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ADIPOR2
Adiponectin receptor 2 (AdipoR2) is a protein which in humans is encoded by the ''ADIPOR2'' gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR2. Structure Similar to G protein-coupled receptors (GPCRs), AdipoR2 also possesses 7 transmembrane domains. However, AdipoR2 is orientated oppositely to GPCRs in the membrane (i.e., cytoplasmic N-terminus, extracellular C-terminus) and does not associate with G proteins. Function The adiponectin receptors, AdipoR1 and AdipoR2, serve as receptors for globular and full-length adiponectin and mediate increased AMPK and PPAR-α ligand activities, as well as fatty acid oxidation and glucose uptake by adiponectin. In 2016, the University of Tokyo announced that it would launch an investigation into claims of fabrication of AdipoR1 and AdipoR2 identification data, as accused by an anonymous person/group called Ordinary_researchers.
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G Protein-coupled Receptor
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of evolutionarily-related proteins that are cell surface receptors that detect molecules outside the cell and activate cellular responses. Coupling with G proteins, they are called seven-transmembrane receptors because they pass through the cell membrane seven times. Text was copied from this source, which is available under Attribution 2.5 Generic (CC BY 2.5) license. Ligands can bind either to extracellular N-terminus and loops (e.g. glutamate receptors) or to the binding site within transmembrane helices (Rhodopsin-like family). They are all activated by agonists although a spontaneous auto-activation of an empty receptor can also be observed. G protein-coupled receptors are found only in eukaryotes, including yeast, choanoflagellates, and ...
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Adiponectin Receptor 1
Adiponectin receptor 1 (AdipoR1) is a protein which in humans is encoded by the ''ADIPOR1'' gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR1. Structure Similar to G protein-coupled receptors (GPCRs), AdipoR1 also possesses 7 transmembrane domains. However, AdipoR1 is orientated oppositely to GPCRs in the membrane (i.e., cytoplasmic N-terminus, extracellular C-terminus) and does not associate with G proteins. Function The adiponectin receptors, AdipoR1 and AdipoR2, serve as receptors for globular and full-length adiponectin and mediate increased AMP-activated protein kinase, AMPK and Peroxisome proliferator-activated receptor alpha, PPAR-α ligand activities, as well as fatty acid oxidation and glucose uptake by adiponectin. In 2016, the University of Tokyo announced that it would launch an investigation into claims of fabrication of AdipoR1 and AdipoR2 identification data, as accused by an anonymous person/group called Ordinar ...
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AdipoR1
Adiponectin receptor 1 (AdipoR1) is a protein which in humans is encoded by the ''ADIPOR1'' gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR1. Structure Similar to G protein-coupled receptors (GPCRs), AdipoR1 also possesses 7 transmembrane domains. However, AdipoR1 is orientated oppositely to GPCRs in the membrane (i.e., cytoplasmic N-terminus, extracellular C-terminus) and does not associate with G proteins. Function The adiponectin receptors, AdipoR1 and AdipoR2, serve as receptors for globular and full-length adiponectin and mediate increased AMP-activated protein kinase, AMPK and Peroxisome proliferator-activated receptor alpha, PPAR-α ligand activities, as well as fatty acid oxidation and glucose uptake by adiponectin. In 2016, the University of Tokyo announced that it would launch an investigation into claims of fabrication of AdipoR1 and AdipoR2 identification data, as accused by an anonymous person/group called Ordinar ...
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Adiponectin
Adiponectin (also referred to as GBP-28, apM1, AdipoQ and Acrp30) is a protein hormone and adipokine, which is involved in regulating glucose levels as well as fatty acid breakdown. In humans it is encoded by the ''ADIPOQ'' gene and it is produced in primarily in adipose tissue, but also in muscle, and even in the brain. Structure Adiponectin is a 244-amino-acid-long polypeptide (protein). There are four distinct regions of adiponectin. The first is a short signal sequence that targets the hormone for secretion outside the cell; next is a short region that varies between species; the third is a 65-amino acid region with similarity to collagenous proteins; the last is a globular domain. Overall this protein shows similarity to the complement 1Q factors (C1Q). However, when the 3-dimensional structure of the globular region was determined, a striking similarity to TNFα was observed, despite unrelated protein sequences. Function Adiponectin is a protein hormone that modulates ...
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Adiponectin Receptor
The adiponectin receptors (AdipoRs) include the following two receptors, which are bound and activated by adiponectin: * Adiponectin receptor 1 (AdipoR1, PAQR1) * Adiponectin receptor 2 (AdipoR2, PAQR2) They are members of the progestin and adipoQ receptor (PAQR) family. In 2016, the University of Tokyo announced that it would launch an investigation into claims of fabrication of AdipoR1 and AdipoR2 identification data, as accused by an anonymous person/group called Ordinary_researchers In 2010s, a series of separate allegations of scientific misconducts were raised involving several scientific papers from various Japanese universities. Shigeaki Kato In February 1996, Shigeaki Kato, who had studied in the laboratory of Pierre Ch ....
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Taxifoliol
Taxifolin (5,7,3',4'-flavan-on-ol), also known as dihydroquercetin, belongs to the subclass flavanonols in the flavonoids, which in turn is a class of polyphenols. Stereocenters Taxifolin has two stereocenters on the C-ring, as opposed to quercetin which has none. For example, (+)-taxifolin has (2R,3R)-configuration, making it 1 out of 4 stereoisomers that comprise 2 pairs of enantiomers. Natural occurrences Taxifolin is found in non-glutinous rice boiled with adzuki bean (adzuki-meshi). It can be found in conifers like the Siberian larch, ''Larix sibirica'', in Russia, in ''Pinus roxburghii'', in ''Cedrus deodara'' and in the Chinese yew, '' Taxus chinensis var. mairei''. It is also found in the silymarin extract from the milk thistle seeds. Taxifolin is present in vinegars aged in cherry wood. Taxifolin, and flavonoids in general, can be found in many beverages and products. Specifically, taxifolin is found in plant-based foods like fruit, vegetables, wine, tea, and coco ...
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Syringing (drug)
A syringe is a simple reciprocating pump consisting of a plunger (though in modern syringes, it is actually a piston) that fits tightly within a cylindrical tube called a barrel. The plunger can be linearly pulled and pushed along the inside of the tube, allowing the syringe to take in and expel liquid or gas through a discharge orifice at the front (open) end of the tube. The open end of the syringe may be fitted with a hypodermic needle, a nozzle or tubing to direct the flow into and out of the barrel. Syringes are frequently used in clinical medicine to administer injections, infuse intravenous therapy into the bloodstream, apply compounds such as glue or lubricant, and draw/measure liquids. There are also prefilled syringes (disposable syringes marketed with liquid inside). The word "syringe" is derived from the Greek σύριγξ (''syrinx'', meaning "Pan flute", "tube"). Medical syringes Sectors in the syringe and needle market include disposable and safety syr ...
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Parthenolide
Parthenolide is a sesquiterpene lactone of the germacranolide class which occurs naturally in the plant feverfew (''Tanacetum parthenium''), after which it is named, and in the closely related tansy (''Tanacetum vulgare''). It is found in highest concentration in the flowers and fruit. Parthenolide's molecular structure depiction is often incorrect regarding the stereochemistry of the epoxide, although X-ray single crystal structures are available. Lack of solubility in water and bioavailability limits the potential of parthenolide as a drug. ''In vitro'' research Parthenolide has a variety of reported ''in vitro'' biological activities, including: *Inhibition of HDAC1 protein without affecting other class I/II HDACs, which leads to sustained DNA damage response in certain cells (required for apoptosis). *Modulation of the NF-κB-mediated inflammatory responses in experimental atherosclerosis. *Inducing apoptosis in acute myelogenous leukemia (AML) cells, leaving normal bone marr ...
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Deoxyschizandrin
Deoxyschizandrin is a bio-active isolate of ''Schisandra chinensis''. Deoxyschizandrin has been found to act as an agonist of the adiponectin receptor 2 Adiponectin receptor 2 (AdipoR2) is a protein which in humans is encoded by the ''ADIPOR2'' gene. It is a member of the progestin and adipoQ receptor (PAQR) family, and is also known as PAQR2. Structure Similar to G protein-coupled receptors (GPCR ... (AdipoR2). References Adiponectin receptor agonists Phytochemicals {{organic-compound-stub ...
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AdipoRon
AdipoRon is a selective, orally active, synthetic small-molecule agonist of the adiponectin receptor 1 (AdipoR1) and adiponectin receptor 2 (AdipoR2) (Kd = 1.8 μM and 3.1 μM, respectively). It activates AMPK and PPARα signaling and ameliorates insulin resistance, dyslipidemia, and glucose intolerance in ''db/db'' mice (an animal model for type II diabetes and obesity). Moreover, AdipoRon has been found to extend the lifespans of ''db/db'' mice fed a high-fat diet, as well as improve exercise endurance. The compound was discovered by Japanese researchers in 2013 via screening of a compound library, and is the first orally active, small-molecule agonist of the adiponectin receptors to be identified. Adiponectin receptor agonists such as AdipoRon have attracted interest as potential therapies for obesity, diabetes, cardiovascular disease, non-alcoholic fatty liver disease, and a panoply of other conditions. In addition, adiponectin has recently been elucidated to mediate the anti ...
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