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ARQ197
Tivantinib (ARQ197; by Arqule, Inc.) is an experimental small molecule anti-cancer drug. It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase ''in vitro''. (MET is a growth factor receptor.) Tivantinib is being tested clinically as a highly selective MET inhibitor. However, the mechanism of action of tivantinib is still unclear. Tivantinib displays cytotoxic activity via molecular mechanisms that are independent from its ability to bind MET, notably tubulin binding, which likely underlies tivantinib cytotoxicity. Possible applications include non-small-cell lung carcinoma, hepatocellular carcinoma, and oesophageal cancer. In 2017, it was announced that a phase III clinical trial for advanced hepatocellular carcinoma Hepatocellular carcinoma (HCC) is the most common type of primary liver cancer in adults and is currently the most common cause of death in people with cirrhosis. HCC is the third leading cause of cancer-related deaths worldwide. It oc ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MET Inhibitor
c-Met inhibitors are a class of small molecules that inhibit the enzymatic activity of the c-Met tyrosine kinase, the receptor of hepatocyte growth factor/scatter factor (HGF/SF). These inhibitors may have therapeutic application in the treatment of various types of cancers. Many c-Met inhibitors are currently in clinical trials. Crizotinib and cabozantinib were the first to be approved by the U.S. FDA. Crizotinib received accelerated approval in 2011 for the treatment of patients with locally advanced or metastatic non-small cell lung cancer, while cabozantinib was approved in 2012 for the treatment of medullary thyroid cancer and it has also started clinical trials for the treatment of several other types of cancer. c-Met stimulates cell scattering, invasion, protection from apoptosis and angiogenesis. c-Met is a receptor tyrosine kinase, which can cause a wide variety of different cancers, such as renal, gastric and small cell lung carcinomas, central nervous system tumours, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
MET Kinase
c-Met, also called tyrosine-protein kinase Met or hepatocyte growth factor receptor (HGFR), is a protein that in humans is encoded by the ''MET'' gene. The protein possesses tyrosine kinase activity. The primary single chain precursor protein is post-translationally cleaved to produce the alpha and beta subunits, which are disulfide linked to form the mature receptor. MET is a single pass tyrosine kinase receptor essential for embryonic development, organogenesis and wound healing. Hepatocyte growth factor, Hepatocyte growth factor/Scatter Factor (HGF/SF) and its splicing isoform (NK1, NK2) are the only known ligands of the MET receptor. MET is normally expressed by cells of epithelium, epithelial origin, while expression of HGF/SF is restricted to cells of mesenchymal stem cell, mesenchymal origin. When HGF/SF binds its cognate receptor MET it induces its dimerization through a not yet completely understood mechanism leading to its activation. Abnormal MET activation in cancer c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bisindolylmaleimide
Bisindolylmaleimide is an organic compound that forms the core chemical structure of a variety of biologically active compounds. This core structure includes a central maleimide group with two indole groups attached. Examples of bisindolylmaleimide derivatives include: * Bisindolylmaleimide I * Enzastaurin * Ruboxistaurin * Tivantinib Tivantinib (ARQ197; by Arqule, Inc.) is an experimental small molecule anti-cancer drug. It is a bisindolylmaleimide that binds to the dephosphorylated MET kinase ''in vitro''. (MET is a growth factor receptor.) Tivantinib is being tested clinica ... References External links {{heterocyclic-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
In Vitro
''In vitro'' (meaning in glass, or ''in the glass'') studies are performed with microorganisms, cells, or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in biology and its subdisciplines are traditionally done in labware such as test tubes, flasks, Petri dishes, and microtiter plates. Studies conducted using components of an organism that have been isolated from their usual biological surroundings permit a more detailed or more convenient analysis than can be done with whole organisms; however, results obtained from ''in vitro'' experiments may not fully or accurately predict the effects on a whole organism. In contrast to ''in vitro'' experiments, ''in vivo'' studies are those conducted in living organisms, including humans, and whole plants. Definition ''In vitro'' ( la, in glass; often not italicized in English usage) studies are conducted using components of an organism that have been isolated fro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Growth Factor Receptor
A growth factor receptor is a receptor that binds to a growth factor. Growth factor receptors are the first stop in cells where the signaling cascade for cell differentiation and proliferation begins. Growth factors, which are ligands that bind to the receptor are the initial step to activating the growth factor receptors and tells the cell to grow and/or divide. These receptors may use the JAK/STAT, MAP kinase, and PI3 kinase pathways. A majority of growth factor receptors consists of receptor tyrosine kinases (RTKs). There are 3 dominant receptor types that are exclusive to research : the epidermal growth factor receptor, the neurotrophin receptor, and the insulin receptors. All growth factor receptors are membrane bound and composed of 3 general protein domains: extracellular, transmembrane, and cytoplasmic. The extracellular domain region is where a ligand may bind, usually with very high specificity. In RTKs, the binding of a ligand to the extracellular ligand binding sit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Non-small-cell Lung Carcinoma
Non-small-cell lung cancer (NSCLC) is any type of epithelial lung cancer other than small-cell lung carcinoma (SCLC). NSCLC accounts for about 85% of all lung cancers. As a class, NSCLCs are relatively insensitive to chemotherapy, compared to small-cell carcinoma. When possible, they are primarily treated by surgical resection with curative intent, although chemotherapy has been used increasingly both preoperatively (Neoadjuvant therapy, neoadjuvant chemotherapy) and postoperatively (Adjuvant therapy, adjuvant chemotherapy). Types The most common types of NSCLC are squamous-cell carcinoma, large-cell carcinoma, and adenocarcinoma, but several other types occur less frequently. A few of the less common types are pleomorphic, carcinoid tumor, salivary gland carcinoma, and unclassified carcinoma. All types can occur in unusual histologic variants and as mixed cell-type combinations. Nonsquamous-cell carcinoma almost occupies the half of NSCLC. In the tissue classification, the cent ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hepatocellular Carcinoma
Hepatocellular carcinoma (HCC) is the most common type of primary liver cancer in adults and is currently the most common cause of death in people with cirrhosis. HCC is the third leading cause of cancer-related deaths worldwide. It occurs in the setting of chronic liver inflammation, and is most closely linked to chronic viral hepatitis infection (hepatitis B or C) or exposure to toxins such as alcohol, aflatoxin, or pyrrolizidine alkaloids. Certain diseases, such as hemochromatosis and alpha 1-antitrypsin deficiency, markedly increase the risk of developing HCC. Metabolic syndrome and NASH are also increasingly recognized as risk factors for HCC. As with any cancer, the treatment and prognosis of HCC vary depending on the specifics of tumor histology, size, how far the cancer has spread, and overall health. The vast majority of HCC cases and the lowest survival rates after treatment occur in Asia and sub-Saharan Africa, in countries where hepatitis B infection is endem ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oesophageal Cancer
Esophageal cancer is cancer arising from the esophagus—the food pipe that runs between the throat and the stomach. Symptoms often include difficulty in swallowing and weight loss. Other symptoms may include pain when swallowing, a hoarse voice, enlarged lymph nodes ("glands") around the collarbone, a dry cough, and possibly coughing up or vomiting blood. The two main sub-types of the disease are esophageal squamous-cell carcinoma (often abbreviated to ESCC), which is more common in the developing world, and esophageal adenocarcinoma (EAC), which is more common in the developed world. A number of less common types also occur. Squamous-cell carcinoma arises from the epithelial cells that line the esophagus. Adenocarcinoma arises from glandular cells present in the lower third of the esophagus, often where they have already transformed to intestinal cell type (a condition known as Barrett's esophagus). Causes of the squamous-cell type include tobacco, alcohol, very hot drinks, ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Intracellular Chemotherapeutic Agents
This glossary of biology terms is a list of definitions of fundamental terms and concepts used in biology, the study of life and of living organisms. It is intended as introductory material for novices; for more specific and technical definitions from sub-disciplines and related fields, see Glossary of genetics, Glossary of evolutionary biology, Glossary of ecology, and Glossary of scientific naming, or any of the organism-specific glossaries in :Glossaries of biology. A B C D E ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Growth Factor Receptor Modulators
Growth may refer to: Biology * Auxology, the study of all aspects of human physical growth * Bacterial growth * Cell growth * Growth hormone, a peptide hormone that stimulates growth * Human development (biology) * Plant growth * Secondary growth, growth that thickens woody plants Economics * Economic growth, the increase in the inflation-adjusted market value of the goods and services * Growth investing, a style of investment strategy focused on capital appreciation Mathematics * Exponential growth, also called geometric growth * Hyperbolic growth * Linear growth, refers to two distinct but related notions * Logistic growth, characterized as an S curve Social science * Developmental psychology * Erikson's stages of psychosocial development * Human development (humanity) * Personal development * Population growth Other uses * ''Growth'' (film), a 2010 American horror film * Izaugsme (''Growth''), a Latvian political party * ''Grown'' (album), by 2PM See also * Grow (disamb ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
