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Trodusquemine
Trodusquemine is an aminosterol (polyamine steroid conjugate) that inhibits protein tyrosine phosphatase 1B (PTP1B) activity. The compound exhibits broad-spectrum antimicrobial activity and numerous regenerative, neuroprotective, anti-atherosclerotic, antitumor, antiangiogenic, antiobesity, and anxiolytic properties. Phase I clinical trials of trodusquemine have demonstrated good tolerability, but several planned phase II trials were halted due to financial difficulties of the developer. Chemistry Trodusquemine is a spermine metabolite of cholesterol. The steroid ring consists of a cholestane with a hydroxyl group at C-7 and sulfate group at C-24; spermine is conjugated to the steroid moiety at C-3. It is structurally similar to squalamine, which features a spermidine moiety instead of spermine. Pharmacology Trodusquemine is a non-competitive allosteric inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 1 μmol/L. Inhibition of PTP1B prevents d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Polyamine
A polyamine is an organic compound having two or more amino groups. Alkyl polyamines occur naturally, but some are synthetic. Alkylpolyamines are colorless, hygroscopic, and water soluble. Near neutral pH, they exist as the ammonium derivatives. Most aromatic polyamines are crystalline solids at room temperature. Natural polyamines Low-molecular-weight linear polyamines are found in all forms of life. The principal examples are the triamine spermidine and the tetraamine spermine. They are structurally and biosynthetically related to the diamines putrescine and cadaverine. Polyamine metabolism is regulated by the activity of the enzyme ornithine decarboxylase (ODC). Polyamines are found in high concentrations in the mammalian brain. File:Spermidine-2D-skeletal.svg, spermidine File:Spermine.svg, spermine Synthetic polyamines Ethyleneamines are a commercially-important class of synthetic polyamines with ethylene ( linkages); global production capacity was estimated at 385,00 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
IC50
Half maximal inhibitory concentration (IC50) is a measure of the potency of a substance in inhibiting a specific biological or biochemical function. IC50 is a quantitative measure that indicates how much of a particular inhibitory substance (e.g. drug) is needed to inhibit, ''in vitro'', a given biological process or biological component by 50%. The biological component could be an enzyme, cell, cell receptor or microbe. IC50 values are typically expressed as molar concentration. IC50 is commonly used as a measure of antagonist drug potency in pharmacological research. IC50 is comparable to other measures of potency, such as EC50 for excitatory drugs. EC50 represents the dose or plasma concentration required for obtaining 50% of a maximum effect ''in vivo''. IC50 can be determined with functional assays or with competition binding assays. Sometimes, IC50 values are converted to the pIC50 scale. :\ce = -\log_ \ce Due to the minus sign, higher values of pIC50 indicate ex ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
American Chemical Society
The American Chemical Society (ACS) is a scientific society based in the United States that supports scientific inquiry in the field of chemistry. Founded in 1876 at New York University, the ACS currently has more than 155,000 members at all degree levels and in all fields of chemistry, chemical engineering, and related fields. It is one of the world's largest scientific societies by membership. The ACS is a 501(c) organization, 501(c)(3) non-profit organization and holds a congressional charter under Title 36 of the United States Code. Its headquarters are located in Washington, D.C., and it has a large concentration of staff in Columbus, Ohio. The ACS is a leading source of scientific information through its peer-reviewed scientific journals, national conferences, and the Chemical Abstracts Service. Its publications division produces over 80 Scientific journal, scholarly journals including the prestigious ''Journal of the American Chemical Society'', as well as the weekly tr ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Squaliformes
The Squaliformes are an order of sharks that includes about 126 species in seven families. Members of the order have two dorsal fins, which usually possess spines, they usually have a sharp head, no anal fin or nictitating membrane, and five to seven gill slits. In most other respects, however, they are quite variable in form and size. Most species of the squaliform order live in saltwater or brackish water. They are found worldwide, from northern to tropical waters, and from shallow coastal seas to the open ocean. All members of the family Etmoperidae and Dalatiidae and ''Zameus squamulosus'' possess photophores, luminous organs, and exhibit intrinsic bioluminescence. Bioluminescence evolved once in Squaliformes, approximately 111–153 million years ago, and helped the Squaliformes radiate and adapt to the deep sea. The common ancestor of Dalatiidae, Etmopteridae, Somniosidae, and Oxynotidae possessed a luminous organ and used bioluminescence for camouflage by co ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Squalus Acanthias
The spiny dogfish (''Squalus acanthias''), spurdog, mud shark, or piked dogfish is one of the best known species of the Squalidae (dogfish) family of sharks, which is part of the Squaliformes order. While these common names may apply to several species, ''Squalus acanthias'' is distinguished by two spines (one anterior to each dorsal fin) and no anal fin. It lives in shallow waters and further offshore in most parts of the world, especially in temperate waters. Those in the northern Pacific Ocean were reevaluated in 2010 and found to constitute a separate species, now called the Pacific spiny dogfish (''Squalus suckleyi''). Description and behaviour The spiny dogfish has dorsal fins, no anal fin, and white spots along its back. The caudal fin has asymmetrical lobes, forming a heterocercal tail. The species name ''acanthias'' refers to the shark's two spines. These are used defensively. If captured, the shark can arch its back to pierce its captor with spines near the d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Geroprotector
A geroprotector aims to affect the root cause of aging and age-related diseases, and thus prolong the life span of animals. Some possible geroprotectors include melatonin, carnosine, metformin, rapamycin, nicotinamide mononucleotide (NMN), delta sleep-inducing peptide and glycine. Geroprotectors could belong to multiple classes, depending on which of the ''hallmarks of aging'' they influence. The distinction between geroprotectors and senotherapeutics is an evolving area of aging research. Geroprotectors broadly aim to target multiple mechanisms of aging, prolonging lifespan and healthspan by addressing the fundamental causes of aging. Senotherapeutics, on the other hand, are a subset of therapies that specifically target ''senescent cells'', which are dysfunctional cells that accumulate with age and contribute to inflammation and age-related diseases. See also * Anti-aging product * Growth hormone * Senolytic A senolytic (from the words ''senescence'' and ''-lytic'', "d ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Parkinson's Disease
Parkinson's disease (PD), or simply Parkinson's, is a neurodegenerative disease primarily of the central nervous system, affecting both motor system, motor and non-motor systems. Symptoms typically develop gradually and non-motor issues become more prevalent as the disease progresses. The motor symptoms are collectively called parkinsonism and include tremors, bradykinesia, spasticity, rigidity as well as postural instability (i.e., difficulty maintaining balance). Non-motor symptoms develop later in the disease and include behavior change (individual), behavioral changes or mental disorder, neuropsychiatric problems such as sleep abnormalities, psychosis, anosmia, and mood swings. Most Parkinson's disease cases are idiopathic disease, idiopathic, though contributing factors have been identified. Pathophysiology involves progressive nerve cell death, degeneration of nerve cells in the substantia nigra, a midbrain region that provides dopamine to the basal ganglia, a system invo ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Caenorhabditis Elegans
''Caenorhabditis elegans'' () is a free-living transparent nematode about 1 mm in length that lives in temperate soil environments. It is the type species of its genus. The name is a Hybrid word, blend of the Greek ''caeno-'' (recent), ''rhabditis'' (rod-like) and Latin ''elegans'' (elegant). In 1900, Émile Maupas, Maupas initially named it ''Rhabditidae, Rhabditides elegans.'' Günther Osche, Osche placed it in the subgenus ''Caenorhabditis'' in 1952, and in 1955, Ellsworth Dougherty, Dougherty raised ''Caenorhabditis'' to the status of genus. ''C. elegans'' is an unsegmented pseudocoelomate and lacks respiratory or circulatory systems. Most of these nematodes are hermaphrodites and a few are males. Males have specialised tails for mating that include spicule (nematode), spicules. In 1963, Sydney Brenner proposed research into ''C. elegans,'' primarily in the area of neuronal development. In 1974, he began research into the molecular biology, molecular and developmental ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
LDL Receptor
The low-density lipoprotein receptor (LDL-R) is a mosaic protein of 839 amino acids (after removal of 21-amino acid signal peptide) that mediates the endocytosis of cholesterol-rich low-density lipoprotein (LDL). It is a cell-surface receptor that recognizes apolipoprotein B100 (ApoB100), which is embedded in the outer phospholipid layer of very low-density lipoprotein (VLDL), their remnants—i.e. intermediate-density lipoprotein (IDL), and LDL particles. The receptor also recognizes apolipoprotein E (ApoE) which is found in chylomicron remnants and IDL. In humans, the LDL receptor protein is encoded by the gene on chromosome 19. It belongs to the low density lipoprotein receptor gene family. It is most significantly expressed in bronchial epithelial cells and adrenal gland and cortex tissue. Michael S. Brown and Joseph L. Goldstein were awarded the 1985 Nobel Prize in Physiology or Medicine for their identification of LDL-R and its relation to cholesterol metaboli ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Leptin Receptor
Leptin receptor, also known as LEP-R or OB-R, is a type I cytokine receptor, a protein that in humans is encoded by the ''LEPR'' gene. LEP-R functions as a receptor for the fat cell-specific hormone leptin. LEP-R has also been designated as CD295 (cluster of differentiation 295). Its location is the cell membrane, and it has extracellular, trans-membrane and intracellular sections (''protein regions''). History The Leptin Receptor was discovered in 1995 by Louis Tartaglia and his colleagues at Millennium Pharmaceuticals. This same team demonstrated the leptin receptor was expressed by the mouse db gene. Furthermore, in 1996, after co-discovering the Leptin gene with Jeffrey Friedman et al. in 1994, (which involved a reverse genetic/positional cloning strategy to clone ''ob'' and ''db)'', Rudolph Leibel, working with collaborators also at Millennium Pharmaceuticals and colleague Streamson Chua, confirmed cloning of the leptin receptor by demonstrating that an apparent leptin ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ob/ob Mouse
The ''ob/ob'' or ''obese'' mouse is a mutant mouse that eats excessively due to mutations in the gene responsible for the production of leptin and becomes profoundly obese. It is an animal model of type II diabetes. Identification of the gene mutated in ''ob'' led to the discovery of the hormone leptin, which is important in the control of appetite. The first ''ob/ob'' mouse arose by chance in a colony at the Jackson Laboratory in 1949. The mutation is recessive. Mutant mice are phenotypically indistinguishable from their unaffected littermates at birth, but gain weight rapidly throughout their lives, reaching a weight three times that of unaffected mice. ''ob/ob'' mice develop high blood sugar, despite an enlargement of the pancreatic islets and increased levels of insulin. The gene affected by the ''ob'' mutation was identified by positional cloning. The gene produces a hormone, called leptin, that is produced predominantly in adipose tissue. One role of leptin is to regula ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Norepinephrine Transporter
The norepinephrine transporter (NET), also known as noradrenaline transporter (NAT), is a protein that in humans is encoded by the solute carrier family 6 member 2 (SLC6A2) gene. NET is a monoamine transporter and is responsible for the sodium-chloride (Na+/Cl−)-dependent reuptake of extracellular norepinephrine (NE), which is also known as noradrenaline. NET can also reuptake extracellular dopamine (DA). The reuptake of these two neurotransmitters is essential in regulating concentrations in the synaptic cleft. NETs, along with the other monoamine transporters, are the targets of many antidepressants and recreational drugs. In addition, altered NET availability is associated with ADHD. There is evidence that single-nucleotide polymorphisms in the NET gene (''SLC6A2'') may be an underlying factor in some of these disorders. Gene The norepinephrine transporter gene, SLC6A2 is located on human chromosome 16 locus 16q12.2. This gene is encoded by 14 exons. Based on the nucleotid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
