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Halichondrin B
Halichondrin B is a polyether macrolide originally isolated from the marine sponge ''Halichondria okadai'' by Hirata and Uemura in 1986. In the same report, these authors also reported the exquisite anticancer activity of halichondrin B against murine cancer cells both in culture and in ''in vivo'' studies. Halichondrin B was highly prioritized for development as a novel anticancer therapeutic by the United States National Cancer Institute and, in 1991, was the original test case for identification of mechanism of action (in this case, tubulin-targeted mitotic inhibitor) by NCI's then-brand-new " 60-cell line screen" The complete chemical synthesis of halichondrin B was achieved by Yoshito Kishi and colleagues at Harvard University in 1992, an achievement that ultimately enabled the discovery and development of the structurally simplified and pharmaceutically optimized analog eribulin (E7389, ER-086526, NSC-707389). Eribulin was approved by the U.S. Food and Drug Administration ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Polyether
In organic chemistry, ethers are a class of compounds that contain an ether group—an oxygen atom connected to two alkyl or aryl groups. They have the general formula , where R and R′ represent the alkyl or aryl groups. Ethers can again be classified into two varieties: if the alkyl or aryl groups are the same on both sides of the oxygen atom, then it is a simple or symmetrical ether, whereas if they are different, the ethers are called mixed or unsymmetrical ethers. A typical example of the first group is the solvent and anaesthetic diethyl ether, commonly referred to simply as "ether" (). Ethers are common in organic chemistry and even more prevalent in biochemistry, as they are common linkages in carbohydrates and lignin. Structure and bonding Ethers feature bent C–O–C linkages. In dimethyl ether, the bond angle is 111° and C–O distances are 141 pm. The barrier to rotation about the C–O bonds is low. The bonding of oxygen in ethers, alcohols, and water ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Macrolide
The Macrolides are a class of natural products that consist of a large macrocyclic lactone ring to which one or more deoxy sugars, usually cladinose and desosamine, may be attached. The lactone rings are usually 14-, 15-, or 16-membered. Macrolides belong to the polyketide class of natural products. Some macrolides have antibiotic or antifungal activity and are used as pharmaceutical drugs. Rapamycin is also a macrolide and was originally developed as an antifungal, but is now used as an immunosuppressant drug and is being investigated as a potential longevity therapeutic. Macrolides are bacteriostatic in that they suppress or inhibit bacterial growth rather than killing bacteria completely. Definition In general, any macrocyclic lactone having greater than 8-membered rings are candidates for this class. The macrocycle may contain amino nitrogen, amide nitrogen (but should be differentiated from cyclopeptides), an oxazole ring, or a thiazole ring. Benzene rings are e ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Halichondria
''Halichondria'' is a genus of sea sponges belonging to the family Halichondriidae. These are massive, amorphous sponges with clearly separated inner and outer skeletons consisting of bundles of spicules arranged in a seemingly random pattern. This genus of sponges became important through the discovery of cell division limiting properties of the extract Halichondrin B, which inhibits cell mitosis. The drug Eribulin, a related compound and an inhibitor of microtubule function, has become an important chemotherapy treatment for certain types of cancer. Species The following species are recognised in the genus ''Halichondria'': * Subgenus ''Eumastia'' Schmidt, 1870 ** '' Halichondria attenuata'' (Topsent, 1915) ** '' Halichondria maraensis'' Kim & Sim, 2009 ** '' Halichondria schmidti'' Dendy, 1895 ** '' Halichondria sitiens'' (Schmidt, 1870) * Subgenus ''Halichondria'' Fleming, 1828 ** '' Halichondria adelpha'' de Laubenfels, 1954 ** '' Halichondria agglomerans'' Cabioch, 1968 ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Anticancer
An anticarcinogen (also known as a carcinopreventive agent) is a substance that counteracts the effects of a carcinogen or inhibits the development of cancer. Anticarcinogens are different from anticarcinoma agents (also known as anticancer or anti-neoplastic agents) in that anticarcinoma agents are used to selectively destroy or inhibit cancer cells ''after'' cancer has developed. Interest in anticarcinogens is motivated primarily by the principle that it is preferable to prevent disease ( preventive medicine) than to have to treat it ( rescue medicine). In theory, anticarcinogens may act via different mechanisms including enhancement of natural defences against cancer, deactivation of carcinogens, and blocking the mechanisms by which carcinogens act (such as free radical damage to DNA). Confirmation that a substance possesses anticarcinogenic activity requires extensive '' in vitro'', '' in vivo'', and clinical investigation. Health claims for anticarcinogens are regulated ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
National Cancer Institute
The National Cancer Institute (NCI) coordinates the United States National Cancer Program and is part of the National Institutes of Health (NIH), which is one of eleven agencies that are part of the U.S. Department of Health and Human Services. The NCI conducts and supports research, training, health information dissemination, and other activities related to the causes, prevention, diagnosis, and treatment of cancer; the supportive care of cancer patients and their families; and cancer survivorship. NCI is the oldest and has the largest budget and research program of the 27 institutes and centers of the NIH ($6.9 billion in 2020). It fulfills the majority of its mission via an extramural program that provides grants for cancer research. Additionally, the National Cancer Institute has intramural research programs in Bethesda, Maryland, and at the Frederick National Laboratory for Cancer Research at Fort Detrick in Frederick, Maryland. The NCI receives more than in funding ea ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tubulin
Tubulin in molecular biology can refer either to the tubulin protein superfamily of globular proteins, or one of the member proteins of that superfamily. α- and β-tubulins polymerize into microtubules, a major component of the eukaryotic cytoskeleton. Microtubules function in many essential cellular processes, including mitosis. Tubulin-binding drugs kill cancerous cells by inhibiting microtubule dynamics, which are required for DNA segregation and therefore cell division. In eukaryotes, there are six members of the tubulin superfamily, although not all are present in all species.Turk E, Wills AA, Kwon T, Sedzinski J, Wallingford JB, Stearns "Zeta-Tubulin Is a Member of a Conserved Tubulin Module and Is a Component of the Centriolar Basal Foot in Multiciliated Cells"Current Biology (2015) 25:2177-2183. Both α and β tubulins have a mass of around 50 kDa and are thus in a similar range compared to actin (with a mass of ~42 kDa). In contrast, tubulin polymers (microtubules) t ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Mitotic Inhibitor
A mitotic inhibitor is a drug that inhibits mitosis, or cell division. These drugs disrupt microtubules, which are structures that pull the chromosomes apart when a cell divides. Mitotic inhibitors are used in cancer treatment, because cancer cells are able to grow and eventually spread through the body (metastasize) through continuous mitotic division. Thus, cancer cells are more sensitive to inhibition of mitosis than normal cells. Mitotic inhibitors are also used in cytogenetics (the study of chromosomes), where they stop cell division at a stage where chromosomes can be easily examined. Mitotic inhibitors are derived from natural substances such as plant alkaloids, and prevent cells from undergoing mitosis by disrupting microtubule polymerization, thus preventing cancerous growth. Microtubules are long, ropelike proteins that extend through the cell and move cellular components around. Microtubules are long polymers made of smaller units (monomers) of the protein tubulin. Micro ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
NCI-60
The NCI-60 cancer cell line panel is a group of 60 human cancer cell lines used by the National Cancer Institute (NCI) for the screening of compounds to detect potential anticancer activity. Purpose The screening procedure is called the NCI-60 Human Tumor Cell Lines Screen, and it is one of the Discovery & Development Services of NCI's Developmental Therapeutics Program (DTP). The screening rates for each cell line the cytostatic and cytotoxic impact of tested substances. Due to the diversity of the cell lines, it is possible to compare tested compounds by their effect patterns, high correlation potentially corresponding to similar effect mechanisms. An automated comparison against a database of more than 88,000 pure compounds and more than 34,000 crude extracts () is provided by the COMPARE tool, which shows a list of substances ranked by the Pearson correlation coefficients for a given test substance. The same panel is used in the Molecular Target Program for the ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Yoshito Kishi
is a Japanese chemist who is the Morris Loeb Professor of Chemistry at Harvard University. He is known for his contributions to the sciences of organic synthesis and total synthesis. Kishi was born in Nagoya, Japan and attended Nagoya University, where he obtained both his BS and PhD degrees. He was a postdoctoral research fellow at Harvard University where he worked with Robert Burns Woodward. From 1966 through 1974, he was a professor of chemistry at Nagoya University. Since 1974, Kishi has been a professor of chemistry at Harvard University. Kishi's research has focused on the total synthesis of complex natural products. The accomplishments of his research group include the total syntheses of palytoxin, mycolactones, halichondrins, saxitoxin, tetrodotoxin, geldanamycin, batrachotoxin and many others. Kishi has also contributed to the development of new chemical reactions including the Nozaki–Hiyama–Kishi reaction. Recognition *1999 Imperial Prize of the Japan A ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Harvard University
Harvard University is a private Ivy League research university in Cambridge, Massachusetts. Founded in 1636 as Harvard College and named for its first benefactor, the Puritan clergyman John Harvard, it is the oldest institution of higher learning in the United States and one of the most prestigious and highly ranked universities in the world. The university is composed of ten academic faculties plus Harvard Radcliffe Institute. The Faculty of Arts and Sciences offers study in a wide range of undergraduate and graduate academic disciplines, and other faculties offer only graduate degrees, including professional degrees. Harvard has three main campuses: the Cambridge campus centered on Harvard Yard; an adjoining campus immediately across Charles River in the Allston neighborhood of Boston; and the medical campus in Boston's Longwood Medical Area. Harvard's endowment is valued at $50.9 billion, making it the wealthiest academic institution in the world. Endow ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eribulin
Eribulin, sold under the brand name Halaven, is an anticancer medication used to treat breast cancer and liposarcoma. The most common side effects include fatigue, nausea, hair loss (alopecia), constipation, certain nerve damage causing weakness or numbness in the hands and feet (peripheral neuropathy), abdominal pain and fever (pyrexia). Eribulin may also cause low levels of infection-fighting white blood cells (neutropenia) or decreased levels of potassium or calcium. Approvals and indications Eribulin was approved for medical use in the European Union in March 2011, and it is indicated for the treatment of: * people with locally advanced or metastatic breast cancer who have progressed after at least one chemotherapeutic regimens for advanced disease. Prior therapy should have included an anthracycline and a taxane unless the people were not suitable for these treatments. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provide ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Eribulin
Eribulin, sold under the brand name Halaven, is an anticancer medication used to treat breast cancer and liposarcoma. The most common side effects include fatigue, nausea, hair loss (alopecia), constipation, certain nerve damage causing weakness or numbness in the hands and feet (peripheral neuropathy), abdominal pain and fever (pyrexia). Eribulin may also cause low levels of infection-fighting white blood cells (neutropenia) or decreased levels of potassium or calcium. Approvals and indications Eribulin was approved for medical use in the European Union in March 2011, and it is indicated for the treatment of: * people with locally advanced or metastatic breast cancer who have progressed after at least one chemotherapeutic regimens for advanced disease. Prior therapy should have included an anthracycline and a taxane unless the people were not suitable for these treatments. Text was copied from this source which is © European Medicines Agency. Reproduction is authorized provide ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
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