processes. PDE2 inhibitors have also been shown to have anti-inflammatory and anti-cancer effects, and are being studied as potential treatments for inflammatory diseases and cancer. However, more research is needed to fully understand the therapeutic potential of PDE2 inhibitors and to develop safe and effective drugs for these indications.
Phosphoric diester hydrolases are a group of enzymes that catalyze the hydrolysis of phosphoric diesters, which are esters of phosphoric acid. These enzymes are involved in a variety of biological processes, including the breakdown of nucleic acids, the metabolism of lipids, and the regulation of signaling pathways. In the medical field, phosphoric diester hydrolases are important for the proper functioning of the body. For example, they are involved in the breakdown of nucleic acids, which are the building blocks of DNA and RNA. This process is essential for the replication and repair of DNA, as well as the production of proteins from genetic information. Phosphoric diester hydrolases are also involved in the metabolism of lipids, which are a type of fat that is stored in the body. These enzymes help to break down lipids into smaller molecules that can be used for energy or stored for later use. In addition, phosphoric diester hydrolases play a role in the regulation of signaling pathways, which are the communication networks that allow cells to respond to changes in their environment. These enzymes help to control the activity of signaling molecules, which can affect a wide range of cellular processes, including cell growth, differentiation, and death. Overall, phosphoric diester hydrolases are important enzymes that play a variety of roles in the body. They are involved in the breakdown of nucleic acids, the metabolism of lipids, and the regulation of signaling pathways, and are essential for the proper functioning of the body.
2',3'-Cyclic-Nucleotide Phosphodiesterases (CNP) are a family of enzymes that play a crucial role in regulating the levels of cyclic nucleotides, such as cyclic AMP (cAMP) and cyclic GMP (cGMP), in the body. These enzymes are responsible for breaking down cyclic nucleotides into their corresponding monophosphates, which are then further degraded into inorganic phosphate and ribose or guanine. Cyclic nucleotides are important signaling molecules that regulate a wide range of cellular processes, including gene expression, cell growth and differentiation, and ion channel activity. CNP enzymes are involved in the regulation of these processes by controlling the levels of cyclic nucleotides in the cell. There are several different types of CNP enzymes, including 2',3'-Cyclic-Nucleotide 3'-Phosphodiesterase (CNP), 2',3'-Cyclic-Nucleotide 5'-Phosphodiesterase (CNPB), and 2',3'-Cyclic-Nucleotide 5'-Phosphodiesterase (CNPA). These enzymes are found in a variety of tissues and cells throughout the body, including the brain, heart, and immune system. Abnormalities in the function of CNP enzymes have been linked to a number of diseases and disorders, including hypertension, heart failure, and certain types of cancer. As such, CNP enzymes are an important area of research in the field of medicine, with potential therapeutic applications in the treatment of these conditions.
In the medical field, "Nucleotides, Cyclic" refers to a class of molecules that are composed of a cyclic structure containing a nitrogenous base, a pentose sugar, and a phosphate group. These molecules are important components of DNA and RNA, which are the genetic material of all living organisms. Cyclic nucleotides are a subclass of nucleotides that have a cyclic structure formed by the condensation of the sugar and phosphate groups. They are involved in various cellular signaling pathways and have been implicated in the regulation of a wide range of physiological processes, including blood pressure, heart rate, and immune function. Examples of cyclic nucleotides include cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). These molecules are synthesized from their respective nucleoside triphosphates (ATP and GTP) by the action of enzymes called adenylate cyclase and guanylate cyclase, respectively.
3',5'-Cyclic-GMP Phosphodiesterases (cGMP-PDEs) are a family of enzymes that play a crucial role in regulating the levels of cyclic guanosine monophosphate (cGMP) in the body. cGMP is a second messenger molecule that is involved in a wide range of cellular processes, including smooth muscle relaxation, neurotransmission, and immune cell function. cGMP-PDEs are responsible for breaking down cGMP into guanosine monophosphate (GMP), thereby terminating the signaling effects of cGMP. There are 11 different subtypes of cGMP-PDEs, each with different tissue distribution and substrate specificity. In the medical field, cGMP-PDEs are of particular interest because they are targeted by a class of drugs called phosphodiesterase inhibitors (PDE inhibitors). PDE inhibitors are used to treat a variety of conditions, including erectile dysfunction, pulmonary hypertension, and glaucoma. By inhibiting cGMP-PDEs, PDE inhibitors increase the levels of cGMP in the body, leading to the desired therapeutic effects.
Cyclic Nucleotide Phosphodiesterases, Type 5 (PDE5) are a group of enzymes that break down cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP) in the body. These enzymes play a crucial role in regulating various physiological processes, including blood flow, smooth muscle contraction, and neurotransmission. In the context of sexual function, PDE5 inhibitors are a class of drugs that work by blocking the action of PDE5, thereby increasing levels of cGMP in the penis. This leads to improved blood flow to the penis and helps to achieve and maintain an erection during sexual activity. PDE5 inhibitors are commonly used to treat erectile dysfunction (ED) and are also being studied for other conditions, such as pulmonary hypertension and vision loss.
Cyclic GMP (cGMP) is a signaling molecule that plays a crucial role in regulating various physiological processes in the body, including smooth muscle contraction, neurotransmission, and blood pressure regulation. It is synthesized from guanosine triphosphate (GTP) by the enzyme guanylate cyclase and is degraded by the enzyme phosphodiesterase. In the medical field, cGMP is often studied in the context of its role in the regulation of blood vessels and the cardiovascular system. For example, cGMP is involved in the dilation of blood vessels, which helps to lower blood pressure and improve blood flow. It is also involved in the regulation of heart rate and contractility. Abnormal levels of cGMP can lead to a variety of medical conditions, including hypertension, heart failure, and erectile dysfunction. In these cases, medications that either increase or decrease cGMP levels may be used to treat the underlying condition.
Cyclic Nucleotide Phosphodiesterases, Type 7 (PDE7) are a family of enzymes that break down cyclic nucleotides, such as cyclic AMP (cAMP) and cyclic GMP (cGMP), in the body. These enzymes play a crucial role in regulating various cellular processes, including cell growth, differentiation, and apoptosis. In the medical field, PDE7 inhibitors are being studied as potential therapeutic agents for a variety of diseases, including cancer, inflammatory disorders, and neurological disorders. These inhibitors work by blocking the activity of PDE7 enzymes, leading to an accumulation of cyclic nucleotides in the cell and activation of downstream signaling pathways. PDE7 inhibitors have shown promise in preclinical studies for the treatment of various types of cancer, including breast cancer, prostate cancer, and lung cancer. They have also been shown to have anti-inflammatory effects and may have potential as treatments for inflammatory disorders such as psoriasis and rheumatoid arthritis. Additionally, PDE7 inhibitors have been shown to have neuroprotective effects and may have potential as treatments for neurological disorders such as Alzheimer's disease and Parkinson's disease.
Cyclic AMP (cAMP) is a signaling molecule that plays a crucial role in many cellular processes, including metabolism, gene expression, and cell proliferation. It is synthesized from adenosine triphosphate (ATP) by the enzyme adenylyl cyclase, and its levels are regulated by various hormones and neurotransmitters. In the medical field, cAMP is often studied in the context of its role in regulating cellular signaling pathways. For example, cAMP is involved in the regulation of the immune system, where it helps to activate immune cells and promote inflammation. It is also involved in the regulation of the cardiovascular system, where it helps to regulate heart rate and blood pressure. In addition, cAMP is often used as a tool in research to study cellular signaling pathways. For example, it is commonly used to activate or inhibit specific signaling pathways in cells, allowing researchers to study the effects of these pathways on cellular function.
Rolipram is a medication that belongs to a class of drugs called phosphodiesterase type 4 (PDE4) inhibitors. It is primarily used to treat asthma and chronic obstructive pulmonary disease (COPD) by relaxing the muscles in the airways and improving breathing. Rolipram may also be used to treat other conditions, such as psoriasis and inflammatory bowel disease, by reducing inflammation in the body. It is usually taken by mouth in the form of tablets or capsules.
1-Methyl-3-isobutylxanthine, also known as IBMX, is a chemical compound that belongs to the xanthine family. It is a selective inhibitor of the enzyme phosphodiesterase type 4 (PDE4), which is involved in the breakdown of cyclic AMP (cAMP) in cells. In the medical field, IBMX is used as a research tool to study the effects of PDE4 inhibition on various physiological processes, including inflammation, pain, and airway smooth muscle contraction. It has also been investigated as a potential treatment for a variety of conditions, including asthma, chronic obstructive pulmonary disease (COPD), and psoriasis. However, IBMX is not currently approved for use as a therapeutic agent in humans, as it can have significant side effects, including nausea, vomiting, diarrhea, and increased heart rate. Additionally, prolonged use of IBMX can lead to the development of tolerance and dependence.
Purinones are a class of organic compounds that are derived from purine, a nitrogen-containing heterocyclic base found in nucleic acids such as DNA and RNA. Purinones are important in the field of medicine because they are involved in various biological processes, including energy metabolism, cell signaling, and immune function. One of the most well-known purinones is adenosine, which is a signaling molecule that plays a role in regulating blood flow, inflammation, and neurotransmission. Adenosine is also a precursor to ATP, the primary energy currency of cells. Other purinones include hypoxanthine, xanthine, and uric acid, which are involved in the metabolism of purines and the production of uric acid, a waste product that is excreted by the kidneys. High levels of uric acid in the blood can lead to gout, a painful joint condition. Purinones are also used in the development of drugs for a variety of medical conditions, including cancer, cardiovascular disease, and inflammatory disorders. For example, the drug allopurinol is used to lower uric acid levels in people with gout, while the drug caffeine is a purine derivative that is used to stimulate the central nervous system.
In the medical field, isoenzymes refer to different forms of enzymes that have the same chemical structure and catalytic activity, but differ in their amino acid sequence. These differences can arise due to genetic variations or post-translational modifications, such as phosphorylation or glycosylation. Isoenzymes are often used in medical diagnosis and treatment because they can provide information about the function and health of specific organs or tissues. For example, the presence of certain isoenzymes in the blood can indicate liver or kidney disease, while changes in the levels of specific isoenzymes in the brain can be indicative of neurological disorders. In addition, isoenzymes can be used as biomarkers for certain diseases or conditions, and can be targeted for therapeutic intervention. For example, drugs that inhibit specific isoenzymes can be used to treat certain types of cancer or heart disease.
Calmodulin is a small, calcium-binding protein that plays a crucial role in regulating various cellular processes in the body. It is found in all eukaryotic cells and is involved in a wide range of physiological functions, including muscle contraction, neurotransmitter release, and gene expression. Calmodulin is a tetramer, meaning that it is composed of four identical subunits, each of which contains two EF-hand calcium-binding domains. When calcium ions bind to these domains, the structure of calmodulin changes, allowing it to interact with and regulate the activity of various target proteins. In the medical field, calmodulin is often studied in the context of various diseases and disorders, including cardiovascular disease, cancer, and neurological disorders. For example, abnormal levels of calmodulin have been associated with the development of certain types of cancer, and calmodulin inhibitors have been investigated as potential therapeutic agents for treating these diseases. Additionally, calmodulin has been implicated in the pathogenesis of various neurological disorders, including Alzheimer's disease and Parkinson's disease.
In the medical field, an amino acid sequence refers to the linear order of amino acids in a protein molecule. Proteins are made up of chains of amino acids, and the specific sequence of these amino acids determines the protein's structure and function. The amino acid sequence is determined by the genetic code, which is a set of rules that specifies how the sequence of nucleotides in DNA is translated into the sequence of amino acids in a protein. Each amino acid is represented by a three-letter code, and the sequence of these codes is the amino acid sequence of the protein. The amino acid sequence is important because it determines the protein's three-dimensional structure, which in turn determines its function. Small changes in the amino acid sequence can have significant effects on the protein's structure and function, and this can lead to diseases or disorders. For example, mutations in the amino acid sequence of a protein involved in blood clotting can lead to bleeding disorders.
Cyclic Nucleotide Phosphodiesterases, Type 6 (PDE6) are a family of enzymes that are responsible for breaking down cyclic nucleotides, such as cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP), in the retina of the eye. These enzymes play a crucial role in regulating the transmission of visual signals from the retina to the brain. PDE6 is a heterodimeric enzyme composed of two subunits, alpha and beta, which are encoded by different genes. The alpha subunit contains the catalytic site of the enzyme, while the beta subunit is involved in the regulation of the enzyme's activity. Mutations in the genes encoding PDE6 can cause a group of inherited eye disorders known as cone-rod dystrophies, which affect the photoreceptor cells in the retina responsible for color vision and night vision. These disorders are characterized by progressive vision loss and can lead to blindness in affected individuals.
In the medical field, nucleotides are the building blocks of nucleic acids, which are the genetic material of cells. Nucleotides are composed of three components: a nitrogenous base, a pentose sugar, and a phosphate group. There are four nitrogenous bases in DNA: adenine (A), thymine (T), cytosine (C), and guanine (G). There are also four nitrogenous bases in RNA: adenine (A), uracil (U), cytosine (C), and guanine (G). The sequence of these nitrogenous bases determines the genetic information encoded in DNA and RNA.
Dibutyryl cyclic guanosine monophosphate (db-cGMP) is a synthetic analog of cyclic guanosine monophosphate (cGMP), a signaling molecule that plays a crucial role in various physiological processes, including smooth muscle relaxation, neurotransmission, and immune cell function. Db-cGMP is a stable, long-lasting form of cGMP that can be used in research to study the effects of cGMP on cellular signaling pathways. It is often used as a tool to investigate the function of cGMP-dependent protein kinases (PKG) and other signaling proteins that are activated by cGMP. In the medical field, db-cGMP has been studied as a potential therapeutic agent for a variety of conditions, including erectile dysfunction, hypertension, and glaucoma. It has also been used in research to investigate the role of cGMP in various diseases, including cancer, cardiovascular disease, and neurodegenerative disorders.
Theophylline is a medication that is used to treat a variety of respiratory conditions, including asthma, chronic obstructive pulmonary disease (COPD), and bronchitis. It works by relaxing the muscles in the airways, making it easier to breathe. Theophylline is available in both oral and inhaled forms, and it is usually taken on a regular basis to prevent symptoms from occurring. It is important to note that theophylline can have side effects, including nausea, vomiting, and an irregular heartbeat, and it should only be taken under the supervision of a healthcare provider.
Phosphodiesterase I (PDE1) is an enzyme that breaks down cyclic nucleotides, such as cyclic AMP (cAMP) and cyclic GMP (cGMP), into their corresponding monophosphates. These cyclic nucleotides are important signaling molecules in the body that regulate various cellular processes, including muscle contraction, neurotransmission, and gene expression. PDE1 is primarily found in the brain and smooth muscle tissue, where it plays a role in regulating the levels of cAMP and cGMP. In the brain, PDE1 is involved in the regulation of learning, memory, and mood. In smooth muscle tissue, PDE1 is involved in the regulation of blood pressure and heart rate. Inhibition of PDE1 has been shown to have therapeutic potential in the treatment of various conditions, including hypertension, heart failure, and cognitive disorders. However, the use of PDE1 inhibitors can also have side effects, such as headache, nausea, and dizziness.
Cyclic Nucleotide-Gated Cation Channels (CNGCs) are a family of ion channels that are activated by the binding of cyclic nucleotides, such as cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP). These channels are found in a variety of cell types, including photoreceptor cells in the retina, olfactory sensory neurons, and neurons in the brain and spinal cord. CNGCs are responsible for mediating a number of physiological processes, including the transduction of light in the retina, the detection of odorants in the nose, and the regulation of neuronal excitability. They are also involved in a number of diseases, including retinitis pigmentosa, olfactory loss, and certain types of epilepsy. CNGCs are composed of five subunits, each of which contains a pore-forming region and a cyclic nucleotide-binding domain. When cyclic nucleotides bind to the cyclic nucleotide-binding domain, it causes a conformational change in the channel that opens the pore and allows cations to flow through. The flow of cations generates an electrical signal that can be detected by the cell.
Phosphorus-Oxygen Lyases are a group of enzymes that catalyze the transfer of a phosphate group from a donor molecule to an acceptor molecule, with the release of oxygen. These enzymes are involved in various metabolic pathways, including the breakdown of certain amino acids and the synthesis of nucleotides. In the medical field, phosphorus-oxygen lyases are of interest because they play a role in the metabolism of certain drugs and toxins, and may be involved in the development of certain diseases. For example, some phosphorus-oxygen lyases are involved in the metabolism of alcohol, and their activity may be altered in individuals with alcohol use disorder. Additionally, some phosphorus-oxygen lyases are involved in the metabolism of certain drugs, and their activity may be affected by the use of these drugs.
Milrinone is a medication that is used to treat heart failure and to improve blood flow in the body. It is a type of medication called a phosphodiesterase inhibitor, which works by relaxing the muscles in blood vessels and increasing the strength of heart contractions. Milrinone is usually given as an intravenous infusion, and it can be used to treat both acute and chronic heart failure. It is also sometimes used to treat low blood pressure during surgery.
Bucladesine is a medication that is used to treat certain types of cancer, including lung cancer and pancreatic cancer. It works by slowing the growth of cancer cells and preventing them from dividing and multiplying. Bucladesine is usually given as an injection into a vein, and it is typically administered in a hospital setting. It is important to note that bucladesine is not a cure for cancer, but it can help to slow the progression of the disease and improve the quality of life for people who are living with cancer.
Pyrrolidinones are a class of organic compounds that contain a five-membered ring with four carbon atoms and one nitrogen atom. They are commonly used in the medical field as intermediates in the synthesis of various drugs and as active ingredients in some medications. One example of a drug that contains a pyrrolidinone moiety is metformin, which is used to treat type 2 diabetes. Metformin is a biguanide, which is a class of drugs that work by reducing the amount of glucose produced by the liver and improving the body's sensitivity to insulin. Pyrrolidinones are also used as chelating agents, which are compounds that bind to metal ions and help to remove them from the body. One example of a pyrrolidinone chelating agent is dimercaprol, which is used to treat heavy metal poisoning, such as from mercury or lead. In addition to their use in medicine, pyrrolidinones have a wide range of other applications, including as solvents, plasticizers, and corrosion inhibitors.
Adenine nucleotides are a type of nucleotide that contains the nitrogenous base adenine (A) and a sugar-phosphate backbone. They are important molecules in the cell and play a crucial role in various biological processes, including energy metabolism and DNA synthesis. There are three types of adenine nucleotides: adenosine monophosphate (AMP), adenosine diphosphate (ADP), and adenosine triphosphate (ATP). AMP is the simplest form of adenine nucleotide, with only one phosphate group attached to the sugar. ADP has two phosphate groups attached to the sugar, while ATP has three phosphate groups. ATP is often referred to as the "energy currency" of the cell because it stores and releases energy through the transfer of phosphate groups. When ATP is broken down, one of its phosphate groups is released, releasing energy that can be used by the cell for various processes. When ATP is synthesized, energy is required to attach a new phosphate group to the molecule. Adenine nucleotides are involved in many cellular processes, including muscle contraction, nerve impulse transmission, and the synthesis of proteins and nucleic acids. They are also important in the regulation of gene expression and the maintenance of cellular homeostasis.
Cyclic AMP-dependent protein kinases (also known as cAMP-dependent protein kinases or PKA) are a family of enzymes that play a crucial role in regulating various cellular processes in the body. These enzymes are activated by the presence of cyclic AMP (cAMP), a second messenger molecule that is produced in response to various stimuli, such as hormones, neurotransmitters, and growth factors. PKA is a heterotetrameric enzyme composed of two regulatory subunits and two catalytic subunits. The regulatory subunits bind to cAMP and prevent the catalytic subunits from phosphorylating their target proteins. When cAMP levels rise, the regulatory subunits are activated and release the catalytic subunits, allowing them to phosphorylate their target proteins. PKA is involved in a wide range of cellular processes, including metabolism, gene expression, cell proliferation, and differentiation. It phosphorylates various proteins, including enzymes, transcription factors, and ion channels, leading to changes in their activity and function. In the medical field, PKA plays a critical role in various diseases and disorders, including cancer, diabetes, and cardiovascular disease. For example, PKA is involved in the regulation of insulin secretion in pancreatic beta cells, and its dysfunction has been implicated in the development of type 2 diabetes. PKA is also involved in the regulation of blood pressure and heart function, and its dysfunction has been linked to the development of hypertension and heart disease.
Cyclic GMP-dependent protein kinases (PKG) are a family of enzymes that play a crucial role in regulating various cellular processes, including smooth muscle contraction, neurotransmitter release, and gene expression. These enzymes are activated by the second messenger molecule cyclic guanosine monophosphate (cGMP), which is produced in response to various stimuli such as nitric oxide (NO) and other signaling molecules. PKG is a serine/threonine kinase that phosphorylates target proteins on specific amino acid residues, leading to changes in their activity or localization. The activity of PKG is tightly regulated by its subcellular localization, substrate availability, and the concentration of cGMP. In the medical field, PKG is of great interest due to its role in various diseases, including cardiovascular disease, hypertension, and erectile dysfunction. PKG inhibitors have been developed as potential therapeutic agents for these conditions, and ongoing research is exploring the potential of PKG activators as novel treatments for various diseases.
Adenylate cyclase is an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic adenosine monophosphate (cAMP), a second messenger molecule that plays a crucial role in many cellular signaling pathways. In the medical field, adenylate cyclase is often studied in the context of its role in regulating various physiological processes, including heart rate, blood pressure, and glucose metabolism. It is also involved in the regulation of hormone signaling, particularly in the endocrine system, where hormones such as adrenaline and thyroid hormones bind to specific receptors on the cell surface and activate adenylate cyclase, leading to the production of cAMP and the activation of downstream signaling pathways. Abnormalities in adenylate cyclase activity have been implicated in a number of diseases, including diabetes, hypertension, and certain forms of heart disease. As such, understanding the regulation and function of adenylate cyclase is an important area of research in the medical field.
Papaverine is a medication that is used to treat a variety of medical conditions, including erectile dysfunction, Raynaud's disease, and glaucoma. It is a vasodilator, which means that it helps to widen blood vessels and improve blood flow. Papaverine is usually administered intravenously or intramuscularly, and it can cause side effects such as headache, nausea, and dizziness. It is important to note that papaverine should only be used under the supervision of a healthcare professional.
I'm sorry, but I'm not aware of any medical term or abbreviation called "Cyclic IMP." It's possible that you may have misspelled the term or that it is a term used in a specific medical field or specialty that I am not familiar with. If you could provide more context or information about where you heard or saw this term, I may be able to provide a more accurate answer.
In the medical field, a base sequence refers to the specific order of nucleotides (adenine, thymine, cytosine, and guanine) that make up the genetic material (DNA or RNA) of an organism. The base sequence determines the genetic information encoded within the DNA molecule and ultimately determines the traits and characteristics of an individual. The base sequence can be analyzed using various techniques, such as DNA sequencing, to identify genetic variations or mutations that may be associated with certain diseases or conditions.
Colforsin is a synthetic decapeptide that mimics the action of adenosine, a naturally occurring molecule that plays a role in regulating various physiological processes in the body. It is used in the medical field as a bronchodilator, which means it helps to relax and widen the airways in the lungs, making it easier to breathe. Colforsin is typically administered as an aerosol or nebulizer solution and is used to treat conditions such as asthma, chronic obstructive pulmonary disease (COPD), and bronchitis. It works by activating adenosine receptors in the lungs, which leads to the release of calcium from the cells lining the airways, causing them to relax and open up.
Guanylate cyclase is an enzyme that plays a crucial role in the regulation of various physiological processes in the body, including blood pressure, smooth muscle contraction, and immune function. It is a membrane-bound protein that catalyzes the conversion of guanosine triphosphate (GTP) to cyclic guanosine monophosphate (cGMP), a second messenger molecule that regulates the activity of various proteins in the cell. In the cardiovascular system, guanylate cyclase is activated by nitric oxide (NO), a signaling molecule that is released by endothelial cells in response to various stimuli, such as shear stress or the presence of certain hormones. Activation of guanylate cyclase by NO leads to an increase in cGMP levels, which in turn causes relaxation of smooth muscle cells in blood vessels, leading to vasodilation and a decrease in blood pressure. Guanylate cyclase is also involved in the regulation of immune function, as it is activated by various immune cells and cytokines. Activation of guanylate cyclase by immune cells leads to the production of cGMP, which regulates the activity of immune cells and helps to maintain immune homeostasis. In addition, guanylate cyclase is involved in the regulation of various other physiological processes, such as neurotransmission, vision, and hearing. It is a key enzyme in the regulation of these processes and plays a crucial role in maintaining normal physiological function.
Cloning, molecular, in the medical field refers to the process of creating identical copies of a specific DNA sequence or gene. This is achieved through a technique called polymerase chain reaction (PCR), which amplifies a specific DNA sequence to produce multiple copies of it. Molecular cloning is commonly used in medical research to study the function of specific genes, to create genetically modified organisms for therapeutic purposes, and to develop new drugs and treatments. It is also used in forensic science to identify individuals based on their DNA. In the context of human cloning, molecular cloning is used to create identical copies of a specific gene or DNA sequence from one individual and insert it into the genome of another individual. This technique has been used to create transgenic animals, but human cloning is currently illegal in many countries due to ethical concerns.
8-Bromo Cyclic Adenosine Monophosphate (8-Br-cAMP) is a synthetic analog of cyclic adenosine monophosphate (cAMP), a signaling molecule that plays a crucial role in various cellular processes, including cell growth, differentiation, and metabolism. In the medical field, 8-Br-cAMP is used as a tool to study the effects of cAMP on cellular signaling pathways. It is often used in cell culture experiments to increase intracellular cAMP levels and investigate the downstream effects on gene expression, protein synthesis, and cellular behavior. 8-Br-cAMP is also used in some clinical applications, such as the treatment of certain types of cancer. It has been shown to inhibit the growth of some cancer cells by blocking the activity of certain enzymes involved in cell proliferation. However, more research is needed to fully understand the potential therapeutic applications of 8-Br-cAMP in medicine.
Calcium is a chemical element with the symbol Ca and atomic number 20. It is a vital mineral for the human body and is essential for many bodily functions, including bone health, muscle function, nerve transmission, and blood clotting. In the medical field, calcium is often used to diagnose and treat conditions related to calcium deficiency or excess. For example, low levels of calcium in the blood (hypocalcemia) can cause muscle cramps, numbness, and tingling, while high levels (hypercalcemia) can lead to kidney stones, bone loss, and other complications. Calcium supplements are often prescribed to people who are at risk of developing calcium deficiency, such as older adults, vegetarians, and people with certain medical conditions. However, it is important to note that excessive calcium intake can also be harmful, and it is important to follow recommended dosages and consult with a healthcare provider before taking any supplements.
Guanine nucleotides are a type of nucleotide that contains the nitrogenous base guanine. They are important components of DNA and RNA, which are the genetic material of all living organisms. In DNA, guanine nucleotides are paired with cytosine nucleotides to form the base pair G-C, which is one of the four possible base pairs in DNA. In RNA, guanine nucleotides are paired with uracil nucleotides to form the base pair G-U. Guanine nucleotides play a crucial role in the structure and function of DNA and RNA, and are involved in many important biological processes, including gene expression, DNA replication, and protein synthesis.
In the medical field, the term "cattle" refers to large domesticated animals that are raised for their meat, milk, or other products. Cattle are a common source of food and are also used for labor in agriculture, such as plowing fields or pulling carts. In veterinary medicine, cattle are often referred to as "livestock" and may be treated for a variety of medical conditions, including diseases, injuries, and parasites. Some common medical issues that may affect cattle include respiratory infections, digestive problems, and musculoskeletal disorders. Cattle may also be used in medical research, particularly in the fields of genetics and agriculture. For example, scientists may study the genetics of cattle to develop new breeds with desirable traits, such as increased milk production or resistance to disease.
Isoproterenol is a synthetic beta-adrenergic agonist that is used in the medical field as a medication. It is a drug that mimics the effects of adrenaline (epinephrine) and can be used to treat a variety of conditions, including asthma, heart failure, and bradycardia (a slow heart rate). Isoproterenol works by binding to beta-adrenergic receptors on the surface of cells, which triggers a cascade of events that can lead to increased heart rate, relaxation of smooth muscle, and dilation of blood vessels. This can help to improve blood flow and oxygen delivery to the body's tissues, and can also help to reduce inflammation and bronchoconstriction (narrowing of the airways). Isoproterenol is available in a variety of forms, including tablets, inhalers, and intravenous solutions. It is typically administered as a short-acting medication, although longer-acting formulations are also available. Side effects of isoproterenol can include tremors, palpitations, and increased heart rate, and the drug may interact with other medications that affect the heart or blood vessels.
Xanthines are a group of compounds that include caffeine, theophylline, and theobromine. They are naturally occurring alkaloids found in plants such as coffee, tea, and cocoa. In the medical field, xanthines are used as bronchodilators to treat conditions such as asthma and chronic obstructive pulmonary disease (COPD). They work by relaxing the muscles in the airways, allowing air to flow more easily. Xanthines can also be used to treat heart rhythm disorders and to prevent blood clots. However, they can have side effects such as nausea, vomiting, and increased heart rate, and may interact with other medications.
In the medical field, binding sites refer to specific locations on the surface of a protein molecule where a ligand (a molecule that binds to the protein) can attach. These binding sites are often formed by a specific arrangement of amino acids within the protein, and they are critical for the protein's function. Binding sites can be found on a wide range of proteins, including enzymes, receptors, and transporters. When a ligand binds to a protein's binding site, it can cause a conformational change in the protein, which can alter its activity or function. For example, a hormone may bind to a receptor protein, triggering a signaling cascade that leads to a specific cellular response. Understanding the structure and function of binding sites is important in many areas of medicine, including drug discovery and development, as well as the study of diseases caused by mutations in proteins that affect their binding sites. By targeting specific binding sites on proteins, researchers can develop drugs that modulate protein activity and potentially treat a wide range of diseases.
In the medical field, a catalytic domain is a region of a protein that is responsible for catalyzing a specific chemical reaction. Catalytic domains are often found in enzymes, which are proteins that speed up chemical reactions in the body. These domains are typically composed of a specific sequence of amino acids that form a three-dimensional structure that allows them to bind to specific substrates and catalyze their breakdown or synthesis. Catalytic domains are important for many biological processes, including metabolism, signal transduction, and gene expression. They are also the target of many drugs, which can be designed to interfere with the activity of specific catalytic domains in order to treat diseases.
Vinca alkaloids are a group of naturally occurring compounds derived from the Madagascar periwinkle plant (Vinca rosea). They are used in the treatment of various types of cancer, including leukemia, lymphoma, and solid tumors such as breast, ovarian, and lung cancer. Vinca alkaloids work by binding to microtubules, which are essential components of the cell's cytoskeleton. By binding to microtubules, vinca alkaloids prevent the formation of new microtubules and stabilize existing ones, leading to cell death. The most commonly used vinca alkaloids in cancer treatment are vinblastine and vincristine. These drugs are typically administered intravenously and can cause a range of side effects, including nausea, vomiting, hair loss, and peripheral neuropathy (numbness or tingling in the hands and feet). However, they are often effective in controlling the growth of cancer cells and can be used in combination with other chemotherapy drugs to improve treatment outcomes.
In the medical field, cyclic P-oxides refer to a class of organic compounds that contain a ring of atoms with a double bond between two oxygen atoms and a single bond between one of the oxygen atoms and a phosphorus atom. These compounds are also known as phosphorus oxides or phosphorus ylides. Cyclic P-oxides are often used as intermediates in organic synthesis reactions, particularly in the synthesis of heterocyclic compounds such as pyrroles, furans, and thiophenes. They can also be used as reagents in organic reactions, such as in the Staudinger reduction, which is a method for converting aldehydes and ketones into primary amines. In addition to their use in organic synthesis, cyclic P-oxides have also been studied for their potential medicinal applications. For example, some cyclic P-oxides have been shown to have antitumor activity, and they are being investigated as potential treatments for cancer. Other cyclic P-oxides have been studied for their potential to treat neurological disorders, such as Alzheimer's disease and Parkinson's disease.
Cyclic nucleotide phosphodiesterase
CGMP-specific phosphodiesterase type 5
Benjamin Weiss (scientist)
Discovery and development of phosphodiesterase 5 inhibitors
List of EC numbers (EC 3)
Pharmacology of antidepressants
Cyclic nucleotide phosphodiesterase - Wikipedia
PDE - Esterases (Phosphodi-) - Hydrolases - Enzymes - Products
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- The homeostatic role of phosphodiesterases (PDEs) as related to the intracellular levels of cAMP and cGMP was first described by Sutherland (Sutherland, Rall, 1958) who, due to this, was awarded the Nobel Prize for Physiology and Medicine in 1971. (biomedjournal.com)
- Phosphodiesterases (PDEs) hydrolyze the phosphodiester bond of cAMP and cGMP to form the inactive 5′-AMP and 5′-GMP. (biomedjournal.com)
- Fertel and Weiss, 1976) therefore preventing the inactivation of the intracellular second messengers cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) by the respective PDE subtype(s). (biomedjournal.com)
- History The cyclic nucleotides, cGMP and cAMP are essential second messengers recognized to control many mobile procedures, such as irritation. (oscars2019info.com)
- l-arginine, an NO precursor, and the phosphodiesterase (PDE) 5 inhibitor sildenafil, which potentiates cGMP, were studied in adults with sickle cell disease (SCD) who were stably on HU. (johnshopkins.edu)
- When cGMP (1000 μM) was added to the cell culture medium for 5 days the cell densities were reduced with 37% below baseline and cGMP in increased from 5.3 to 195 pmol/10 7 cells. (scirp.org)
- IBMX alone (1000 μM) reduced cell densities with 48% and elevated cGMP in (from 5.2 to 9.3 pmol/10 7 cells). (scirp.org)
- The effect of 10 μM SNP was reinforced on proliferation (from 13% to 90%) and elevation of cGMP levels (from 7.6 to 13.5 pmol/10 7 cells). (scirp.org)
- The antiproliferative effect of cGMP increased from 30% to 89% and the cGMP in increased from 240 to 480 pmol/10 7 cells. (scirp.org)
- 2005 ). cAMP and cGMP are hydrolyzed by phosphodiesterase (PDE) enzymes, and inhibitors of PDEs (PDE-Is) produce cognition-enhancing effects in animal models of cognition. (springer.com)
- In earlier investigations it was demonstrated that the adenosine-mediated flow reserve (CFR) of the left anterior descending (LAD) artery is reduced to values in the lower normal range in most diabetic patients, indicating disturbance of microvascular flow dynamics [ 7 ]. (biomedcentral.com)
- 2. Benau D., Szabo E.I., Terner C. Endogenous inhibitors of cyclic adenosine 3',5'-monophosphate-phosphodiesterase in rat epididymis. (abvpress.ru)
- 3. Razzaboni B., Terner C. Cyclic adenosine 3',5'-monophosphate-phosphodiesterases in epididymis and prostate of castrate and of aged rats. (abvpress.ru)
- Phosphodiesterase inhibitors (PDIs) have important vascular and myocardial protective effects and thus have shown therapeutic usefulness in the clinical settings for treatment of patients with heart failure, pulmonary hypertension, and coronary artery disease. (biomedjournal.com)
- The potential activity for selective phosphodiesterase inhibitors as therapeutic agents was predicted as early as 1977 by Weiss and Hait (Weiss and Hait, 1977). (biomedjournal.com)
- Type 4 phosphodiesterases (PDE4) are key cAMP-hydrolyzing enzymes, and PDE4 inhibitors are considered as immunosuppressors to various inflammatory responses. (ox.ac.uk)
- Selective phosphodiesterase (PDE) inhibitors improve the formation of hippocampus-dependent memories in several rodent models of cognition. (springer.com)
- 6. Mewe M., Bauer C.K., Müller D., Middendorff R. Regulation of spontaneous contractile activity in the bovine epididymal duct by cyclic guanosine 5'-monophosphate-dependent pathways. (abvpress.ru)
- Garg, U.C. and Hassid, A. (1989) Nitric Oxide-Generating Vasodilators and 8-Bromo-cyclic Guanosine Monophosphate Inhibit Mitogenesis and Proliferation of Cultured Rat Vascular Smooth Muscle Cells. (scirp.org)
- 1] Molecular biology of the cyclic AMP-specific cyclic nucleotide phosphodiesterases: a diverse family of regulatory enzymes. (axonmedchem.com)
- This study was designed to investigate the effects of Hunteria umbellata (HU) seeds and Cylicodiscus gabunensis (CG) stem barks aqueous extracts on key enzymes relevant to erectile dysfunction (phosphodiesterase-5 and arginase) and type-2 diabetes (α-amylase and α-glucosidase). (degruyter.com)
- In ascertaining the erectogenic and antidiabetic properties of the extracts, the effects of the extracts on activities of some enzymes relevant to erectile dysfunction (arginase and phosphodiesterase-5) and type-2 diabetes (α-amylase and α-glucosidase) were determined. (degruyter.com)
- The ability of samples' extract to inhibit some of key enzymes relevant to erectile dysfunction and type-2 diabetes could render them cheap, natural and alternative therapy with erectogenic and antidiabetic potentials. (degruyter.com)
- 2001). The substrate specificities include the enzymes which are specific for cAMP hydrolysis, those for cyclic GMP hydrolysis (Mehats et al. (biomedjournal.com)
- The just means the cell possesses to degrade the indication mediated by cyclic nucleotides is certainly through the actions of a big category of Cefdinir enzymes, the cyclic nucleotide phosphodiesterases . (oscars2019info.com)
- RORγ Inhibitor web Methylxanthines had been thought to work, in element, by inhibiting phosphodiesterases (PDEs), the enzymes accountable for cyclic nucleotide degradation. (gpr44.com)
- Chen, Z.S., Lee, K. and Kruh, G.D. (2001) Transport of Cyclic Nucleotides and Estradiol 17-Beta-d-glucuronide by Multidrug Resistance Protein 4. (scirp.org)
- The interaction with the non-selective PDE (cyclic nucleotide phosphodiesterase) inhibitor 3-isobutyl-1-methylxanthine (IBMX) was tested after three days. (scirp.org)
- We aimed to evaluate the effects of the phosphodiesterase 5 inhibitor sildenafil on CFR in diabetics with erectile dysfunction. (biomedcentral.com)
- Types of they are the PDE 3 inhibitor, cilostazol, for the treating intermittent claudication , and sildenafil, a PDE 5 inhibitor, for the treating intimate dysfunction . (oscars2019info.com)
- They are essential regulators of cyclic nucleotide signaling with diverse physiological functions. (axonmedchem.com)
- Given its ability to transport important intra- and intercellular mediators such as cyclic nucleotides and eicosanoids, the physiological repertoire of MRP4 is thought to cover platelet aggregation, cell migration and proliferation, angiogenesis, and cardiomyocyte contraction. (solvobiotech.com)
- 2] Phosphodiesterase: overview of protein structures, potential therapeutic applications and recent progress in drug development. (axonmedchem.com)
- Transformation of znuA mutant with a shuttle vector pBBR1MCS-4 containing znuA gene restored the growth in zinc chelated medium and intracellular replication in HeLa cells and macrophages to a level comparable to that of wild-type strain. (go.jp)
- Our results indicate that context-dependent recruitment of alternative intracellular signaling pathways within a single sensory neuron type conveys opposite hedonic valences, thereby providing a robust mechanism for odorant encoding and discrimination at the periphery. (plos.org)
- Clopidogrel use is associated with an increased risk of bleeding and may cause haematological adverse effects, such as thrombotic thrombocytopenic purpura, haemolytic uremic syndrome, and bone-marrow suppression, manifesting with aplastic anaemia, thrombocytopenia [ 5 ], and neutropenia [ 6 , 7 ]. (hindawi.com)
- Mroczek S, Krwawicz J, Kutner J, Lazniewski M, Kucinski I, Ginalski K, Dziembowski A. C16orf57, a gene mutated in poikiloderma with neutropenia, encodes a putative phosphodiesterase responsible for the U6 snRNA 3' end modification. (medlineplus.gov)
- A phosphodiesterase inhibitor is a drug that blocks one or more of the five subtypes of the enzyme phosphodiesterase (PDE) selectively in the brain. (biomedjournal.com)
- The cyclic nucleotide signalling Rabbit Polyclonal to MOBKL2A/B program is certainly both interlinked and complicated with a great many other pathways , their alerts getting managed by regulating the synthesis and break down of these molecules tightly. (oscars2019info.com)
- 7. Swinnen J.V., Joseph D.R., Conti M. Molecular cloning of rat homologues of the Drosophila melanogaster dunce cAMP phosphodiesterase: evidence for a family of genes. (abvpress.ru)
- An interaction annotation is composed of the interaction type, name of the interactor, assay type (e.g. (yeastgenome.org)
- Phosphodiesterase 4B negatively regulates endotoxin-activated interleukin-1 receptor antagonist responses in macrophages. (ox.ac.uk)
- Of OAM mixture or type/duration of research Irrespective, and in keeping with global research, improved glycemic control was noticed, with one research also reporting equivalent outcomes between youthful and older sufferers  and another (JUN-LAN Research 7) discovering that the addition of step-up bolus insulin to mixture therapy with IGlar and sulfonylurea improved glycemic control . (thetechnoant.info)
- Th EMRS or CRS sufferers with other types of your disease [11,16]. (gpr44.com)
- Evidence for androgen-dependent phosphodiesterase activity in rat seminal vesicle and epididymis. (abvpress.ru)
- We find that such systems naturally support different types of diffraction profiles, including spherical, ellipsoidal, and hyperbolic structures. (bvsalud.org)
- Although mechanisms operating at the level of single sensory neuron types or sensilla in the periphery have also been implicated in this process [ 14 - 21 ], the contributions of sensory neurons to mediating odorant discrimination and olfactory behavioral plasticity are not fully understood. (plos.org)
- RNA exonucleases cut off (cleave) building blocks called nucleotides one at a time from molecules of RNA (a chemical cousin of DNA). (medlineplus.gov)
- Whilst white matter (WM) injury has been the historical focus of preterm brain injury studies, there is increasing evidence of the importance for grey matter (GM) injury in this condition [ 7 ]. (biomedcentral.com)
- Two-Hybrid), annotation type (e.g., manual or high-throughput), and a reference, as well as other experimental details. (yeastgenome.org)
- Pilz, R.B. and Broderick, K.E. (2005) Role of Cyclic GMP in Gene Regulation. (scirp.org)
- Phenotype annotations for a gene are curated single mutant phenotypes that require an observable (e.g., "cell shape"), a qualifier (e.g., "abnormal"), a mutant type (e.g., null), strain background, and a reference. (yeastgenome.org)
- After feeding, ticks return to their cavity dwelling, which includes wood cracks, leaf litter, and small- and medium-size mammal nests and dens ( 2 , 7 , 8 ). (cdc.gov)
- Nevertheless, it is thought that the actual incidence of clopidogrel myelotoxicity could be somewhat underestimated [ 7 ]. (hindawi.com)
- Behavioral studies have shown that NO is involved in learning several types of tasks, some of which are remembered for days (for review, see Hawkins, 1996 ), raising the question of whether NO signaling might also be involved in L-LTP. (jneurosci.org)