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Aurora Inhibitor
Aurora kinase inhibitors are a putative drug class for treating cancer. The Aurora kinase enzymes could be potential targets for novel small-molecule enzyme inhibitors. Aurora kinases regulate cell cycle transit from G2 through cytokinesis, and thus are targets in cancer therapy. There are three mammalian aurora kinase genes, encoding aurora A, B and C. Intense investigation has focused on aurora A and B as they appear to play a role in oncogenesis with aurora A identified as a low penetrance tumor susceptibility gene in mice and humans. Drug development A new approach to inhibiting cancer growth that shows great promise for structure-based drug development is targeting enzymes central to cellular mitosis. Aurora kinases, so named because the scattered mitotic spindles generated by mutant forms resemble the Aurora Borealis, have gained a great deal of attention as possible anticancer drug targets. The Aurora enzymes are particularly significant because they are involved in a dir ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Oncogenic
Carcinogenesis, also called oncogenesis or tumorigenesis, is the formation of a cancer, whereby normal cells are transformed into cancer cells. The process is characterized by changes at the cellular, genetic, and epigenetic levels and abnormal cell division. Cell division is a physiological process that occurs in almost all tissues and under a variety of circumstances. Normally, the balance between proliferation and programmed cell death, in the form of apoptosis, is maintained to ensure the integrity of tissues and organs. According to the prevailing accepted theory of carcinogenesis, the somatic mutation theory, mutations in DNA and epimutations that lead to cancer disrupt these orderly processes by interfering with the programming regulating the processes, upsetting the normal balance between proliferation and cell death. This results in uncontrolled cell division and the evolution of those cells by natural selection in the body. Only certain mutations lead to can ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Activation Loop
In molecular biology, an intrinsically disordered protein (IDP) is a protein that lacks a fixed or ordered three-dimensional structure, typically in the absence of its macromolecular interaction partners, such as other proteins or RNA. IDPs range from fully unstructured to partially structured and include random coil, molten globule-like aggregates, or flexible linkers in large multi-domain proteins. They are sometimes considered as a separate class of proteins along with globular, fibrous and membrane proteins. IDPs are a very large and functionally important class of proteins and their discovery has disproved the idea that three-dimensional structures of proteins must be fixed to accomplish their biological functions. For example, IDPs have been identified to participate in weak multivalent interactions that are highly cooperative and dynamic, lending them importance in DNA regulation and in cell signaling. Many IDPs can also adopt a fixed three-dimensional structure af ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hesperadin
Hesperadin is an aurora kinase inhibitor. The small molecule inhibits chromosome alignment and segregation by limiting the function of mitotic kinases Aurora B and Aurora A. Hesperadin causes cells to enter anaphase much faster, sometimes before the chromosomes are properly bi-oriented. Hesperadin, like other miotic inhibitors, limits and sometimes can stop the process of mitosis in cells. For this reason, some have considered hesperadin's potential as a cancer-preventing drug. Hesperadin works as an inhibitor Inhibitor or inhibition may refer to: In biology * Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity * Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ..., attaching to the active sites of Aurora A and Aurora B kinases. References Protein kinase inhibitors Sulfonamides 1-Piperidinyl compounds Lactams {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Merck & Co
Merck & Co., Inc. is an American multinational pharmaceutical company headquartered in Rahway, New Jersey, and is named for Merck Group, founded in Germany in 1668, of whom it was once the American arm. The company does business as Merck Sharp & Dohme or MSD outside the United States and Canada. Merck & Co. was originally established as the American affiliate of Merck Group in 1891. Merck develops and produces medicines, vaccines, biologic therapies and animal health products. It has multiple blockbuster drugs or products each with 2020 revenues including cancer immunotherapy, anti-diabetic medication and vaccines against HPV and chickenpox. The company is ranked 71st on the 2022 ''Fortune'' 500 and 87th on the 2022 ''Forbes'' Global 2000, both based on 2021 revenues. Products The company develops medicines, vaccines, biologic therapies and animal health products. In 2020, the company had 6 blockbuster drugs or products, each with over $1 billion in revenue: ''Keytrud ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Vertex Pharmaceuticals
Vertex Pharmaceuticals is an American biopharmaceutical company based in Boston, Massachusetts. It was one of the first biotech firms to use an explicit strategy of rational drug design rather than combinatorial chemistry. It maintains headquarters in South Boston, Massachusetts, and three research facilities, in San Diego, California, and Milton Park, near Oxford, England. History Vertex was founded in 1989 by Joshua Boger and Kevin J. Kinsella . to ''"transform the way serious diseases are treated."'' The company's beginnings were profiled by Barry Werth in the 1994 book, ''The Billion-Dollar Molecule''. His 2014 book, ''The Antidote: Inside the World of New Pharma'', chronicled the company's subsequent development over the next two decades. By 2004, its product pipeline focused on viral infections, inflammatory and autoimmune disorders, and cancer. In 2009, the company had about 1,800 employees, including 1,200 in the Boston area. By 2019 there were about 2,500 employee ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Clinical Trial
Clinical trials are prospective biomedical or behavioral research studies on human subject research, human participants designed to answer specific questions about biomedical or behavioral interventions, including new treatments (such as novel vaccines, pharmaceutical drug, drugs, medical nutrition therapy, dietary choices, dietary supplements, and medical devices) and known interventions that warrant further study and comparison. Clinical trials generate data on dosage, safety and efficacy. They are conducted only after they have received institutional review board, health authority/ethics committee approval in the country where approval of the therapy is sought. These authorities are responsible for vetting the risk/benefit ratio of the trial—their approval does not mean the therapy is 'safe' or effective, only that the trial may be conducted. Depending on product type and development stage, investigators initially enroll volunteers or patients into small Pilot experiment, pi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
VX-680
Tozasertib (VX-680) is an aurora inhibitor Aurora kinase inhibitors are a putative drug class for treating cancer. The Aurora kinase enzymes could be potential targets for novel small-molecule enzyme inhibitors. Aurora kinases regulate cell cycle transit from G2 through cytokinesis, and .... Protein kinase inhibitors Pyrimidines Thioethers Pyrazoles Piperazines Cyclopropanes {{antineoplastic-drug-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Hesperadin
Hesperadin is an aurora kinase inhibitor. The small molecule inhibits chromosome alignment and segregation by limiting the function of mitotic kinases Aurora B and Aurora A. Hesperadin causes cells to enter anaphase much faster, sometimes before the chromosomes are properly bi-oriented. Hesperadin, like other miotic inhibitors, limits and sometimes can stop the process of mitosis in cells. For this reason, some have considered hesperadin's potential as a cancer-preventing drug. Hesperadin works as an inhibitor Inhibitor or inhibition may refer to: In biology * Enzyme inhibitor, a substance that binds to an enzyme and decreases the enzyme's activity * Reuptake inhibitor, a substance that increases neurotransmission by blocking the reuptake of a neurotra ..., attaching to the active sites of Aurora A and Aurora B kinases. References Protein kinase inhibitors Sulfonamides 1-Piperidinyl compounds Lactams {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ZM447439
ZM447439 is an aurora inhibitor Aurora kinase inhibitors are a putative drug class for treating cancer. The Aurora kinase enzymes could be potential targets for novel small-molecule enzyme inhibitors. Aurora kinases regulate cell cycle transit from G2 through cytokinesis, and .... References {{pharma-stub Protein kinase inhibitors Quinazolines 4-Morpholinyl compounds Benzamides ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Breast Cancer
Breast cancer is cancer that develops from breast tissue. Signs of breast cancer may include a lump in the breast, a change in breast shape, dimpling of the skin, milk rejection, fluid coming from the nipple, a newly inverted nipple, or a red or scaly patch of skin. In those with distant spread of the disease, there may be bone pain, swollen lymph nodes, shortness of breath, or yellow skin. Risk factors for developing breast cancer include obesity, a lack of physical exercise, alcoholism, hormone replacement therapy during menopause, ionizing radiation, an early age at first menstruation, having children late in life or not at all, older age, having a prior history of breast cancer, and a family history of breast cancer. About 5–10% of cases are the result of a genetic predisposition inherited from a person's parents, including BRCA1 and BRCA2 among others. Breast cancer most commonly develops in cells from the lining of milk ducts and the lobules that supp ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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