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1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetate
DOTA (also known as tetraxetan) is an organic compound with the formula . The molecule consists of a central 12-membered tetraaza (i.e., containing four nitrogen atoms) ring. DOTA is used as a complexing agent, especially for lanthanide ions. Its complexes have medical applications as contrast agents and cancer treatments. Terminology The acronym DOTA (for dodecane tetraacetic acid) is shorthand for both the tetracarboxylic acid and its various conjugate bases. In the area of coordination chemistry, the tetraacid is called H4DOTA and its fully deprotonated derivative is DOTA4−. Many related ligands are referred to using the DOTA acronym, although these derivatives are generally not tetracarboxylic acids or the conjugate bases. The "tetra-" prefix in tetraxetan indicates the four nitrogen atoms in the macrocycle and the four acetic acid arms in the DOTA structure, while "xetan" is a standard suffix for chelators. Structure DOTA is derived from the macrocycle known as cyclen. Th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cyclen
Cyclen (1,4,7,10-tetraazacyclododecane) is an aza-crown ether with the formula (CH2CH2NH)4. It is a white solid. It forms Coordination complex, coordination complexes with metal cations and is used to synthesize the chelating agent DOTA (chelator), DOTA which has several medical applications. Being structurally simple, symmetrical, and polyfunctional, cyclen has been widely investigated. Synthesis Some syntheses exploit the Thorpe-Ingold effect to facilitate ring-formation. Illustrative is the reaction of the deprotonated tosylamides with ditosylates: :TsN(CH2CH2NTsNa)2 + TsN(CH2CH2OTs)2 → (TsNCH2CH2)4 The resulting macrocycle can be deprotected with strong acid. Base gives the tetramine. High dilution conditions result in a low reaction rate penalty and this disadvantage is removed in an alternative procedure starting from triethylenetetraamine and dithiooxamide to a amidine, bisamidine – also a bis(2-Imidazoline, imidazoline) – followed by organic reduction, reduc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
American Medical Association
The American Medical Association (AMA) is an American professional association and lobbying group of physicians and medical students. This medical association was founded in 1847 and is headquartered in Chicago, Illinois. Membership was 271,660 in 2022. The AMA's stated mission is "to promote the art and science of medicine and the betterment of public health." The organization was founded with the goal to raise the standards of medicine in the 19th century primarily through gaining control of education and licensing. In the 20th century, the AMA has frequently lobbied to restrict the supply of physicians, contributing to a doctor shortage in the United States. The organization has also lobbied against allowing physician assistants and other health care providers to perform basic forms of health care. The organization has historically lobbied against various forms of government-run health insurance. The Association also publishes the '' Journal of the American Medical Assoc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Gadolinium
Gadolinium is a chemical element; it has Symbol (chemistry), symbol Gd and atomic number 64. It is a silvery-white metal when oxidation is removed. Gadolinium is a malleable and ductile rare-earth element. It reacts with atmospheric oxygen or moisture slowly to form a black coating. Gadolinium below its Curie point of is ferromagnetism, ferromagnetic, with an attraction to a magnetic field higher than that of nickel. Above this temperature it is the most paramagnetism, paramagnetic element. It is found in nature only in an oxidized form. When separated, it usually has impurities of the other rare earths because of their similar chemical properties. Gadolinium was discovered in 1880 by Jean Charles Galissard de Marignac, Jean Charles de Marignac, who detected its oxide by using spectroscopy. It is named after the mineral gadolinite, one of the minerals in which gadolinium is found, itself named for the Finnish chemist Johan Gadolin. Pure gadolinium was first isolated by the chemis ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yttrium-90
Yttrium-90 () is a radioactive isotope of yttrium. Yttrium-90 has found a wide range of uses in radiation therapy to treat some forms of cancer Cancer is a group of diseases involving Cell growth#Disorders, abnormal cell growth with the potential to Invasion (cancer), invade or Metastasis, spread to other parts of the body. These contrast with benign tumors, which do not spread. Po .... Along with other isotopes of yttrium, it is sometimes called radioyttrium. Decay undergoes beta particles emissions/decay (beta decay, β− decay) to zirconium-90 with a half-life of 64.1 hours and a decay energy of 2.28 MeV with an average beta energy of 0.9336 MeV. It also produces 0.01% 1.7 MeV photons during its decay process to the 0+ state of 90Zr, followed by pair production. The interaction between emitted electrons and matter can lead to the emission of Bremsstrahlung radiation. Production Yttrium-90 is produced by the nuclear decay of strontium-90 which has a half-l ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tacatuzumab
Yttrium (90Y) tacatuzumab tetraxetan is an investigational humanized monoclonal antibody intended for the treatment of cancer. The antibody itself, tacatuzumab, is conjugated with tetraxetan, a chelator for yttrium-90, a radioisotope A radionuclide (radioactive nuclide, radioisotope or radioactive isotope) is a nuclide that has excess numbers of either neutrons or protons, giving it excess nuclear energy, and making it unstable. This excess energy can be used in one of three ... which destroys the tumour cells. References Monoclonal antibodies for tumors Antibody-drug conjugates Radiopharmaceuticals Yttrium compounds Experimental cancer drugs DOTA (chelator) derivatives {{nuclear-med-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOTA-biotin
90Y-DOTA-biotin consists of a radioactive substance (yttrium-90) complexed by a chelating agent (DOTA), which in turn is attached to the vitamin biotin via a chemical linker. It is used experimentally in pretargeted radioimmunotherapy. Animal studies have been conducted as well as clinical studies in humans. In pretargeted radioimmunotherapy, two or three medications are applied in succession. At first, an antibody-drug conjugate is administered, which consists of a monoclonal antibody designed to target the tumour, and a chemical marker which in the case of DOTA-biotin therapy is one of the proteins avidin and streptavidin Streptavidin is a 52 Atomic mass unit, kDa protein (tetramer) purified from the bacterium ''Streptomyces avidinii''. Streptavidin Homotetramer, homo-tetramers have an extraordinarily high affinity for biotin (also known as vitamin B7 or vitamin .... After a time of typically one or two days to let the antibody accumulate in the tumour, a clearing agent may ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Avidin
Avidin is a tetrameric biotin-binding protein produced in the oviducts of birds, reptiles and amphibians and deposited in the whites of their eggs. Dimeric members of the avidin family are also found in some bacteria. In chicken egg white, avidin makes up approximately 0.05% of total protein (approximately 1800 μg per egg). The tetrameric protein contains four identical subunits (homotetramer), each of which can bind to biotin (Vitamin B7, vitamin H) with a high degree of affinity and specificity. The dissociation constant of the avidin-biotin complex is measured to be ''K''D ≈ 10−15 M, making it one of the strongest known non-covalent bonds. In its tetrameric form, avidin is estimated to be 66–69 k Da in size. 10% of the molecular weight is contributed by carbohydrate, composed of four to five mannose and three N-acetylglucosamine residues The carbohydrate moieties of avidin contain at least three unique oligosaccharide structural types that are similar in ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Streptavidin
Streptavidin is a 52 Atomic mass unit, kDa protein (tetramer) purified from the bacterium ''Streptomyces avidinii''. Streptavidin Homotetramer, homo-tetramers have an extraordinarily high affinity for biotin (also known as vitamin B7 or vitamin H). With a dissociation constant (Kd) on the order of ≈10−14 mol/L, the binding of biotin to streptavidin is one of the strongest non-covalent interactions known in nature. Streptavidin is used extensively in molecular biology and bionanotechnology due to the streptavidin-biotin complex's resistance to organic solvents, denaturants (e.g. guanidinium chloride), detergents (e.g. Sodium dodecyl sulfate, SDS, Triton X-100), proteolytic enzymes, and extremes of temperature and pH. Structure The crystal structure of streptavidin with biotin bound was reported by two groups in 1989. The structure was solved using multi wavelength anomalous diffraction by Hendrickson et al. at Columbia University and using multiple isomorphous replacemen ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOTA-TATE
DOTA-TATE (DOTATATE, DOTA-octreotate, oxodotreotide, DOTA-(Tyr3)-octreotate, and DOTA-0-Tyr3-Octreotate) is an eight amino acid long peptide, with a covalently bonded DOTA bifunctional chelator. DOTA-TATE can be reacted with the radionuclides gallium-68 (T1/2 = 68 min), lutetium-177 (T1/2 = 6.65 d) and copper-64 (T1/2 = 12.7 h) to form radiopharmaceuticals for positron emission tomography (PET) imaging or radionuclide therapy. 177Lu DOTA-TATE therapy is a form of peptide receptor radionuclide therapy (PRRT) which targets somatostatin receptors (SSR). In that form of application it is a form of targeted drug delivery. Chemistry and mechanism of action DOTA-TATE is a compound containing tyrosine3-octreotate, an SSR agonist, and the bifunctional chelator DOTA (tetraxetan). SSRs are found with high density in numerous malignancies, including CNS, breast, lung, and lymphatics. The role of SSR agonists (i.e. somatostatin and its analogs such as octreotide, somatuline and va ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
DOTATOC
Edotreotide (United States Adopted Name, USAN, also known as (DOTA (chelator), DOTA0-Phenylalanine, Phe1-Tyrosine, Tyr3) octreotide, DOTA-TOC, DOTATOC) is a substance which, when bound to various radionuclides, is used in the treatment and diagnosis of certain types of cancer. When used therapeutically it is an example of peptide receptor radionuclide therapy. Yttrium-90 A phase I clinical trial of yttrium-90 labelled edotreotide concluded in 2011, aiming to investigated effects in young cancer patients (up to 25 years of age). Specific cancers being included in the trial include neuroblastoma, childhood brain tumours and gastrointestinal cancer. A phase II trial for the use of 90Y DOTA-TOC for patients with metastatic carcinoid, where octreotide treatment was no longer effective, also reported results in 2010. : Lutetium-177 Lutetium-177 labelled edotreotide (177Lu-DOTA-TOC), with the trade name Solucin, is the subject of a phase 3 clinical trial for treatment of GEP-NETs. I ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Neuroendocrine Tumour
Neuroendocrine tumors (NETs) are neoplasms that arise from cells of the endocrine (hormonal) and nervous systems. They most commonly occur in the intestine, where they are often called carcinoid tumors, but they are also found in the pancreas, lung, and the rest of the body. Although there are many kinds of NETs, they are treated as a group of tissue because the cells of these neoplasms share common features, including a similar histological appearance, having special secretory granules, and often producing biogenic amines and polypeptide hormones. The term "neuro" refers to the dense core granules (DCGs), similar to the DCGs in the serotonergic neurons storing monoamines. The term "endocrine" refers to the synthesis and secretion of these monoamines. The neuroendocrine system includes endocrine glands such as the pituitary, the parathyroids and the neuroendocrine adrenals, as well as endocrine islet tissue embedded within glandular tissue such as in the pancreas, and scatter ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Somatostatin Receptor
Somatostatin receptors are receptors for the ligand somatostatin, a small neuropeptide associated with neural signaling, particularly in the post-synaptic response to NMDA receptor co-stimulation/activation. Somatostatin is encoded by a CRE and is very susceptible to gene promoter region activation by transcription factor CREB. There are five known somatostatin receptors: * SST1 () * SST2 () * SST3 () * SST4 () * SST5 () All are G protein-coupled 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 ... seven transmembrane receptors. References External links * G protein-coupled receptors {{transmembranereceptor-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
