Serotonin Receptor Agonists
Serotonin 5-HT1 Receptor Agonists
Serotonin 5-HT2 Receptor Agonists
Adenosine A2 Receptor Agonists
Cannabinoid Receptor Agonists
Serotonin 5-HT4 Receptor Agonists
Dose-Response Relationship, Drug
Adrenergic alpha-2 Receptor Agonists
Receptors, Opioid, kappa
Receptors, Opioid, mu
Receptors, Dopamine D2
Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.
Receptors, Purinergic P1
Receptors, Opioid, delta
A GAMMA-AMINOBUTYRIC ACID derivative that is a specific agonist of GABA-B RECEPTORS. It is used in the treatment of MUSCLE SPASTICITY, especially that due to SPINAL CORD INJURIES. Its therapeutic effects result from actions at spinal and supraspinal sites, generally the reduction of excitatory transmission.
Receptors, Dopamine D1
Receptor, Adenosine A2A
Adrenergic alpha-1 Receptor Agonists
Cell membrane proteins that bind opioids and trigger intracellular changes which influence the behavior of cells. The endogenous ligands for opioid receptors in mammals include three families of peptides, the enkephalins, endorphins, and dynorphins. The receptor classes include mu, delta, and kappa receptors. Sigma receptors bind several psychoactive substances, including certain opioids, but their endogenous ligands are not known.
Enkephalin, D-Penicillamine (2,5)-
Cell surface receptors that bind glucagon with high affinity and trigger intracellular changes which influence the behavior of cells. Activation of glucagon receptors causes a variety of effects; the best understood is the initiation of a complex enzymatic cascade in the liver which ultimately increases the availability of glucose to body organs.
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.
Purinergic P1 Receptor Antagonists
Receptor, Cannabinoid, CB2
Serotonin 5-HT3 Receptor Agonists
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
Receptor, Cannabinoid, CB1
Purinergic P2X Receptor Agonists
Purinergic P2Y Receptor Agonists
Receptors, Dopamine D3
Receptor, Serotonin, 5-HT1B
A serotonin receptor subtype found at high levels in the BASAL GANGLIA and the frontal cortex. It plays a role as a terminal autoreceptor that regulates the rate of SEROTONIN release from nerve endings. This serotonin receptor subtype is closely related to and has similar drug binding properties as the 5-HT1D RECEPTOR. It is particularly sensitive to the agonist SUMATRIPTAN and may be involved in mediating the drug's antimigraine effect.
Receptors, Serotonin, 5-HT4
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
A class of cell surface receptors recognized by its pharmacological profile. Sigma receptors were originally considered to be opioid receptors because they bind certain synthetic opioids. However they also interact with a variety of other psychoactive drugs, and their endogenous ligand is not known (although they can react to certain endogenous steroids). Sigma receptors are found in the immune, endocrine, and nervous systems, and in some peripheral tissues.
Receptor, Serotonin, 5-HT1A
A serotonin receptor subtype found distributed through the CENTRAL NERVOUS SYSTEM where they are involved in neuroendocrine regulation of ACTH secretion. The fact that this serotonin receptor subtype is particularly sensitive to SEROTONIN RECEPTOR AGONISTS such as BUSPIRONE suggests its role in the modulation of ANXIETY and DEPRESSION.
Receptor, Adenosine A3
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Receptor, Serotonin, 5-HT2A
A serotonin receptor subtype found widely distributed in peripheral tissues where it mediates the contractile responses of variety of tissues that contain SMOOTH MUSCLE. Selective 5-HT2A receptor antagonists include KETANSERIN. The 5-HT2A subtype is also located in BASAL GANGLIA and CEREBRAL CORTEX of the BRAIN where it mediates the effects of HALLUCINOGENS such as LSD.
Receptor, Adenosine A1
Receptors, Prostaglandin E
Cell surface receptors which bind prostaglandins with a high affinity and trigger intracellular changes which influence the behavior of cells. Prostaglandin E receptors prefer prostaglandin E2 to other endogenous prostaglandins. They are subdivided into EP1, EP2, and EP3 types based on their effects and their pharmacology.
Cell-surface proteins that bind histamine and trigger intracellular changes influencing the behavior of cells. Histamine receptors are widespread in the central nervous system and in peripheral tissues. Three types have been recognized and designated H1, H2, and H3. They differ in pharmacology, distribution, and mode of action.
Receptors, Histamine H3
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H3 receptors were first recognized as inhibitory autoreceptors on histamine-containing nerve terminals and have since been shown to regulate the release of several neurotransmitters in the central and peripheral nervous systems. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Receptors, Metabotropic Glutamate
One of the catecholamine NEUROTRANSMITTERS in the brain. It is derived from TYROSINE and is the precursor to NOREPINEPHRINE and EPINEPHRINE. Dopamine is a major transmitter in the extrapyramidal system of the brain, and important in regulating movement. A family of receptors (RECEPTORS, DOPAMINE) mediate its action.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Bicyclo Compounds, Heterocyclic
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
Receptor, Serotonin, 5-HT2C
A serotonin receptor subtype found primarily in the CENTRAL NERVOUS SYSTEM and the CHOROID PLEXUS. This receptor subtype is believed to mediate the anorectic action of SEROTONIN, while selective antagonists of the 5-HT2C receptor appear to induce ANXIETY. Several isoforms of this receptor subtype exist, due to adenine deaminase editing of the receptor mRNA.
Receptors, Histamine H2
A class of histamine receptors discriminated by their pharmacology and mode of action. Histamine H2 receptors act via G-proteins to stimulate ADENYLYL CYCLASES. Among the many responses mediated by these receptors are gastric acid secretion, smooth muscle relaxation, inotropic and chronotropic effects on heart muscle, and inhibition of lymphocyte function. (From Biochem Soc Trans 1992 Feb;20(1):122-5)
Receptors, Purinergic P2
Guanosine 5'-(trihydrogen diphosphate), monoanhydride with phosphorothioic acid. A stable GTP analog which enjoys a variety of physiological actions such as stimulation of guanine nucleotide-binding proteins, phosphoinositide hydrolysis, cyclic AMP accumulation, and activation of specific proto-oncogenes.
Adenosine A2 Receptor Antagonists
Receptors, Serotonin, 5-HT1
Receptors, Neuropeptide Y
Receptors, Adrenergic, alpha-2
A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.
Adenosine A1 Receptor Antagonists
A class of G-protein-coupled receptors that are specific for CANNABINOIDS such as those derived from CANNABIS. They also bind a structurally distinct class of endogenous factors referred to as ENDOCANNABINOIDS. The receptor class may play a role in modulating the release of signaling molecules such as NEUROTRANSMITTERS and CYTOKINES.
The communication from a NEURON to a target (neuron, muscle, or secretory cell) across a SYNAPSE. In chemical synaptic transmission, the presynaptic neuron releases a NEUROTRANSMITTER that diffuses across the synaptic cleft and binds to specific synaptic receptors, activating them. The activated receptors modulate specific ion channels and/or second-messenger systems in the postsynaptic cell. In electrical synaptic transmission, electrical signals are communicated as an ionic current flow across ELECTRICAL SYNAPSES.
An electrophysiologic technique for studying cells, cell membranes, and occasionally isolated organelles. All patch-clamp methods rely on a very high-resistance seal between a micropipette and a membrane; the seal is usually attained by gentle suction. The four most common variants include on-cell patch, inside-out patch, outside-out patch, and whole-cell clamp. Patch-clamp methods are commonly used to voltage clamp, that is control the voltage across the membrane and measure current flow, but current-clamp methods, in which the current is controlled and the voltage is measured, are also used.
Serotonin 5-HT1 Receptor Antagonists
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
Receptors, Adrenergic, beta
The endogenous peptides with opiate-like activity. The three major classes currently recognized are the ENKEPHALINS, the DYNORPHINS, and the ENDORPHINS. Each of these families derives from different precursors, proenkephalin, prodynorphin, and PRO-OPIOMELANOCORTIN, respectively. There are also at least three classes of OPIOID RECEPTORS, but the peptide families do not map to the receptors in a simple way.
Potent activator of the adenylate cyclase system and the biosynthesis of cyclic AMP. From the plant COLEUS FORSKOHLII. Has antihypertensive, positive inotropic, platelet aggregation inhibitory, and smooth muscle relaxant activities; also lowers intraocular pressure and promotes release of hormones from the pituitary gland.
Disease Models, Animal
15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
Receptor, Serotonin, 5-HT2B
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
Receptors, Adrenergic, beta-2
A subclass of beta-adrenergic receptors (RECEPTORS, ADRENERGIC, BETA). The adrenergic beta-2 receptors are more sensitive to EPINEPHRINE than to NOREPINEPHRINE and have a high affinity for the agonist TERBUTALINE. They are widespread, with clinically important roles in SKELETAL MUSCLE; LIVER; and vascular, bronchial, gastrointestinal, and genitourinary SMOOTH MUSCLE.
Receptor, Bradykinin B1
A subtype of BRADYKININ RECEPTOR that is induced in response to INFLAMMATION. It may play a role in chronic inflammation and has a high specificity for KININS lacking the C-terminal ARGININE such as des-Arg(10)-kallidin and des-Arg(9)-bradykinin. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE.
Excitatory Amino Acid Antagonists
The voltage differences across a membrane. For cellular membranes they are computed by subtracting the voltage measured outside the membrane from the voltage measured inside the membrane. They result from differences of inside versus outside concentration of potassium, sodium, chloride, and other ions across cells' or ORGANELLES membranes. For excitable cells, the resting membrane potentials range between -30 and -100 millivolts. Physical, chemical, or electrical stimuli can make a membrane potential more negative (hyperpolarization), or less negative (depolarization).
One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.
Serotonin 5-HT2 Receptor Antagonists
Receptors, Prostaglandin E, EP2 Subtype
Receptors, Adenosine A2
A curved elevation of GRAY MATTER extending the entire length of the floor of the TEMPORAL HORN of the LATERAL VENTRICLE (see also TEMPORAL LOBE). The hippocampus proper, subiculum, and DENTATE GYRUS constitute the hippocampal formation. Sometimes authors include the ENTORHINAL CORTEX in the hippocampal formation.
First, the agonist activates a membrane-bound receptor. Second, the activated G-protein produces a primary effector. Third, the ... Anandamide activates both the CB1 receptor, found primarily in the central nervous system, and the CB2 receptor which is found ... eicosanoid receptors) that largely mediate prostaglandin physiology (although some prostaglandins activate nuclear receptors, ... although certain prostaglandins activate nuclear receptors in the PPAR family. (See article eicosanoid receptors for more ...
"Antineoplastic effects of peroxisome proliferator-activated receptor gamma agonists". Lancet Oncol. 5 (7): 419-29. doi:10.1016/ ... Lung cancer cells also increase DLC1 expression in response to peroxisome proliferator-activated receptor γ (PPARγ) activators ... DAG activates protein kinase C (PKC) and triggers a cascade of intracellular signals. DLC1 may have additional role in insulin ... The main function of DLC1 is its Rho-GAP activity: its ability to enhance activated GTP-bound Rho-GTPases' (specifically, RhoA ...
List of drugs banned by WADA
Metabolic modulators including peroxisome proliferator-activated receptor delta (PPARδ) agonists (e.g., GW 1516), PPARδ-AMP- ... activated protein kinase (AMPK) axis agonists (e.g. AICAR) are also banned. Meldonium was banned on 1 January 2016, which was ... or beta-2 agonists (see adrenergic beta-agonist). Andro, DHEA, stanozolol, testosterone, and nandrolone, or derivates (see ... Beta-2 agonists can act as bronchodilators and increase heart rates, in addition to their mild androgenic effects. Other banned ...
It is a potent and selective 5-HT1A receptor full agonist. In recombinant cell lines expressing human 5-HT1A receptors, ... In rat hippocampal membranes it preferentially activates GalphaO proteins. In neurochemical experiments, befiradol activated 5- ... McCreary, AC; Varney, MA; Newman-Tancredi, A (January 2016). "The novel 5-HT1A receptor agonist, NLX-112 reduces l-DOPA-induced ... and orally active agonists at 5-HT1A receptors". J. Med. Chem. 42 (9): 1648-60. CiteSeerX 10.1.1.325.8872. doi:10.1021/ ...
Muscarinic agonists activate muscarinic receptors while nicotinic agonists activate nicotine receptors. Both are direct-acting ... These receptors were named after muscarine, to differentiate them from the other acetylcholine receptors (nicotinic receptors ... Most agonists for muscarine receptors are not selective for subtypes. Muscarinic receptors also signal via other pathways, for ... they produce their effects by binding to and activating cholinergic receptors. Final proof of the structure was given by Franz ...
... a peroxisome proliferator-activated receptor-alpha agonist, exerts anticonvulsive properties". Epilepsia. 50 (4): 943-8. doi: ... Lampen A, Carlberg C, Nau H (2001). "Peroxisome proliferator-activated receptor delta is a specific sensor for teratogenic ... Another potential target of antiepileptic drugs is the peroxisome proliferator-activated receptor alpha. Some anticonvulsants ... Next to the voltage-gated sodium channels and components of the GABA system, their targets include GABAA receptors, the GAT-1 ...
They are small molecules erythropoietin receptor agonists designed to activate the tissue-protective erythropoietin receptor. ... "Erythropoietin and small molecule agonists of the tissue-protective erythropoietin receptor increase FXN expression in neuronal ...
Sahebkar A, Chew GT, Watts GF (March 2014). "New peroxisome proliferator-activated receptor agonists: potential treatments for ... Wolf G (November 2003). "The function of the nuclear receptor peroxisome proliferator-activated receptor delta in energy ... "The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in ... "A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport". Proc. Natl. Acad ...
"Rab5a and rab11a mediate agonist-induced trafficking of protease-activated receptor 2". American Journal of Physiology. Cell ... Rab-11a controls intracellular trafficking of the innate immune receptor TLR4, and thereby also receptor signaling RAB11A has ... "The Rab11a GTPase controls Toll-like receptor 4-induced activation of interferon regulatory factor-3 on phagosomes". Immunity. ...
"The δ opioid receptor agonist SNC80 selectively activates heteromeric μ-δ opioid receptors". ACS Chemical Neuroscience. 3 (7): ... SNC-80 was the first non-peptide compound developed that was regarded as a highly selective agonist for the δ-opioid receptor. ... SNC-80 is an opioid analgesic compound that selectively activates μ-δ opioid receptor heteromers and is used in scientific ... nonpeptide delta opioid receptor agonist". Journal of Medicinal Chemistry. 37 (14): 2125-8. doi:10.1021/jm00040a002. PMID ...
"Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): A review". Biochemical Pharmacology. 92 ( ...
"Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review". Biochemical Pharmacology. 92 ( ... "Momordica charantia and its novel polypeptide regulate glucose homeostasis in mice via binding to insulin receptor". Journal of ...
"Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review". Biochem Pharmacol. 92 (1): 73- ...
In vitro, resveratrol was shown to act as an agonist of Peroxisome proliferator-activated receptor gamma, a nuclear receptor ... "Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review". Biochem Pharmacol. 92 (1): 73- ... The two resveratrol sulfates activate sirtuin 1 at least as much as resveratrol. Anti-inflammatory activity of sulfates against ... In vitro studies indicate resveratrol activates sirtuin 1, although this may be a downstream effect from its immediate ...
November 2014). "Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review". Biochemical ... Echinacea purpurea is used in pharmaceutics because of its ability to mobilize leukocytes, activate phagocytosis, and stimulate ...
These 3 channels are activated by the metabotropic glutamate receptor 1 agonist dihydroxyphenylglycine. In general, TRPC ... Pathological stress or hypertrophic agonists will trigger G-protein coupled receptors (GPCRs) and activates PLC to form DAG and ... TRPC1 channels are activated by receptors coupled to phospholipase C (PLC), mechanical stimulation, and depletion of ... There is at least one report that TRPC1 is also activated by stretching of the membrane and TRPC5 channels are activated by ...
... (OEA) is an endogenous peroxisome proliferator-activated receptor alpha (PPAR-α) agonist. It is a naturally ... OEA has been demonstrated to bind to the novel cannabinoid receptor GPR119. OEA has been suggested to be the receptor's ... 2007). "Novel cannabinoid receptors". Br J Pharmacol. 152 (5): 567-575. doi:10.1038/sj.bjp.0707481. PMC 2190013. PMID 17906678 ... "Deorphanization of a G protein-coupled receptor for oleoylethanolamide and its use in the discovery of small-molecule ...
"15-hydroxyeicosatetraenoic acid is a preferential peroxisome proliferator-activated receptor beta/delta agonist". Molecular ... HETE bind to and activate the G protein-coupled receptor, Leukotriene B4 receptor 2, i.e. BLT2. This receptor activation may ... 15(S)-HpETE and 15(S)-HETE also directly bind with and activate peroxisome proliferator-activated receptor gamma. This ... and activate peroxisome proliferator-activated receptor-γ". Journal of Biological Chemistry. 287 (50): 41651-66. doi:10.1074/ ...
"Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): A review". Biochemical Pharmacology. 92 ( ...
"Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): A review". Biochemical Pharmacology. 92 ( ...
"Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): A review". Biochemical Pharmacology. 92 ( ... full agonist or partial agonist of ERα agonist of G protein-coupled estrogen receptor (affinity of 133 nM) activation of ... However, genistein shows much higher affinity toward estrogen receptor β than toward estrogen receptor α. Data from in vitro ... "Peroxisome Proliferator-activated Receptor γ (PPARγ) as a Molecular Target for the Soy Phytoestrogen Genistein". Journal of ...
November 2014). "Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review". Biochemical ... two polyphenolic compounds that have been demonstrated as peroxisome proliferator-activated receptor gamma (PPAR gamma) ... agonists and GABAA modulators. Preclinical studies have evaluated their various potential applications including antioxidant, ...
However, it was not until 1981 that Stone and Perkins showed that quinolinic acid activates the N-methyl-D-aspartate receptor ( ... It acts as an NMDA receptor agonist. Quinolinic acid has a potent neurotoxic effect. Studies have demonstrated that quinolinic ... Quinolinic acid produces its toxic effect through several mechanisms, primarily as its function as an NMDA receptor agonist, ... This leads to over excitation of the NMDA receptor, which results in an influx of Ca2+ into the neuron. High levels of Ca2+ in ...
"Polyacetylenes from Notopterygium incisum-new selective partial agonists of peroxisome proliferator-activated receptor-gamma". ...
... , marketed as Parmodia, is a peroxisome proliferator-activated receptor alpha (PPARα) agonist. It is developed and ...
This kinase can be activated rapidly by the agonists of G protein-coupled receptors. It resides in both cytoplasm and nucleus, ... This kinase can also be activated after B-cell antigen receptor (BCR) engagement, which requires intact phospholipase C gamma ... 2002). "Novel protein kinase C isoforms regulate human keratinocyte differentiation by activating a p38 delta mitogen-activated ... Protein kinase C (PKC) is a family of serine- and threonine-specific protein kinases that can be activated by calcium and the ...
... new selective partial agonists of peroxisome proliferator-activated receptor-gamma". PLOS ONE. 8 (4): e61755. Bibcode:2013PLoSO ... Falcarindiol which activates the nuclear receptor PPARgamma, and induces expression of antioxidant enzymes in vitro. Phenethyl ... which activates the Nrf2/ARE pathway, leads to cytoprotection against oxidative and electrophilic stress". Archives of ...
Opioids have agonist actions on the intestinal opioid receptors, which when activated cause constipation. Drugs such as ... A notable opioid for the purpose of relief of diarrhoea is loperamide which is only an agonist of the μ opioid receptors in the ...
Type 2 diabetes
... are superior to other inhibitors of the renin-angiotensin system such as angiotensin receptor blockers (ARBs), or ... Fatty acids in the beta cells activate FOXO1, resulting in apopotosis of the beta cells. ... "Association Between Use of Sodium-Glucose Cotransporter 2 Inhibitors, Glucagon-like Peptide 1 Agonists, and Dipeptidyl ... "Effect of angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers on all-cause mortality, cardiovascular ...
Adenosine modulates the preBötC output via activation of the A1 and A2A receptor subtypes. An adenosine A1 receptor agonist has ... The channels are regulated by G protein-coupled receptors that can activate or inhibit the NALCN channels depending on the ... Metabotropic glutamate 1/5 receptors appear to be important for the increase in intracellular calcium that activate ICAN. The ... The suppression of muscarinic receptors and the activation of nicotinic receptors due to prenatal exposure to nicotine have ...
Receptor/signaling modulators GABAA receptor positive modulators GABA metabolism/transport modulators ... GABA-A receptor activity. • transmembrane signaling receptor activity. • inhibitory extracellular ligand-gated ion channel ... Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene. ... GABA-A receptor complex. • postsynaptic membrane. • membrane. • synapse. • integral component of plasma membrane. • chloride ...
Decoy receptors: LEVI-04 (p75NTR-Fc). PDGF. *Agonists: Becaplermin. *Platelet-derived growth factor (A, B, C, D) ... Pituitary adenylate cyclase-activating peptide (PACAP). *Pleiotrophin. *Renalase. *Thrombopoietin (see here instead) ... It is mainly used to treat cases of NSCLC that harbour mutations in the epidermal growth factor receptor (EGFR) gene. ... Afatinib covalently binds to cysteine number 797 of the epidermal growth factor receptor (EGFR) via a Michael addition (IC50 = ...
To further test the role of activated androgen receptors on AHN, flutamide, an antiandrogen drug that competes with ... Agonists. *Cations (incl. aluminum, calcium, gadolinium, magnesium, strontium, zinc). *Dehydroandrosterone. * ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Androgens bind to and activate androgen receptors (ARs) to mediate most of their biological effects. ...
... activities by activating estrogen receptors. Quercetin activates both estrogen receptor alpha (ERα) and beta (ERβ) with ... quercetin has also been found to act as an agonist of the G protein-coupled estrogen receptor (GPER). ... Quercetin also activates or inhibits the activities of a number of proteins. For example, quercetin is a non-specific ... "The stimulation of cell proliferation by quercetin is mediated by the estrogen receptor". (primary). Molecular Nutrition & Food ...
... of the AR but rather are weak partial agonists and are able to activate the receptor in the absence of more potent AR agonists ... Androgen receptor degradersEdit. Selective androgen receptor degraders (SARDs) are another new type of antiandrogen that has ... nonsteroidal AR antagonists are silent antagonists of the AR and do not activate the receptor. This may be why ... thereby preventing them from activating the receptor, AR NTD antagonists bind covalently to the NTD of the AR and prevent ...
receptor binding. • lipid binding. • RNA polymerase II transcription factor activity, ligand-activated sequence-specific DNA ... AgonistsEdit. *Endogenous progestogens (e.g., progesterone). *Synthetic progestogens (e.g., norethisterone, levonorgestrel, ... Main articles: Progesterone receptor A, Progesterone receptor B, and Progesterone receptor C ... The progesterone receptor (PR), also known as NR3C3 or nuclear receptor subfamily 3, group C, member 3, is a protein found ...
GABAA receptor positive allosteric modulator
... and sigma receptors. The neurosteroid Progesterone (PROG) that activates progesterone receptors expressed in peripheral and ... Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) ... The GABAA receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified ... Synaptic action of benzodiazepines: GABAA receptors located at synapses are activated when they are exposed to high ...
Altinicline is a nicotinic acetylcholine receptor agonist that has shown potential in the treatment of Parkinson's disease, ... An inactive palladium PdII catalyst is activated by a reduction to the Pd0 compound. The active palladium catalyst is the 14 ... 3.0.CO;2-G. Parkinson Study, Group (14 February 2006). "Randomized placebo-controlled study of the nicotinic agonist SIB-1508Y ... Recently, a nickel-catalyzed Sonogashira coupling has been developed which allows for the coupling of non-activated alkyl ...
Nuclear receptor modulators. AhR. *Agonists: Arachidonic acid metabolites (e.g., lipoxin A4, prostaglandin G2) ... Moreover, BaP has been found to activate a transposon, LINE1, in humans. ... expression of CYP1A1 depends on TOLL-like receptor 2 (TLR2), which is a eucaryotic receptor for bacterial surface ... Upon binding the transformed receptor translocates to the nucleus where it dimerises with ARNT (aryl hydrocarbon receptor ...
The drug LY354740 (also known as Eglumegad, an agonist of the metabotropic glutamate receptors 2 and 3) has been shown to ... A number of cytokines, such as IL-1, IL-6, IL-10 and TNF-alpha can activate the HPA axis, although IL-1 is the most potent. The ... In the brain, cortisol acts on two types of receptor - mineralocorticoid receptors and glucocorticoid receptors, and these are ... Over time, CRF receptors in the anterior pituitary will become down-regulated, producing depression and anxiety symptoms. ...
"Natural product agonists of peroxisome proliferator-activated receptor gamma (PPARγ): a review". Biochemical Pharmacology. 92 ( ... "Momordica charantia and its novel polypeptide regulate glucose homeostasis in mice via binding to insulin receptor". Journal of ...
Change in the receptor conformation such that binding of the agonist does not activate the receptor. This is seen with ion ... GABA receptors: GABA-A, GABA-C. GABA. Cl− , HCO−3 . Glutamate receptors: NMDA receptor, AMPA receptor, and Kainate receptor ... killer activated and killer inhibitor receptors (KARs and KIRs), complement receptors, Fc receptors, B cell receptors and T ... Antagonists bind to receptors but do not activate them. This results in a receptor blockade, inhibiting the binding of agonists ...
Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ... D1 receptor stimulation activates adenylyl cyclase and raises intracellular cyclic AMP, resulting in vasodilation of most ... Hughes AD, Sever PS (1989). "Action of fenoldopam, a selective dopamine (DA1) receptor agonist, on isolated human arteries". ... is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial agonist. Fenoldopam is used as ...
White blood cell
CD4+ helper T cells: T cells displaying co-receptor CD4 are known as CD4+ T cells. These cells have T-cell receptors and CD4 ... B cells make antibodies that can bind to pathogens, block pathogen invasion, activate the complement system, and enhance ... Medication induced - corticosteroids (for example, prednisone, β-agonists, lithium). *Cancer - either by growth factors ... CD8+ cytotoxic T cells: T cells displaying co-receptor CD8 are known as CD8+ T cells. These cells bind antigens presented on ...
Brain-derived neurotrophic factor
Tropomyosin receptor kinase B § Agonists. References. *^ a b c GRCh38: Ensembl release 89: ENSG00000176697 - Ensembl, May ... When the p75 receptor is activated, it leads to activation of NFkB receptor. Thus, neurotrophic signaling may trigger ... The TrkB receptor is encoded by the NTRK2 gene and is member of a receptor family of tyrosine kinases that includes TrkA and ... receptor binding. • neurotrophin TRKB receptor binding. • growth factor activity. • GO:0001948 protein binding. ...
The normal amount of dopamine released during sex is insufficient to stimulate the larger number of dopamine receptors.[9 ... Upon reaching a climax, chemicals are released in the brain and motor signals are activated that will cause quick cycles of ... Other drugs which may be helpful in the treatment of this condition include dopamine agonists, oxytocin, phosphodiesterase type ... Psychiatric medicine is known to cause the brain to form more dopamine receptors for the dopamine blocking effect. ...
Nociceptinski receptor - Vikipedija, slobodna enciklopedija
1995). „Isolation and structure of the endogenous agonist of opioid receptor-like ORL1 receptor.". Nature. 377 (6549): 532-5. ... 1996). „Expression of alternate forms of brain opioid 'orphan' receptor mRNA in activated human peripheral blood lymphocytes ... Nociceptinski receptor (NOP, orfaninski FQ receptor, kapa tip 3 opioidni receptor) je protein koji je kod čoveka kodiran OPRL1 ... Kalcijum-detektujući receptor • GABA B (1, 2) • Glutamatni receptor (Metabotropni glutamat (1, 2, 3, 4, 5, 6, 7, 8)) • GPRC6A ...
Nikotin - Wikipedija, prosta enciklopedija
Suemaru K, Kohnomi S, Umeda K, Araki H. (2008). "Alpha7 nicotinic receptor agonists have reported to reverse the PPI disruption ... "Nicotine self-administration acutely activates brain reward systems and induces a long-lasting increase in reward sensitivity" ... 2004). "Evidence of association between smoking and alpha7 nicotinic receptor subunit gene in schizophrenia patients". ... Gilbert Lagrue, François Lebargy, Anne Cormier, "From nicotinic receptors to smoking dependence: therapeutic prospects" ...
This receptor is expressed by activated, but not by resting, T and B cells. TRAF2 and TRAF5 can interact with this receptor, ... Agonists: Albinterferon. *Interferon alpha (interferon alfa, IFN-α). *Interferon alfa (IFNA1, IFNA2, IFNA4, IFNA5, IFNA6, IFNA7 ... Receptor/signaling modulators. Signaling peptide/protein receptor modulators. Growth factor receptor modulators. ... transmembrane signaling receptor activity. • tumor necrosis factor-activated receptor activity. • nerve growth factor binding. ...
Decoy receptors: LEVI-04 (p75NTR-Fc). PDGF. *Agonists: Becaplermin. *Platelet-derived growth factor (A, B, C, D) ... Pituitary adenylate cyclase-activating peptide (PACAP). *Pleiotrophin. *Renalase. *Thrombopoietin (see here instead) ...
Endothelium-derived hyperpolarizing factor
An increase in extracellular K+ has been shown to activate an ouabain-sensitive electrogenic Na+-K+-ATPase followed by ... Endothelium-derived CNP has been proposed to act as an EDHF via specific C-subtype of natriuretic peptide receptor, however the ... for the EDHF phenomenon is that direct intercellular communication via gap junctions allows passive spread of agonist-induced ... reach underlying vascular smooth muscle cells at a concentration sufficient to activate ion channels, and initiate smooth ...
Platelet-derived growth factor
There are five different isoforms of PDGF that activate cellular response through two different receptors. Known ligands ... Agonists: des(1-3)IGF-1. *Insulin-like growth factor-1 (somatomedin C) ... The receptor for PDGF, PDGFR is classified as a receptor tyrosine kinase (RTK), a type of cell surface receptor. Two types of ... Like many other growth factors that have been linked to disease, PDGF and its receptors have provided a market for receptor ...
D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: D2 receptor antagonists (e.g., domperidone, ... Receptors. Main article: Bradykinin receptor. *The B1 receptor (also called bradykinin receptor B1) is expressed only as ... The kinin B1 and B2 receptors belong to G protein coupled receptor (GPCR) family. ... This receptor has been also described to play a role in inflammation. Most recently, it has been shown that the kinin B1 ...
Tumor necrosis factor alpha
TNF receptor superfamily modulators. LTB (TNFβ). *Agonists: Lymphotoxin (α (TNFβ), β (TNFC)) ... which then activates JNK. JNK translocates to the nucleus and activates transcription factors such as c-Jun and ATF2. The JNK ... TNF can bind two receptors, TNFR1 (TNF receptor type 1; CD120a; p55/60) and TNFR2 (TNF receptor type 2; CD120b; p75/80). TNFR1 ... TRAF2/Rac activates the JNK-inducing upstream kinases of MLK2/MLK3, TAK1, MEKK1 and ASK1 (either directly or through GCKs ...
Coagulation factor II receptor
Proteinase-activated receptor 1 (PAR1) also known as Protease-activated receptor 1 or coagulation factor II (thrombin) receptor ... Distinct determinants for agonist-triggered versus tonic internalization and intracellular localization". The Journal of ... Howell DC, Laurent GJ, Chambers RC (Apr 2002). "Role of thrombin and its major cellular receptor, protease-activated receptor-1 ... Protease-activated receptor GRCh38: Ensembl release 89: ENSG00000181104 - Ensembl, May 2017 GRCm38: Ensembl release 89: ...
σ receptors, IC50=145μM. Pharmacokinetics. The pharmacokinetics of lamotrigine follow first-order kinetics, with a half- ... However, it does inhibit native and recombinant high-voltage-activated calcium channels (N- and P/Q/R-types) at therapeutic ... Sigma receptor modulators. σ1. *Agonists: 3-PPP. *4-PPBP. *5-MeO-DMT ... NMDA receptor antagonists (e.g., ketamine, dextromethorphan, methadone). *Opioids (e.g., hydrocodone, morphine, oxycodone, ...
... a CD36 receptor agonist) versus thrombin treatment, which may implicate CASS4 mediated signaling in platelet hyperreactivity.[ ... "Phosphoproteomic analysis of platelets activated by pro-thrombotic oxidized phospholipids and thrombin". PLOS ONE. 9 (1): ...
Estrogen insensitivity syndrome
... but none of them were found to be more efficacious than estradiol in activating the mutated receptor and hence in overcoming ... A group of other ERα agonists that included ethinylestradiol, diethylstilbestrol, tamoxifen, clomifene, and raloxifene were ... which is caused by a defective estrogen receptor (ER) - specifically, the estrogen receptor alpha (ERα) - that results in an ... EIS results when the function of the estrogen receptor alpha (ERα) is impaired. The ERα protein (pictured) mediates most of the ...
Systemic Chemotherapy Is Modulated by Platelet-Activating Factor-Receptor Agonists
... Ravi P. Sahu,1,2 Matheus Ferracini,2 and ... Y. Yao, J. E. Wolverton, Q. Zhang et al., "Ultraviolet B radiation generated platelet-activating factor receptor agonist ... "Ultraviolet B radiation of human skin generates platelet-activating factor receptor agonists," Photochemistry and Photobiology ... P. C. Hackler, S. Reuss, R. L. Konger, J. B. Travers, and R. P. Sahu, "Systemic platelet-activating factor receptor activation ...
Protection from liver fibrosis by a peroxisome proliferator-activated receptor δ agonist | PNAS
Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear receptor family of ligand-activated ... Protection from liver fibrosis by a peroxisome proliferator-activated receptor δ agonist. Keiko Iwaisako, Michael Haimerl, Yong ... 2001) A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proc Natl ... Peroxisome proliferator-activated receptor delta (PPARδ), a member of the nuclear receptor family, is emerging as a key ...
Therapeutic Roles of Peroxisome Proliferator-Activated Receptor Agonists | Diabetes
The three peroxisome proliferator-activated receptor (PPAR) isoforms PPARα, -γ, and -δ are nuclear receptors activated by fatty ... Therapeutic Roles of Peroxisome Proliferator-Activated Receptor Agonists Message Subject (Your Name) has forwarded a page to ... Sidhu JS, Cowan D, Kaski JC: The effects of rosiglitazone, a peroxisome proliferator-activated receptor-gamma agonist, on ... In addition, agents that activate multiple PPAR isoforms are now in development: dual PPARα/γ agonists and pan-PPAR agonists ( ...
Modulation Effect of Peroxisome Proliferator-Activated Receptor Agonists on Lipid Droplet Proteins in Liver
... Yun-Xia Zhu,1 Ming ... Peroxisome proliferator-activated receptor (PPAR) agonists are used for treating hyperglycemia and type 2 diabetes. However, ... or administration of PPAR agonists. Mice with diet-induced obesity were treated with the PPARγ or PPARα agonist, pioglitazone ... In mice, LSDP5 was not detected, even in the context of insulin resistance or treatment with PPAR agonists. However, LSDP5 was ...
Protease-Activated Receptor-4, PAR-4 Agonist, amide
PAR-4 Agonist, amide; PAR-4 agonist peptide stimulates thromboxane production by human platelets with the maximal response to ... this agonist being approximately half of that observed after maximal thrombin stimulation.; AYPGKF-NH2; H-Ala-Tyr-Pro-Gly-Lys- ... Peptides , Cardiovascular Related Peptides ,, Protease-Activated Receptor-4, PAR-4 Agonist, amide. ... 2003). Protease-activated receptors 1 and 4 mediate thrombin signaling in endothelial cells Blood 102 doi: 10.1182/blood-2003- ...
Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y2 Receptor. - PubMed - NCBI
Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y2 Receptor.. Rafehi M1, ... A homology model of the nucleotide-activated P2Y2R was created based on the X-ray structures of the P2Y1 receptor. Docking ... Significant reduction in agonist potency was observed for all other receptor mutants (Phe111, His184, Ser193, Phe261, Tyr268, ... An ionic lock between Asp185 and Arg292 that is probably involved in receptor activation interacts with the phosphate groups. ...
Glucagon-like Peptide-1 receptor agonists activate rodent thyroid C-cells causing calcitonin release and C-cell proliferation. ...
... The GLP-1 receptor was localized to rodent C-cells. GLP-1 receptor agonists stimulated calcitonin release, up-regulation of ... In contrast, humans and/or cynomolgus monkeys had low GLP-1 receptor expression in thyroid C-cells, and GLP-1 receptor agonists ... Nevertheless, the long-term consequences of sustained GLP-1 receptor activation in the human thyroid remain unknown and merit ...
The peroxisome proliferator-activated receptor γ agonist pioglitazone reduces the development of cartilage lesions in an...
The peroxisome proliferator-activated receptor γ agonist pioglitazone reduces the development of cartilage lesions in an ... Chamisa L. Herrera, Dae Young Kim, Senthil R. Kumar, Jeffrey N. Bryan, Peroxisome proliferator activated receptor γ protein ... Emerging evidence indicates that peroxisome proliferator-activated receptor γ (PPARγ) may have protective effects in ... Egr-1 contributes to IL-1-mediated down-regulation of peroxisome proliferator-activated receptor γ expression in human ...
In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5'-[gamma-[35S]thio]...
In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5-[gamma-[35S]thio]- ... In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5-[gamma-[35S]thio]- ... In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5-[gamma-[35S]thio]- ... In vitro autoradiography of receptor-activated G proteins in rat brain by agonist-stimulated guanylyl 5-[gamma-[35S]thio]- ...
Antioxidative, Antinitrative, and Vasculoprotective Effects of a Peroxisome Proliferator-Activated Receptor-γ Agonist in...
Antioxidative, Antinitrative, and Vasculoprotective Effects of a Peroxisome Proliferator-Activated Receptor-γ Agonist in ... Antioxidative, Antinitrative, and Vasculoprotective Effects of a Peroxisome Proliferator-Activated Receptor-γ Agonist in ... Antioxidative, Antinitrative, and Vasculoprotective Effects of a Peroxisome Proliferator-Activated Receptor-γ Agonist in ... Antioxidative, Antinitrative, and Vasculoprotective Effects of a Peroxisome Proliferator-Activated Receptor-γ Agonist in ...
PEROXISOME-PROLIFERATOR ACTIVATED RECEPTOR-ALPHA AGONISTS FOR ORGAN PRESERVATION - University of Pittsburgh of the Commonwealth...
... or reversing organ damage and/or enhancing organ preservation by administration of a peroxisome-proliferator activated receptor ... In preferred embodiments, the concentration of the PPARα agonist is present in an amount that activates the nuclear receptor ... PPARβ agonist); dopamine (dopamine receptor agonist dopamine); linolenic acid (essential fatty acid); β-NAD (involved in energy ... PPARα is a ligand-activated transcriptional factor that is a member of the nuclear receptor family (see e.g., van Raalte, Pharm ...
RCSB PDB - 1NYX: Ligand binding domain of the human peroxisome proliferator activated receptor gamma in complex with an agonist
Ligand binding domain of the human peroxisome proliferator activated receptor gamma in complex with an agonist. *DOI: 10.2210/ ... A new and improved synthesis of the peroxisome proliferator-activated receptor (PPAR) agonist ragaglitazar applicable for large ... A new and improved synthesis of the peroxisome proliferator-activated receptor (PPAR) agonist ragaglitazar applicable for large ... peroxisome proliferator activated receptor gamma. A, B. 276. Homo sapiens. Mutation(s): 0 Gene Names: PPARG, NR1C3. ...
Frontiers | Peroxisome proliferator-activated receptor agonists modulate neuropathic pain: a link to chemokines? | Frontiers in...
Peroxisome proliferator-activated receptors are a family of nuclear receptors known for their roles in metabolism. Recent ... PPAR agonists have wide-ranging effects including inhibition of chemokine expression and pain behavior reduction in animal ... PPAR agonists have wide-ranging effects including inhibition of chemokine expression and pain behavior reduction in animal ... In early clinical research, one PPARα agonist, palmitoylethanolamide, shows promise in relieving chronic pain. If this link can ...
Remediated Sequence - 1KNU: LIGAND BINDING DOMAIN OF THE HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA IN...
... dual PPARalpha/gamma agonists with hypolipidemic and antidiabetic activity ... LIGAND BINDING DOMAIN OF THE HUMAN PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA IN COMPLEX WITH A SYNTHETIC AGONIST. ... Chain A: PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA. Chain Downloadable Files. Download FASTA File. View Sequence & DSSP ...
Gating of Transient Receptor Potential Melastatin 8 (TRPM8) Channels Activated by Cold and Chemical Agonists in Planar Lipid...
Gating of Transient Receptor Potential Melastatin 8 (TRPM8) Channels Activated by Cold and Chemical Agonists in Planar Lipid ... Gating of Transient Receptor Potential Melastatin 8 (TRPM8) Channels Activated by Cold and Chemical Agonists in Planar Lipid ... Gating of Transient Receptor Potential Melastatin 8 (TRPM8) Channels Activated by Cold and Chemical Agonists in Planar Lipid ... Gating of Transient Receptor Potential Melastatin 8 (TRPM8) Channels Activated by Cold and Chemical Agonists in Planar Lipid ...
Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in...
Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in ... Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in ... Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in ... Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in ...
Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in...
Dual Peroxisome Proliferator-Activated Receptor α/δ Agonist GFT505 Improves Hepatic and Peripheral Insulin Sensitivity in ... We investigated the effect of GFT505, a dual peroxisome proliferator-activated receptor (PPAR)-α/δ agonist, on peripheral and ... Effects of peroxisome proliferator-activated receptor (PPAR)-α and PPAR-γ agonists on glucose and lipid metabolism in patients ... Mechanism of action of a peroxisome proliferator-activated receptor (PPAR)-δ agonist on lipoprotein metabolism in dyslipidemic ...
IJMS | Free Full-Text | The Peroxisome Proliferator-Activated Receptor (PPAR) α Agonist Fenofibrate Suppresses Chemically...
This study was designed to determine whether fenofibrate, a PPARα agonist, can suppress 4-nitroquinoline 1-oxide (4-NQO)- ... and decreased the immunohistochemical expression of IGF-1 receptor (IGF-1R), phosphorylated Akt, and phosphorylated Erk1/2 in ... Activation of peroxisome proliferator-activated receptor (PPAR) α disrupts growth-related activities in a variety of human ... The Peroxisome Proliferator-Activated Receptor (PPAR) α Agonist Fenofibrate Suppresses Chemically Induced Lung Alveolar ...
Cellular And Biophysical Pipeline For Peroxisome Proliferator-activated Receptor (PPAR) Delta Agonist Screening | 72460
Peroxisome Proliferator Activated Receptors delta (PPARÎ´) has been associated with pathophysiological processes, such as ... Cellular and biophysical pipeline for peroxisome proliferator-activated receptor (PPAR) delta agonist screening. ... Peroxisome Proliferator Activated Receptors delta (PPARδ) has been associated with pathophysiological processes, such as ... without physical interaction with the receptor. Finally, this approach may improve the effectiveness of screening agonists ...
Peroxisome Proliferator-Activated Receptor-γ Agonist 15-Deoxy-Δ12,1412,14-Prostaglandin J2 Ameliorates Experimental Autoimmune...
Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated ... Discrete roles for peroxisome proliferator-activated receptor γ and retinoid X receptor in recruiting nuclear receptor ... Peroxisome Proliferator-Activated Receptor-γ Agonist 15-Deoxy-Δ12,1412,14-Prostaglandin J2 Ameliorates Experimental Autoimmune ... Peroxisome Proliferator-Activated Receptor-γ Agonist 15-Deoxy-Δ12,1412,14-Prostaglandin J2 Ameliorates Experimental Autoimmune ...
Cardiac hypertrophy caused by peroxisome proliferator- activated receptor-gamma agonist treatment occurs independently of...
Peroxisome proliferator-activated receptor (PPAR)-gamma ligands are insulin sensitizers, widely used in the treatment of type 2 ... Cardiac hypertrophy caused by peroxisome proliferator- activated receptor-gamma agonist treatment occurs independently of ... Peroxisome proliferator-activated receptor (PPAR)-gamma ligands are insulin sensitizers, widely used in the treatment of type 2 ... These data indicate that cardiac hypertrophy after PPAR-gamma agonist treatment can occur in the absence of myocardial insulin ...
The B1-agonist [des-Arg10]-kallidin activates transcription factor NF-kappaB and induces homologous upregulation of the...
The bradykinin B1-receptor is strongly upregulated under chronic inflammatory conditions. However, the mechanism and reason are ... is now recognized as a key inflammatory mediator which is activated by the B1-agonist but which is also involved in B1-receptor ... The B1-agonist [des-Arg10]-kallidin activates transcription factor NF-kappaB and induces homologous upregulation of the ... We furthermore report the novel observation that the B1-receptor is upregulated by its own agonist which was completely blocked ...
352017-71-1 - Selective Protease-Activated Receptor 4 (PAR4) Agonist - Ala-Tyr-Pro-Gly-Lys-Phe-NH|sub|2|/sub| - AYPGKF-NH2 -...
Prevention of Ethanol-Induced Liver Injury in Rats by an Agonist of Peroxisome Proliferator-Activated Receptor-γ, Pioglitazone ...
Agonists of peroxisome proliferator-activated receptor (PPAR)-γ have been shown to reduce tumor necrosis factor-α (TNF-α)- ... Prevention of Ethanol-Induced Liver Injury in Rats by an Agonist of Peroxisome Proliferator-Activated Receptor-γ, Pioglitazone ... Prevention of Ethanol-Induced Liver Injury in Rats by an Agonist of Peroxisome Proliferator-Activated Receptor-γ, Pioglitazone ... Prevention of Ethanol-Induced Liver Injury in Rats by an Agonist of Peroxisome Proliferator-Activated Receptor-γ, Pioglitazone ...
Peroxisome Proliferator-activated Receptor γ Agonists Induce Proteasome-dependent Degradation of Cyclin D1 and Estrogen...
Peroxisome Proliferator-activated Receptor γ Agonists Induce Proteasome-dependent Degradation of Cyclin D1 and Estrogen ... Peroxisome Proliferator-activated Receptor γ Agonists Induce Proteasome-dependent Degradation of Cyclin D1 and Estrogen ... Peroxisome Proliferator-activated Receptor γ Agonists Induce Proteasome-dependent Degradation of Cyclin D1 and Estrogen ... Peroxisome Proliferator-activated Receptor γ Agonists Induce Proteasome-dependent Degradation of Cyclin D1 and Estrogen ...
Triglyceride:High-Density Lipoprotein Cholesterol Effects in Healthy Subjects Administered a Peroxisome Proliferator Activated...
Density Lipoprotein Cholesterol Effects in Healthy Subjects Administered a Peroxisome Proliferator Activated Receptor δ Agonist ... Density Lipoprotein Cholesterol Effects in Healthy Subjects Administered a Peroxisome Proliferator Activated Receptor δ Agonist ... Density Lipoprotein Cholesterol Effects in Healthy Subjects Administered a Peroxisome Proliferator Activated Receptor δ Agonist ... Density Lipoprotein Cholesterol Effects in Healthy Subjects Administered a Peroxisome Proliferator Activated Receptor δ Agonist ...
2-furoyl-LIGRLO-amide: A potent and selective Proteinase-Activated Receptor 2 (PAR-2) agonist | Journal of Pharmacology and...
2-furoyl-LIGRLO-amide: A potent and selective Proteinase-Activated Receptor 2 (PAR-2) agonist. John J McGuire, Mahmoud ... 2-furoyl-LIGRLO-amide: A potent and selective Proteinase-Activated Receptor 2 (PAR-2) agonist. John J McGuire, Mahmoud ... 2-furoyl-LIGRLO-amide: A potent and selective Proteinase-Activated Receptor 2 (PAR-2) agonist. John J McGuire, Mahmoud ... 2-furoyl-LIGRLO-amide: A potent and selective Proteinase-Activated Receptor 2 (PAR-2) agonist ...
μ-Opioid Receptors: Correlation of Agonist Efficacy for Signalling with Ability to Activate Internalization. Jamie McPherson, ... 2008) Agonist binding, agonist affinity and agonist efficacy at G protein-coupled receptors. Br J Pharmacol 153:1353-1363. ... μ-Opioid Receptors: Correlation of Agonist Efficacy for Signalling with Ability to Activate Internalization. Jamie McPherson, ... μ-Opioid Receptors: Correlation of Agonist Efficacy for Signalling with Ability to Activate Internalization. Jamie McPherson, ...
Differential gene expression in mouse primary hepatocytes exposed to the peroxisome proliferator-activated receptor α agonists
They function as agonists for peroxisome proliferator-activated receptor alpha (PPARα). PPARα is a transcriptional nuclear ... The peroxisome proliferator-activated receptor mediates the induction of CYP4A6, a cytochrome P450 fatty acid omega-hydroxylase ... Schoonjans K, Staels B, Auwerx J. Role of the peroxisome proliferator-activated receptor (PPAR) in mediating the effects of ... Role of peroxisome proliferator-activated receptor alpha in altered cell cycle regulation in mouse liver. Carcinogenesis. 1998; ...
Agonist-Dependent Modulation of G Protein-Coupled Receptor Kinase 2 by Mitogen-Activated Protein Kinases | Molecular...
Agonist-Dependent Modulation of G Protein-Coupled Receptor Kinase 2 by Mitogen-Activated Protein Kinases. Ana Elorza, Susana ... Agonist-Dependent Modulation of G Protein-Coupled Receptor Kinase 2 by Mitogen-Activated Protein Kinases. Ana Elorza, Susana ... Agonist-Dependent Modulation of G Protein-Coupled Receptor Kinase 2 by Mitogen-Activated Protein Kinases. Ana Elorza, Susana ... Agonist-Dependent Modulation of G Protein-Coupled Receptor Kinase 2 by Mitogen-Activated Protein Kinases ...
PPARPPARsMitogen-activaLigandsProteinsAntagonistsPioglitazonePeroxisome Proliferator-RosiglitazonePlatelet-activating factoFenofibrateLipidHuman peroxisome proliInflammationSelectiveIntracellularRetinoid X receptInducePhosphorylationMicePeptideInhibitionInhibitEndogenousTranscriptionGenesProtein-coupled receptorsMetabolismMuscarinic receptorsBindsEfficacyProliferator-activatedProtease-activatedMediateGPCRSkeletalKinaseModulateMechanismsExtracellularInsulinAntagonistSuppressSyntheticActivationInflammatoryPAR2Gene expressionThromboxanePPARgammaStimulate
- Peroxisome proliferator-activated receptor delta (PPARδ), a member of the nuclear receptor family, is emerging as a key metabolic regulator with pleiotropic actions on various tissues including fat, skeletal muscle, and liver. (pnas.org)
- Here we show that the PPARδ agonist KD3010, but not the well-validated GW501516, dramatically ameliorates liver injury induced by carbon tetrachloride (CCl 4 ) injections. (pnas.org)
- In conclusion, our data demonstrate that an orally active PPARδ agonist has hepatoprotective and antifibrotic effects in animal models of liver fibrosis, suggesting a possible mechanistic and therapeutic approach in treating patients with chronic liver diseases. (pnas.org)
- All three subtypes of PPARs, including PPARδ, can be activated by fatty acids and fatty-acid derivatives. (pnas.org)
- Based on studies using gene deletion and synthetic agonists, PPARδ is emerging as a key metabolic regulator. (pnas.org)
- PPARδ agonists improve glucose and lipid homeostasis ( 4 , 5 ) and increase skeletal muscle fatty-acid metabolism. (pnas.org)
- PPARδ agonists have been shown to be exercise mimetics and to increase endurance in mice that already are undergoing exercise ( 6 ). (pnas.org)
- To determine whether PPARδ agonists are beneficial in experimental liver fibrosis, mice were treated orally with a PPARδ agonist, KD3010, or with the well-validated PPARδ agonist GW501516. (pnas.org)
- PPARδ Agonist KD3010 Protects from Liver Injury. (pnas.org)
- Liver injury was induced by repeated injections of CCl 4 , and mice were treated daily with vehicle, the widely used PPARδ agonist GW501516 ( 6 ), or the PPARδ agonist KD3010 by oral gavage. (pnas.org)
- Peroxisome proliferator-activated receptors (PPARs) play key roles in the regulation of energy homeostasis and inflammation, and agonists of PPARα and -γ are currently used therapeutically. (diabetesjournals.org)
- Fibrates, first used in the 1970s for their lipid-modifying properties, were later shown to activate PPARα. (diabetesjournals.org)
- PPARγ agonists are therefore used to treat type 2 diabetes. (diabetesjournals.org)
- PPARα and -γ agonists also affect inflammation, vascular function, and vascular remodeling. (diabetesjournals.org)
- Dual PPARα/γ agonists (currently in development) look set to combine the properties of thiazolidinediones and fibrates, and they hold considerable promise for improving the management of type 2 diabetes and providing an effective therapeutic option for treating the multifactorial components of CVD and the metabolic syndrome. (diabetesjournals.org)
- The three peroxisome proliferator-activated receptor (PPAR) isoforms PPARα, -γ, and -δ are nuclear receptors activated by fatty acids and fatty acid-derived eicosanoids. (diabetesjournals.org)
- Subsequently, the thiazolidinediones, which are structural analogs of fibrates, were shown to activate PPARγ. (diabetesjournals.org)
- Synthetic PPARδ agonists have recently been developed, and preclinical work is clarifying the function of this receptor. (diabetesjournals.org)
- In addition, agents that activate multiple PPAR isoforms are now in development: dual PPARα/γ agonists and pan-PPAR agonists (PPARα/γ/δ). (diabetesjournals.org)
- This review examines the efficacy of PPAR agonists in conditions for which they are currently indicated (dyslipidemia and type 2 diabetes) and discusses their potential in the treatment of other conditions, including cardiovascular disease (CVD) and the metabolic syndrome. (diabetesjournals.org)
- Peroxisome proliferator-activated receptor (PPAR) agonists are used for treating hyperglycemia and type 2 diabetes. (hindawi.com)
- Here, we evaluated the expression levels of FSP27/CIDEC and LSDP5 and the regulation of these proteins by consumption of a high-fat diet (HFD) or administration of PPAR agonists. (hindawi.com)
- Mice with diet-induced obesity were treated with the PPAR γ or PPAR α agonist, pioglitazone or fenofibrate, respectively. (hindawi.com)
- In mice, LSDP5 was not detected, even in the context of insulin resistance or treatment with PPAR agonists. (hindawi.com)
- Emerging evidence indicates that peroxisome proliferator-activated receptor γ (PPARγ) may have protective effects in osteoarthritis (OA). (wiley.com)
- The aim of this study was to evaluate the in vivo effect of a PPARγ agonist, pioglitazone, on the development of lesions in a canine model of OA, and to explore the influence of pioglitazone on the major signaling and metabolic pathways involved in OA pathophysiologic changes. (wiley.com)
- Background- Peroxisome proliferator-activated receptor (PPAR) signaling pathways have been reported to exert anti-inflammatory effects and attenuate atherosclerosis formation. (ahajournals.org)
- The present study tested the hypothesis that a PPARγ agonist may exert significant endothelial protection by antioxidative and antinitrative effects. (ahajournals.org)
- Methods and Results- Male New Zealand White rabbits were randomized to receive a normal (control) or a high-cholesterol diet and treated with vehicle or rosiglitazone (a PPARγ agonist) 3 mg · kg −1 · d −1 for 5 weeks beginning 3 weeks after the high-cholesterol diet. (ahajournals.org)
- Conclusions- The PPARγ agonist rosiglitazone exerted a significant vascular protective effect in hypercholesterolemic rabbits, most likely by attenuation of oxidative and nitrative stresses. (ahajournals.org)
- The endothelial protective effects of PPARγ agonists may reduce leukocyte accumulation in vascular walls and contribute to their antiatherosclerotic effect. (ahajournals.org)
- 3 Considerable evidence indicates that treatment with PPARγ agonists improves endothelial function in diabetic animal models and diabetic patients. (ahajournals.org)
- 4 However, whether this endothelial protective effect is secondary to improved glucose metabolism by the drug or PPARγ agonists exert direct endothelial protection remains unknown. (ahajournals.org)
- Methods and compositions for reducing, preventing or reversing organ damage and/or enhancing organ preservation by administration of a peroxisome-proliferator activated receptor-alpha (PPARα) agonist to the organ. (freepatentsonline.com)
- 1. A method for preventing, reducing or reversing organ damage or enhancing organ preservation comprising contacting the organ with a PPARα agonist in an amount effective to prevent, reduce or reverse organ damage or enhance organ preservation. (freepatentsonline.com)
- 2. The method of claim 1, wherein the PPARα agonist comprises a fibric acid derivative. (freepatentsonline.com)
- 4. The method of claim 1, wherein the PPARα agonist is gemfibrozil. (freepatentsonline.com)
- 5. The method of claim 1, wherein the PPARα agonist is 4-chloro-6-(2,3-xylidino)-2-pyrimidinylthioacetic acid. (freepatentsonline.com)
- 12. The method of claim 1, wherein the PPARα agonist is delivered into the organ's blood supply while the organ is being perfused by a cardiovascular system. (freepatentsonline.com)
- 17. The method of claim 14, wherein the PPARα agonist is gemfibrozil. (freepatentsonline.com)
- 18. The method of claim 14, wherein the PPARα agonist is 4-chloro-6-(2,3-xylidino)-2-pyrimidinylthioacetic acid. (freepatentsonline.com)
- A new and improved synthesis of the peroxisome proliferator-activated receptor (PPAR) agonist ragaglitazar applicable for large-scale preparation has been developed. (rcsb.org)
- PPAR agonists have wide-ranging effects including inhibition of chemokine expression and pain behavior reduction in animal models. (frontiersin.org)
- Experimental evidence suggests a connection between the pain ameliorating effects of PPAR agonists and suppression of inflammatory gene expression, including chemokines. (frontiersin.org)
- In early clinical research, one PPARα agonist, palmitoylethanolamide (PEA), shows promise in relieving chronic pain. (frontiersin.org)
- If this link can be better established, PPAR agonists may represent a new drug therapy for neuropathic pain. (frontiersin.org)
- Early clinical trials indicate that PPAR agonists can be effective at alleviating neuropathic pain, even in patients who failed to respond to other treatments. (frontiersin.org)
- While much remains to be understood about how PPAR agonists achieve this effect, it seems probable that inhibiting the expression of pain-causing inflammatory mediators like chemokines represents at least one mechanism for pain reduction. (frontiersin.org)
- We investigated the effect of GFT505, a dual peroxisome proliferator-activated receptor (PPAR)-α/δ agonist, on peripheral and hepatic insulin sensitivity. (diabetesjournals.org)
- CONCLUSIONS The dual PPARα/δ agonist GFT505 is a liver-targeted insulin-sensitizer that is a promising drug candidate for the treatment of type 2 diabetes and nonalcoholic fatty liver disease. (diabetesjournals.org)
- Activation of peroxisome proliferator-activated receptor (PPAR) α disrupts growth-related activities in a variety of human cancers. (mdpi.com)
- This study was designed to determine whether fenofibrate, a PPARα agonist, can suppress 4-nitroquinoline 1-oxide (4-NQO)-induced proliferative lesions in the lung of obese hyperlipidemic mice. (mdpi.com)
- Peroxisome Proliferator Activated Receptors delta (PPARδ) has been associated with pathophysiological processes, such as inflammation, obesity, dyslipidemia, diabetes, cancer, and cardiovascular diseases, being considered as new therapeutic targets for these processes. (omicsonline.org)
- Here, we developed and set up one way to perform a screening to drive PPARδ agonists. (omicsonline.org)
- As example, we could find one plant extract that contains interesting molecules, capable to binding and activate PPARδ. (omicsonline.org)
- In conclusion, this pipeline presented more efficacy in comparison to the single activation screening, because it can exclude false-positives that may promote indirect PPARδ activation, without physical interaction with the receptor. (omicsonline.org)
- Finally, this approach may improve the effectiveness of screening agonists targeting PPARδ for drug development. (omicsonline.org)
- Her PhD project deals with the development of a screening pipeline for PPAR delta agonists. (omicsonline.org)
- Peroxisome proliferator-activated receptors (PPAR) are members of a nuclear hormone receptor superfamily that includes receptors for steroids, retinoids, and thyroid hormone, all of which are known to affect the immune response. (jimmunol.org)
- PPAR binds to the peroxisome proliferator-responsive element as a heterodimer with retinoid X receptor (RXR). (jimmunol.org)
- RXR also forms heterodimers with other members of the nuclear receptor superfamily, and these interactions influence the PPAR-regulated transcriptional activation because of the competition among various RXR heterodimerization partners for RXR ( 5 , 6 ). (jimmunol.org)
- Peroxisome proliferator-activated receptor (PPAR)-gamma ligands are insulin sensitizers, widely used in the treatment of type 2 diabetes. (nih.gov)
- We treated mice with cardiomyocyte-restricted knockout of insulin receptors (CIRKO) and littermate controls (wild type) with 2-(2-(4-phenoxy-2-propylphenoxy) ethyl) indole-5-acetic acid (COOH), which is a non-thiazolidinedione PPAR-gamma agonist for 2 wk. (nih.gov)
- These data indicate that cardiac hypertrophy after PPAR-gamma agonist treatment can occur in the absence of myocardial insulin signaling and is likely secondary to the hemodynamic consequences of plasma volume expansion. (nih.gov)
- Treatment of MCF-7 cells with the peroxisome proliferator-activated receptor (PPAR) γ agonists ciglitazone or 15-deoxy-Δ12,14-prostaglandin J2 resulted in a concentration- and time-dependent decrease of cyclin D1 and estrogen receptor (ER) α proteins, and this was accompanied by decreased cell proliferation and G 1 -G 0 →S-phase progression. (aacrjournals.org)
- Down-regulation of cyclin D1 and ERα by PPARγ agonists was inhibited in cells cotreated with the proteasome inhibitors MG132 and PSII, but not in cells cotreated with the protease inhibitors calpain II and calpeptin. (aacrjournals.org)
- PPARγ is widely expressed in multiple tumors and cell lines, and this receptor has also become a target for developing new anticancer drugs that will take advantage of the antiproliferative effects mediated through PPARγ. (aacrjournals.org)
- Wild-type PPARγ mRNA was expressed in all tumor specimens, and receptor mutants were not detected in any of these samples. (aacrjournals.org)
- Studies in breast cancer cells show that PPARγ agonists inhibit growth of ER-positive and -negative cell lines. (aacrjournals.org)
- Agonists of peroxisome proliferator-activated receptor (PPAR)-γ have been shown to reduce tumor necrosis factor-α (TNF-α)-induced insulin resistance. (aspetjournals.org)
- This study was intended to determine whether pioglitazone, a PPAR-γ agonist, could prevent alcohol-induced liver injury. (aspetjournals.org)
- Fibrates are a unique hypolipidemic drugs that lower plasma triglyceride and cholesterol levels through their action as peroxisome proliferator-activated receptor alpha (PPARα) agonists. (pubmedcentralcanada.ca)
- To understand the molecular mechanisms responsible for the pleiotropic effects of PPARα agonists, we treated mouse primary hepatocytes with three PPARα agonists (bezafibrate, fenofibrate, and WY-14,643) at multiple concentrations (0, 10, 30, and 100 μM) for 24 hours. (pubmedcentralcanada.ca)
- Global gene expression profiles in response to PPARα agonists were obtained by microarray analysis. (pubmedcentralcanada.ca)
- Our results suggest that treatment of PPARα agonists results in the production of oxidative stress and increased peroxisome proliferation, thus providing a better understanding of mechanisms underlying PPARα agonist-induced hepatic disorders and hepatocarcinomas. (pubmedcentralcanada.ca)
- They function as agonists for peroxisome proliferator-activated receptor alpha (PPARα). (pubmedcentralcanada.ca)
- PPARα is a transcriptional nuclear receptor and forms a heterodimer with another nuclear receptor, retinoid X receptor (RXR). (pubmedcentralcanada.ca)
- To discuss the relationship between Bax expression level and lung cancer cell apoptosis induced by peroxisome proliferator-activated receptor-γ (PPAR-γ) agonists. (springer.com)
- RT-PCR and Western blot analysis were used to detect PPAR-γ expression in the lung cancer cells, and TUNEL was used to detect apoptosis induced by PPAR-γ agonists, while in situ hybridization and immunohistochemistry were used to monitor the changes of Bax mRNA and protein expression levels after apoptosis induced. (springer.com)
- PPAR-γ expression was detectable in two kinds of lung cancer cells (including Non-small cell lung cancer and small cell lung cancer), and PPAR-γ agonists could inhibit lung cancer growth through inducing apoptosis. (springer.com)
- PPAR-γ is predicted to be a new target in treating lung cancer in the future, and Bax is most likely to work in treating lung cancer apoptosis induced by PPAR-γ agonists as a factor to induced apoptosis. (springer.com)
- Peroxisome proliferator activated receptor-gamma (PPAR-gamma) mediates the action of gamma linolenic acid in breast cancer cells. (springer.com)
- Expression of peroxisome proliferator-activated receptor (PPAR)-gamma in human lung cancer. (springer.com)
- Given that aleglitazar is a PPAR-α agonist as well, significant changes in lipid parameters were also noted. (acc.org)
- Peroxisome proliferator-activated receptor (PPAR)-γ is required for adipogenesis but is also found in the cardiovascular system, where it has been proposed to oppose inflammatory pathways and act as a growth suppressor. (ahajournals.org)
- PPAR-γ agonists, thiazolidinediones (TZDs), inhibit cardiomyocyte growth in vitro and in pressure overload models. (ahajournals.org)
- Rosiglitazone increased cardiac phosphorylation of p38 mitogen-activated protein kinase independent of PPAR-γ, whereas rosiglitazone induced phosphorylation of extracellular signal-related kinase 1/2 in the heart dependent of PPAR-γ. (ahajournals.org)
- 9 The role of PPAR-γ in suppression of growth and inflammation in the cardiovascular system has been inferred by determining the effects of its agonists, thiazolidinediones (TZDs), 10-13 although PPAR-γ does not always mediate the effects of TZDs. (ahajournals.org)
- 19 PPAR-γ agonists inhibit mechanical stress-induced hypertrophy of cultured neonatal rat ventricular cardiomyocytes, reflecting, at least in part, inhibition of nuclear factor κB (NF-κB). (ahajournals.org)
- 11 Similarly, PPAR-γ agonists inhibit cardiac hypertrophy induced by aortic constriction in rats and mice. (ahajournals.org)
- In conclusion, differences in the pharmacokinetics of two novel PPAR agonists, both cleared, predominantly, by conjugation, were evident in genetically obese Zucker rats compared with Sprague-Dawley rats. (aspetjournals.org)
- MRL-I, (2 R )-7-[3-[2-chloro-4-(4-fluorophenoxy)phenoxy]propoxy]-2-ethyl-3,4-dihydro-2 H -benzopyran-2-carboxylic acid ( Fig. 1 ), is a PPAR α/γ dual agonist that is structurally distinct from marketed PPAR agonists. (aspetjournals.org)
- MRL-II, (2 R )-7-[3-[2-chloro-4-(2,2,2-trifluoroethoxy)phenoxy]propoxy]-3,4-dihydro-2-methyl-2 H -benzopyran-2-carboxylic acid ( Fig. 1 ), is chemically similar to MRL-I but has PPAR α-selective agonist properties. (aspetjournals.org)
- Structures of PPAR agonists evaluated in this study. (aspetjournals.org)
- INTRODUCTION Novel peroxisome proliferator-activated receptor (PPAR) modulators (selective PPAR modulators [SPPARMs]) and dual PPAR agonists may have an important role in the treatment of cardiometabolic disorders owing to lipid-modifying, insulin-sensitizing and anti-inflammatory effects. (semanticscholar.org)
- PPAR Agonists and Metabolic Syndrome: An Established Role? (semanticscholar.org)
- The present study aims to explore any possible beneficial effect of a peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist in alleviating the tubulointerstitial inflammation in IgAN.Methods. (hku.hk)
- Human proximal tubular epithelial cells (PTEC) were pre-treated with increasing concentration of a PPAR-γ agonist rosiglitazone or troglitazone (0-5 μM) followed by further incubation with the conditioned medium (IgA-HMC) collected from human mesangial cells (HMC) incubated with polymeric IgA isolated from IgAN patients. (hku.hk)
- The upregulated gene expression and protein synthesis of IL-6 and ATR1 in PTEC induced by the IgA-HMC conditioned medium were readily attenuated following pre-treatment with a PPAR-γ agonist, thiazolidinedione (TZD). (hku.hk)
- The ATR1-downregulating effect exerted by the PPAR-γ agonist occurred through the inhibition of ERK12 activation. (hku.hk)
- Our current findings suggest that the PPAR-γ agonist attenuates excessive inflammatory response in activated PTEC in IgAN through suppressing ATR1 expression. (hku.hk)
- In rodents, treatment with peroxisome proliferator-activated receptor alpha (PPARα) agonists results in peroxisome proliferation, hepatocellular hypertrophy, and hepatomegaly. (ovid.com)
- Drugs in the fibrate class of PPARα agonists have also been reported to produce rare skeletal muscle toxicity. (ovid.com)
- Although target-driven hepatic effects of PPARα treatment have been extensively studied, a characterization of the transcriptional effects of this nuclear receptor/transcription factor on skeletal muscle responses has not been reported. (ovid.com)
- In this study we investigated the effects of PPARα agonists on skeletal muscle gene transcription in rats. (ovid.com)
- By comparing the transcriptional responses of agonists that signal through different nuclear receptors and using a selection/deselection analytical strategy based on ANOVA, we identified a PPARα activation signature that is evident in type I (soleus), but not type II (quadriceps femoris), skeletal muscle fibers. (ovid.com)
- Peroxisome Proliferator-Activated Receptor (PPAR) Agonist - Pipeline Insight, 2018" report by DelveInsight offers comprehensive insights of the pipeline (under development) therapeutics scenario and growth prospects across "Peroxisome Proliferator-Activated Receptor (PPAR) Agonist development. (nxtgenreports.com)
- Descriptive coverage of pipeline development activities for "Peroxisome Proliferator-Activated Receptor (PPAR) Agonist - Pipeline therapeutics development coverage provides descriptive product profiles including (but not limited to) drug description, product development and R&D activities encompassing clinical and pre-clinical studies, designations, collaborations, licensing deals, grants, technologies and patent details. (nxtgenreports.com)
- The report assesses the active Peroxisome Proliferator-Activated Receptor (PPAR) Agonist pipeline products by developmental stage, product type, molecule type, and administration route. (nxtgenreports.com)
- Although sEHi as a therapeutic approach is promising, it could be more effective for the treatment of cardiometabolic syndrome when combined with peroxisome proliferator activated receptor γ (PPARγ) agonists. (elsevier.com)
- We hypothesized that the PPARγ agonist, rosiglitazone in combination with a sEHi (tAUCB) will provide synergistic actions to decrease blood pressure, improve vascular function, decrease inflammation, and prevent renal damage in spontaneously hypertensive obese rats (SHROB). (elsevier.com)
- These results indicate that even though sEHi or PPARγ agonist have benefits when used individually, the combination is more beneficial for the multidisease features in cardiometabolic syndrome. (elsevier.com)
- PPAR alpha and gamma agonists are approved as hypolipidemic and antidiabetic agents, respectively. (eurekaselect.com)
- Combination of PPAR alpha and gamma agonistic effects in a single molecule (i.e. dual PPAR agonists) has been tried to achieve a better multiple cardiovascular risk management. (eurekaselect.com)
- Despite their efficacy, dual PPAR agonists has been discontinued due to safety concerns. (eurekaselect.com)
- Here, we review pursuits for a new PPAR class, and discuss the potential role for selective peroxisome proliferator activated receptor modulators (SPPARMs) as new patented molecules. (eurekaselect.com)
- Background Peroxisome proliferator-activated receptors (PPARα, PPARγ, and PPARδ) are physiological sensors for glucose and lipid homeostasis. (uit.no)
- such as fibrates as PPARα agonists which lower lipid level, and glitazones as PPARγ agonists which lower glucose level. (uit.no)
- As diabetes and metabolic diseases are often associated with high blood glucose and lipid levels, drugs that activate both PPARα/γ would be a logical approach. (uit.no)
- But synthetically developed PPARα/γ dual agonists and glitazones are showing side effects such as weight gain and edema. (uit.no)
- These fatty acids act as PPAR agonists that transcript the genes involved in glucose and lipid homeostasis. (uit.no)
- Present hypothesis suggests that the derivatives of these fatty acids are stronger PPAR agonists than the parent compounds. (uit.no)
- Implications of the hypothesis: Present hypothesis is framed on the basis of molecular structure of natural PPAR agonists. (uit.no)
- Therefore, this hypothesis bridges the concept of natural PPAR agonists and the use of structural information in designing new drugs against diabetes and metabolic syndrome. (uit.no)
- Previous studies established that 15d-delta 12,14-prostaglandin J2 (15d-PGJ2) selectively inhibits Prm3 activity and TP beta expression through a peroxisome proliferator-activated receptor (PPAR)gamma mechanism without affecting Prm1 activity or TPalpha expression in human megakaryocytic erythroleukemia (HEL) 92.1.7 cells. (ucd.ie)
- OBJECTIVE: Our objective was to test whether PPAR agonists alter cortisol secretion and peripheral regeneration by 11beta-HSD1 in humans and whether reduced cortisol action contributes to metabolic effects of PPARgamma agonists. (ox.ac.uk)
- The renoprotective potential of the peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist pioglitazone was explored in an immune model of progressive nephropathy, passive Heymann nephritis (PHN), compared with that of an angiotensin II receptor antagonist, taken as standard therapy for renoprotection. (elsevier.com)
- Electrophoretic mobility shift assay experiments showed a direct interaction of PPAR/retinoid X receptor heterodimers to PPRE present in the enhancer region of the nephrin promoter. (elsevier.com)
- Enhancement of nephrin gene transcription through specific PPRE in its promoter discloses a novel mechanism of renoprotection for PPAR-γ agonists. (elsevier.com)
- It has been proposed that the antihypelipidemic and antihypercholesteremic effect of fibrates is a result of activating the peroxisome proliferator-activated receptor alpha (PPARα), leading to the enhancement of lipid catabolism. (imedpub.com)
- Binding iron may also be responsible for anemia reported in patients receiving members of this class of PPARα agonists. (imedpub.com)
- It has been reported that a beneficial cardiovascular effect in response to the PPARα agonists, fibrates may result from their ability to reduce serum triglycerides and cholesterol [ 3 ]. (imedpub.com)
- It is indeed intriguing that patients treated with clofibrate suffer from diminished hemoglobin levels, suggesting that this class of PPARα agonists interferes with iron homeostasis [ 7 ]. (imedpub.com)
- Treatment of mice with PPAR agonist The selective PPAR agonist GW0742 4-[2-(3-fluoro-4-trifluoromethylphenyl)-4-methylthiazol-5-ylmethylsulfanyl]- 2-methylphenoxy)-acetic acidity was synthesized at GlaxoSmithKline as explained previously buy Imiquimod (Aldara) (Sznaidman et al. (researchhunt.com)
- This dosage is comparable to that previously make use of by our group while others for research of additional PPAR agonists in EAE versions (Feinstein et al. (researchhunt.com)
- agonists from the ZINC library, and 10,000 of these were selected for docking with PPAR? (edu.au)
- PPARγ is the functioning receptor for the thiazolidinedione (TZD) class of antidiabetes drugs including rosiglitazone and pioglitazone 1 . (nature.com)
- These drugs are full classical agonists for this nuclear receptor, but recent data have shown that many PPARγ-based drugs have a separate biochemical activity, blocking the obesity-linked phosphorylation of PPARγ by Cdk5 (ref. 2 ). (nature.com)
- An antidiabetic thiazolidinedione is a high affinity ligand for peroxisome proliferator-activated receptor γ (PPARγ). (nature.com)
- N -(2-Benzoylphenyl)- l -tyrosine PPARγ agonists. (nature.com)
- Chawla, A., Schwarz, E. J., Dimaculangan, D. D. & Lazar, M. A. Peroxisome proliferator-activated receptor (PPAR) gamma: adipose-predominant expression and induction early in adipocyte differentiation. (nature.com)
- The alternation of serum HBV antigens in mouse models after PPAR agonists treatment. (biomedcentral.com)
- Peroxisome proliferator activated recptor (PPAR)α is the target for fibrates , used for treatment of hyperlipidemia. (ntnu.no)
- In paper II and III we demonstrate that PPARα and PPARγ agonists have opposite skeletal impacts in both normal and ovariectomized rats. (ntnu.no)
- In vitro studies in human and murine bone cells confirm that PPARα and PPARγ agonists exhibit opposite skeletal effects. (ntnu.no)
- The purpose of this review is to highlight the role that the nuclear receptor PPARδ plays in skeletal muscle. (aspetjournals.org)
- The role and underlying mechanisms of rosiglitazone, a peroxisome proliferator-activated receptor-gamma (PPAR-γ) agonist, on myocardial infarction are poorly understood. (elsevier.com)
- We investigated the effects of this PPAR-γ agonist on the expression of tissue factor (TF), a primary molecule for thrombosis, and elucidated its underlying mechanisms. (elsevier.com)
- The PPAR-γ agonist inhibited TF expression in response to TNF-α in human umbilical vein endothelial cells, human monocytic leukemia cell line, and human umbilical arterial smooth muscle cells. (elsevier.com)
- The overexpression of TF was mediated by increased phosphorylation of mitogen-activated protein kinase (MAPK), which was blocked by the PPAR-γ agonist. (elsevier.com)
- Luciferase and ChIP assays showed that transcription factor, activator protein-1 (AP-1), was a pivotal target of the PPAR-γ agonist to lower TF transcription. (elsevier.com)
- Intriguingly, two main drugs for drug-eluting stent, paclitaxel or rapamycin, significantly exaggerated thrombin-induced TF expression, which was also effectively blocked by the PPAR-γ agonist in all cell types. (elsevier.com)
- This PPAR-γ agonist did not impair TF pathway inhibitor (TFPI) in three cell types. (elsevier.com)
- Also, this PPAR-γ agonist reversed the paclitaxel-induced aggravation of TF expression, which suggests a possibility that the benefits might outweigh its risks in a group of patients with paclitaxel-eluting stent implanted. (elsevier.com)
- abstract = "Treatment of MCF-7 cells with the peroxisome proliferator-activated receptor (PPAR) γ agonists ciglitazone or 15-deoxy-Δ12,14-prostaglandin J2 resulted in a concentration- and time-dependent decrease of cyclin D1 and estrogen receptor (ER) α proteins, and this was accompanied by decreased cell proliferation and G1-G0S→phase progression. (houstonmethodist.org)
- In the present work , N-acetylcysteine (NAC), ascorbic acid (AA), some nonsteroidal anti-inflammatory drugs ( NSAIDs ) and peroxisome proliferator-activated receptor gamma ( PPAR γ) agonists were tested for their ability to interfere with rotavirus ECwt infectivity as detected by the percentage of viral antigen -positive cells of small intestinal villi isolated from ECwt-infected ICR mice . (bvsalud.org)
- A series of novel indole-based PPAR agonists is described leading to discovery of 10k, a highly potent PPAR pan-agonist. (elsevier.com)
- Optically active (S)-2-ethylphenylpropanoic acid derivatives, dual agonists for human peroxisome proliferator-activated receptor (PPAR) α and δ, were efficiently prepared by using Evan's chiral oxazolidinone technique and reductive amide N-alkylation as key steps. (elsevier.com)
- To investigate the effects of peroxisome proliferator-activated receptor ( PPAR ) α/γ agonist on atherosclerotic plaque stabilization in diabetic LDL receptor knockout (LDLr-/-) mice . (bvsalud.org)
- Saroglitazar, a novel dual peroxisome proliferator activated receptor (PPAR) agonist, in clinical trials, has shown an improvement in lipid and glycemic parameters through the PPAR-α and γ agonist actions, respectively. (biomedcentral.com)
- In recent years, dual peroxisome proliferator activated receptor (PPAR) α/γ agonists have attracted global attention as promising new treatment options for diabetic dyslipidemia due to a unique mechanism of action in improving lipid and glucose profile simultaneously [ 9 , 10 ]. (biomedcentral.com)
- Many dual PPAR α/γ agonists were developed but failed during preclinical stage or the clinical development stage due to lack of efficacy or safety issues [ 9 , 10 ]. (biomedcentral.com)
- Saroglitazar, developed by Zydus Cadila, is a novel dual PPAR α/γ agonist (predominant PPAR-α and moderate PPAR-γ actions), aiming to improve lipid and glucose profiles without significant weight gain and edema (common in PPAR-γ agonists such as thiazolidinediones) [ 9 ]. (biomedcentral.com)
- Ciglitazone, a PPAR-γ agonist with anti-inflammatory properties, was evaluated for its ability to influence the course of brain abscess development when treatment was initiated 3 days following infection. (nebraska.edu)
- The aim of the present study was to evaluate the influence of PPAR-β/δ receptor in a model of edematous pancreatitis induced in mice by administration of cerulein at supramaximal doses, as well as in necrohemorrhagic model induced by intraductal administration of sodium taurocholate (STC). (unict.it)
- In addition, the pancreatic water content was reduced in mice treated with PPAR-β/δ agonist. (unict.it)
- Numerous studies suggest the potential therapeutic effects of peroxisome proliferator-activated receptor-gamma ( PPAR -Î³) in different brain disorders . (bvsalud.org)
- This research evaluates the utility of selective agonist of PPAR -Î³, pioglitazone in postnatal propionic acid induced ASD related symptomatology in male Wistar rats . (bvsalud.org)
- Surprisingly, GW0742 behaved as a PPAR agonist and antagonist, activating transcription at lower concentrations and inhibiting this effect at higher concentrations. (houstonmethodist.org)
- Despite previous reports of potential adverse cardiovascular effects of peroxisome proliferator-activated receptor (PPAR) agonists, the promise for PPAR agonists to positively affect risk of cardiovascular disease in patients with type 2 diabetes is of continued interest. (naver.com)
- The SYNCHRONY study aimed to establish the glucose-lowering and lipid-modifying effects, and safety profile, of the dual PPAR-α and PPAR-γ agonist aleglitazar. (naver.com)
- It has been demonstrated that peroxisome-proliferator activated receptor-alpha (PPARα) has a potent neuroprotective role in various pathological events of the nervous tissue. (aimsci.com)
- Since oxidative damage is associated with development of seizure, we aimed to examine whether the PPARα agonist, fenofibrate, exerts protective effects against the repeated seizures in pentylenetetrazol (PTZ) kindling model in mice through improving the brain antioxidant capacity. (aimsci.com)
- In view of the critical protective role of antioxidants in seizures, the findings of the present study suggested that the PPARα agonist, fenofibrate, might modulate the seizure behaviors in the PTZ kindling model in mice through improving the brain antioxidant capacity. (aimsci.com)
- The identification of peroxisome proliferator-activated receptor gamma (PPARγ) as a nuclear receptor, which has pleiotropic function in inflammation, cell growth and differentiation, apoptosis, and carbohydrate and fat metabolism, has offered new opportunities to understand and manipulate several key mechanisms of atherogenesis (Spiegelman et al. (springer.com)
- Peroxisome proliferator-activated receptor (PPAR) gamma: adipose-predominant expression and induction early in adipocyte differentiation. (springer.com)
- The nuclear receptor PPARγ and immunoregulation: PPARγ mediates inhibition of helper T cell responses. (springer.com)
- Recently, a subgroup of AT 1 receptor blockers has been identified as ligands for the peroxisome proliferator-activated receptor γ (PPAR-γ). (ahajournals.org)
- Here we characterize the PPAR-γ-activating properties of the 2 active losartan metabolites. (ahajournals.org)
- Maximum PPAR-γ-LBD activation by EXP3179 reached 51% of the maximum response induced by the full PPAR-γ agonist pioglitazone, identifying EXP3179 as a partial PPAR-γ agonist. (ahajournals.org)
- The present study characterizes the active losartan metabolite EXP3179 as a partial PPAR-γ agonist. (ahajournals.org)
- We and others recently demonstrated that a subset of ARBs, including losartan, induces the activity of a nuclear hormone receptor named peroxisome proliferator-activated receptor γ (PPAR-γ) by partial agonism. (ahajournals.org)
- 2,3 The direct activation of the ligand-binding domain of PPAR-γ by ARBs is independent of their angiotensin type 1 receptor (AT 1 R) blocking actions. (ahajournals.org)
- 4 Activated by synthetic full agonists like thiazolidinediones/glitazones, PPAR-γ markedly improves whole-body insulin sensitivity resulting in decreased levels of fasting plasma glucose, fasting plasma insulin, and plasma triglycerides. (ahajournals.org)
- We hypothesized that the PPAR-γ-activating properties of losartan in vivo might be enhanced by its active metabolites and that PPAR-γ activation by losartan metabolites may provide a potential mechanism of the antidiabetic actions of losartan observed in clinical trials. (ahajournals.org)
- Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear receptor family of ligand-activated transcription factors. (pnas.org)
- Activation of PPARs leads to the formation of heterodimers with retinoid-X receptors (RXRs). (diabetesjournals.org)
- Peroxisome proliferator-activated receptors (PPARs) are transcription factors belonging to the nuclear receptor superfamily. (ahajournals.org)
- Peroxisome proliferator-activated receptors (PPARs) are a family of nuclear receptors known for their roles in metabolism. (frontiersin.org)
- Here, for the first time, we present a review of the literature linking chemokines in neuropathic pain to activation of peroxisome proliferator-activated receptors (PPARs). (frontiersin.org)
- Among the genes repressed by activated PPARs are those of chemokines and their receptors. (frontiersin.org)
- Peroxisome proliferator-activated receptors (PPARs) are members of the nuclear hormone receptor superfamily of ligand-activated transcriptional factors that include receptors for steroids, thyroid hormone, vitamin D, and retinoic acid ( 4 ). (jimmunol.org)
- Activation of PPARs is a multistep process that involves ligand binding and heterodimerization with the retinoic X receptor, interaction with sequence-specific gene promoter elements, and recruitment of coactivators and other nuclear coregulatory proteins. (aacrjournals.org)
- Peroxisome proliferator activated receptors (PPARs) are claimed to play critical roles in metabolic adaptation to changing environmental factors. (eurekaselect.com)
- Small structural changes in the molecular structure of fatty acids have a great influence on activating different PPARs. (uit.no)
- Peroxisome proliferator-activated receptors (PPARs) are members of the steroid receptor superfamily [ 1 , 2 ]. (imedpub.com)
- PPARs are activated by a vast number of compounds including synthetic drugs such as the clofibrate and anti-diabetic thiazoldinediones, polyunsaturated fatty acids, and a number of eicosanoids, including prostaglandins, lipoxygenase products and oxidized low density lipoprotein [ 2 ]. (imedpub.com)
- In EAE (experimental autoimmune encephalomyelitis), agonists of PPARs (peroxisome proliferator-activated receptors) provide scientific benefit and reduce harm. (researchhunt.com)
- Agonists directed against the α and γ isoforms of the peroxisome proliferator-activated receptors (PPARs) have become important for the respective treatment of hypertriglyceridemia and insulin resistance associated with metabolic disease. (aspetjournals.org)
- Recent data indicate that GRK2 and β-arrestins also play an important role in the stimulation of the extracellular signal-regulated kinases (ERK)/mitogen-activated protein kinase (MAPK) cascade by GPCRs. (aspetjournals.org)
- The mitogen-activated protein kinase extracellular signal-related kinase 12 (ERK12) activation was examined by western blot.Results. (hku.hk)
- Topical photodynamic therapy induces systemic immunosuppression via generation of platelet-activating factor receptor ligands," Journal of Investigative Dermatology , vol. 135, no. 1, pp. 321-323, 2014. (hindawi.com)
- We have compared the ability of a number of μ-opioid receptor (MOPr) ligands to activate G proteins with their abilities to induce MOPr phosphorylation, to promote association of arrestin-3 and to cause MOPr internalization. (aspetjournals.org)
- however, non-coplanar PCBs are not ligands for AhR, but may be ligands for members of the nuclear receptor family of proteins. (surrey.ac.uk)
- Inhibitory activity of clinical thiazolidinedione peroxisome proliferator activating receptor-gamma ligands toward internal mammary artery, radial artery, and saphenous vein smooth muscle cell proliferation. (springer.com)
- While numerous receptors are found in most cells, each receptor will only bind with ligands of a particular structure, much like how locks will only accept specifically shaped keys. (wikipedia.org)
- Nuclear receptors - While they are called nuclear receptors, they are actually located in the cytoplasm and migrate to the nucleus after binding with their ligands. (wikipedia.org)
- FPR2 is activated by an array of ligands, which include structurally unrelated lipids and peptide/proteins agonists, resulting in different intracellular responses in a ligand-specific fashion. (mdpi.com)
- Most of the FPR2 agonists are peptides, with the exception of the eicosanoid, lipoxin A4 (LXA4), and of the synthetic small-molecular weight ligands isolated by compound library screens. (mdpi.com)
- So far, PAR2 has been co-crystallized with two different antagonist ligands, while an agonist-bound state model of PAR2 (with the endogenous ligand SLIGKV) has been determined through mutagenesis and structure-based drug design. (wikipedia.org)
- We now report that this reaction can be used to neuroanatomically localize receptor-activated G proteins in brain sections by in vitro autoradiography of GTP[gamma-35S] binding. (pnas.org)
- This technique provides a method of functional neuroanatomy that identifies changes in the activation of G proteins by specific receptors. (pnas.org)
- These data indicate that for the majority of MOPr agonists the ability to induce receptor phosphorylation, arrestin-3 recruitment, and internalization can be predicted from their ability as agonists to activate G proteins. (aspetjournals.org)
- This event promotes the binding of regulatory proteins termed β-arrestins to GPCRs, leading to uncoupling from G proteins and receptor internalization. (aspetjournals.org)
- We investigated the distribution of GABA B receptors on spider leg mechanosensilla using specific antibodies against 2 proteins needed to form functional receptors and an antibody that labels the synaptic vesicles on presynaptic sites. (physiology.org)
- Using Western blot analysis we tested specific antibodies against the two essential GABA B receptor subtypes in spider brain and peripheral nerve tissues and we located both receptor proteins on the mechanosensilla using immunocytochemistry. (physiology.org)
- Receptor proteins can be classified by their location. (wikipedia.org)
-  The aforementioned receptors are coupled to different intracellular effector systems via G proteins . (wikipedia.org)
- Insulin also plays an important role in the metabolism of fat and proteins and exerts its influence at the peroxisome proliferator-activated receptor level. (clinicaltrials.gov)
- Formyl-peptide receptors 1, 2 and 3 (FPR1, FPR2 and FPR3) form a subgroup of receptors linked to inhibitory G-proteins (G i ). (mdpi.com)
- The interaction of interleukin-1 (IL-1) with its receptor (IL-1R) or pathogen-associated molecular patterns with Toll-like receptors (TLRs) induces the recruitment of the adaptor protein MyD88 to the receptors, which is followed by the recruitment of interleukin receptor-associated kinase 4 (IRAK4) to MyD88 via interactions between the N-terminal death domains of these proteins. (portlandpress.com)
- PAR2 is a member of the large family of 7-transmembrane receptors that couple to guanosine-nucleotide-binding proteins. (wikipedia.org)
- Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y2 Receptor. (nih.gov)
- Molecular Recognition of Agonists and Antagonists by the Nucleotide-Activated G Protein-Coupled P2Y 2 Receptor. (nih.gov)
- For opioid and cannabinoid receptors, agonist stimulation of GTP[gamma-35S] binding was blocked by incubation with agonists in the presence of the appropriate antagonists (naloxone for mu opioid and SR-141716A for cannabinoid), thus demonstrating that the effect was specifically receptor mediated. (pnas.org)
- Structure-activity relationships were used to derive new PAR2 agonists and antagonists containing nonpeptidic moieties. (monash.edu)
- Fairlie, David P. / Novel agonists and antagonists for human protease activated receptor 2 . (monash.edu)
- Thus, tryptase inhibitors and antagonists of proteinase-activated receptor 2 may be useful anti-inflammatory agents. (nyu.edu)
- Antagonists bind to receptors and do not activate either receptor state. (news-medical.net)
- Potent and selective small molecule agonists and antagonists for PAR2 have been discovered. (wikipedia.org)
- In conclusion, pioglitazone exerts an antiproteinuric effect in immune-mediated glomerulonephritis as angiotensin II receptor antagonist does. (elsevier.com)
- The peroxisome proliferator-activated receptor-γ agonists, the thiazolidinediones, pioglitazone and rosiglitazone, are insulin sensitizing agents, that are licensed for the management of hyperglycaemia. (cardiffmet.ac.uk)
- Our research objective was to understand how PPARgamma agonists induce HS in mice, using the prototypical sarcomagenic troglitazone (TG) and non-sarcomagenic pioglitazone (P1O). (zhangqiaokeyan.com)
- TAK-559 has partial peroxisome proliferator-activated receptor-alpha agonist activity, potent peroxisome proliferator-activated receptor-alpha activity, and modest peroxisome proliferator-activated receptor-gamma activity at high concentrations in nonclinical models. (clinicaltrials.gov)
- Treatment with a TZD, rosiglitazone, induced cardiac hypertrophy in both littermate control mice and CM-PGKO mice and activated distinctly different hypertrophic pathways from CM-PGKO. (ahajournals.org)
- The Macrophage-Mediated Effects of the Peroxisome Proliferator-Activated Receptor-Gamma Agonist Rosiglitazone Attenuate Tactile Allodynia in the Early Phase of Neuropathic Pain Development. (painresearchforum.org)
- INTERVENTIONS, OUTCOME MEASURES, AND RESULTS: In nine healthy men, 7 d of PPARalpha agonist (fenofibrate) or PPARgamma agonist (rosiglitazone) had no effect on cortisol secretion, hepatic cortisol generation after oral cortisone administration, or tracer kinetics during 9,11,12,12-[(2)H](4)-cortisol infusion, although rosiglitazone marginally reduced cortisol generation in sc adipose tissue measured by in vivo microdialysis. (ox.ac.uk)
- Ultraviolet B radiation generated platelet-activating factor receptor agonist formation involves EGF-R-mediated reactive oxygen species," The Journal of Immunology , vol. 182, no. 5, pp. 2842-2848, 2009. (hindawi.com)
- Fenofibrate also significantly reduced the serum insulin and insulin-like growth factor (IGF)-1 levels, and decreased the immunohistochemical expression of IGF-1 receptor (IGF-1R), phosphorylated Akt, and phosphorylated Erk1/2 in lung adenocarcinomas. (mdpi.com)
- Our data demonstrate conclusively that TRPM8 is gated by cold and its chemical agonists directly, and that dependence of its gating on PI(4,5)P 2 is a result of direct specific interactions with the lipid. (jneurosci.org)
- To examine whether the TRPM8 agonists exert their effects on the channel directly, we have characterized the regulation of TRPM8 gating in a reconstituted system using planar lipid bilayers. (jneurosci.org)
- Despite the large number of ion channels being activated by this lipid ( Suh and Hille, 2008 ), a definitive proof for direct activation by PI(4,5)P 2 is lacking. (jneurosci.org)
- These receptors regulate multiple genes involved in energy production, glucose and lipid metabolism and influence the pathology of numerous diseases including obesity, diabetes, atherosclerosis, inflammation and cancer [ 2 ]. (imedpub.com)
- If inflammatory conditions prevail and risk factors such as dyslipidemia persist, the lipid pool can grow, and proteinases secreted by the activated leukocytes can degrade the extracellular matrix and cause cell death while proinflammatory cytokines that stimulate Th1 activity can limit the synthesis of new collagen. (asnjournals.org)
- This nuclear receptor is proposed to mediate the activity of lipid-lowering drugs such as the fibrates. (lacienciadelvino.com)
- For this reason, peroxisome proliferator-activated receptors play a pivotal role in glucose homeostasis, adipocyte differentiation, and lipid storage. (clinicaltrials.gov)
- As such, peroxisome proliferator-activated receptor-alpha agonists have their greatest effect on lipid metabolism and vascular biology. (clinicaltrials.gov)
- In addition to the anti-inflammatory lipid, lipoxin A4, several other endogenous agonists also bind FPR2, including serum amyloid A, glucocorticoid-induced annexin 1, urokinase and its receptor, suggesting that the activation of FPR2 may result in potent pro- or anti-inflammatory responses. (mdpi.com)
Human peroxisome proli2
- Molecular genetic analysis of the von Hippel-Lindau and human peroxisome proliferator-activated receptor gamma tumor-suppressor genes in adenocarcinomas of the gastroesophageal junction. (springer.com)
- Beamera BA, Negria C, Yen CJ, Gavrilova O. Chromosomal localization and partial genomic structure of the human peroxisome proliferator activated receptor-gamma (hPPARγ) gene. (springer.com)
- Because a better understanding of the mechanism of the upregulation will help in understanding its potential importance in inflammation, we have studied the molecular mechanism of B1-receptor upregulation in cultured human lung fibroblasts (IMR 90) in response to IL-1beta and the B1-agonist [des-Arg10]-kallidin. (nih.gov)
- The multi-ligand receptor Receptor for Advanced Glycated End Products, RAGE has been implicated in the pathogenesis of several chronic diseases such as inflammation, atherosclerosis and Diabetes. (cardiffmet.ac.uk)
- Trypsin and mast cell tryptase cleave proteinase-activated receptor 2 and, by unknown mechanisms, induce widespread inflammation. (nyu.edu)
- Chronic inflammation associated with activated macrophages may lead to the development of neoplasia, such as those found surrounding tuberculosis scars. (wikipedia.org)
- Selcuk Dagdelen, " From Dual Peroxisome Proliferator Activated Receptor Agonists to Selective Peroxisome Proliferator Activated Receptor Modulators", Recent Patents on Endocrine, Metabolic & Immune Drug Discovery (2008) 2: 24. (eurekaselect.com)
- Distinct properties and advantages of a novel peroxisome proliferator-activated protein γ selective modulator. (nature.com)
- A selective peroxisome proliferator-activated receptor-Î³ agonist benefited propionic acid induced autism-like behavioral phenotypes in rats by attenuation of neuroinflammation and oxidative stress. (bvsalud.org)
- The probability that the receptor-evoked shortlasting Ca2+ spikes would initiate more substantial Ca2+ waves was dramatically increased by intracellular perfusion with solutions containing high concentrations of the mobile low affinity Ca2+ buffers citrate (10-40 mM) or ATP (10-20 mM). (epfl.ch)
- Agonist GB110 (19, EC 50 0.28 μM) selectively induced PAR2-, but not PAR1-, mediated intracellular Ca 2+ release in HT29 human colorectal carcinoma cells. (monash.edu)
- Intracellular recordings from sensory neurons innervating the slit sensilla of the spider legs revealed that application of GABA B receptor agonists attenuated voltage-activated Ca 2+ current and enhanced voltage-activated outward K + current, providing 2 possible mechanisms for controlling the neurons' excitability. (physiology.org)
- The mechanisms by which agonists stimulate mobilization and plasma membrane translocation of G protein-coupled receptors from intracellular stores are unexplored. (nyu.edu)
- Our results reveal a major role for PKD and Gβγ in agonist-evoked mobilization of intracellular PAR 2 stores that is required for sustained signaling by extracellular proteases. (nyu.edu)
-  Intracellular receptors are those found inside the cell, and include cytoplasmic receptors and nuclear receptors . (wikipedia.org)
- Type 3: Kinase-linked and related receptors (see " Receptor tyrosine kinase ", and " Enzyme-linked receptor ") - They are composed of an extracellular domain containing the ligand binding site and an intracellular domain, often with enzymatic-function, linked by a single transmembrane alpha helix. (wikipedia.org)
- Here, we review and discuss the most significant findings on the intracellular pathways and on the cross-communication between FPR2 and tyrosine kinase receptors triggered by different FPR2 agonists. (mdpi.com)
Retinoid X recept1
- They form heterodimers with retinoid X receptor (RXR) and bind to consensus DNA sites. (pnas.org)
- For the prototypic MOPr agonist morphine, its relatively weak ability to induce MOPr internalization can be explained by its low agonist efficacy. (aspetjournals.org)
- The agonist-induced phosphorylation of MOPr at Ser 375 , considered a key step in MOPr regulation, and agonist-induced internalization of MOPr were each found to correlate well with arrestin-3 recruitment. (aspetjournals.org)
- Interestingly, we have found that purified ERK1/MAPK can directly phosphorylate the C-terminal domain of GRK2, and that the phosphorylation process is favored by the presence of Gβγ-subunits or an activated receptor. (aspetjournals.org)
- Their activation by specific agonists leads to transient calcium fluxes, extracellular signal-regulated kinase (ERK) phosphorylation and chemotaxis. (mdpi.com)
- GLP-1 receptor agonists stimulated calcitonin release, up-regulation of calcitonin gene expression, and subsequently C-cell hyperplasia in rats and, to a lesser extent, in mice. (nih.gov)
- For example, low-density lipoprotein-receptor knockout mice lacking leptin (LDLR −/− ob/ob ) develop more atherosclerotic lesions than LDLR −/− control mice. (ahajournals.org)
- Specifically, we compared the vasodilator effectiveness of the PAR2 activating peptide 2-furoyl-LIGRLO-amide in aortas of wild-type PAR2 homozygous (PAR2-WT) and PAR2-HET mice. (mun.ca)
- Evaluation of the mode of action and human relevance of peroxisome proliferator activated receptor gamma agonist-induced hemangiosarcomas in mice. (zhangqiaokeyan.com)
- Peroxisome proliferator-activated receptor β/δ agonist GW0742 ameliorates cerulein- and taurocholate-induced acute pancreatitis in mice. (unict.it)
- PAR-4 agonist peptide stimulates thromboxane production by human platelets with the maximal response to this agonist being approximately half of that observed after maximal thrombin stimulation. (anaspec.com)
- Glucagon-like Peptide-1 receptor agonists activate rodent thyroid C-cells causing calcitonin release and C-cell proliferation. (nih.gov)
- Peptide agonists are widely used to characterize physiological roles for PAR2 but typically have low potency (e.g. (monash.edu)
- We found that a large proportion of primary spinal afferent neurons, which express proteinase-activated receptor 2, also contain the proinflammatory neuropeptides calcitonin gene-related peptide and substance P. Trypsin and tryptase directly signal to neurons to stimulate release of these neuropeptides, which mediate inflammatory edema induced by agonists of proteinase-activated receptor 2. (nyu.edu)
-  A molecule that binds to a receptor is called a ligand , and can be a protein or peptide (short protein), or another small molecule such as a neurotransmitter , hormone , pharmaceutical drug, toxin, or parts of the outside of a virus or microbe. (wikipedia.org)
- The formyl peptide receptor 2 (FPR2) is a remarkably versatile transmembrane protein belonging to the G-protein coupled receptor (GPCR) family. (mdpi.com)
- On the other hand, many FPR2 peptide agonists have been identified and purified from living organisms. (mdpi.com)
- These receptors can also be activated non-protealytically, by exogenous peptide sequences that mimic the final amino acids of the tethered ligand, or by other proteases at cleavage sites that are not related to signaling and that can make them then irresponsive to further protease exposure. (wikipedia.org)
- UVB radiation-mediated inhibition of contact hypersensitivity reactions is dependent on the platelet-activating factor system," Journal of Investigative Dermatology , vol. 128, no. 7, pp. 1780-1787, 2008. (hindawi.com)
- Although, it was originally assumed that TRPM8 channels are activated by cold and the chemical agonists directly, several independent articles challenged this view by showing that TRPM8 activation could be prevented by inhibition of the phospholipase A 2 (PLA 2 ) pathway (Abeele et al. (jneurosci.org)
- Coimmunoprecipitation of MAPK and GRK2 is blocked by inhibition of the MAPK cascade and is not observed upon activation of MAPK in the absence of β 2 -AR stimulation, thus indicating that both an active MAPK and agonist occupancy of GPCR are required for the association to occur. (aspetjournals.org)
- Inhibition of human lung cancer cell growth by the peroxisome proliferator-activated receptor-gamma agonists through induction of apoptosis. (springer.com)
- Most of these efferent fibers are immunoreactive to γ-aminobutyric acid (GABA), and the sensory neurons respond to agonists of ionotropic GABA receptors with a rapid and complete inhibition. (physiology.org)
- In addition to relatively fast inhibition by ionotropic receptors, GABA can modulate many signal transduction pathways by activating metabotropic G protein coupled GABA B receptors that play critical roles in long-term modulation of synaptic transmission ( Bowery 1993 ). (physiology.org)
- Blocking PAF-R agonist production either by systemic antioxidants or treatment with serum PAF-acetyl hydrolase enzyme blocked both the CS-mediated generation of PAF-R agonists and PAF-R-dependent inhibition of contact hypersensitivity (CHS) reactions, indicating a role for oxidized glycerophosphocholines with PAF-R agonistic activity in this process. (jimmunol.org)
- In addition, cyclooxygenase-2 inhibition did not block PAF-R agonist production but prevented CS-induced inhibition of CHS. (jimmunol.org)
- A Schild regression analysis of the inhibition by a PAR2 antagonist (GB-83) of PAR2 agonist-induced aortic ring relaxations was used to compare receptor expression in PAR2-WT to PAR2-HET. (mun.ca)
- Pressure-dependent constriction to a 100-mm Hg pressure step, constriction to nitric oxide synthase inhibition (100 μmol/L N ω -nitro- l -arginine methyl ester), and endothelium-dependent vasodilation to bradykinin (1.6 μmol/L), 2-f-LIGRLO-NH 2 (1 μmol/L, a protease-activated receptor-2 agonist), and A23187 (2 μmol/L) were evaluated in middle cerebral arteries at 100 mm Hg with a pressure myograph. (ahajournals.org)
- Antagonist GB83 (36, IC 50 2 μM) is the first compound at micromolar concentrations to reversibly inhibit PAR2 activation by both proteases and other PAR2 agonists (e.g., trypsin, 2f-furoyl-LIGRLO-NH 2 , 19). (monash.edu)
- A high-throughput screening campaign was conducted to identify small molecules with the ability to inhibit the interaction between the vitamin D receptor (VDR) and steroid receptor coactivator 2. (houstonmethodist.org)
- Analgesics such as non-steroidal anti-inflammatory drugs (NSAIDs) attach themselves to cyclooxygenase (COX) receptors - COX1 or COX2, and inhibit these enzymes. (news-medical.net)
- The data obtained with SB649146 also suggest that the constitutively active endogenous S1P1 receptor enhances PDGFinduced cell migration. (strath.ac.uk)
- Nevertheless, the VDR-meditated downstream process of cell differentiation was antagonized by GW0742 in HL-60 cells that were pretreated with the endogenous VDR agonist 1,25-dihydroxyvitamin D 3 . (houstonmethodist.org)
-  In this sense, a receptor is a protein-molecule that recognizes and responds to endogenous chemical signals, e.g. an acetylcholine receptor recognizes and responds to its endogenous ligand , acetylcholine . (wikipedia.org)
- The endogenously designated -molecule for a particular receptor is referred to as its endogenous ligand. (wikipedia.org)
- E.g. the endogenous ligand for the nicotinic acetylcholine receptor is acetylcholine but the receptor can also be activated by nicotine and blocked by curare . (wikipedia.org)
- PAR2 is activated by several different endogenous and exogenous proteases. (wikipedia.org)
- B1-agonist-induced upregulation was correlated to the induction of transcription factor nuclear factor kappaB (NF-kappaB) which efficiently bound to the NF-kappaB-like sequence located in the promoter region of the human B1-receptor gene. (nih.gov)
- This correlation was further confirmed by reporter gene assays which showed that this NF-kappaB-like sequence, in the B1-receptor promoter context, could contribute to IL-1beta and DLBK-induced B1-receptor transcription activation, and by the effect of NF-kappaB inhibitor pyrrolidinedithiocarbamate which diminished both B1-receptor upregulation and NF-kappaB activation. (nih.gov)
- Peroxisome proliferator-activated receptor receptors are ligand-activated transcription elements that regulate gene expression necessary for metabolism. (clinicaltrials.gov)
- The genes predominantly targeted by transcription activity of activated peroxisome proliferator-activated receptor-alpha receptors are those that mediate fatty acid uptake, fatty acid oxidation, and lipoprotein metabolism. (clinicaltrials.gov)
- Non-coplanar PCBs act as direct activators for the nuclear receptors PXR and CAR, and are able to elicit transcriptional activation of target genes in a substitution- and tissue-dependent manner. (surrey.ac.uk)
- The GW0742-inhibited NR-coactivator binding resulted in a reduced level of expression of five different NR target genes in LNCaP cells in the presence of agonist. (houstonmethodist.org)
- Four mammalian genes, termed HCN1 - HCN4 , encode hyperpolarization-activated, nonselective cation channels. (jneurosci.org)
- A variety of G protein-coupled receptors (GPCRs) are phosphorylated by G protein-coupled receptor kinase 2 (GRK2). (aspetjournals.org)
- Agonist-evoked endocytosis of G protein-coupled receptors has been extensively studied. (nyu.edu)
- G protein-coupled receptors (metabotropic) - This is the largest family of receptors and includes the receptors for several hormones and slow transmitters e.g. dopamine, metabotropic glutamate. (wikipedia.org)
- 1 Leptin has a variety of important central and peripheral actions to regulate energy balance and metabolism, fertility, and bone metabolism that are mediated by specific cell surface leptin receptors. (ahajournals.org)
- Intestine farnesoid X receptor agonist and the gut microbiota activate G-protein bile acid receptor-1 signaling to improve metabolism. (omeka.net)
- Bile acids activate farnesoid X receptor (FXR) and G protein-coupled bile acid receptor-1 (aka Takeda G protein-coupled receptor-5 [TGR5]) to regulate bile acid metabolism and glucose and insulin sensitivity. (omeka.net)
- In this study, we used the intestine-restricted FXR agonist fexaramine (FEX) to study the effect of activation of intestinal FXR on the gut microbiome, bile acid metabolism, and FXR and TGR5 signaling. (omeka.net)
- In pancreatic acinar cells activation of muscarinic receptors typically evokes sinusoidal oscillations whereas stimulation of cholecystokinin (CCK) receptors evokes transient oscillations consisting of Ca2+ waves with long intervals between them. (epfl.ch)
- An interesting secondary finding was that relaxations induced by agonists of PAR2 and muscarinic receptors were larger in females than in males. (mun.ca)
-  Muscarinic agonists activate muscarinic receptors while nicotinic agonists activate nicotine receptors. (wikipedia.org)
- A prostaglandin J2 metabolite binds peroxisome proliferator-activated receptor γ and promotes adipocyte differentiation. (nature.com)
- An agonist that binds to and activates platelet-activating factor receptors. (ebi.ac.uk)
- When a ligand binds to its corresponding receptor, it activates or inhibits the receptor's associated biochemical pathway. (wikipedia.org)
- An agonist that binds to and activates aryl hydrocarbon receptors (AhRs). (ebi.ac.uk)
- The efficacy and potency of drugs used in dentistry is determined by how well the drug binds with the receptors and triggers the desired response. (news-medical.net)
- Our results show that overall there is a very good correlation between efficacy for G protein activation and arrestin-3 recruitment, whereas a few agonists, in particular endomorphins 1 and 2, display apparent bias toward arrestin recruitment. (aspetjournals.org)
- An important element in the analysis of opioid tolerance is the ability to obtain accurate measurements of agonist efficacy. (aspetjournals.org)
- Perhaps a more useful measure of efficacy is relative intrinsic efficacy ( Furchgott and Bursztyn, 1967 ), which enables comparison of responses produced by equivalent fractional occupancy of the receptors by different agonists in the same tissue. (aspetjournals.org)
- Peroxisome proliferator-activated receptor agonists modulate neuropathic pain: a link to chemokines? (frontiersin.org)
- Peroxisome proliferator-activated receptor-gamma: from adipogenesis to carcinogenesis. (springer.com)
- Peroxisome proliferator-activated receptor gamma induces pancreatic cancer cell apoptosis. (springer.com)
- Activation of peroxisome proliferator-activated receptor-gamma stimulates the growth arrest and DNA-damage inducible 153 gene in non-small cell lung carcinoma cells. (springer.com)
- New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. (semanticscholar.org)
- Early atheroma-derived agonists of peroxisome proliferator-activated receptor-γ trigger intramedial angiogenesis in a smooth muscle cell-dependent manner. (semanticscholar.org)
- Munin: Are fish oil omega-3 long-chain fatty acids and their derivatives peroxisome proliferator-activated receptor agonists? (uit.no)
- Effects of peroxisome proliferator-activated receptor-alpha and -gamma agonists on 11beta-hydroxysteroid dehydrogenase type 1 in subcutaneous adipose tissue in men. (ox.ac.uk)
- CONTEXT: In animals, peroxisome proliferator-activated receptor-alpha (PPARalpha) and PPARgamma agonists down-regulate 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) mRNA and activity in liver and adipose tissue, respectively, and PPARgamma agonists reduce ACTH secretion from corticotrope cells. (ox.ac.uk)
- Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening. (duke.edu)
- Elafibranor is an agonist of the peroxisome proliferator-activated receptor-α and peroxisome proliferator-activated receptor-δ. (duke.edu)
- this effect was seen with other peroxisomal proliferator-activated receptor- agonists. (deiodinase.org)
- Purpose : Lobeglitazone, a peroxisome proliferator-activated receptor-γ agonist, was developed for the treatment of diabetes mellitus. (yonsei.ac.kr)
- Kasuga, JI, Hashimoto, Y & Miyachi, H 2006, ' Concise and efficient asymmetric synthesis of (S)-2-ethylphenylpropanoic acid derivatives: Dual agonists for human peroxisome proliferator-activated receptor α and δ ', Bioorganic and Medicinal Chemistry Letters , vol. 16, no. 4, pp. 771-774. (elsevier.com)
- Peroxisome proliferator activated receptor gamma (PPARgamma) agonists are non-genotoxic pharmaceuticals for the treatment of type II diabetes mellitus. (zhangqiaokeyan.com)
- Pterostilbene, a new agonist for the peroxisome proliferator-activated receptor alpha-isoform, lowers plasma lipoproteins and cholesterol in hypercholesterolemic hamsters. (lacienciadelvino.com)
- We investigated whether resveratrol and its three analogues (pterostilbene, piceatannol, and resveratrol trimethyl ether) would activate the peroxisome proliferator-activated receptor alpha (PPARalpha) isoform. (lacienciadelvino.com)
- Ashok Kumar M, Veera Subhashini NG, Kanthimathi S, SaiBabu R, Ramesh A, Cherian KM, Emmanuel C. Associations for lipoprotein lipase and peroxisome proliferator-activated receptor-gamma gene and coronary artery disease in an Indian population. (springer.com)
- Thus, as insulin activates peroxisome proliferator-activated receptor-alpha receptors, this results in the cellular uptake of glucose. (clinicaltrials.gov)
- Human protease activated receptor 2 (PAR2) is a G protein-coupled receptor that is associated with inflammatory diseases and cancers. (monash.edu)
- To investigate the therapeutic effects of protease-activated receptor 2 (PAR-2) agonist SLIGRL-NH 2 on loperamide-induced Sprague-Dawley (SD) rat constipation animal models. (scienceopen.com)
- Protease-activated receptor- 2 (PAR2 ) traffics to lysosomes, and sustained protease signaling requires mobilization and plasma membrane trafficking of PAR 2 from Golgi stores. (nyu.edu)
- Bunnett, Nigel W. / Protein kinase D and Gβγ subunits mediate agonist-evoked translocation of protease-activated receptor-2 from the golgi apparatus to the plasma membrane . (nyu.edu)
- a protease-activated receptor-2 agonist), and bradykinin elicited endothelium-dependent vasodilation by the activation of endothelial Ca 2+ -activated K + channels. (ahajournals.org)
- Protease activated receptor 2 (PAR2) also known as coagulation factor II (thrombin) receptor-like 1 (F2RL1) or G-protein coupled receptor 11 (GPR11) is a protein that in humans is encoded by the F2RL1 gene. (wikipedia.org)
- PAR2 is also a member of the protease-activated receptor family. (wikipedia.org)
- In contrast, little is known about metabotropic GABA B receptors that may mediate long-term effects. (physiology.org)
- For a model of G protein-coupled receptor (GPCR) activation where all agonists stabilize a single active conformation of the receptor, a close correlation between signaling outputs might be expected. (aspetjournals.org)
- These findings are the first to report that a GPCR inverse-agonist reduces growth factor-induced receptor tyrosine kinase signaling, fundamentally broadening their mechanism of action. (strath.ac.uk)
- Agonists in Skeletal Myocytes. (deiodinase.org)
- Physical exercise activates thyroid hormone in skeletal muscle. (deiodinase.org)
- The thyroid hormone activating type 2 deiodinase (D2) is known to play a role in brown adipose tissue-mediated adaptive thermogenesis in rodents, but the finding of D2 in skeletal muscle raises the possibility of a broader metabolic role. (deiodinase.org)
- Upregulation by the B1-agonist was blocked by a specific protein kinase C inhibitor. (nih.gov)
- The complex permits the utilization of active G-protein subunits (made available by constitutively active S1P1 receptor) by the PDGFβ receptor kinase to transmit signals to p42/p44 MAPK in response to PDGF. (strath.ac.uk)
- Therefore, an inverse agonist of the S1P1 receptor is predicted to reduce signal transduction from PDGFβ receptor tyrosine kinase by blocking the constitutive activity of the G-protein coupled receptor. (strath.ac.uk)
- We have developed the first assays that measure the protein kinase activities of interleukin-1 receptor-associated kinase 1 (IRAK1) and IRAK4 reliably in human cell extracts, by employing Pellino1 as a substrate in conjunction with specific pharmacological inhibitors of IRAK1 and IRAK4. (portlandpress.com)
- These findings support the hypothesis that GABA B receptors are present in the spider mechanosensilla where their activation may modulate information transmission. (physiology.org)
- We also tested whether specific GABA B receptor agonists modulate the voltage-activated currents and the excitability of identified peripheral mechanosensory neurons. (physiology.org)
- Agonist-specific cytosolic Ca2+ oscillation patterns can be observed in individual cells and these have been explained by the co-existence of separate oscillatory mechanisms. (epfl.ch)
- Although IRAK1 and IRAK4 were identified many years ago, the mechanisms by which they are activated in vivo are still incompletely understood. (portlandpress.com)
- Identifying the currents and receptor mechanisms involved in depolarization of layer I interneurons is essential for understanding the functional role of these cells and their modulation by dopamine. (jneurosci.org)
- The insulin receptor is an example. (wikipedia.org)
- The highest antagonist activity for GW0742 was found for VDR and the androgen receptor. (houstonmethodist.org)
- Previous studies have established that pro-oxidative stressors suppress host immunity because of their ability to generate oxidized lipids with platelet-activating factor receptor (PAF-R) agonist activity. (jimmunol.org)
- they highlight further differences in TPalpha and TPbeta expression/regulation and point to essential differences between natural and synthetic PPARgamma agonists in mediating those effects. (ucd.ie)
- PAR2 is activated by serine proteases that cleave its N-terminus and by synthetic peptides corresponding to the new N-terminus. (monash.edu)
- Platelet-activating factor induces up-regulation of antiapoptotic factors in a melanoma cell line through nuclear factor- κ B activation," Cancer Research , vol. 66, no. 9, pp. 4681-4686, 2006. (hindawi.com)
- An ionic lock between Asp185 and Arg292 that is probably involved in receptor activation interacts with the phosphate groups. (nih.gov)
- Nevertheless, the long-term consequences of sustained GLP-1 receptor activation in the human thyroid remain unknown and merit further investigation. (nih.gov)
- We show that activation of β 2 -adrenergic receptors (β 2 -AR) promotes the rapid association of GRK2 and MAPK in living cells, as assessed by coimmunoprecipitation experiments in COS-7 cells transfected with β 2 -AR, GRK2, and an epitope-tagged MAPK. (aspetjournals.org)
- Third, SB649146 blocked the S1P-induced activation of p42/p44 MAPK in airway smooth muscle cells, a response that is mediated by the S1P1 receptor. (strath.ac.uk)
- In paper IV we demonstrate that adipocytes, in resemblance with osteoblasts, express a functional system for receptor activation, reuptake and synthesis of serotonin. (ntnu.no)
- and, activation of these receptors results in changes in ion movement across a membrane. (wikipedia.org)
- Toll-like receptor agonists may also cause macrophage activation. (wikipedia.org)
- Pathogenic antigens can bind to toll-like receptors that stimulate macrophage activation and response. (wikipedia.org)
- We conclude that the lower PAR2-mediated responses in PAR2-HET aortas are consistent with evidence of a lower quantity of functional receptor expression, despite the apparently normal PAR2 mRNA content in PAR2-HET aortas. (mun.ca)
- PAR2 is known to transactivate TLR4 and epidermal growth factor receptor in diseases. (wikipedia.org)
- Augmentation of UVB radiation-mediated early gene expression by the epidermal platelet-activating factor receptor," Journal of Investigative Dermatology , vol. 128, no. 2, pp. 455-460, 2008. (hindawi.com)
- Non-coplanar PCBs were also able to activate PXR/CAR target gene expression in a substitution- and tissue-specific manner. (surrey.ac.uk)
- The human thromboxane (TX)A2 receptor (TP) gene encodes two TP isoforms, TPalpha and TP beta that are regulated by distinct promoters designated promoter (Prm) 1 and Prm3, respectively. (ucd.ie)
- In myographs under isometric tension conditions, isolated aortic rings were contracted by alpha 1-adrenoeceptor agonist (phenylephrine), and thromboxane receptor agonist (U46619) and then relaxation responses by the additions of 2-furoyl-LIGRLO-amide, acetylcholine, and nitroprusside were recorded. (mun.ca)
- Inverse agonists selectively stimulate the inactive receptor state by initiating the cellular response opposite to that generated by a natural agonist. (news-medical.net)