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SRT2104
SRT-2104 is an experimental drug that was studied by Sirtris Pharmaceuticals as a small-molecule activator of the sirtuin subtype SIRT1. The compound progressed to Phase II human trials for Type II diabetes before development was discontinued, however it continues to be widely used in animal research into the functions of SIRT1. See also * SRT-1460 * SRT-1720 * SRT-2183 * SRT-3025 * STAC-9 STAC-9 is an experimental drug that was developed by GlaxoSmithKline as a small-molecule activator of the sirtuin subtype SIRT1, with potential applications in the treatment of diabetes. See also * SRT-1460 * SRT-1720 * SRT-2104 * SRT-2183 ... References Anti-aging substances 4-Morpholinyl compunds Thiazoles 3-Pyridyl compounds Amides {{pharm-stub ...
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Sirtris Pharmaceuticals
Sirtris Pharmaceuticals, Inc. was a biotechnology company based in Cambridge, MA that developed therapies for type 2 diabetes, cancer, and other diseases. Conceived in 2004 by Harvard University biologist David Sinclair and serial entrepreneur Andrew Perlman, and founded that year by Sinclair and Perlman, along with Christoph Westphal, Richard Aldrich, Richard Pops, and Paul Schimmel, the company was focused on developing Sinclair's research into activators of sirtuins, work that began in the laboratory of Leonard P. Guarente where Sinclair worked as a post-doc before starting his own lab. Synopsis The company was specifically focused on resveratrol formulations and derivatives as activators of the SIRT1 enzyme; Sinclair became known for making statements about resveratrol like: “(It's) as close to a miraculous molecule as you can find.... One hundred years from now, people will maybe be taking these molecules on a daily basis to prevent heart disease, stroke, and cancer.” ...
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Sirtuin
Sirtuins are a family of signaling proteins involved in metabolic regulation. They are ancient in animal evolution and appear to possess a highly conserved structure throughout all kingdoms of life. Chemically, sirtuins are a class of proteins that possess either mono- ADP-ribosyltransferase or deacylase activity, including deacetylase, desuccinylase, demalonylase, demyristoylase and depalmitoylase activity. The name Sir2 comes from the yeast gene 'silent mating-type information regulation 2', the gene responsible for cellular regulation in yeast. From ''in vitro'' studies, sirtuins are implicated in influencing cellular processes like aging, transcription, apoptosis, inflammation and stress resistance, as well as energy efficiency and alertness during low-calorie situations. As of 2018, there was no clinical evidence that sirtuins affect human aging. Yeast Sir2 and some, but not all, sirtuins are protein deacetylases. Unlike other known protein deacetylases, which simply hyd ...
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SRT-1720
SRT-1720 is an experimental drug that was studied by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. The compound has been studied in animals, but safety and efficacy in humans have not been established. Animal research In animal models of obesity and diabetes SRT1720 was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increase mitochondrial and metabolic function. In mice rendered obese and diabetic by feeding a high-fat, high-sugar diet, a study performed at the National Institute of Aging found that feeding chow infused with the highest dose of SRT1720 beginning at one year of age increased mean lifespan by 18%, and maximum lifespan by 5%, as compared to other short-lived obese, diabetic mice; however, treated animals still lived substantially shorter lives than normal-weight mice fed normal chow with no drug. In a later study, SRT1720 increased mean lifespan of obese, diab ...
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Small-molecule
Within the fields of molecular biology and pharmacology, a small molecule or micromolecule is a low molecular weight (≤ 1000 daltons) organic compound that may regulate a biological process, with a size on the order of 1 nm. Many drugs are small molecules; the terms are equivalent in the literature. Larger structures such as nucleic acids and proteins, and many polysaccharides are not small molecules, although their constituent monomers (ribo- or deoxyribonucleotides, amino acids, and monosaccharides, respectively) are often considered small molecules. Small molecules may be used as research tools to probe biological function as well as leads in the development of new therapeutic agents. Some can inhibit a specific function of a protein or disrupt protein–protein interactions. Pharmacology usually restricts the term "small molecule" to molecules that bind specific biological macromolecules and act as an effector, altering the activity or function of the target. Smal ...
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Sirtuin Activator
Sirtuin-activating compounds (STAC) are chemical compounds having an effect on sirtuins, a group of enzymes that use NAD+ to remove acetyl groups from proteins. They are caloric restriction mimetic compounds that may be helpful in treating various aging-related diseases. Context Leonard P. Guarente is recognized as the leading proponent of the hypothesis that caloric restriction slows aging by activation of Sirtuins. STACs have been discovered by Konrad Howitz of Biomol Inc and biologist David Sinclair. In September 2003, Howitz and Sinclair et al. published a highly cited paper reporting that polyphenols such as resveratrol activate human SIRT1 and extend the lifespan of budding yeast (Howitz et al., Nature, 2003). Other examples of such products are butein, piceatannol, isoliquiritigenin, fisetin, and quercetin. Sirtuins depend on the crucial cellular molecule called nicotinamide adenine dinucleotide (NAD+) for their function. Falling NAD+ levels during aging may adversely i ...
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SIRT1
Sirtuin 1, also known as NAD-dependent deacetylase sirtuin-1, is a protein that in humans is encoded by the SIRT1 gene. SIRT1 stands for sirtuin (silent mating type information regulation 2 homolog) 1 (''S. cerevisiae''), referring to the fact that its sirtuin homolog (biological equivalent across species) in yeast ''(Saccharomyces cerevisiae)'' is Sir2. SIRT1 is an enzyme located primarily in the cell nucleus that deacetylates transcription factors that contribute to cellular regulation (reaction to stressors, longevity). Function Sirtuin 1 is a member of the sirtuin family of proteins, homologs of the Sir2 gene in ''S. cerevisiae''. Members of the sirtuin family are characterized by a sirtuin core domain and grouped into four classes. The functions of human sirtuins have not yet been determined; however, yeast sirtuin proteins are known to regulate epigenetic gene silencing and suppress recombination of rDNA. Studies suggest that the human sirtuins may function as intracel ...
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Type II Diabetes
Type 2 diabetes, formerly known as adult-onset diabetes, is a form of diabetes mellitus that is characterized by high blood sugar, insulin resistance, and relative lack of insulin. Common symptoms include increased thirst, frequent urination, and unexplained weight loss. Symptoms may also include increased hunger, feeling tired, and sores that do not heal. Often symptoms come on slowly. Long-term complications from high blood sugar include heart disease, strokes, diabetic retinopathy which can result in blindness, kidney failure, and poor blood flow in the limbs which may lead to amputations. The sudden onset of hyperosmolar hyperglycemic state may occur; however, ketoacidosis is uncommon. Type 2 diabetes primarily occurs as a result of obesity and lack of exercise. Some people are genetically more at risk than others. Type 2 diabetes makes up about 90% of cases of diabetes, with the other 10% due primarily to type 1 diabetes and gestational diabetes. In type 1 diabete ...
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SRT-1460
SRT-1460 is a drug in development by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. It has similar activity in animal studies to the known SIRT1 activator resveratrol, but is closer in potency to SRT-1720. In animal studies it was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increased mitochondrial and metabolic function. However, the claim that SRT1460 is a SIRT1 activator has been questioned and further defended. See also * SRT-2183 * STAC-9 STAC-9 is an experimental drug that was developed by GlaxoSmithKline as a small-molecule activator of the sirtuin subtype SIRT1, with potential applications in the treatment of diabetes. See also * SRT-1460 * SRT-1720 * SRT-2104 * SRT-2183 * ... References Piperazines {{pharmacology-stub ...
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SRT-2183
SRT-2183 is a drug in development by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. It has similar activity in animal studies to another SIRT1 activator SRT-1720, but is closer in potency to resveratrol. In animal studies it was found to improve insulin sensitivity and lower plasma glucose levels in fat, muscle and liver tissue, and increased mitochondrial and metabolic function. However, the claim that SRT-2183 is a SIRT1 activator has been questioned and further defended. See also *SRT-1460 SRT-1460 is a drug in development by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. It has similar activity in animal studies to the known SIRT1 activator resveratrol, but is closer in potency to SRT ... References 2-Naphthyl compounds {{gastrointestinal-drug-stub ...
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SRT-3025
SRT-3025 is an experimental drug that was studied by Sirtris Pharmaceuticals as a small-molecule activator of the sirtuin subtype SIRT1. It has been investigated as a potential treatment for osteoporosis, and anemia. See also * SRT-1460 * SRT-1720 * SRT-2104 * SRT-2183 * STAC-9 STAC-9 is an experimental drug that was developed by GlaxoSmithKline as a small-molecule activator of the sirtuin subtype SIRT1, with potential applications in the treatment of diabetes. See also * SRT-1460 * SRT-1720 * SRT-2104 * SRT-2183 ... References {{pharm-stub Pyrrolidines Thiazoles Amides ...
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STAC-9
STAC-9 is an experimental drug that was developed by GlaxoSmithKline as a small-molecule activator of the sirtuin subtype SIRT1, with potential applications in the treatment of diabetes. See also * SRT-1460 * SRT-1720 * SRT-2104 * SRT-2183 SRT-2183 is a drug in development by Sirtris Pharmaceuticals intended as a small-molecule activator of the sirtuin subtype SIRT1. It has similar activity in animal studies to another SIRT1 activator SRT-1720, but is closer in potency to resverat ... * SRT-3025 References {{pharm-stub Trifluoromethyl compounds 4-Pyridyl compounds Amides ...
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Anti-aging Substances
The anti-aging movement is a social movement devoted to eliminating or reversing aging, or reducing the effects of it. A substantial portion of the attention of the movement is on the possibilities for life extension, but there is also interest in techniques such as cosmetic surgery which ameliorate the effects of aging rather than delay or defeat it. There are many scientists of this movement with different approaches. Two of the most popular proponents of the anti-aging movement include Ray Kurzweil, who says humanity can defeat aging through the advance of technology, and Aubrey de Grey, who says that the human body is a very complicated machine and, thus, can be repaired indefinitely. Other scientists and significant contributors to the movement include molecular biologists, geneticists, and biomedical gerontologists such as Gary Ruvkun, Cynthia Kenyon, and Arthur D. Levinson. However, figures in the gerontology community in 2003 tried to distance their research from the percei ...
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