Exercise Mimetic
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Exercise Mimetic
An exercise mimetic is a drug that mimics some of the biological effects of physical exercise. Exercise is known to have an effect in preventing, treating, or ameliorating the effects of a variety of serious illnesses, including cancer, type 2 diabetes, cardiovascular disease, and psychiatric and neurological diseases such as Alzheimer's disease. As of 2021, no drug is known to have the same benefits. Known biological targets affected by exercise have also been targets of drug discovery In the fields of medicine, biotechnology, and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered by identifying the active ingredient from traditional remedies or ..., with limited results. These known targets include: The majority of the effect of exercise in reducing cardiovascular and all-cause mortality cannot be explained via improvements in quantifiable risk factors, such as blood cholesterol. This further ...
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Multiple Tissues And Organ Systems Are Affected By Exercise, Initiating Diverse Homeostatic Responses
Multiple may refer to: Economics *Multiple finance, a method used to analyze stock prices *Multiples of the P/E, price-to-earnings ratio *Chain stores, are also referred to as 'Multiples' *Box office multiple, the ratio of a film's total gross to that of its opening weekend Sociology *Multiples (sociology), a theory in sociology of science by Robert K. Merton, see Science *Multiple (mathematics), multiples of numbers *List of multiple discoveries, instances of scientists, working independently of each other, reaching similar findings *Multiple birth, because having twins is sometimes called having "multiples" *Multiple sclerosis, an inflammatory disease *Parlance for people with multiple identities, sometimes called "multiples"; often theorized as having dissociative identity disorder *Multiple myeloma (MM), a cancer that forms in a type of white blood cell (WBC) called plasma cells. Printing *Printmaking, where ''multiple'' is often used as a term for a print, especially in the ...
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GW501516
GW501516 (also known as GW-501,516, GW1516, GSK-516, cardarine, and on the black market as endurobol) is a PPARδ receptor agonist that was invented in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. It entered into clinical development as a drug candidate for metabolic and cardiovascular diseases, but was abandoned in 2007 because animal testing showed that the drug caused cancer to develop rapidly in several organs. In 2007, research was published showing that high doses of GW501516 given to mice dramatically improved their physical performance; the work was widely discussed in popular media, and led to a black market for the drug candidate and to its abuse by athletes as a doping agent. The World Anti-Doping Agency (WADA) developed a test for GW501516 and other related chemicals and added them to the prohibited list in 2009; it has issued additional warnings to athletes that GW501516 is not safe. History GW501516 was initially discovered d ...
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Myostatin Inhibitors
Myostatin inhibitors are a class of drugs that work by blocking the effect of myostatin, which inhibits muscle growth. In animal models and limited human studies, myostatin inhibitors have increased muscle size. They are being developed to treat obesity, sarcopenia, muscular dystrophy, and other illnesses. Background Myostatin, a member of the transforming growth factor superfamily, is a negative regulator of bone and muscle growth. It may also play a role in obesity, insulin resistance, cardiovascular disease, and chronic kidney disease. Mechanisms Follistatin is an endogenous protein that negatively regulates myostatin. Reduction of myostatin expression is one of the mechanisms for the effects of androgens in promoting muscle growth. Androgens both regulate myostatin expression directly and upregulate follistatin expression. YK-11, a selective androgen receptor modulator, is also a myostatin inhibitor. Resistance training reduces myostatin activity and increases follistatin ...
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Myostatin
Myostatin (also known as growth differentiation factor 8, abbreviated GDF8) is a protein that in humans is encoded by the ''MSTN'' gene. Myostatin is a myokine that is produced and released by myocytes and acts on muscle cells to inhibit muscle growth. Myostatin is a secreted growth differentiation factor that is a member of the TGF beta protein family. Myostatin is assembled and produced in skeletal muscle before it is released into the blood stream. Most of the data regarding the effects of myostatin comes from studies performed on mice. Animals either lacking myostatin or treated with substances that block the activity of myostatin have significantly more muscle mass. Furthermore, individuals who have mutations in both copies of the myostatin gene (popularly called the "Hercules gene") have significantly more muscle mass and are stronger than normal. There is hope that studies into myostatin may have therapeutic application in treating muscle wasting diseases such as muscul ...
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Transient Receptor Potential
Transient receptor potential channels (TRP channels) are a group of ion channels located mostly on the plasma membrane of numerous animal cell types. Most of these are grouped into two broad groups: Group 1 includes TRPC ( "C" for canonical), TRPV ("V" for vanilloid), TRPVL ("VL" for vanilloid-like), TRPM ("M" for melastatin), TRPS ("S" for soromelastatin), TRPN ("N" for mechanoreceptor potential C), and TRPA (channel), TRPA ("A" for ankyrin). Group 2 consists of TRPP ("P" for polycystic) and TRPML ("ML" for mucolipin). Other less-well categorized TRP channels exist, including yeast channels and a number of Group 1 and Group 2 channels present in non-animals. Many of these channels mediate a variety of sensations such as pain, temperature, different kinds of taste, pressure, and vision. In the body, some TRP channels are thought to behave like microscopic thermometers and used in animals to sense hot or cold. Some TRP channels are activated by molecules found in spices like garlic ...
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NFE2L2
Nuclear factor erythroid 2-related factor 2 (NRF2), also known as nuclear factor erythroid-derived 2-like 2, is a transcription factor that in humans is encoded by the ''NFE2L2'' gene. NRF2 is a bZIP domain, basic leucine zipper (bZIP) protein that may regulate the expression of antioxidant proteins that protect against oxidative stress, oxidative damage triggered by injury and inflammation, according to preliminary research. ''In vitro'', NRF2 binds to antioxidant response elements (AREs) in the promoter regions of genes encoding antioxidant, cytoprotective proteins. NRF2 induces the expression of Heme oxygenase#Heme oxygenase 1, heme oxygenase 1 ''in vitro'' leading to an increase in Drug metabolism#Phase II – conjugation, phase II enzymes. NRF2 also inhibits the NLRP3 inflammasome. NRF2 appears to participate in a complex regulatory network and performs a pleiotropic role in the regulation of metabolism, inflammation, autophagy, proteostasis, mitochondrial physiology, and i ...
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SLU-PP-332
SLU-PP-332 is a compound which is a potent but non-selective estrogen-related receptor (ERR) agonist, acting most strongly at ERRα with an EC50 of 98 nM. It was found to counteract metabolic syndrome Metabolic syndrome is a clustering of at least three of the following five medical conditions: abdominal obesity, high blood pressure, high blood sugar, high serum triglycerides, and low serum high-density lipoprotein (HDL). Metabolic syndro ... in mice, suggesting a possible role for compounds from this class as medications for the treatment of obesity. References {{Estrogen-related receptor modulators 4-Hydroxyphenyl compounds Benzamides Naphthalenes Hydrazides Exercise mimetics Estrogen-related receptor modulators ...
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Estrogen-related Receptor Alpha
Estrogen-related receptor alpha (ERRα), also known as NR3B1 (nuclear receptor subfamily 3, group B, member 1), is a nuclear receptor that in humans is encoded by the ''ESRRA'' (Estrogen Related Receptor Alpha) gene. ERRα was originally cloned by DNA sequence homology to the estrogen receptor alpha (ERα, NR3A1), but subsequent ligand binding and reporter-gene transfection experiments demonstrated that estrogens did not regulate ERRα. Currently, ERRα is considered an orphan nuclear receptor. Tissue distribution ERRα has wide tissue distribution but it is most highly expressed in tissues that preferentially use fatty acids as energy sources such as kidney, heart, brown adipose tissue, cerebellum, intestine, and skeletal muscle. Recently, ERRα has been detected in normal adrenal cortex tissues, in which its expression is possibly related to adrenal development, with a possible role in fetal adrenal function, in DHEAS production in adrenarche, and also in steroid production o ...
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Estrogen-related Receptor γ
Estrogen-related receptor gamma (ERR-gamma), also known as NR3B3 (nuclear receptor subfamily 3, group B, member 3), is a nuclear receptor that in humans is encoded by the ESRRG (EStrogen Related Receptor Gamma) gene. It behaves as a constitutive activator of transcription. This protein is a member of nuclear hormone receptor family of steroid hormone receptors. No physiological activating ligand is known for this orphan receptor, but 4-hydroxytamoxifen and diethylstilbestrol act as inverse agonists and deactivate ESRRG. It also seems to be the target of bisphenol A (see below). Bisphenol A binding There is evidence that bisphenol A functions as a xenoestrogen by binding strongly to ERR-γ. BPA as well as its nitrated and chlorinated metabolites seems to binds strongly to ERR-γ (dissociation constant = 5.5 nM), but not to the estrogen receptor (ER)., BPA binding to ERR-γ preserves its basal constitutive activity. It can also protect it from deactivation from the selective es ...
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Peroxisome Proliferator-activated Receptor Delta
A peroxisome () is a membrane-bound organelle, a type of microbody, found in the cytoplasm of virtually all eukaryotic cells. Peroxisomes are oxidative organelles. Frequently, molecular oxygen serves as a co-substrate, from which hydrogen peroxide (H2O2) is then formed. Peroxisomes owe their name to hydrogen peroxide-generating and scavenging activities. They perform key roles in lipid metabolism and the redox, reduction of reactive oxygen species. Peroxisomes are involved in the catabolism of very long chain fatty acids, branched chain fatty acids, bile acid intermediates (in the liver), D-amino acids, and polyamines. Peroxisomes also play a role in the biosynthesis of plasmalogens: ether phospholipids critical for the normal function of mammalian brains and lungs. Peroxisomes contain approximately 10% of the total activity of two enzymes (Glucose-6-phosphate dehydrogenase and Phosphogluconate dehydrogenase, 6-Phosphogluconate dehydrogenase) in the pentose phosphate pathway, ...
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