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Quizartinib
Quizartinib (AC220) is a small molecule receptor tyrosine kinase inhibitor, originally from Ambit Biosciences and later acquired by Daiichi Sankyo, that is currently under development for the treatment of acute myeloid leukaemia. Quizartinib is sold under the brand name Vanflyta in Japan. Its molecular target is FLT3, also known as CD135 which is a proto-oncogene. Flt3 mutations are among the most common mutations in acute myeloid leukaemia due to internal tandem duplication of Flt3. The presence of this mutation is a marker of adverse outcome. __TOC__ Mechanism Specifically, quizartinib selectively inhibits class III receptor tyrosine kinases, including FMS-related tyrosine kinase 3 (FLT3/STK1), colony-stimulating factor 1 receptor (CSF1R/ FMS), stem cell factor receptor (SCFR/KIT), and platelet derived growth factor receptors (PDGFR Platelet-derived growth factor receptors (PDGF-R) are cell surface tyrosine kinase receptors for members of the platelet-derived growth factor ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Daiichi Sankyo
is a global pharmaceutical company and the second-largest pharmaceutical company in Japan. It achieved JPY 981.8 billion in revenue in 2019. The company owns the American biotechnology company Plexxikon, American pharmaceutical company American Regent, German biotechnology company U3 Pharma, and recently sold Ranbaxy Laboratories in India. Daiichi Sankyo Co., Ltd. is the producer of Benicar (Olmesartan), an angiotensin II receptor antagonist and top selling drug in the U.S. Global sales of Olmesartan in 2013 were 300.2 billion yen. Daiichi Sankyo, Inc. (DSI) began operating in the U.S. in 2006. It is the U.S. subsidiary of Daiichi Sankyo Company, Limited, and a member of the Daiichi Sankyo Group. The organization, which includes U.S. commercial operations and global clinical development (Daiichi Sankyo Pharma Development), is headquartered in Basking Ridge, New Jersey. Daiichi Sankyo Europe, GmbH (DSE), the European subsidiary, is headquartered in Munich, Germany. The organizat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ambit Biosciences
Ambit was an American pharmaceutical company focused on development of kinase inhibitor therapeutics to treat a variety of human diseases.The SEC 10K submission for 2013 indicates that the company is a "biopharmaceutical" company, which implies that they are primarily developing biopharmaceuticals; however, their lead product is a small molecule therapeutic, calling into question the term used in the SEC submission. , the company was based in San Diego, California, and consisted of a single facility. Ambit made an initial public offering in May 2013, and was listed on the NASDAQ exchange under the symbol "AMBI". Ambit was acquired by Daiichi Sankyo in 2014 and is no longer traded on the NASDAQ exchange. Products , three products were under development, of which quizartinib was their lead drug candidate. Business model In June 2010, Ambit completed a Series D-2 round of equity financing, raising $30 million in new capital. The investor syndicate was led by Apposite Capital LLP a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Tyrosine Kinase
Receptor tyrosine kinases (RTKs) are the high- affinity cell surface receptors for many polypeptide growth factors, cytokines, and hormones. Of the 90 unique tyrosine kinase genes identified in the human genome, 58 encode receptor tyrosine kinase proteins. Receptor tyrosine kinases have been shown not only to be key regulators of normal cellular processes but also to have a critical role in the development and progression of many types of cancer. Mutations in receptor tyrosine kinases lead to activation of a series of signalling cascades which have numerous effects on protein expression. Receptor tyrosine kinases are part of the larger family of protein tyrosine kinases, encompassing the receptor tyrosine kinase proteins which contain a transmembrane domain, as well as the non-receptor tyrosine kinases which do not possess transmembrane domains. History The first RTKs to be discovered were EGF and NGF in the 1960s, but the classification of receptor tyrosine kinases was no ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Ureas
220 px, B vitamin, is a urea.">B_vitamins.html" ;"title="Biotin, a water-soluble B vitamins">B vitamin, is a urea. In chemistry, ureas are a class of organic compounds with the formula (R2N)2CO where R = H, alkyl, aryl, etc. Thus, in addition to describing the specific chemical compound urea ((H2N)2CO), urea is the name of a functional group that is found in many compounds and materials of both practical and theoretical interest. Generally ureas are colorless crystalline solids, which, owing to the presence of fewer hydrogen bonds, exhibit melting points lower than that of urea itself. Synthesis Ureas can be prepared many methods, but rarely by direct carbonation, which is the route to urea itself. Instead, methods can be classified according those that assemble the urea functionality and those that start with preformed urea. Assembly of N-substituted urea functionality Phosgenation entails the reaction of amines with phosgene, proceeding via the isocyanate (or carbamoyl ch ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Isoxazoles
Isoxazole is an electron-rich azole with an oxygen atom next to the nitrogen. It is also the class of compounds containing this ring. Isoxazolyl is the univalent radical derived from isoxazole. Occurrence Isoxazole rings are found in some natural products, such as ibotenic acid and muscimol. Synthesis Isoxazole can be synthesised via a variety of methods. Examples include via a 1,3-dipolar cycloaddition of nitrile oxides with alkynes; or the reaction of hydroxylamine with 1,3-diketones or derivatives of propiolic acid. Photochemistry The photolysis of isoxazole was first reported in 1966. Due to the weak N-O bond, the isoxazole ring tends to collapse under UV irradiation, rearranging to oxazole through azirine intermediate. Meanwhile, the azirine intermediate can react with nucleophiles, especially carboxylic acids. Given the photoreactions, isoxazole group is developed as a native photo-cross-linker for photoaffinity labeling and chemoproteomic studies. Pharmaceuticals and h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Receptor Tyrosine Kinase Inhibitors , a device for the reception of electromagnetic signals ...
Receptor may refer to: *Sensory receptor, in physiology, any structure which, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and responds to a neurotransmitter, or other substance **Cell surface receptor, a receptor on the outer surface of a cell membrane, that takes part in communication between the cell and the outside world **Nuclear receptor, a receptor found within cells that is responsible for sensing steroid and thyroid hormones and certain other molecules **Immune receptor, a receptor that occurs on the surface of immunocytes and binds to antigens *Receiver (radio) In radio communications, a radio receiver, also known as a receiver, a wireless, or simply a radio, is an electronic device that receives radio waves and converts the information carried by them to a usable form. It is used with an antenna. Th ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Experimental Cancer Drugs
An experiment is a procedure carried out to support or refute a hypothesis, or determine the efficacy or likelihood of something previously untried. Experiments provide insight into cause-and-effect by demonstrating what outcome occurs when a particular factor is manipulated. Experiments vary greatly in goal and scale but always rely on repeatable procedure and logical analysis of the results. There also exist natural experimental studies. A child may carry out basic experiments to understand how things fall to the ground, while teams of scientists may take years of systematic investigation to advance their understanding of a phenomenon. Experiments and other types of hands-on activities are very important to student learning in the science classroom. Experiments can raise test scores and help a student become more engaged and interested in the material they are learning, especially when used over time. Experiments can vary from personal and informal natural comparisons (e. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PDGFR
Platelet-derived growth factor receptors (PDGF-R) are cell surface tyrosine kinase receptors for members of the platelet-derived growth factor (PDGF) family. PDGF subunits -A and -B are important factors regulating cell proliferation, cellular differentiation, cell growth, development and many diseases including cancer. There are two forms of the PDGF-R, alpha and beta each encoded by a different gene. Depending on which growth factor is bound, PDGF-R homo- or heterodimerizes. Mechanism of action The PDGF family consists of PDGF-A, -B, -C and -D, which form either homo- or hetero dimers (PDGF-AA, -AB, -BB, -CC, -DD). The four PDGFs are inactive in their monomeric forms. The PDGFs bind to the protein tyrosine kinase receptors PDGF receptor-α and -β. These two receptor isoforms dimerize upon binding the PDGF dimer, leading to three possible receptor combinations, namely -αα, -ββ and -αβ. The extracellular region of the receptor consists of five immunoglobulin- ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stem Cell Factor Receptor
Proto-oncogene c-KIT is the gene encoding the receptor tyrosine kinase protein known as tyrosine-protein kinase KIT, CD117 (cluster of differentiation 117) or mast/stem cell growth factor receptor (SCFR). Multiple transcript variants encoding different isoforms have been found for this gene. KIT was first described by the German biochemist Axel Ullrich in 1987 as the cellular homolog of the feline sarcoma viral oncogene v-kit. Function KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT is a receptor tyrosine kinase type III, which binds to stem cell factor , also known as "steel factor" or "c-kit ligand". When this receptor binds to stem cell factor (SCF) it forms a dimer that activates its intrinsic tyrosine kinase activity, that in turn phosphorylates and activates signal transduction molecules that propagate the signal in the cell. After a ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
KIT (gene)
Proto-oncogene c-KIT is the gene encoding the receptor tyrosine kinase protein known as tyrosine-protein kinase KIT, CD117 ( cluster of differentiation 117) or mast/stem cell growth factor receptor (SCFR). Multiple transcript variants encoding different isoforms have been found for this gene. KIT was first described by the German biochemist Axel Ullrich in 1987 as the cellular homolog of the feline sarcoma viral oncogene v-kit. Function KIT is a cytokine receptor expressed on the surface of hematopoietic stem cells as well as other cell types. Altered forms of this receptor may be associated with some types of cancer. KIT is a receptor tyrosine kinase type III, which binds to stem cell factor , also known as "steel factor" or "c-kit ligand". When this receptor binds to stem cell factor (SCF) it forms a dimer that activates its intrinsic tyrosine kinase activity, that in turn phosphorylates and activates signal transduction molecules that propagate the signal in the cell. After ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
FMS (gene)
FMS may refer to: Organizations Education * Faculty of Management Studies, one of several schools * Farmington Municipal Schools, in New Mexico, United States * Florida Military School, United States * Fuchs Mizrachi School, in Beachwood, Ohio, United States Government * Federal Magistrates Service, now the Federal Magistrates' Court of Australia * Federal Migration Service (Russian Federation) * Federated Malay States, a historical British protectorate in then British Malaya * Fiji Meteorological Service * Financial Management Service, a bureau of the United States Treasury Department * Foreign Military Sales, a program of the United States Department of Defense Other organizations * Fatima Memorial System, a healthcare complex in Lahore, Pakistan * Finnish Missionary Society * Fisichella Motor Sport, an Italian motor racing team * Marist Brothers (Latin: '), a Catholic religious order Science and technology Health and medicine * False memory syndrome * Fibromyalgia sy ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
