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Src Inhibitor
Src inhibitor is a class of inhibitors that targets the Src kinase family of tyrosine kinase, which is transcribed by the Src proto-oncogene (short for "sarcoma gene") that potentially induce malignant transformations of certain cells. Because of the crucial position of the Src kinase in cells, Src inhibitors are potential antineoplastic agents for e.g. pancreatic cancer, breast cancer and stomach cancer Examples * KX2-391 is an oral src inhibitor and the first clinical inhibitor with GI50 of 9–60 nM in cancer cell lines. * Bosutinib has been developed for the treatment of chronic myelogenous leukemia by Pfizer. * Saracatinib, the first Src inhibitor to show inhibition of the Src pathway in human tumor tissue, has anti-tumor activity alone or in combination with chemotherapeutic agents. * PP1, PP2 (kinase inhibitor) are both inhibitors of Lck and FynT. * Dasatinib Dasatinib, sold under the brand name Sprycel among others, is a targeted therapy medication used to treat c ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
KX2-391
KX and variants may refer to: Businesses and brands * Pentax KX, a 35mm film SLR camera model * Pentax K-x, a digital SLR camera model * Cayman Airways (IATA code KX) * KX Television, a network of four CBS affiliates under flagship KXMC-TV * Kx Systems, a software company focused on real-time analytics * KX 91.5. Philippines, a brand name for DXKX Other uses * Family Kx, a large group of the New Testament manuscripts * Kings Cross railway station, London * k͡x, symbol for the voiceless velar affricate The voiceless velar affricate is a type of consonantal sound, used in some spoken languages. The symbols in the International Phonetic Alphabet that represents this sound are and , and the equivalent X-SAMPA symbol is k_x. The tie bar may be omi ... in the International Phonetic Alphabet See also * 9945 Karinaxavier or 1990 KX, an asteroid {{disambig ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bosutinib
Bosutinib (rINN/USAN; codenamed SKI-606, marketed under the trade name Bosulif) is a small molecule BCR-ABL and src tyrosine kinase inhibitor used for the treatment of chronic myelogenous leukemia. Originally synthesized by Wyeth, it is being developed by Pfizer. Mechanism It is an ATP-competitive Bcr-Abl tyrosine-kinase inhibitor with an additional inhibitory effect on Src family kinases (including Src, Lyn and Hck). It has also shown activity against the receptors for platelet derived growth factor and vascular endothelial growth factor. Bosutinib inhibited 16 of 18 imatinib-resistant forms of Bcr-Abl expressed in murine myeloid cell lines, but did not inhibit T315I and V299L mutant cells. Bosutinib is metabolized through CYP3A4. Medical uses Bosutinib received US FDA and EU European Medicines Agency approval in September 2012, and March 2013, respectively for the treatment of adults with Philadelphia chromosome The Philadelphia chromosome or Philadelphia translocat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Cancer Research
''Clinical Cancer Research'' is a peer-reviewed medical journal on oncology, including the cellular and molecular characterization, prevention, diagnosis, and therapy of human cancer, medical and hematological oncology, radiation therapy, pediatric oncology, pathology, surgical oncology, and clinical genetics. The applications of the disciplines of pharmacology, immunology, cell biology, and molecular genetics to intervention in human cancer are also included. One of the main interests of ''Clinical Cancer Research'' is on clinical trials that evaluate new treatments together with research on pharmacology and molecular alterations or biomarkers that predict response or resistance to treatment. Another priority for ''Clinical Cancer Research'' is laboratory and animal studies of new drugs as well as molecule-targeted agents with the potential to lead to clinical trials, and studies of targetable mechanisms of oncogenesis, progression of the malignant phenotype, and metastatic disease. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Dasatinib
Dasatinib, sold under the brand name Sprycel among others, is a targeted therapy medication used to treat certain cases of chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL). Specifically it is used to treat cases that are Philadelphia chromosome-positive (Ph+). It is taken by mouth. Common adverse effects include low white blood cells, low blood platelets, anemia, swelling, rash, and diarrhea. Severe adverse effects may include bleeding, pulmonary edema, heart failure, and prolonged QT syndrome. Use during pregnancy may result in harm to the baby. It is a tyrosine-kinase inhibitor and works by blocking a number of tyrosine kinases such as Bcr-Abl and the Src kinase family. Dasatinib was approved for medical use in the United States and in the European Union in 2006. It is on the World Health Organization's List of Essential Medicines. Medical uses Dasatinib is used to treat people with chronic myeloid leukemia and people with acute lymphoblastic le ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PP2 (kinase Inhibitor)
PP2 is a substance that has frequently been used in cancer research as a "selective" inhibitor for Src-family kinases. It strongly inhibits the kinases Lck ( IC50=4 nM), Fyn (5 nM) and Hck (5 nM), shows weaker inhibition of EGFR (480 nM) and practically no inhibition of ZAP-70 (100 μM) and JAK2 Janus kinase 2 (commonly called JAK2) is a non-receptor tyrosine kinase. It is a member of the Janus kinase family and has been implicated in signaling by members of the type II cytokine receptor family (e.g. interferon receptors), the GM-CSF rec ... (50 μM). Despite its extensive use as a Src-selective inhibitor, recent research has shown that PP2 is non-selective and inhibits many other kinases with similar affinities. References Protein kinase inhibitors Pyrazolopyrimidines Chloroarenes Aromatic amines {{biochemistry-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
PP1 Chemical Structure
Protein phosphatase 1 (PP1) belongs to a certain class of phosphatases known as protein serine/threonine phosphatases. This type of phosphatase includes metal-dependent protein phosphatases (PPMs) and aspartate-based phosphatases. PP1 has been found to be important in the control of glycogen metabolism, muscle contraction, cell progression, neuronal activities, splicing of RNA, mitosis, cell division, apoptosis, protein synthesis, and regulation of membrane receptors and channels. Structure Each PP1 enzyme contains both a catalytic subunit and at least one regulatory subunit. The catalytic subunit consists of a 30-kD single-domain protein that can form complexes with other regulatory subunits. The catalytic subunit is highly conserved among all eukaryotes, thus suggesting a common catalytic mechanism. The catalytic subunit can form complexes with various regulatory subunits. These regulatory subunits play an important role in substrate specificity as well as compartmentalizatio ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Saracatinib
Saracatinib (AZD-0530) is an experimental drug being developed by AstraZeneca. It acts as a dual kinase inhibitor, with selective actions as a Src inhibitor and a Bcr-Abl tyrosine-kinase inhibitor. It was originally under development for the treatment of cancer, but while it appeared promising in animal studies and was well tolerated in humans, it failed to show sufficient efficacy in cancer patients and was ultimately not developed further for this application. However, saracatinib has subsequently been researched for other applications such as Alzheimer's disease. AZD0530 is an inhibitor of Src and Abl family kinases1. It has been developed as treatment for malignancies because these kinases play a role in tumor invasion and proliferation. However, the Src family kinases (SFKs) are highly expressed in brain and have major effects on synaptic plasticity2. Moreover, the investigators have recently shown that a specific SFK, namely Fyn, is aberrantly activated by specific conformat ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Pfizer
Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfizer (1824–1906) and his cousin Charles F. Erhart (1821–1891). Pfizer develops and produces medicines and vaccines for immunology, oncology, cardiology, endocrinology, and neurology. The company has several blockbuster drugs or products that each generate more than billion in annual revenues. In 2020, 52% of the company's revenues came from the United States, 6% came from each of China and Japan, and 36% came from other countries. Pfizer was a component of the Dow Jones Industrial Average stock market index from 2004 to August 2020. The company ranks 64th on the Fortune 500 and 49th on the Forbes Global 2000. History 1849–1950: Early history Pfizer was founded in 1849 by Charles Pfizer and Charles F. Erhart, two cousins who had i ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Leukemia
Leukemia ( also spelled leukaemia and pronounced ) is a group of blood cancers that usually begin in the bone marrow and result in high numbers of abnormal blood cells. These blood cells are not fully developed and are called ''blasts'' or ''leukemia cells''. Symptoms may include bleeding and bruising, bone pain, fatigue, fever, and an increased risk of infections. These symptoms occur due to a lack of normal blood cells. Diagnosis is typically made by blood tests or bone marrow biopsy. The exact cause of leukemia is unknown. A combination of genetic factors and environmental (non-inherited) factors are believed to play a role. Risk factors include smoking, ionizing radiation, petrochemicals (such as benzene), prior chemotherapy, and Down syndrome. People with a family history of leukemia are also at higher risk. There are four main types of leukemia— acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML), chronic lymphocytic leukemia (CLL) and chronic myeloi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Frontiers In Pharmacology
Frontiers Media SA is a publisher of peer-reviewed, open access, scientific journals currently active in science, technology, and medicine. It was founded in 2007 by Kamila and Henry Markram, and has since expanded to other academic fields. Frontiers is based in Lausanne, Switzerland, with other offices in London, Madrid, Seattle and Brussels. In 2022, Frontiers employed more than 1,400 people, across 14 countries. All Frontiers journals are published under a Creative Commons Attribution License. As of 2022, Frontiers publishes over 185 academic journals, including 48 journals indexed within the Science Citation Index Expanded, and 4 journals indexed within the Social Sciences Citation Index, with a total of 51 journals ranked with an impact factor. Frontiers journals are included in the Directory of Open Access Journals (DOAJ). Frontiers is also a member of the Open Access Scholarly Publishers Association (OASPA), a participating publisher and supporter of the Initiative for O ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Src Kinase Family
Src kinase family is a family of non-receptor tyrosine kinases that includes nine members: Src, Yes, Fyn, and Fgr, forming the SrcA subfamily, Lck, Hck, Blk, and Lyn in the SrcB subfamily, and Frk in its own subfamily. Frk has homologs in invertebrates such as flies and worms, and Src homologs exist in organisms as diverse as unicellular choanoflagellates, but the SrcA and SrcB subfamilies are specific to vertebrates. Src family kinases contain six conserved domains: a N-terminal myristoylated segment, a SH2 domain, a SH3 domain, a linker region, a tyrosine kinase domain, and C-terminal tail. Src family kinases interact with many cellular cytosolic, nuclear and membrane proteins, modifying these proteins by phosphorylation of tyrosine residues. A number of substrates have been discovered for these enzymes. Deregulation, including constitutive activation or over expression, may contribute to the progression of cellular transformation and oncogenic activity. Structure S ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Stomach Cancer
Stomach cancer, also known as gastric cancer, is a cancer that develops from the lining of the stomach. Most cases of stomach cancers are gastric carcinomas, which can be divided into a number of subtypes, including gastric adenocarcinomas. Lymphomas and mesenchymal tumors may also develop in the stomach. Early symptoms may include heartburn, upper abdominal pain, nausea, and loss of appetite. Later signs and symptoms may include weight loss, yellowing of the skin and whites of the eyes, vomiting, difficulty swallowing, and blood in the stool, among others. The cancer may spread from the stomach to other parts of the body, particularly the liver, lungs, bones, lining of the abdomen, and lymph nodes. The most common cause is infection by the bacterium ''Helicobacter pylori'', which accounts for more than 60% of cases. Certain types of ''H. pylori'' have greater risks than others. Smoking, dietary factors such as pickled vegetables and obesity are other risk factors. About 10% ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
