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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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
SRT-2104
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 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 ... * STAC-9 References Anti-aging substances 4-Morpholinyl compunds Thiazoles 3-Pyridyl compounds Amides {{pharm-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GlaxoSmithKline
GSK plc, formerly GlaxoSmithKline plc, is a British multinational pharmaceutical and biotechnology company with global headquarters in London, England. Established in 2000 by a merger of Glaxo Wellcome and SmithKline Beecham. GSK is the tenth largest pharmaceutical company and #294 on the 2022 ''Fortune'' Global 500, ranked behind other pharmaceutical companies China Resources, Sinopharm, Johnson & Johnson, Pfizer, Roche, AbbVie, Novartis, Bayer, and Merck. The company has a primary listing on the London Stock Exchange and is a constituent of the FTSE 100 Index. , it had a market capitalisation of £70 billion, the eighth largest on the London Stock Exchange. It has a secondary listing on the New York Stock Exchange. The company developed the first malaria vaccine, RTS,S, which it said in 2014 it would make available for five percent above cost. Legacy products developed at GSK include several listed in the World Health Organization's List of Essential Medicines, such ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Diabetes
Diabetes, also known as diabetes mellitus, is a group of metabolic disorders characterized by a high blood sugar level ( hyperglycemia) over a prolonged period of time. Symptoms often include frequent urination, increased thirst and increased appetite. If left untreated, diabetes can cause many health complications. Acute complications can include diabetic ketoacidosis, hyperosmolar hyperglycemic state, or death. Serious long-term complications include cardiovascular disease, stroke, chronic kidney disease, foot ulcers, damage to the nerves, damage to the eyes, and cognitive impairment. Diabetes is due to either the pancreas not producing enough insulin, or the cells of the body not responding properly to the insulin produced. Insulin is a hormone which is responsible for helping glucose from food get into cells to be used for energy. There are three main types of diabetes mellitus: * Type 1 diabetes results from failure of the pancreas to produce enough insulin due to lo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Trifluoromethyl Compounds
The trifluoromethyl group is a functional group that has the formula -CF3. The naming of is group is derived from the methyl group (which has the formula -CH3), by replacing each hydrogen atom by a fluorine atom. Some common examples are trifluoromethane H–, 1,1,1-trifluoroethane –, and hexafluoroacetone –CO–. Compounds with this group are a subclass of the organofluorines. Properties The trifluoromethyl group has a significant electronegativity that is often described as being intermediate between the electronegativities of fluorine and chlorine. For this reason, trifluoromethyl-substituted compounds are often strong acids, such as trifluoromethanesulfonic acid and trifluoroacetic acid. Conversely, the trifluoromethyl group lowers the basicity of compounds like trifluoroethanol. Uses The trifluoromethyl group occurs in certain pharmaceuticals, drugs, and abiotically synthesized natural fluorocarbon based compounds. The medicinal use of the trifloromethyl group dates from ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
