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Bryostatins
Bryostatins are a group of macrolide lactones from the marine organism ''Bugula neritina'' that were first collected and provided to JL Hartwell’s anticancer drug discovery group at the National Cancer Institute (NCI) by Jack Rudloe. Bryostatins are potent modulators of protein kinase C. They have been studied in clinical trials as anti-cancer agents, as anti-AIDS/HIV agents and in people with Alzheimer's disease. Biological effects Bryostatin 1 is a potent modulator of protein kinase C (PKC). It showed activity in laboratory tests in cells and model animals, so it was brought into clinical trials. As of 2014 over thirty clinical trials had been conducted, using bryostatin alone and in combination with other agents, in both solid tumors and blood tumors; it did not show a good enough risk:benefit ratio to be advanced further. It showed enough promise in animal models of Alzheimer's disease that a Phase II trial was started by 2010; the trial was sponsored by the Blanchett ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bryostatin Biosynthetic Diagram
Bryostatins are a group of macrolide lactones from the marine organism ''Bugula neritina'' that were first collected and provided to JL Hartwell’s anticancer drug discovery group at the National Cancer Institute (NCI) by Jack Rudloe. Bryostatins are potent modulators of protein kinase C. They have been studied in clinical trials as anti-cancer agents, as anti-AIDS/HIV agents and in people with Alzheimer's disease. Biological effects Bryostatin 1 is a potent modulator of protein kinase C (PKC). It showed activity in laboratory tests in cells and model animals, so it was brought into clinical trials. As of 2014 over thirty clinical trials had been conducted, using bryostatin alone and in combination with other agents, in both solid tumors and blood tumors; it did not show a good enough risk:benefit ratio to be advanced further. It showed enough promise in animal models of Alzheimer's disease that a Phase II trial was started by 2010; the trial was sponsored by the Blanchett ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Bugula Neritina
''Bugula neritina'' ( commonly known as brown bryozoan or common bugula) is a cryptic species complex of sessile marine animal in the genus ''Bugula''.Gordon, D. (2015). Bugula neritina (Linnaeus, 1758). In: Bock, P.; Gordon, D. (2015) World List of Bryozoa. Accessed through: World Register of Marine Species at http://www.marinespecies.org/aphia.php?p=taxdetails&id=111158 on 2015-09-02 It is invasive with a cosmopolitan distribution. ''Bugula neritina'' is of interest from a drug discovery perspective because its bacterial symbiont, ''Candidatus'' Endobugula sertula, produces the bryostatins, a group of around twenty bioactive natural products. The bryostatins are under investigation for their therapeutic potential directed at cancer immunotherapy, treatment of Alzheimer's disease, and HIV/AIDS eradication, due to their low toxicity and antineoplastic activity. The draft whole genome of ''Bugula neritina'' has recently been sequenced. This adds to the growing number of geno ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Jack Rudloe
Jack Rudloe is a writer, naturalist, and environmental activist from Panacea, Florida, United States, who co-founded Gulf Specimen Marine Laboratory. Biography Jack Rudloe was born in Brooklyn, New York on February 17, 1943. At age 14, he moved to Carrabelle, Florida. His first work, "Experiments With Sensitive Plants, ''Cassia Nictitans''", was published in ''Scientific American'' while he was attending Tallahassee's Leon High School. He later enrolled in Florida State University, but left after only two months.Boyle Panacea For A Salty YankeeSports Illustrated The Vault, April 20, 1970, Retrieved March 14, 2015 According to Rudloe's first book, ''The Sea Brings Forth'', he was asked to leave FSU by the dean, who had decided Rudloe was not college material and advised that he should consider a trade instead. In spite of his premature departure from FSU, Rudloe was hired by marine biologist Dexter M. Easton of Harvard University to collect striped burrfish and bat fish. Thi ... [...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 exclude ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Lactone
Lactones are cyclic carboxylic esters, containing a 1-oxacycloalkan-2-one structure (), or analogues having unsaturation or heteroatoms replacing one or more carbon atoms of the ring. Lactones are formed by intramolecular esterification of the corresponding hydroxycarboxylic acids, which takes place spontaneously when the ring that is formed is five- or six-membered. Lactones with three- or four-membered rings (α-lactones and β-lactones) are very reactive, making their isolation difficult. Special methods are normally required for the laboratory synthesis of small-ring lactones as well as those that contain rings larger than six-membered. Nomenclature Lactones are usually named according to the precursor acid molecule (''aceto'' = 2 carbon atoms, ''propio'' = 3, ''butyro'' = 4, ''valero'' = 5, ''capro'' = 6, etc.), with a ''-lactone'' suffix and a Greek letter prefix that specifies the number of carbon atoms in the heterocycle — that is, the distance between the relevant -OH ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Protein Kinase C
In cell biology, Protein kinase C, commonly abbreviated to PKC (EC 2.7.11.13), is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins, or a member of this family. PKC enzymes in turn are activated by signals such as increases in the concentration of diacylglycerol (DAG) or calcium ions (Ca2+). Hence PKC enzymes play important roles in several signal transduction cascades. In biochemistry, the PKC family consists of fifteen isozymes in humans. They are divided into three subfamilies, based on their second messenger requirements: conventional (or classical), novel, and atypical. Conventional (c)PKCs contain the isoforms α, βI, βII, and γ. These require Ca2+, DAG, and a phospholipid such as phosphatidylserine for activation. Novel (n)PKCs include the δ, ε, η, and θ isoforms, and require DAG, but do not require Ca2+ for ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Cancer
Cancer is a group of diseases involving abnormal cell growth with the potential to invade or spread to other parts of the body. These contrast with benign tumors, which do not spread. Possible signs and symptoms include a lump, abnormal bleeding, prolonged cough, unexplained weight loss, and a change in bowel movements. While these symptoms may indicate cancer, they can also have other causes. Over 100 types of cancers affect humans. Tobacco use is the cause of about 22% of cancer deaths. Another 10% are due to obesity, poor diet, lack of physical activity or excessive drinking of alcohol. Other factors include certain infections, exposure to ionizing radiation, and environmental pollutants. In the developing world, 15% of cancers are due to infections such as ''Helicobacter pylori'', hepatitis B, hepatitis C, human papillomavirus infection, Epstein–Barr virus and human immunodeficiency virus (HIV). These factors act, at least partly, by changing the genes of ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
