An imidazole derivative which is a metabolite of the antineoplastic agents BIC and DIC. By itself, or as the ribonucleotide, it is used as a condensation agent in the preparation of nucleosides and nucleotides. Compounded with orotic acid, it is used to treat liver diseases.
A PYRIDOXAL PHOSPHATE-containing enzyme that catalyzes the transfer of a formyl group from L-GLUTAMATE to N-formimidoyl-L-glutamate and TETRAHYDROFOLATE. This enzyme may also catalyze formyl transfer from 5-formyltetrahydrofolate to L-GLUTAMATE. This enzyme was formerly categorized as EC 2.1.2.6.
An enzyme that catalyzes the conversion of aminoimidazole-4-carboxamide ribonucleotide to 5-formyl-aminoimidazole-4-carboxamide ribonucleotide in the purine de novo synthesis pathway. It requires the cofactor N(10)-FORMYLTETRAHYDROFOLATE as the formyl donor.
Enzymes that catalyze the transfer of hydroxymethyl or formyl groups. EC 2.1.2.
Nucleotides in which the purine or pyrimidine base is combined with ribose. (Dorland, 28th ed)
Enzymes that catalyze the joining of two molecules by the formation of a carbon-nitrogen bond. EC 6.3.
An enzyme that catalyzes the transfer of a formyl group from N10-formyltetrahydrofolate to N1-(5-phospho-D-ribosyl)glycinamide to yield N2-formyl-N1-(5-phospho-D-ribosyl)glycinamide and tetrahydrofolate. It plays a role in the de novo purine biosynthetic pathway.
3-((4-Amino-2-methyl-5-pyrimidinyl)methyl)-5-(2- hydroxyethyl)-4-methylthiazolium chloride.
Enzymes that catalyze the joining of glutamine-derived ammonia and another molecule. The linkage is in the form of a carbon-nitrogen bond. EC 6.3.5.
A genus of large, brightly colored SPONGES in the family Agelasidae, possessing a skeleton of spongin fibers with a core of large spicules (megascleres).
A series of heterocyclic compounds that are variously substituted in nature and are known also as purine bases. They include ADENINE and GUANINE, constituents of nucleic acids, as well as many alkaloids such as CAFFEINE and THEOPHYLLINE. Uric acid is the metabolic end product of purine metabolism.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
Enzymes that catalyze the addition of a carboxyl group to a compound (carboxylases) or the removal of a carboxyl group from a compound (decarboxylases). EC 4.1.1.
A class of enzymes that catalyze the formation of a bond between two substrate molecules, coupled with the hydrolysis of a pyrophosphate bond in ATP or a similar energy donor. (Dorland, 28th ed) EC 6.
A subgenus of Salmonella containing several medically important serotypes. The habitat for the majority of strains is warm-blooded animals.
Nucleosides in which the purine or pyrimidine base is combined with ribose. (Dorland, 28th ed)
Catalyze the hydrolysis of nucleotides with the elimination of ammonia.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
Intracellular signaling protein kinases that play a signaling role in the regulation of cellular energy metabolism. Their activity largely depends upon the concentration of cellular AMP which is increased under conditions of low energy or metabolic stress. AMP-activated protein kinases modify enzymes involved in LIPID METABOLISM, which in turn provide substrates needed to convert AMP into ATP.
An enzyme that catalyzes the phosphorylation of AMP to ADP in the presence of ATP or inorganic triphosphate. EC 2.7.4.3.
A biguanide hypoglycemic agent with actions and uses similar to those of METFORMIN. Although it is generally considered to be associated with an unacceptably high incidence of lactic acidosis, often fatal, it is still available in some countries. (From Martindale, The Extra Pharmacopoeia, 30th ed, p290)
Injections into the cerebral ventricles.
A publication issued at stated, more or less regular, intervals.
The delivery of a drug into a fluid-filled cavity of the brain.
A bibliographic database that includes MEDLINE as its primary subset. It is produced by the National Center for Biotechnology Information (NCBI), part of the NATIONAL LIBRARY OF MEDICINE. PubMed, which is searchable through NLM's Web site, also includes access to additional citations to selected life sciences journals not in MEDLINE, and links to other resources such as the full-text of articles at participating publishers' Web sites, NCBI's molecular biology databases, and PubMed Central.
(GTP cyclohydrolase I) or GTP 7,8-8,9-dihydrolase (pyrophosphate-forming) (GTP cyclohydrolase II). An enzyme group that hydrolyzes the imidazole ring of GTP, releasing carbon-8 as formate. Two C-N bonds are hydrolyzed and the pentase unit is isomerized. This is the first step in the synthesis of folic acid from GTP. EC 3.5.4.16 (GTP cyclohydrolase I) and EC 3.5.4.25 (GTP cyclohydrolase II).
A primary source of energy for living organisms. It is naturally occurring and is found in fruits and other parts of plants in its free state. It is used therapeutically in fluid and nutrient replacement.
A subtype of striated muscle, attached by TENDONS to the SKELETON. Skeletal muscles are innervated and their movement can be consciously controlled. They are also called voluntary muscles.
A 51-amino acid pancreatic hormone that plays a major role in the regulation of glucose metabolism, directly by suppressing endogenous glucose production (GLYCOGENOLYSIS; GLUCONEOGENESIS) and indirectly by suppressing GLUCAGON secretion and LIPOLYSIS. Native insulin is a globular protein comprised of a zinc-coordinated hexamer. Each insulin monomer containing two chains, A (21 residues) and B (30 residues), linked by two disulfide bonds. Insulin is used as a drug to control insulin-dependent diabetes mellitus (DIABETES MELLITUS, TYPE 1).
Maintenance of a constant blood glucose level by perfusion or infusion with glucose or insulin. It is used for the study of metabolic rates (e.g., in glucose, lipid, amino acid metabolism) at constant glucose concentration.
An antibiotic purine ribonucleoside that readily substitutes for adenosine in the biological system, but its incorporation into DNA and RNA has an inhibitory effect on the metabolism of these nucleic acids.
A subtype of GPI-anchored folate receptors that is expressed in tissues of epithelial origin. This protein is also identified as an ovarian-tumor-specific antigen.
Cell surface receptors that bind to and transport FOLIC ACID, 5-methyltetrahydrofolate, and a variety of folic acid derivatives. The receptors are essential for normal NEURAL TUBE development and transport folic acid via receptor-mediated endocytosis.
The process of cleaving a chemical compound by the addition of a molecule of water.
A ubiquitously expressed folic acid transporter that functions via an antiporter mechanism which is coupled to the transport of organic phosphates.
Inflammation of part or all of the uvea, the middle (vascular) tunic of the eye, and commonly involving the other tunics (sclera and cornea, and the retina). (Dorland, 27th ed)
Proteins which bind with RETINOL. The retinol-binding protein found in plasma has an alpha-1 mobility on electrophoresis and a molecular weight of about 21 kDa. The retinol-protein complex (MW=80-90 kDa) circulates in plasma in the form of a protein-protein complex with prealbumin. The retinol-binding protein found in tissue has a molecular weight of 14 kDa and carries retinol as a non-covalently-bound ligand.
Exclusive legal rights or privileges applied to inventions, plants, etc.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Infrequent or difficult evacuation of FECES. These symptoms are associated with a variety of causes, including low DIETARY FIBER intake, emotional or nervous disturbances, systemic and structural disorders, drug-induced aggravation, and infections.
Drugs used for their effects on serotonergic systems. Among these are drugs that affect serotonin receptors, the life cycle of serotonin, and the survival of serotonergic neurons.
Planned post-marketing studies of diagnostic, therapeutic, or prophylactic drugs, devices, or techniques that have been approved for general sale. These studies are often conducted to obtain additional data about the safety and efficacy of a product. This concept includes phase IV studies conducted in both the U.S. and in other countries.
A selective and potent serotonin-2 antagonist that is effective in the treatment of a variety of syndromes related to anxiety and depression. The drug also improves the subjective quality of sleep and decreases portal pressure.
A pharmacologic congener of serotonin that contracts smooth muscle and has actions similar to those of tricyclic antidepressants. It has been proposed as an oxytocic.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Agents that produce a soft formed stool, and relax and loosen the bowels, typically used over a protracted period, to relieve CONSTIPATION.
Lipid-containing polysaccharides which are endotoxins and important group-specific antigens. They are often derived from the cell wall of gram-negative bacteria and induce immunoglobulin secretion. The lipopolysaccharide molecule consists of three parts: LIPID A, core polysaccharide, and O-specific chains (O ANTIGENS). When derived from Escherichia coli, lipopolysaccharides serve as polyclonal B-cell mitogens commonly used in laboratory immunology. (From Dorland, 28th ed)
The relatively long-lived phagocytic cell of mammalian tissues that are derived from blood MONOCYTES. Main types are PERITONEAL MACROPHAGES; ALVEOLAR MACROPHAGES; HISTIOCYTES; KUPFFER CELLS of the liver; and OSTEOCLASTS. They may further differentiate within chronic inflammatory lesions to EPITHELIOID CELLS or may fuse to form FOREIGN BODY GIANT CELLS or LANGHANS GIANT CELLS. (from The Dictionary of Cell Biology, Lackie and Dow, 3rd ed.)
A DNA-dependent RNA polymerase present in bacterial, plant, and animal cells. It functions in the nucleoplasmic structure and transcribes DNA into RNA. It has different requirements for cations and salt than RNA polymerase I and is strongly inhibited by alpha-amanitin. EC 2.7.7.6.
A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.

Absorption, metabolism, and excretion of 14C-temozolomide following oral administration to patients with advanced cancer. (1/623)

The purpose of this study is to characterize the absorption, metabolism, and excretion of carbon 14-labeled temozolomide (14C-TMZ) administered p.o. to adult patients with advanced solid malignancies. On day 1 of cycle 1, six patients received a single oral 200-mg dose of 14C-TMZ (70.2 microCi). Whole blood, plasma, urine, and feces were collected from days 1-8 and on day 14 of cycle 1. Total radioactivity was measured in all samples. TMZ, 5-(3-methyltriazen-1-yl)imidazole-4-carboxamide (MTIC), and 4-amino-5-imidazole-carboxamide (AIC) concentrations were determined in plasma, and urine and plasma samples were profiled for metabolite/degradation products. Maximum TMZ plasma concentrations were achieved between 0.33 to 2 h (mean, 1.2 h), and half-life, apparent volume of distribution, and oral clearance values averaged 1.9 h, 17 liters/m2, and 104 ml/min/m2, respectively. A first-order absorption, one-compartment linear model, which included first-order formation of MTIC from TMZ and elimination of MTIC via degradation to AIC, and a peripheral distribution compartment for AIC, adequately described the plasma TMZ, MTIC, and AIC concentrations. MTIC systemic clearance was estimated to be 5384 ml/min/m2, and the half-life was calculated to be 2.5 min. Metabolite profiles of plasma at 1 and 4 h after treatment showed that 14C-derived radioactivity was primarily associated with TMZ, and a smaller amount was attributed to AIC. Profiles of urine samples from 0-24 h revealed that 14C-TMZ-derived urinary radioactivity was primarily associated with unchanged drug (5.6%), AIC (12%), or 3-methyl-2,3-dihydro-4-oxoimidazo[5,1-d]tetrazine-8-carboxyl ic acid (2.3%). The recovered radioactive dose (39%) was principally eliminated in the urine (38%), and a small amount (0.8%) was excreted in the feces. TMZ exhibits rapid oral absorption and high systemic availability. The primary elimination pathway for TMZ is by pH-dependent degradation to MTIC and further degradation to AIC. Incomplete recovery of radioactivity may be explained by the incorporation of AIC into nucleic acids.  (+info)

Apoptosis induced by growth factor withdrawal in fibroblasts overproducing fructose 2,6-bisphosphate. (2/623)

Fructose 2,6-bisphosphate is a potent endogenous stimulator of glycolysis. A high aerobic glycolytic rate often correlates with increased cell proliferation. To investigate this relationship, we have produced clonal cell lines of Rat-1 fibroblasts that stably express transgenes coding for 6-phosphofructo-2-kinase, which catalyzes the synthesis of fructose 2,6-bisphosphate, or for fructose 2,6-bisphosphatase, which catalyzes its degradation. While serum deprivation in culture reduced the growth rate of control cells, it caused apoptosis in cells overproducing fructose 2,6-bisphosphate. Apoptosis was inhibited by 5-amino-4-imidazolecarboxamide riboside, suggesting that 5'-AMP-activated protein kinase interferes with this phenomenon.  (+info)

Effect of AMPK activation on muscle glucose metabolism in conscious rats. (3/623)

The effect of AMP-activated protein kinase (AMPK) activation on skeletal muscle glucose metabolism was examined in awake rats by infusing them with 5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside (AICAR; 40 mg/kg bolus and 7.5 mg. kg-1. min-1 constant infusion) along with a variable infusion of glucose (49.1 +/- 2.4 micromol. kg-1. min-1) to maintain euglycemia. Activation of AMPK by AICAR caused 2-deoxy-D-[1,2-3H]glucose (2-DG) uptake to increase more than twofold in the soleus and the lateral and medial gastrocnemius compared with saline infusion and occurred without phosphatidylinositol 3-kinase activation. Glucose uptake was also assessed in vitro by use of the epitrochlearis muscle incubated either with AICAR (0.5 mM) or insulin (20 mU/ml) or both in the presence or absence of wortmannin (1.0 microM). AICAR and insulin increased muscle 2-DG uptake rates by approximately 2- and 2.7-fold, respectively, compared with basal rates. Combining AICAR and insulin led to a fully additive effect on muscle glucose transport activity. Wortmannin inhibited insulin-stimulated glucose uptake. However, neither wortmannin nor 8-(p-sulfophenyl)-theophylline (10 microM), an adenosine receptor antagonist, inhibited the AICAR-induced activation of glucose uptake. Electrical stimulation led to an about threefold increase in glucose uptake over basal rates, whereas no additive effect was found when AICAR and contractions were combined. In conclusion, the activation of AMPK by AICAR increases skeletal muscle glucose transport activity both in vivo and in vitro. This cellular pathway may play an important role in exercise-induced increase in glucose transport activity.  (+info)

5' AMP-activated protein kinase activation causes GLUT4 translocation in skeletal muscle. (4/623)

It has previously been reported that exercise causes an increase in glucose uptake in skeletal muscle and also an increase in 5' AMP-activated protein kinase (AMPK) activity. 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICA-riboside), an analog of adenosine, is taken up into cells and phosphorylated to form AICA-riboside monophosphate (ZMP), which can also activate AMPK. This study was designed to determine whether the increase in glucose uptake observed with AMPK activation by AICA-riboside is due to GLUT4 translocation from an intracellular location to the plasma membranes, similar to that seen in response to contraction. Rat hindlimbs were perfused with Krebs-Henseleit bicarbonate containing 4% bovine serum albumin, washed bovine erythrocytes, 8 mmol/l glucose, and +/-2 mmol/AICA-riboside or +/-60 nmol/l insulin. Perfusion medium containing AICA-riboside was found to significantly increase AMPK activity, glucose uptake, and GLUT4 translocation in skeletal muscle above basal levels. Insulin-perfused muscles showed significant increases in glucose uptake and GLUT4 translocation, but AMPK activation was not significantly changed from basal levels. These results provide evidence that the increased glucose uptake observed with AMPK activation by AICA-riboside in perfused rat hindlimb muscles is due to an increase in the translocation of GLUT4 to surface membranes.  (+info)

Translocation of myocardial GLUT-4 and increased glucose uptake through activation of AMPK by AICAR. (5/623)

Insulin increases glucose uptake through the translocation of GLUT-4 via a pathway mediated by phosphatidylinositol 3-kinase (PI3K). In contrast, myocardial glucose uptake during ischemia and hypoxia is stimulated by the translocation of GLUT-4 to the surface of cardiac myocytes through a PI3K-independent pathway that has not been characterized. AMP-activated protein kinase (AMPK) activity is also increased by myocardial ischemia, and we examined whether AMPK stimulates glucose uptake and GLUT-4 translocation. In isolated rat ventricular papillary muscles, 5-aminoimidazole-4-carboxyamide-1-beta-D-ribofuranoside (AICAR), an activator of AMPK, as well as cyanide-induced chemical hypoxia and insulin, increased 2-[(3)H]deoxyglucose uptake two- to threefold. Wortmannin, a PI3K inhibitor, did not affect either the AICAR- or the cyanide-stimulated increase in deoxyglucose uptake but eliminated the insulin-stimulated increase in deoxyglucose uptake. Immunofluorescence studies demonstrated translocation of GLUT-4 to the myocyte sarcolemma in response to stimulation with AICAR, cyanide, or insulin. Preincubation of papillary muscles with the kinase inhibitor iodotubercidin or adenine 9-beta-D-arabinofuranoside (araA), a precursor of araATP (a competitive inhibitor of AMPK), decreased AICAR- and cyanide-stimulated glucose uptake but did not affect basal or insulin-stimulated glucose uptake. In vivo infusion of AICAR caused myocardial AMPK activation and GLUT-4 translocation in the rat. We conclude that AMPK activation increases cardiac muscle glucose uptake through translocation of GLUT-4 via a pathway that is independent of PI3K. These findings suggest that AMPK activation may be important in ischemia-induced translocation of GLUT-4 in the heart.  (+info)

Improvement by 5-amino-4-imidazole carboxamide riboside of the contractile dysfunction that follows brief periods of ischemia through increases in ecto-5-nucleotidase activity and adenosine release in canine hearts. (6/623)

5-Amino-4-imidazole carboxamide (AICA) riboside increases adenosine release in ischemic myocardium, suggesting that AICA riboside improves contractile dysfunction. In 49 open-chest dogs, contractile function assessed by fractional shortening (FS) was observed 3 h after the onset of reperfusion following 15 min of occlusion of the left anterior descending coronary artery. During reperfusion, the treatment with AICA riboside increased adenosine concentration in the coronary venous blood (536+/-44 vs. 281+/-21 pmol/ml at 3 min of reperfusion, p<0.001) and peak coronary hyperemic flow (367+/-13 vs. 300+/-21 ml/100 g per min, p<0.001) when compared with the untreated group. FS at 3h of reperfusion increased in the AICA riboside group (21.1+/-2.3 vs. 12.8+/-0.6% in the untreated group, p<0.001). AICA riboside increased myocardial ecto-5'-nucleotidase activity. Administration of adenosine also augmented coronary hyperemic flow and increased FS to the levels of the AICA riboside group. Either 8-phenyltheophylline (an antagonist of adenosine receptors) or alpha,beta-methylene-adenosine 5'-diphosphate (an inhibitor of ecto-5'-nucleotidase) completely abolished the increased coronary hyperemic flow and improvements of myocardial contractile function due to AICA riboside. Thus it was concluded that AICA riboside improves the contractile dysfunction that follows a brief period of ischemia via adenosine-dependent mechanisms.  (+info)

Effect of methotrexate on blood purine and pyrimidine levels in patients with rheumatoid arthritis. (7/623)

OBJECTIVE: The mechanism of anti-inflammatory effects of methotrexate (MTX) at low dose may relate to a decrease in availability of the purine precursor or it may depend on accumulation of 5-aminoimidazole-4-carboxamide (AICAR) and the anti-inflammatory nucleoside adenosine. The aim of this study was to evaluate the possible mechanism of action by analysis of changes in blood concentrations of purine and pyrimidine metabolites during MTX treatment. METHODS: Venous blood samples were collected from rheumatoid arthritis patients before and at different times for up to 7 days after the start of MTX treatment. Whole blood concentrations of adenosine, uridine, hypoxanthine, uric acid and erythrocyte nucleotides were measured by HPLC. RESULTS: The initial blood adenosine concentration was 0.073 +/- 0.013 microM and no differences were observed during MTX treatment. However, a decrease in uric acid concentration was observed from 205.5+/-13.5 to 160. 9+/-13.5 microM (P<0.05) within 24 h after MTX administration. The hypoxanthine concentration decreased in parallel with uric acid, while the uridine concentration decreased 48 h after MTX administration. No accumulation of AICAR-triphosphate (ZTP) was observed in the erythrocytes. CONCLUSIONS: MTX decreases circulating purine and pyrimidine concentrations, and their availability for DNA and RNA synthesis, which may affect immune cell proliferation and protein (cytokine) expression. The absence of adenosine concentration changes and lack of ZTP formation is evidence against an AICAR/adenosine mechanism, although localized adenosine concentration changes cannot be excluded.  (+info)

Chronic activation of 5'-AMP-activated protein kinase increases GLUT-4, hexokinase, and glycogen in muscle. (8/623)

This study was designed to determine whether chronic chemical activation of AMP-activated protein kinase (AMPK) would increase glucose transporter GLUT-4 and hexokinase in muscles similarly to periodic elevation of AMPK that accompanies endurance exercise training. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR), has previously been shown to be taken up by cells and phosphorylated to form a compound (5-aminoimidazole-4-carboxamide ribonucleotide) that mimics the effect of AMP on AMPK. A single injection of AICAR resulted in a marked increase in AMPK in epitrochlearis and gastrocnemius/plantaris muscles 60 min later. When rats were injected with AICAR (1 mg/g body wt) for 5 days in succession and were killed 1 day after the last injection, GLUT-4 was increased by 100% in epitrochlearis muscle and by 60% in gastrocnemius muscle in response to AICAR. Hexokinase was also increased approximately 2. 5-fold in the gastrocnemius/plantaris. Gastrocnemius glycogen content was twofold higher in AICAR-treated rats than in controls. Chronic chemical activation of AMPK, therefore, results in increases in GLUT-4 protein, hexokinase activity, and glycogen, similarly to those induced by endurance training.  (+info)

Abstract In the present study, the effect of 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) on long-chain fatty acid oxidation by hepatocytes isolated from suckled neonatal pig liver (a low ketogenic and lipogenic tissue) was tested. Incubation of hepatocytes with AICAR (0.5 mM) in the presence of 1 mM of carnitine and 10 mM of glucose for 1 hour at 37and#176;C had no significant effect on total [1-14C]-palmitate (0.5 mM) oxidation (14CO2 and 14C-Acid soluble products (ASP)). Consistent with the fatty acid oxidation, carnitine palmitoyltransferase I activity and inhibition of its activity by malonyl-CoA (10 and#956;M) assayed in cell homogenate also remained constant. However, addition of AICAR to the hepatocytes decreased 14CO2 production by 18% compared to control (p andlt; 0.06). The reduction of labeled carboxylic carbon accumulated in CO2 caused a significant difference in distribution of oxidative products between 14CO2 and 14C-ASP (p andlt; 0.03) compared with the control. It was ...
We tested the hypothesis that repeated activation of AMPK induces mitochondrial and glucose membrane transporter gene/protein expression via a peroxisome proliferator activated receptor Upsilon co-activator (PGC)-1alpha dependent mechanism. Whole body PGC-1alpha knockout (KO) and littermate wild type (WT) mice were given either a single or repeated subcutaneous injection of the AMPK activator AICAR or saline. Skeletal muscles were dissected either 1h or 4h after the single AICAR treatment or 24h after the last injection following the repeated AICAR treatment. Repeated AICAR treatment increased GLUT4, cytochrome c oxidase (COX)I and cytochrome (cyt) c protein expression ~10-40% relative to saline in white muscles of the WT mice, but not of the PGC-1alpha KO mice. In line, GLUT4 and cyt c mRNA content increased 30-60% 4h after a single AICAR injection relative to saline only in WT mice. One hour after a single AICAR treatment, phosphorylation of AMP-activated protein kinase (AMPK) and the ...
BACKGROUND: Insulin-induced microvascular recruitment is important for optimal muscle glucose uptake. 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR, an activator of AMP-activated protein kinase), can also induce microvascular recruitment, at doses that do not acutely activate glucose transport in rat muscle. Whether low doses of AICAR can augment physiologic insulin action is unknown. In the present study we used the euglycemic hyperinsulinemic clamp to assess whether insulin action is augmented by low dose AICAR. METHODS: Anesthetized rats were studied during saline infusion or euglycemic insulin (3 mU/kg/min) clamp for 2 h in the absence or presence of AICAR for the last hour (5 mg bolus followed by 3.75 mg/kg/min). Muscle glucose uptake (Rg) was determined radioisotopically with (14)C-2-deoxyglucose and muscle microvascular perfusion by contrast-enhanced ultrasound with microbubbles. RESULTS: AICAR did not affect blood glucose, or lower leg Rg, although it significantly (p | 0.05)
The present study is the first demonstration that administration of AICAR to insulin-resistant HF rats simultaneously increases glucose and FA uptake into skeletal muscle in close association with activation of AMPK. These effects occurred preferentially in white muscle and were consistent with the previously described improvement of insulin sensitivity in white muscle 24 h after AICAR treatment (8). Contrary to our initial speculation, there was no higher FA uptake in red muscle to balance the lack of AICAR effect on glucose uptake in this muscle type.. It is known that fluxes of glucose and FA into muscle are increased from the circulation during exercise (1,23,24). Recent studies have revealed an important role of AMPK in exercise-induced changes in fuel metabolism (1,2). However, many other factors are also important metabolic regulators in contracting muscle (7), such as decreased energy storage (ATP and creatine phosphate content) (25), increases in metabolic rate, muscle blood flow, and ...
The report generally describes 4-amino-5-imidazolecarboxamide hydrochloride, examines its uses, production methods, patents. 4-Amino-5-imidazolecarboxamide
AMP-activated kinase is a cellular energy sensor which is activated in stages of increased ATP consumption. Its activation has been associated with a number of beneficial effects such as decreasing inflammatory processes and the disease progress of diabetes and obesity, respectively. Furthermore, AM …
5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR) is an established pharmacological activator of AMP-activated protein kinase (AMPK). Both, AICAR and AMPK were reported to attenuate inflammation. However, AICAR is known for many AMPK-independent effects, although the mechanisms remain incompletely understood. Here we report a potent suppression of lipopolysaccharide (LPS)-induced inflammatory gene expression by AICAR in primary human macrophages, which occurred independently of its conversion to AMPK-activating 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranosyl monophosphate. Although AICAR did not interfere with activation of cytosolic signalling cascades and nuclear translocation of nuclear factor - κB (NFκB) by LPS, it prevented the recruitment of NFκB and RNA polymerase II to target gene promoters. AICAR also inhibited signal transducer and activator of transcription 3 (STAT3)-dependent induction of interleukin (IL) IL-6 and IL-10 targets, while leaving STAT6 and HIF1α-dependent gene
No hope of ever seeing this in bulk is there? Its outrageously expensive in small amounts now. AMP-kinase activation with AICAR simultaneously
Effects of an AICAR treatment on the differentiation of MC3T3-E1 cells. AICAR (0.5 mM), a AMP kinase stimulator, was added after the cells reached confluency. T
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor. - Mechanism of Action & Protocol.
Ultraviolet (UV) radiation and reactive oxygen species (ROS) impair the physiological functions of retinal pigment epithelium (RPE) cells by inducing cell apoptosis, which is the main cause of age-related macular degeneration (AMD). The mechanism by which UV/ROS induces RPE cell death is not fully addressed. Here, we observed the activation of a ceramide-endoplasmic reticulum (ER) stress-AMP activated protein kinase (AMPK) signaling axis in UV and hydrogen peroxide (H2O2)-treated RPE cells. UV and H2O2 induced an early ceramide production, profound ER stress and AMPK activation. Pharmacological inhibitors against ER stress (salubrinal), ceramide production (fumonisin B1) and AMPK activation (compound C) suppressed UV- and H2O2-induced RPE cell apoptosis. Conversely, cell permeable short-chain C6 ceramide and AMPK activator AICAR (5-amino-1-β-D-ribofuranosyl-imidazole-4-carboxamide) mimicked UV and H2O2s effects and promoted RPE cell apoptosis. Together, these results suggest that UV/H2O2 activates the
The present study demonstrates an apparent insulin-sensitizing effect of the AMPK activator AICAR 24 h after its administration in the insulin-resistant HF rat. A major contributor to this was an improvement in insulin-mediated suppression of HGO. In addition, insulin action was enhanced in muscle, with a greater relative enhancement in white compared with red muscle. In both tissues, these effects were associated with a decrease in the concentration of malonyl CoA and in liver a decrease in the concentration of triglyceride. Although our investigation focused on AICAR effects in the insulin-resistant HF rat, follow-up studies demonstrated that at least some insulin-sensitizing effects after AICAR injection also occur in normal rats that were fed a standard diet, notably also with significant enhancement of insulin-stimulated glucose uptake in white muscle.. AMPK plays a crucial role in mediating glucose and lipid metabolism during exercise (2,26,28). A previous study from our laboratory showed ...
Our results show that, even in LKB1-null tumor cells, activation of AMPK is sufficient for cell-cycle arrest, and necessary for the arrest induced by Ca2+-elevating agents. Inhibition of cell proliferation and G1 arrest in response to AMPK activation has been demonstrated previously in cells expressing LKB1 (12-14). However, those studies relied on the use of the pharmacologic activator 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR), which can have AMP-independent off-target effects (42), or on overexpression of activated AMPK, which might also lead to nonphysiologic effects. Our results show that the G1 arrest (25) and consequent inhibition of proliferation (24) caused by the reexpression of LKB1 in LKB1-null tumor cells is mediated by AMPK and not by any of the AMPK-related kinases (ARK). We have previously shown that the ARKs that have detectable activity in HeLa cells, that is, SIK1, SIK2, SIK3, NUAK2, MARK1, MARK2/3, and MARK4, were (unlike AMPK) not activated in the cells by ...
Attention! In the May issue of Drug Testing and Analysis (Thevis. 2011), Mario Thevis and his colleagues from the Center for Preventive Doping Research - Institute of Biochemistry at the German Sport University in Cologne report that the powdered form of AICAR they had purchased from dubious Internet sources along with GW1516 another AMPK agonist and PPARδ modulator and a SARM (MK-2866), back in 2010, and which had passed customs mislabeled as containing amino acids and green tea extract did in fact contain the inosine monophosphate intermediate 5-Aminoimidazole-4-carboxamide ribotide. Yet, of the 100mg of white powder the scientists received, only 45% contained the active ingredient. In this context it is also noteworthy, that a) AICAR is not yet approved as a drug by any federal agency, I know of, so that your doctor could not even prescribe it at the moment and b) it is not even likely that it will ever be approved, because BigPharma wont be interested in a naturally occurring and thus ...
60 caps X 5 mg. Each capsules contains 5mg. AICAR (chemical name: 5-Aminoimidazole-4-carboxamide ribonucleotide) is a peptide, which is an intermediate within the generation of inosine monophosphate and directly related to metabolic regulation. The most important mechanism that AICAR is known for is its ability to block enzymes both in intracellular and extracellular levels, which, in turn, allows for an accelerated stimulation of glucose uptake and increase protein kinases in skeletal muscle tissue. These two functions allow for more energy conversion, which helps burn fat and also sustain output in activity. This is what scientists and athletes/bodybuilders are interested in, but there are some amazing side effects.. Interestingly, AICAR has been shown to protect against ischemic injury. This type of injury is directly related to the restriction of blood to tissues, which can cause insufficient amounts of oxygen and glucose needed to keep the tissue alive. This can lead to thrombosis, ...
Product Number , 74454497. CAS Number , 72-40-2. EC , 200-778-3. Molecular Formula , C4H6N4OHCl. Molecular Weight , 162.58. Storage Temp , Harmonized Tariff code , 29332990. Signal Word , ...
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Background: 17-β-estradiol has been shown to play an important role in regulating vascular function and vasomotor tone. We have previously demonstrated sex differences in rapid estrogen receptor signaling during vascular relaxation. We recently observed that estrogen activates AMPK-activated protein kinase (AMPK), suggesting that AMPK is a likely mediator of estrogen receptor (ER) signaling in vasomotor function. AMPK has been reported to participate in vascular relaxation. Furthermore, our recent studies found that incubating vascular rings with 5-aminoimidazole-4-carboxamide (AICAR), an AMPK activator, results in greater vasorelaxation of female C57BL/6J mouse vessels when compared with male vessels. However, the precise mechanisms involving estrogen receptor signaling and AMPK in promoting vascular relaxation remain unknown.. Methods and Results: To elucidate a critical role of ERα-AMPK signaling and downstream targets involved in vascular relaxation, including the potential sex difference ...
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Effects of siRNA-AdipoR1 transfection or AICAR treatments on Osterix mRNA expression in MC3T3-E1 cells. Total RNA was collected at 4, 7, 10 days after siRNA-Adi
Searching for some dosing information for the AICAR in the Ripped to the Bone Stack on Research Peptides.. http://www.precisionpeptides.com/store/Stacks/Ripped%20to%20the%20Bone%20Stack.html I am good with everything else, but I am not too familiar with this and cannot find anything on it, or I am not looking in the right place. This will be my first Peptide Cycle also.. If this is a better option, please weigh in..
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TY - JOUR. T1 - Aminoimidazole carboxamide ribonucleotide ameliorates experimental autoimmune uveitis. AU - Suzuki, Jun. AU - Yoshimura, Takeru. AU - Simeonova, Marina. AU - Takeuchi, Kimio. AU - Murakami, Yusuke. AU - Morizane, Yuki. AU - Miller, Joan W.. AU - Sobrin, Lucia. AU - Vavvas, Demetrios G.. PY - 2012/6/1. Y1 - 2012/6/1. N2 - PURPOSE. To investigate the anti-inflammatory effect of an adenosine monophosphate (AMP) analog, aminoimidazole carboxamide ribonucleotide (AICAR), in experimental autoimmune uveoretinitis (EAU). METHODS. C57BL/6 mice were injected daily with AICAR (200 mg/kg, intraperitoneally [IP]) from day 0, the day of interphotoreceptor retinoid-binding protein (IRBP) immunization, until day 21. The severity of uveitis was assessed clinically and histopathologically. T-cell proliferation and cytokine production of IFN-γ, IL-17, and IL-10 in response to IRBP stimulation were determined. In addition, regulatory T-cell (Treg) populations were measured. Co-stimulatory molecule ...
The 5′ adenosine monophosphate-activated protein kinase (AMPK) is a heterotrimeric, evolutionary conserved enzyme which has emerged as a critical regulator of skeletal muscle cellular bioenergetics. AMPK is activated by both chemical (adipokines) and mechanical (stretch, contraction) stimuli leading to metabolic changes within muscle cells that include increased fatty acid oxidation, glucose uptake and glycolysis, as well as the stimulation and regulation of mitochondrial biogenesis. Collectively these acute responses and chronic adaptations act to reduce cellular disturbances, resulting in tighter metabolic control and maintenance of energy homeostasis. This brief review will describe the structure, function and activation of AMPK in skeletal muscle and how this ubiquitous molecule may be a plausible target for the treatment of several lifestyle-related metabolic disorders.
TY - JOUR. T1 - Inhibition of AMP-activated protein kinase at the allosteric drug-binding site promotes islet insulin release. AU - Scott, John W. AU - Galic, Sandra. AU - Graham, Kate L. AU - Foitzik, Richard. AU - Ling, Naomi X Y. AU - Dite, Toby A. AU - Issa, Samah M A. AU - Langendorf, Chris G. AU - Weng, Qing Ping. AU - Thomas, Helen E. AU - Kay, Thomas W. AU - Birnberg, Neal C. AU - Steinberg, Gregory R. AU - Kemp, Bruce E. AU - Oakhill, Jonathan S. PY - 2015. Y1 - 2015. N2 - The AMP-activated protein kinase (AMPK) is a metabolic stress-sensing αβγ heterotrimer responsible for energy homeostasis. Pharmacological inhibition of AMPK is regarded as a therapeutic strategy in some disease settings including obesity and cancer; however, the broadly used direct AMPK inhibitor compound C suffers from poor selectivity. We have discovered a dihydroxyquinoline drug (MT47-100) with novel AMPK regulatory properties, being simultaneously a direct activator and inhibitor of AMPK complexes containing ...
Mitochondrial DNA (mtDNA) deletions occur sporadically in zygotic and somatic tissues and reach their highest concentration in substantia nigra. Previously, we noted the increase of the adenosine monophosphate (AMP)-activated protein kinase (AMPK) transcript by microarray in multiple cells and tissues bearing deletions. In this work, we demonstrate that the induction of AMPK transcript is dependent on deletions by quantitative polymerase chain reaction, and also demonstrate a deficiency in adenosine triphosphate (ATP) synthesis in the same cells. Consistent with AMPK induction, its known targets SREBF1 (sterol regulatory element binding protein-1) and ATG12 were inhibited and induced, respectively. AMPK induction is known to decrease secretory processes in some cells, and the secretion of both osteoprotegerin (OPG) and fibronectin (FN) proteins to the extracellular space was significantly deficient. Deletions caused a defect in the adenosine diphosphate (ADP)-ribosylation factor-like 2 (ARL2) ...
Looking for online definition of 5-aminoimidazole ribose 5-phosphate in the Medical Dictionary? 5-aminoimidazole ribose 5-phosphate explanation free. What is 5-aminoimidazole ribose 5-phosphate? Meaning of 5-aminoimidazole ribose 5-phosphate medical term. What does 5-aminoimidazole ribose 5-phosphate mean?
Exercise-induced glucose uptake in skeletal muscle is mediated by an insulin-independent mechanism, but the actual signals to glucose transport in response to muscle contraction have not been identified. The 5´-AMP-activated protein kinase (AMPK) has emerged as a putative mediator of contraction-induced glucose transport, although no conclusive evidence has been provided so far. Recent experiments in AMPK transgenic mice suggest that glucose transport induced by 5-amino-4-imidazolecarboxamide riboside (AICAR) or hypoxia is mediated by AMPK. In contrast, contraction-induced glucose transport in rodent skeletal muscle induced by electrical stimulation in vitro or in situ is not influenced or is only partially reduced by abolishing both or one of the catalytic AMPK subunits. This is compatible with exercise studies done in humans, where no tight correlation is found between AMPK activity and glucose uptake during exercise. Taken together, these results question an essential role of AMPK in ...
Mammalian AMP-activated protein kinase presents strong structural and functional similarities with the yeast sucrose non-fermenting 1 (Snf1) kinase involved in the derepression of glucose-repressed genes. It is now clearly established that AMP-activated protein kinase in the liver decreases glycolytic/lipogenic gene expression as well as genes involved in hepatic glucose production. This is achieved through a decreased transcriptional efficiency of transcription factors such as sterol-regulatory-element-binding protein-1c, carbohydrate-response-element-binding protein, hepatocyte nuclear factor 4α or forkhead-related protein. Clearly, the long-term consequences of AMP-activated protein kinase activation have to be taken into account if activators of this enzyme are to be designed as anti-diabetic drugs.. ...
TY - JOUR. T1 - Regulation of adenosine 5,monophosphate-activated protein kinase and lipogenesis by androgens contributes to visceral obesity in an estrogen-deficient state. AU - McInnes, Kerry. AU - Corbould, Anne Margaret. AU - Simpson, Evan R. AU - Jones, Margaret E. PY - 2006. Y1 - 2006. UR - http://www.scopus.com/record/display.url?eid=2-s2.0-33751517959&origin=resultslist&sort=plf-f&src=s&st1=protein+kinase+and+lipogenesis+by+androgens+co. U2 - 10.1210/en.2006-0879. DO - 10.1210/en.2006-0879. M3 - Article. VL - 147. SP - 5907. EP - 5913. JO - Endocrinology. JF - Endocrinology. SN - 0013-7227. IS - 12. ER - ...
AICA-Riboside - CAS 2627-69-2 - Calbiochem AICA-Riboside, CAS 2627-69-2, is a cell-permeable nucleoside compound whose phosphorylated metabolite activates AMPK and acts as a regulator of de novo purine synthesis. - Find MSDS or SDS, a COA, data sheets and more information.
Activation of AMP-activated protein kinase (AMPK) is considered a valid strategy for the treatment of type 2 diabetes. However, despite the importance of adipose tissue for whole-body energy homeostasis, the effect of AMPK activation in adipocytes has only been studied to a limited extent and mainly with the AMP-mimetic 5-aminoimidazole-4-carboxamide-1-b-d-ribofuranoside (AICAR), which has limited specificity. The aim of this study was to evaluate the effect of the allosteric AMPK activators A‑769662 and 991 on glucose uptake in adipocytes. For this purpose, primary rat or human adipocytes, and cultured 3T3-L1 adipocytes, were treated with either of the allosteric activators, or AICAR, and basal and insulin-stimulated glucose uptake was assessed. Additionally, the effect of AMPK activators on insulin-stimulated phosphorylation of Akt and Akt substrate of 160 kDa was assessed. Furthermore, primary adipocytes from ADaM site binding drug-resistant AMPKb1 S108A knock-in mice were employed to ...
AICAR accumulates in a purH mutant and inhibits the conversion of AIR to HMP, a step catalyzed by the SAM radical protein ThiC (14). The ThiC reaction has been reconstituted in vitro and is not affected by AICAR, indicating the effect in vivo was indirect (26). The present study was initiated to determine the mechanism by which AICAR accumulation inhibits the conversion of AIR to HMP.. The ThiC reaction uses SAM as a cosubstrate and is sensitive to fluctuations in CoA levels in vivo (14, 23, 24, 50). Nutritional studies led to the hypothesis that one metabolic consequence of AICAR accumulation was decreased CoA levels. Metabolite pool measurements confirmed that strains that accumulated AICAR had ∼3-fold-lower total CoA levels than the wild type. Although this level of CoA reduction does not generate a thiamine requirement in an otherwise wild-type strain, conditions that reduce flux through the purine biosynthetic pathway (i.e., adenine in the medium) increase the CoA requirement for thiamine ...
The protein kinase AMPK (adenosine monophosphate-activated protein kinase) directly monitors cellular energy stores as reflected by changes in cellular concentrations of AMP, adenosine diphosphate (ADP), and adenosine triphosphate (ATP). Through phosphorylation of its targets, it helps to control metabolism, polarity, autophagy, and the restraint of cell proliferation. Activation of AMPK is also proposed to be beneficial for the treatment of diseases, including cancer and diabetes. Hawley et al. (see the Perspective by Shaw and Cantley) report that AMPK can be activated by high concentrations of salicylate, a compound derived from the very commonly used drug aspirin. In mice, salicylate promoted fatty acid and carbohydrate metabolism in an AMPK-dependent fashion.. S. A. Hawley, M. D. Fullerton, F. A. Ross, J. D. Schertzer, C. Chevtzoff, K. J. Walker, M. W. Peggie, D. Zibrova, K. A. Green, K. J. Mustard, B. E. Kemp, K. Sakamoto, G. R. Steinberg, D. G. Hardie, The ancient drug salicylate directly ...
Regular exercise can protect the heart against external stimuli, but the mechanism is not well comprehended. sympathetic nervous system and the consequent launch of catecholamines, which stimulate the -adrenergic receptors in the heart, are very important. Isoproterenol (ISO), a nonselective -adrenergic receptor agonist, can robustly induce cardiac fibrosis in animal models. As well, transgenic mice with cardiac overexpressing -adrenergic receptors showed cardiac fibrosis [1]. Exercise teaching offers been shown to reduce fibrosis and matrix metalloproteinase dysregulation in the heart of aged rats [2]. However, the mechanism by which exercise teaching alleviates cardiac redesigning remains elusive. Adenosine monophosphate-activated protein kinase (AMPK) is an evolutionarily conserved serine/threonine protein kinase that is a expert regulator of energy status from your single-cell to whole-body levels [3]. AMPK can be triggered by conditions that increase intracellular AMP such as exercise [4], ...
If you have problems with a majority of the weight loss pillars, you might consider increasing the activity of a key cellular switch: AMPK (adenosine monophosphate-activated protein kinase). AMPK is… ...
TY - JOUR. T1 - Structural Insight into AMPK Regulation. T2 - ADP Comes into Play. AU - Jin, Xiangshu. AU - Townley, Robert. AU - Shapiro, Lawrence. PY - 2007/10/16. Y1 - 2007/10/16. N2 - The AMP-activated protein kinase (AMPK), a sensor of cellular energy status found in all eukaryotes, responds to changes in intracellular adenosine nucleotide levels resulting from metabolic stresses. Here we describe crystal structures of a heterotrimeric regulatory core fragment from Schizosaccharomyces pombe AMPK in complex with ADP, ADP/AMP, ADP/ATP, and 5-aminoimidazole-4-carboxamide 1-β-D-ribofuranotide (AICAR phosphate, or ZMP), a well-characterized AMPK activator. Prior crystallographic studies had revealed a single site in the γ subunit that binds either ATP or AMP within Bateman domain B. Here we show that ZMP binds at this site, mimicking the binding of AMP. An analogous site in Bateman domain A selectively accommodates ADP, which binds in a distinct manner that also involves direct ligation to ...
The AMP-activated protein kinase (AMPK) is an evolutionarily conserved sensor of cellular energy status, and recent data demonstrate that it also plays a critical role in systemic energy balance. AMPK integrates nutritional and hormonal signals in peripheral tissues and the hypothalamus. It mediates …
AMP-activated protein kinase (AMPK) is an evolutionally conserved protein kinase that serves as an energy guardian to help cells adapt to various metabolic stress including hypoxia. Because the role of AMPK in cancers has not been fully elucidated, in this study we investigated the expression and activation of AMPK in lung adenocarcinoma (LADC) cells and tissue ...
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Role of AMPK2 in basal, training-, and AICAR-induced GLUT4, hexokinase II, and mitochondrial protein expression in mouse muscle Am J Physiol Endocrinol Metab 292: E331-E339, 2007. First published September 5, 2006; doi:10.1152/ajpendo.00243.2006.- We investigated the role of AMPK2 in basal, exercise training-, and AICAR-induced protein expression of GLUT4, hexokinase II (HKII), mitochondrial markers, and AMPK…
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Connexios Life Sciences and Boehringer Ingelheim are collaborating on the development of AMP-activated protein kinase (AMPK) stimulants for the treatment of
Of interest were the observations that after cells had accumulated ZMP, and AICAR was removed or 5-iodotubercidin was added, the intracellular ZMP level rapidly decreased and the augmentation of folate transport was reversed. Hence, continued synthesis of ZMP is required to sustain intracellular ZMP levels and the augmentation of RFC-mediated transport. Neither AICAR itself nor ZTP within the cells resulted in augmentation of folate transport. The basis for the rapid decrease of intracellular ZMP under these conditions is due in part to the conversion of ZMP to ZTP and to export mediated by RFC. It is also possible that a component of the decrease in cell ZMP was due to rapid hydrolysis back to the base.. This interaction between ZMP and folates at the level of a common carrier is a classic exchange reaction in which the transmembrane gradient for one substrate drives the uphill transport of another. Most uphill systems for members of the SLC superfamily of solute transport carriers derive their ...
AMPK alpha 1 + AMPK alpha 2小鼠单克隆抗体[34.2](ab80039)可与小鼠, 大鼠, 人, 果蝇样本反应并经WB, IP, ELISA, IHC, ICC/IF实验严格验证,被4篇文献引用并得到5个独立的用户反馈。
AMPK signaling pathway, a fuel sensor and regulator, promotes ATP-producing and inhibits ATP-consuming pathways in various tissues. AMPK is a heterotrimer composed of alpha-catalytic and beta and gamma-regulatory subunits. Humans and rodents have two alpha and beta and three gamma isoforms; some genes are subject to alternative splicing increasing the range of possible heterotrimer combinations. Cellular stresses that inhibit ATP production or increase its consumption change the AMP:ATP ratio and activate the pathway. AMPK activation by AMP is not completely understood; the current model states that binding of AMP to the gamma subunit leads to conformational changes that allosterically activate AMPK and render phosphorylated-Thr172 unavailable for inhibitory dephosphorylation. ATP antagonizes the effect of AMP; both AMP and ATP bind in a mutually exclusive manner to the Bateman (CBS) domains of the gamma subunit. The upstream kinase, known as Lkb1, is a complex of one catalytic and two ...
0001 Vynález sa týka zlúčenin, ktoré sú priamymi aktivátormi AMPK (AMPaktivovanej proteínkinázy) a ich použitia pri liečení porúch regulovaných deaktiváciou AMPK. Napríklad zlúčeniny podľa vynálezu sú použiteľné naDoterajší stav techniky a úvod vynálezu0002 AMPK je dobre zavedený ako senzor a regulátor homeostázy bunkovej energie (Hardie D. G. a Hawley S. A., AMP-activated protein kinase the energy charge hypothesis revisited Bioassays, 23, 1112, (2001), Kemp B. E. a kol. AMP-activated protein kinase, super metabolic regulator, Biochem Soc. Transactions, 31. 162 (2003. Alosterická aktivácia tejto kinázy vdaka zvýšeniu množstva AMP vedie k stavom svyčerpaním bunkovej energie. Výsledná fosforylácia serínu/treoninu cieľových enzýmov vedie kadaptácii bunkového metabolizmu na nízkoenergetický stav. Celkový efekt zmien vyvolaných aktiváciou AMPK je inhibícia procesov spotrebovávajúcich ATP a aktivácia metabolických ciest vytvárajúcich ATP, a ...
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The mammalian 5-AMP-activated protein kinase (AMPK) is a heterotrimericprotein consisting of alpha-, beta-, and gamma-subunits. The alpha-subunitis the catalytic subunit and is related to the yeast Snf1p kinase. In thisstudy, we report the cloning of full-length cDNAs for the non-catalyticbeta- and gamma-subunits. The rat liver AMPK beta-subunit clone predicts aprotein of 30,464 Da, which is related to the Sip1p, Sip2p, and Gal83psubfamily of yeast proteins that interact with Snf1p and are involved inglucose regulation of gene expression. The AMPK beta-subunit, whenexpressed in bacteria and in mammalian cells, migrates anomalously on SDSgels at an apparent molecular mass of 40 kDa. Rat and human liver AMPKgamma-subunit clones predict a protein of 37,577 Da (AMPK-gamma1), whichis related to the yeast Snf4p protein that copurifies with Snf1p and to alarger family of other human AMPK gamma-isoforms. The mRNAs for both AMPK-beta and AMPK-gamma1 are widely expressed in rat tissues, consistent witha ...
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In cancer cells, the epithelial-mesenchymal transition (EMT) confers the ability to invade basement membranes and metastasize to distant sites, establishing it as an appealing target for therapeutic intervention. Here, we report a novel function of the master metabolic kinase AMPK in suppressing EMT by modulating the Akt-MDM2-Foxo3 signaling axis. This mechanistic link was supported by the effects of siRNA-mediated knockdown and pharmacological activation of AMPK on epithelial and mesenchymal markers in established breast and prostate cancer cells. Exposure of cells to OSU-53, a novel allosteric AMPK activator, as well as metformin and AICAR, was sufficient to reverse their mesenchymal phenotype. These effects were abrogated by AMPK silencing. Phenotypic changes were mediated by Foxo3a activation, insofar as silencing or overexpressing Foxo3a mimicked the effects of AMPK silencing or OSU-53 treatment on EMT, respectively. Mechanistically, Foxo3a activation led to the transactivation of the ...
AMP-activated protein kinase (AMPK) functions as a sensor to maintain energy balance and is therefore a potential target for drug design against metabolic syndrome. The crystal structure of the complex between the phosphorylated-state mimic T172D mutant AMPK α2 kinase domain and a selective inhibitor, compound C, has been determined, revealing the unique inhibitor-binding mode of this protein kinase ...
AMPK alpha 2山羊多克隆抗体(ab105028)可与小鼠, 大鼠, 人样本反应并经WB, sELISA实验严格验证。所有产品均提供质保服务,中国75%以上现货。
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The ratio between ATP and AMP is used as a way for a cell to sense how much energy is available and control the metabolic pathways that produce and consume ATP. The body attempts to maintain a specific ratio of AMP:ATP; when this ratio is out of balance, the cells adjust their metabolism accordingly. As the ratio increases either by increased levels of AMP or decreased levels of ATP, the body is signaled to produced more ATP. The AMP:ATP ratio is primarily regulated by an enzyme known as AMP-activated protein kinase (AMPK). When activated, AMPK sets in motion a series of events which switch cells from active ATP consumption to ATP production ...
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During 2 years, we enrolled 25 patients diagnosed with typewriter tinnitus and evaluated the types of AICA loops in the IAC and CPA and the types of neurovascular contact by using 3T 3D T2-VISTA imaging in 15 patients. When we compared the symptomatic sides of patients with typewriter tinnitus (group 1) with the asymptomatic sides of those with typewriter tinnitus (group 2) and healthy controls (group 3), the difference was not statistically significant (Table). However, considering that in a previous study, type II and type III AICA loops were observed in 38.0% of 332 patients with ipsilateral auditory symptoms,13 our results, which demonstrated that 56.3% of group 1 and 18.8% of group 3 had type II and III AICA loops, showed a definite tendency toward type II and III AICA loops on the symptomatic sides of subjects with typewriter tinnitus. Moreover, the 3 groups in this study had significantly different (Table) neurovascular contact types. In group 1, 68.8% of the subjects showed type II or ...
Contraindicaciones del ampk. adversos, si bien la píldora del día después no presenta particulares indicaciones de uso, ni muchos efectos particulares,.
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5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR) is an intermediate in the generation of inosine monophosphate. AICAR is ... 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? ... 5-Aminoimidazole-4-carboxamide-1- β - d -ribofuranoside Increases Myocardial Glucose Uptake during Reperfusion and Induces Late ... 2006)doi:10.1152/ajpheart.00906.2005 Longnus SL, Wambolt RB, Parsons HL, Brownsey RW, Allard MF 5-Aminoimidazole-4-carboxamide ...
August 2007). "5-aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside acutely stimulates skeletal muscle 2-deoxyglucose uptake ... Acadesine (INN), also known as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA-riboside, and AICAR, is an AMP- ... Cronstein BN, Kamen BA (December 2007). "5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside (AICA-riboside) as a targeting ... Corton JM, Gillespie JG, Hawley SA, Hardie DG (April 1995). "5-aminoimidazole-4-carboxamide ribonucleoside. A specific method ...
The systematic name of this enzyme class is 10-formyltetrahydrofolate:5-phosphoribosyl-5-amino-4-imidazole-carb oxamide N- ... aminoimidazolecarboxamide ribonucleotide transformylase, and. *transformylase,. *bifunctional purine biosynthesis protein PURH, ...
Rayl EA, Moroson BA, Beardsley GP (Mar 1996). "The human purH gene product, 5-aminoimidazole-4-carboxamide ribonucleotide ... It has two functions: EC 2.1.2.3 - 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase EC 3.5.4.10 - IMP ... Vergis JM, Bulock KG, Fleming KG, Beardsley GP (2001). "Human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase/ ... "Entrez Gene: ATIC 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase". Rasmussen HH, van Damme ...
Bazurto JV, Heitman NJ, Downs DM (September 2015). Metcalf WW (ed.). "Aminoimidazole Carboxamide Ribotide Exerts Opposing ... In bacteria, HMP-P arises by conversion of the purine biosynthetic precursor 5-aminoimidazole ribotide (AIR) through the action ...
... and 5-aminoimidazole-4-carboxamide (AIC). Other metabolites include temozolomide acid and unidentified hydrophilic substances. ... imidazole-4-carboxamide (MTIC). MTIC splits into monomethylhydrazine, probably the active methylating agent, ...
... reduced folate carrier-mediated folate/antifolate transport through an antiport mechanism with 5-aminoimidazole-4-carboxamide ...
It primarily inhibits the enzyme thymidylate synthase, but also has effects on DHFR, aminoimidazole carboxamide ribonucleotide ...
... to 5-aminoimidazole-4-carboxamide ribotide (AICAR) and fumarate. AICAR proceeds through three more reactions before it becomes ... In the first reaction, ASL converts 5-aminoimidazole- (N-succinylocarboxamide) ribotide (SAICAR) ...
... forming N-succinyl-5-aminoimidazole-4-carboxamide ribonucleotide (SAICAR). SAICAR lyase removes the carbon skeleton of the ... leaving the amino group and forming 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR). AICAR transformylase transfers a ... Firestine, SM; Poon, SW; Mueller, EJ; Stubbe, J; Davisson, VJ (Oct 4, 1994). "Reactions catalyzed by 5-aminoimidazole ... forming the 5-membered imidazole ring 5-aminoimidazole ribonucleotide (AIR). N5-CAIR synthetase transfers a carboxyl group, ...
... the removal of the carbon skeleton of aspartate by SAICAR lyase results in 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR ... as 5-aminoimidazole ribonucleotide (AIR). A carboxyl group is attached to AIR by N5-CAIR synthetase to form N5- ... along with amino group from aspartate forms an amide bond to create N-succinyl-5-aminoimidazale-4-carboxamide ribonucleotide ( ... forming N-formylaminoimidazole-4-carboxamide ribonucleotide (FAICAR). Lastly, closure of the second ring structure is carried ...
... and replacement with an amino group results in the natural purine synthetic precursor 5-aminoimidazole-4-carboxamide-1-β-D- ... The most successful ribavirin derivative to date is the 3-carboxamidine derivative of the parent 3-carboxamide, first reported ... 4-triazole-3-carboxamide". Science. 177 (4050): 705-6. Bibcode:1972Sci...177..705S. doi:10.1126/science.177.4050.705. PMID ...
... aminoimidazole carboxamide MeSH D03.383.129.308.040 - antazoline MeSH D03.383.129.308.080 - biotin MeSH D03.383.129.308.090 - ...
... purine biosynthesis which leads to the accumulation of the de novo purine synthesis intermediate 5-aminoimidazole-4-carboxamide ...
Activation of AMP-activated protein kinase (AMPK), the cellular energy sensor, by 5-aminoimidazole-4-carboxamide ribonucleoside ...
5-aminoimidazole-4-carboxamide ribonucleotide (ProFAR) to N-[(5-phosphoribulosyl)formimino]-5-aminoimidazole-4-carboxamide ...
... both of which involve the β-elimination of fumarate to produce aminoimidazole carboxamide ribotide (AICAR) from SAICAR or ...
It primarily inhibits the enzyme thymidylate synthase, but also has effects on DHFR, aminoimidazole carboxamide ribonucleotide ...
Compare 5-Aminoimidazole 4-Carboxamide Ribonucleotide Formyltransferase ELISA Kits from leading suppliers on Biocompare. View ... 5-Aminoimidazole 4-Carboxamide Ribonucleotide Formyltransferase ELISA Kits. The ELISA (enzyme-linked immunosorbent assay) is a ... Your search returned 13 5-Aminoimidazole 4-Carboxamide Ribonucleotide Formyltransferase ELISA ELISA Kit across 5 suppliers. ...
AnabolicMinds.com , Forum , Supplement Forum , Supplements , AICAR (5-aminoimidazole-4-carboxamide riboside) ... AICAR (5-aminoimidazole-4-carboxamide riboside) No hope of ever seeing this in bulk is there? Its outrageously expensive in ...
We show in this study that the intracerebroventricular infusion of 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside ( ... 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside, controls muscle glycogen synthesis.. Perrin C1, Knauf C, Burcelin R. ...
5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) is an activator of AMP activated protein kinase (AMPK) and a ... Cell cycle regulation via p53 phosphorylation by a 5-AMP activated protein kinase activator, 5-aminoimidazole- 4-carboxamide-1 ... Aminoimidazole Carboxamide/analogs & derivatives*. *Aminoimidazole Carboxamide/pharmacology*. *Carcinoma, Hepatocellular/ ...
5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase), Authors: Jean-Loup Huret. Published in: ... ATIC (5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase). Written. 2001-08. Jean-Loup Huret. ... ATIC (5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase). Atlas Genet Cytogenet Oncol Haematol ... Characterization of molecularly cloned human 5-aminoimidazole-4-carboxamide ribonucleotide transformylase.. Sugita T, Aya H, ...
5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating AMP-activated protein kinase in intact cells? ... Rattan R, Giri S, Singh AK, Singh I. 5-Aminoimidazole-4-carboxamide-1-β-d-ribofuranoside inhibits cancer cell proliferation in ... Because of its ability to mimic a low energy status of the cell, the cell-permeable nucleoside 5-aminoimidazole-4-carboxamide ( ... Methotrexate enhances the antianabolic and antiproliferative effects of 5-aminoimidazole-4-carboxamide riboside. Annelies ...
ZMP, 5-aminoimidazole-4-carboxamide ribonucleoside. Skeletal muscle is the major site of whole-body glucose disposal during ... Bergeron R, Previs SF, Cline GW, Perret P, Russell RR 3rd, Young LH, Shulman GI: Effect of 5-aminoimidazole-4-carboxamide-1-β-d ... 5-Aminoimidazole-4-Carboxamide 1-β-d-Ribofuranoside Acutely Stimulates Skeletal Muscle 2-Deoxyglucose Uptake in Healthy Men. ... 5-Aminoimidazole-4-Carboxamide 1-β-d-Ribofuranoside Acutely Stimulates Skeletal Muscle 2-Deoxyglucose Uptake in Healthy Men ...
5-Aminoimidazole-4-carboxamide-15N2 Hydrochloride (>90%). High Quality CRMs, Reference Materials, Proficiency Testing & More at ... 5-Aminoimidazole-4-carboxamide-15N2 Hydrochloride (>90%). 5-Aminoimidazole-4-carboxamide-15N2 Hydrochloride (>90%). ...
Aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR Tfase), one of the two folate-dependent enzymes in the de ... Aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR Tfase), one of the two folate-dependent enzymes in the de ... Crystal structure of avian aminoimidazole-4-carboxamide ribonucleotide transformylase in complex with a novel non-folate ...
Effect of 5-Aminoimidazole-4-Carboxamide-1-β-d-Ribofuranoside Infusion on In Vivo Glucose and Lipid Metabolism in Lean and ... Effect of 5-Aminoimidazole-4-Carboxamide-1-β-d-Ribofuranoside Infusion on In Vivo Glucose and Lipid Metabolism in Lean and ... Effect of 5-Aminoimidazole-4-Carboxamide-1-β-d-Ribofuranoside Infusion on In Vivo Glucose and Lipid Metabolism in Lean and ... Effect of 5-Aminoimidazole-4-Carboxamide-1-β-d-Ribofuranoside Infusion on In Vivo Glucose and Lipid Metabolism in Lean and ...
Nath N Giri S Prasad R Salem ML Singh AK Singh I . 5-aminoimidazole-4-carboxamide ribonucleoside: a novel immunomodulator with ... Giri S Nath N Smith B Viollet B Singh AK Singh I . 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside inhibits ... Inhibitory Effect of Aminoimidazole Carboxamide Ribonucleotide (AICAR) on Endotoxin-Induced Uveitis in Rats ... Inhibitory Effect of Aminoimidazole Carboxamide Ribonucleotide (AICAR) on Endotoxin-Induced Uveitis in Rats ...
5-Aminoimidazole-4-carboxamide-1-β-4-ribofuranoside (AICAR), an analog of AMP is widely used as an activator of AMP-kinase ( ... Aminoimidazole Carboxamide Ribonucleotide (AICAR) Inhibits the Growth of Retinoblastoma In Vivo by Decreasing Angiogenesis and ... Aminoimidazole carboxamide ribonucleotide (AICAR) inhibits the growth of retinoblastoma in vivo by decreasing angiogenesis and ... Aminoimidazole Carboxamide Ribonucleotide (AICAR) Inhibits the Growth of Retinoblastoma In Vivo by Decreasing Angiogenesis and ...
Aminoimidazole carboxamide ribonucleoside toxicity: a model for study of pyrimidine starvation. J Cell Physiol 1981;107:335-44. ... AICAr (5-aminoimidazole-4-carboxamide-1-β-riboside) is a nucleoside that is taken up by cells by adenosine transporters and ... 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside inhibits cancer cell proliferation in vitro and in vivo via AMP- ... 5-Aminoimidazole-4-carboxamide riboside induces apoptosis in Jurkat cells, but the AMP-activated protein kinase is not involved ...
5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR, an activator of AMP-activated protein kinase), can also induce ... 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR, an activator of AMP-activated protein kinase), can also induce ... Enhancement of insulin-mediated rat muscle glucose uptake and microvascular perfusion by 5-aminoimidazole-4-carboxamide-1-beta- ... Enhancement of insulin-mediated rat muscle glucose uptake and microvascular perfusion by 5-aminoimidazole-4-carboxamide-1-beta- ...
5-aminoimidazole-4-carboxamide riboside. MTX. methotrexate. ZMP. 5-aminoimidazole-4-carboxamide ribotide monophosphate. 5- ... 5-aminoimidazole-4-carboxamide ribotide diphosphate. ZTP. 5-aminoimidazole-4-carboxamide ribotide triphosphate. mTOR. mammalian ... 2005) 5-Aminoimidazole-4-carboxamide-1-β-d-ribofuranoside inhibits cancer cell proliferation in vitro and in vivo via AMP- ... 1981) Aminoimidazole carboxamide ribonucleoside toxicity: a model for study of pyrimidine starvation. J Cell Physiol 107:335- ...
Inhibitory effect of aminoimidazole carboxamide ribonucleotide (AICAR) on endotoxin-induced uveitis in rats. Invest Ophthalmol ... Purpose.: To investigate the efficacy of topical 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside (AICAR) in a mouse model ... Giri S, Nath N, Smith B, Viollet B, Singh AK, Singh I. 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside inhibits ... Nath N, Giri S, Prasad R, Salem ML, Singh AK, Singh I. 5-aminoimidazole-4-carboxamide ribonucleoside: a novel immunomodulator ...
"Aminoimidazole Carboxamide" by people in this website by year, and whether "Aminoimidazole Carboxamide" was a major or minor ... "Aminoimidazole Carboxamide" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ( ... Nath N, Giri S, Prasad R, Salem ML, Singh AK, Singh I. 5-aminoimidazole-4-carboxamide ribonucleoside: a novel immunomodulator ... Rattan R, Giri S, Singh AK, Singh I. 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside inhibits cancer cell proliferation ...
Our previous studies demonstrated that 5-aminoimidazole-4-carboxamide ribonucleoside (AICAr) induced differentiation of ... 5-aminoimidazole-4-carboxamide ribonucleoside induces differentiation in a subset of primary acute myeloid leukemia blasts. * ... Dembitz, V., Lalic, H., Kodvanj, I. et al. 5-aminoimidazole-4-carboxamide ribonucleoside induces differentiation in a subset of ... Lalic H, Dembitz V, Lukinovic-Skudar V, Banfic H, Visnjic D. 5-Aminoimidazole-4-carboxamide ribonucleoside induces ...
AMINOIMIDAZOLE 4-CARBOXAMIDE RIBONUCLEOTIDE. Find entries where: AMZ. is present as a standalone ligand in 22 entries ... 5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR) is an intermediate in the generation of inosine monophosphate and analog ...
Aminoimidazole carboxamide ribonucleotide ameliorates experimental autoimmune uveitis. Jun Suzuki, Takeru Yoshimura, Marina ... Aminoimidazole carboxamide ribonucleotide ameliorates experimental autoimmune uveitis. Investigative Ophthalmology and Visual ... Aminoimidazole carboxamide ribonucleotide ameliorates experimental autoimmune uveitis. / Suzuki, Jun; Yoshimura, Takeru; ... title = "Aminoimidazole carboxamide ribonucleotide ameliorates experimental autoimmune uveitis",. abstract = "PURPOSE. To ...
AICAR, 5-Aminoimidazole-4-Carboxamide-1-β-4-Ribofuranoside; AK, adenosine kinase; AMPK, AMP activated protein kinase; PI3K, ... Rattan R, Giri S, Singh AK, Singh I: 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside inhibits cancer cell proliferation ... Corton JM, Gillespie JG, Hawley SA, Hardie DG: 5-aminoimidazole-4-carboxamide ribonucleoside. A specific method for activating ... Cytotoxic effect of 5-aminoimidazole-4-carboxamide-1-β-4-ribofuranoside (AICAR) on childhood acute lymphoblastic leukemia (ALL ...
T1 - Short-term adenosine monophosphate-activated protein kinase activator 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside ... Short-term adenosine monophosphate-activated protein kinase activator 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside ... Short-term adenosine monophosphate-activated protein kinase activator 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside ... Short-term adenosine monophosphate-activated protein kinase activator 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside ...
0030]In various embodiments, siRNAs that target 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP ... Patent application title: siRNA targeting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase ( ... Patent application title: siRNA targeting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase/IMP cyclohydrolase ( ...
Granisetron[49] (aminoimidazole carboxamide). Approved by FDA for. CINV. RINV. Dolasetron[50] (aminoimidazole carboxamide). ... Ondansetron[48] (aminoimidazole carboxamide). Antiemetic: centrally acting agents that prevent serotonin from initiating ...
... and by examining several mutants defective in various pathways of 5-aminoimidazole-4-carboxamide ribonucleolide (AICAR) ... Exogenous application of the purine precursor 5-aminoimidazole-4-carboxamide (AICA) riboside restores infection and enhances ... Exogenous application of the purine precursor 5-aminoimidazole-4-carboxamide (AICA) riboside restores infection and enhances ... Requirement for Rhizobial Production of 5-Aminoimidazole-4-Carboxamide Ribonucleotide (AICAR) for Infection of Bean ...
On the purification and mechanism of action of 5-aminoimidazole-4-carboxamide-ribonucleotide transformylase from chicken liver ... phosphoribosyl-5-aminoimidazole-4-carboxamide (AICAR) and 10-formyltetrahydrofolate to form 5-phosphoribosyl-5- ... 5-phosphoribosyl-5-aminoimidazole-4-carboxamide (AICAR) + 10-formyltetrahydrofolate =, 5-phosphoribosyl-5-formaminoimidazole- ... 5-phosphoribosyl-5-aminoimidazole-4-carboxamide (AICAR) + 10-formyltetrahydrofolate => 5-phosphoribosyl-5-formaminoimidazole- ...
5-Aminoimidazole-4-carboxamide-riboside. AMPK. Adenosine 5′-monophosphate-activated protein kinase ... 1H-indole-2-carboxamide). The Journal of Pharmacology and Experimental Therapeutics, 321, 45-50.CrossRefPubMedGoogle Scholar ... Caudal fourth ventricular administration of the AMPK activator 5-aminoimiazole-4-carboxamide-riboside regulates glucose and ...
... we aimed to evaluate the therapeutic potential of 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), an activator of AMP- ... In this study, we aimed to evaluate the therapeutic potential of 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), an ... The adenosine monophosphate analogue 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR) activates AMP-dependent protein ...
... which occurred independently of its conversion to AMPK-activating 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranosyl ... 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR) is an established pharmacological activator of AMP-activated ... 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR) was one of the first pharmacological AMPK activators12. Once it is ... Aminoimidazole carboxamide ribonucleotide ameliorates experimental autoimmune uveitis. Invest. Ophthalmol. Vis. Sci. 53, 4158- ...
  • We show in this study that the intracerebroventricular infusion of 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR), a pharmacological AMP-activated kinase activator, increased insulin-stimulated muscle glycogen synthesis and insulin sensitivity during a hyperinsulinemic clamp. (nih.gov)
  • 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) is an activator of AMP activated protein kinase (AMPK) and a regulator of de novo purine synthesis. (nih.gov)
  • Activation of AMP-activated protein kinase (AMPK) in rodent muscle by exercise, metformin, 5-aminoimidazole-4-carboxamide 1-β- d -ribofuranoside (AICAR), and adiponectin increases glucose uptake. (diabetesjournals.org)
  • AMPK may be pharmacologically activated by AICAR, which undergoes intracellular metabolism to 5-aminoimidazole-4-carboxamide ribonucleoside (ZMP), which mimics the AMP effects on AMPK signaling ( 12 ). (diabetesjournals.org)
  • Aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR Tfase), one of the two folate-dependent enzymes in the de novo purine biosynthesis pathway, is a promising target for anti-neoplastic chemotherapy. (nih.gov)
  • Activation of AMP-activated protein kinase (AMPK) with 5-aminoimidazole-4-carboxamide-1-β- d -ribofuranoside (AICAR) increases glucose transport in skeletal muscle via an insulin-independent pathway. (diabetesjournals.org)
  • Recent evidence indicates that pharmacological activation of AMP-activated protein kinase (AMPK) by 5-aminoimidazole-4-carboxamide-1-β- d -ribofuranoside (AICAR) stimulates glucose transport activity in skeletal muscle ( 11 12 13 ) and heart ( 14 ) in the absence of phosphoinositide 3-kinase activation, suggesting that this action is independent of the insulin-signaling pathway. (diabetesjournals.org)
  • To investigate the anti-inflammatory effect of aminoimidazole carboxamide ribonucleotide (AICAR), an analog of adenosine monophosphate (AMP), in endotoxin-induced uveitis (EIU). (arvojournals.org)
  • 5-Aminoimidazole-4-carboxamide-1-β-4-ribofuranoside (AICAR), an analog of AMP is widely used as an activator of AMP-kinase (AMPK), a protein that regulates the responses of the cell to energy change. (harvard.edu)
  • To investigate the mechanism by which 5-aminoimidazole-4-carboxamide-1-β-riboside (AICAr) induces apoptosis in multiple myeloma cells, we conducted an unbiased metabolomics screen. (aacrjournals.org)
  • 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR, an activator of AMP-activated protein kinase), can also induce microvascular recruitment, at doses that do not acutely activate glucose transport in rat muscle. (garvan.org.au)
  • 5-Aminoimidazole-4-carboxamide riboside (AICAR), an agent with diverse pharmacological properties, augments transport of folates and antifolates. (aspetjournals.org)
  • Transport stimulation correlated with the accumulation of 5-aminoimidazole-4-carboxamide ribotide monophosphate (ZMP), the monophosphate derivative of AICAR, within cells as established by liquid chromatography. (aspetjournals.org)
  • To investigate the efficacy of topical 5-aminoimidazole-4-carboxamide-1-β-d-ribofuranoside (AICAR) in a mouse model of experimental dry eye (EDE). (arvojournals.org)
  • Cytotoxic effect of 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside (AICAR) on childhood acute lymphoblastic leukemia (ALL) cells: implication for targeted therapy. (healthsciencessc.org)
  • Our previous studies demonstrated that 5-aminoimidazole-4-carboxamide ribonucleoside (AICAr) induced differentiation of monocytic cell lines by activating the ATR/Chk1 via pyrimidine depletion. (biomedcentral.com)
  • 5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR) is an intermediate in the generation of inosine monophosphate and analog of adenosine monophosphate (AMP) that is capable of stimulating AMP-dependent protein kinase (AMPK) activity. (rcsb.org)
  • The purpose of the present study was to examine the effect of AMPK activation with the administration of AMPK activator 5-aminoimidazole-4- carboxamide-1-β-d-ribofuranoside (AICAR) to rats on skeletal muscle SIRT1 protein expression as well as peroxisome proliferator activated receptor γ coactivator-1α (PGC-1α) and glucose transporter 4 (GLUT4) protein expression and hexokinase activity. (elsevier.com)
  • The uniqueness of AICA riboside as an effector was shown by testing varying concentrations of AICA riboside and purines for this effect, and by examining several mutants defective in various pathways of 5-aminoimidazole-4-carboxamide ribonucleolide (AICAR) synthesis. (marquette.edu)
  • and Noel, K. Dale, "Requirement for Rhizobial Production of 5-Aminoimidazole-4-Carboxamide Ribonucleotide (AICAR) for Infection of Bean" (1995). (marquette.edu)
  • The phosphoribosylaminoimidazolecarboxamide formyltransferase activity of cytosolic ATIC (bifunctional purine biosynthesis protein PURH) catalyzes the reaction of 5'-phosphoribosyl-5-aminoimidazole-4-carboxamide (AICAR) and 10-formyltetrahydrofolate to form 5'-phosphoribosyl-5-formaminoimidazole-4-carboxamide (FAICAR) and tetrahydrofolate. (reactome.org)
  • In this study, we aimed to evaluate the therapeutic potential of 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), an activator of AMP-activated protein kinase, for ameliorating high-fat diet (HFD)-induced pathophysiology in mice. (springer.com)
  • 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR) is an established pharmacological activator of AMP-activated protein kinase (AMPK). (nature.com)
  • Here we report a potent suppression of lipopolysaccharide (LPS)-induced inflammatory gene expression by AICAR in primary human macrophages, which occurred independently of its conversion to AMPK-activating 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranosyl monophosphate. (nature.com)
  • Once it is taken up by the cell, AICAR undergoes phosphorylation by adenosine kinase to form 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranosyl monophosphate (ZMP). (nature.com)
  • Abstract In the present study, the effect of 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) on long-chain fatty acid oxidation by hepatocytes isolated from suckled neonatal pig liver (a low ketogenic and lipogenic tissue) was tested. (uwi.edu)
  • In order to determine whether AMPK activation reverses lipid-induced mTOR activation, L6 myotubes were exposed to 0.4 mM palmitate to activate mTORC1/2 in the absence or presence of 5′-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside (AICAR). (calstate.edu)
  • ATIC [5-aminoimidazole-4-carboxamide ribonucleotide transformylase (AICAR Tfase)-inosine monophosphate cyclohydrolase (IMPCH)] is a bifunctional enzyme that catalyzes the penultimate and final steps in the de novo purine biosynthesis pathway and thus is an attractive anticancer target. (scripps.edu)
  • Given the important role of the AMP-activated protein kinase (AMPK) in the regulation of fat oxidation and mitochondrial biogenesis, we examined AMPK activity in young and old rats and found that acute stimulation of AMPK-alpha(2) activity by 5'-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside (AICAR) and exercise was blunted in skeletal muscle of old rats. (nih.gov)
  • 5-Aminoimidazole-4-carboxamide ribonucleotide (AICAR) is an intermediate in the generation of inosine monophosphate. (wikipedia.org)
  • 2006)doi:10.1152/ajpheart.00906.2005 Longnus SL, Wambolt RB, Parsons HL, Brownsey RW, Allard MF 5-Aminoimidazole-4-carboxamide 1-beta-D-ribofuranoside (AICAR) stimulates myocardial glycogenolysis by allosteric mechanisms. (wikipedia.org)
  • Acadesine (INN), also known as 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside, AICA-riboside, and AICAR, is an AMP-activated protein kinase activator which is used for the treatment of acute lymphoblastic leukemia and may have applications in treating other disorders such as diabetes. (wikipedia.org)
  • Chemical activation of AMPK with the compound 5-aminoimidazole-4-carboxamide ribonucleoside (AICAR) leads to increased glucose uptake ( 15 - 19 ) and enhanced insulin sensitivity in muscle ( 20 , 21 ). (diabetesjournals.org)
  • A potential role of AMPK in suppression of inflammatory responses has been suggested by studies using the pharmacological activator of AMPK, 5-aminoimidazole-4-carboxamide ribose (AICAR). (jimmunol.org)
  • However, AICAR is taken up by cells and converted to AMP analog 5-aminoimidazole-4-carboxamide-1-β- d -ribofuranotide, which mimics the effect of AMP, thus AICAR is a nonspecific activator of AMPK and has the potential to activate other AMP-sensitive enzymes ( 15 ). (jimmunol.org)
  • It is an essential enzyme involved in purine metabolism, and catalyzes two non-sequential reactions in the de novo purine biosynthetic pathway: the conversion of succinylaminoimidazole carboxamide ribotide (SAICAR) to aminoimidazole carboxamide ribotide (AICAR) and the conversion of adenylosuccinate (S-AMP) to aden. (genecards.org)
  • Aminoimidazole carboxamide ribotide (AICAR) is a purine biosynthetic intermediate and a by-product of histidine biosynthesis. (asm.org)
  • Methotrexate polyglutamates are potent inhibitors of the enzyme aminoimidazole carboxamide ribonucleotide (AICAR) transformylase, among others. (thefreedictionary.com)
  • 5-Aminoimidazole-4-carboxamide riboside or acadesine (AICAR) induces apoptosis in chronic lymphocytic leukemia (CLL) cells. (biomedsearch.com)
  • Aminoimidazole-4-carboxamide ribonucleotide (AICAR) transformylase/IMP cyclohydrolase (ATIC) is a bifunctional enzyme with folate-dependent AICAR transformylase and IMP cyclohydrolase activities that catalyzes the last two steps of purine biosynthesis. (embl-heidelberg.de)
  • Because of its ability to mimic a low energy status of the cell, the cell-permeable nucleoside 5-aminoimidazole-4-carboxamide (AICA) riboside was proposed as an antineoplastic agent switching off major energy-consuming processes associated with the malignant phenotype (lipid production, DNA synthesis, cell proliferation, cell migration, etc. (aacrjournals.org)
  • In a recent attempt to explore the feasibility of targeting the energy sensing system as a strategy in the treatment of cancer, cancer cells were treated with 5-aminoimidazole-4-carboxamide (AICA) riboside, a cell-permeable nucleoside ( 1 - 3 ). (aacrjournals.org)
  • Exogenous application of the purine precursor 5-aminoimidazole-4-carboxamide (AICA) riboside restores infection and enhances the development of bean ( Phas-eolus vulgaris ) root nodules elicited by Rhizobium etli purine auxotrophs. (marquette.edu)
  • A 5-aminoimidazole-4-carboxamide (AICA) riboside, a purine nucleoside analog, and a nucleotide biosynthesis precursor with B cell pro-apoptotic activity. (cancer.gov)
  • 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside (AICA-riboside) as a targeting agent for therapy of patients with acute lymphoblastic leukemia: are we there and are there pitfalls? (wikipedia.org)
  • Here, we took advantage of the ability of the cell-permeable nucleoside 5-aminoimidazole-4-carboxamide (AICA) riboside to increase the intracellular levels of AICA ribotide, an AMP analogue, mimicking a low energy status of the cell. (aacrjournals.org)
  • Bai A, Yong M, Ma AG, Ma Y, Weiss CR, Guan Q, Bernstein CN, Peng Z. Novel anti-inflammatory action of 5-aminoimidazole-4-carboxamide ribonucleoside with protective effect in dextran sulfate sodium-induced acute and chronic colitis. (healthsciencessc.org)
  • Nath N, Giri S, Prasad R, Salem ML, Singh AK, Singh I. 5-aminoimidazole-4-carboxamide ribonucleoside: a novel immunomodulator with therapeutic efficacy in experimental autoimmune encephalomyelitis. (healthsciencessc.org)
  • 5-aminoimidazole-4-carboxamide ribonucleoside. (wikipedia.org)
  • D-ribofuranosyl)imidazole-4-carboxamide and 5-amino-1-(.beta. (wikipedia.org)
  • 1-(5-phospho-beta-D-ribosyl)-5-((5-phospho-beta-D-ribosylamino)methylideneamino)imidazole-4-carboxamide = 5-((5-phospho-1-deoxy-D-ribulos-1-ylamino)methylideneamino)-1-(5-phospho-beta-D-ribosyl)imidazole-4-carboxamide. (uniprot.org)
  • Catalyzes two non-sequential steps in de novo AMP synthesis: converts (S)-2-(5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamido)succinate (SAICAR) to fumarate plus 5-amino-1-(5-phospho-D-ribosyl)imidazole-4-carboxamide, and thereby also contributes to de novo IMP synthesis, and converts succinyladenosine monophosphate (SAMP) to AMP and fumarate. (genecards.org)
  • HisA is a phosphoribosylformimino-5-aminoimidazole carboxamide ribotide isomerase ( EC:5.3.1.16 ), involved in the fourth step of histidine biosynthesis. (ebi.ac.uk)
  • Your search returned 13 5-Aminoimidazole 4-Carboxamide Ribonucleotide Formyltransferase ELISA ELISA Kit across 5 suppliers. (biocompare.com)
  • Catalytic mechanism of the cyclohydrolase activity of human aminoimidazole carboxamide ribonucleotide formyltransferase/inosine monophosphate cyclohydrolase. (embl-heidelberg.de)
  • Crystal structures of human bifunctional enzyme aminoimidazole-4-carboxamide ribonucleotide transformylase/IMP cyclohydrolase in complex with potent sulfonyl-containing antifolates. (embl-heidelberg.de)
  • The bifunctional enzyme aminoimidazole carboxamide ribonucleotide transformylase/inosine monophosphate cyclohydrolase (ATIC) is responsible for catalysis of the last two steps in the de novo purine pathway. (embl-heidelberg.de)
  • Intracerebroventricular infusion of glucose, insulin, and the adenosine monophosphate-activated kinase activator, 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside, controls muscle glycogen synthesis. (nih.gov)
  • ATIC encodes an enzyme which generates inosine monophosphate from aminoimidazole carboxamide ribonucleotide. (wikibooks.org)
  • Cell cycle regulation via p53 phosphorylation by a 5'-AMP activated protein kinase activator, 5-aminoimidazole- 4-carboxamide-1-beta-D-ribofuranosi. (nih.gov)
  • Rattan R, Giri S, Singh AK, Singh I. 5-Aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside inhibits cancer cell proliferation in vitro and in vivo via AMP-activated protein kinase. (healthsciencessc.org)
  • 5-Aminoimidazole-4-carboxamide-1- β - d -ribofuranoside Increases Myocardial Glucose Uptake during Reperfusion and Induces Late Pre-conditioning : Potential Role of AMP-Activated Protein Kinase. (wikipedia.org)
  • Relationship between 5-aminoimidazole-4-carboxamide-ribotide and AMP-activated protein kinase activity in the perfused mouse heart. (wikipedia.org)
  • The yeast His7 protein is a bifunctional protein which catalyzes an amido-transferase reaction that generates imidazole-glycerol phosphate and 5-aminoimidazol-4-carboxamide. (ebi.ac.uk)
  • SAICAR is converted from 5-aminoimidazole-4-carboxyribonucleotide (CAIR) via phosphoribosylaminoimidazolesuccinocarboxamide synthetase (EC: 6.3.2.6) or SAICAR synthase. (hmdb.ca)
  • Another feature glycinamide ribonucleotide and 5-amino-4-imidazole of intracellular folate metabolism is the compart- carboxamide ribonucleotide), pyrimidine nucleotide mentation of folate coenzymes between the cytosol biosynthesis (methylation of deoxyuridylic acid to thy- and the mitochondria. (yudu.com)
  • Significantly increased recovery of activity of key pathway enzymes (particularly of labile aminoimidazole ribonucleotide synthetase) coupled with improved assay methods and the use of Percoll in addition to sucrose for gradient centrifugation have together contributed to much higher reaction rates and more definitive analyses of particulate fractions. (plantphysiol.org)
  • Larvicidal and fungicidal activity of compounds with hydrazine carboxamide and diazenecarboxamide moieties. (thefreedictionary.com)
  • Aminoimidazole Carboxamide" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (healthsciencessc.org)
  • Immunomodulatory effect of combination therapy with lovastatin and 5-aminoimidazole-4-carboxamide-1-beta-D-ribofuranoside alleviates neurodegeneration in experimental autoimmune encephalomyelitis. (healthsciencessc.org)
  • 5-aminoimidazole-4-carboxamide-1-beta-4-ribofuranoside attenuates experimental autoimmune encephalomyelitis via modulation of endothelial-monocyte interaction. (healthsciencessc.org)
  • To investigate the Pharmacokinetics of L19IL2, dacarbazine and 5-aminoimidazole -4 carboxamide (AIC). (clinicaltrials.gov)
  • Environmental Protection Agency and Canadian Pest Management Regulatory Agency registration process for bixafen, a new pyrazole carboxamide fungicide that belongs to a new generation of succinate dehydrogenase inhibitors (SDHI). (thefreedictionary.com)
  • br>Tthe cloning, expression, purification, crystallization and preliminary X-ray crystallographic analysis of a bifunctional purine-biosynthesis enzyme from E. coli which possesses aminoimidazole-4-carboxamide ribonucleotide transformylase. (iaea.org)
  • 5-Aminoimidazole-4-carboxamide ribonucleotide or AICAR 50MG / AICAR POWDER is an analogue of adenosine monophosphate. (kihorsemed.com)
  • Aica-Ribonucleotide, or AICAR (aminoimidazole carboxamide ribonucleotide), acts as a protein kinase agent activated by AMP. (sarmsupplements.co.uk)