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Monastrol
Monastrol is a cell-permeable small molecule inhibitor discovered by Thomas U. Mayer in the lab of Tim Mitchison. Monastrol was shown to inhibit the kinesin A kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule (MT) filaments and are powered by the hydrolysis of adenosine triphosphate (ATP) (thus kinesins are ATPases, a type of enzy ...-5 (also known as KIF11, Kinesin Eg5), a motor protein important for spindle bipolarity. Mechanism of action Monastrol binds to a long loop that is specific to the Eg5 (also known as KIF11 or kinesin-5) kinesin family, and allosterically inhibits ATPase activity of the kinesin References GABAA receptor positive allosteric modulators GHB receptor agonists Thioureas Pyrimidines {{pharma-stub ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
KIF11
Kinesin-like protein KIF11 is a molecular motor protein that is essential in mitosis. In humans it is coded for by the gene ''KIF11''. Kinesin-like protein KIF11 is a member of the kinesin superfamily, which are nanomotors that move along microtubule tracks in the cell. Named from studies in the early days of discovery, it is also known as Kinesin-5, or as BimC, Eg5 or N-2, based on the founding members of this kinesin family. Currently, there are over 70 different eukaryotic kinesin-5 proteins identified by sequence similarity. Members of this protein family are known to be involved in various kinds of spindle dynamics and essential for mitosis. The function of this gene product includes chromosome positioning, centrosome separation and establishing a bipolar spindle during cell mitosis. The human kinesin-5 protein has been actively studied for its role in mitosis and its potential as a therapeutic target for cancer. Function KIF11 (also known as kinesin-5 and Eg5) is a h ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Tim Mitchison
Timothy John Mitchison is a cell biologist and systems biologist and Hasib Sabbagh Professor of Systems Biology at Harvard Medical School in the United States. He is known for his discovery, with Marc Kirschner, of dynamic instability in microtubules, for studies of the mechanism of cell division, and for contributions to chemical biology. Education and early life Mitchison was educated at Haberdashers' Aske's Boys' School and completed his Bachelor of Arts degree in Biochemistry at the University of Oxford where he was an undergraduate student of Merton College, Oxford, from 1976 to 1979. He moved to the University of California, San Francisco (UCSF) in 1979 for his PhD which was supervised by Marc Kirschner and investigated the dynamic instability of microtubules. Career and research Mitchison returned to the UK for postdoctoral research at the National Institute for Medical Research (NIMR) in London. In 1988 he returned to San Francisco where he was appointed assistan ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Kinesin
A kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule (MT) filaments and are powered by the hydrolysis of adenosine triphosphate (ATP) (thus kinesins are ATPases, a type of enzyme). The active movement of kinesins supports several cellular functions including mitosis, meiosis and transport of cellular cargo, such as in axonal transport, and intraflagellar transport. Most kinesins walk towards the plus end of a microtubule, which, in most cells, entails transporting cargo such as protein and membrane components from the center of the cell towards the periphery. This form of transport is known as anterograde transport. In contrast, dyneins are motor proteins that move toward the minus end of a microtubule in retrograde transport. Discovery Kinesins were discovered in 1985, based on their motility in cytoplasm extruded from the giant axon of the squid. They turned out as MT-based anterograde intracellular trans ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Motor Protein
Motor proteins are a class of molecular motors that can move along the cytoplasm of cells. They convert chemical energy into mechanical work by the hydrolysis of ATP. Flagellar rotation, however, is powered by a proton pump. Cellular functions Motor proteins are the driving force behind most active transport of proteins and vesicles in the cytoplasm. Kinesins and cytoplasmic dyneins play essential roles in intracellular transport such as axonal transport and in the formation of the spindle apparatus and the separation of the chromosomes during mitosis and meiosis. Axonemal dynein, found in cilia and flagella, is crucial to cell motility, for example in spermatozoa, and fluid transport, for example in trachea. The muscle protein myosin "motors" the contraction of muscle fibers in animals. Diseases associated with motor protein defects The importance of motor proteins in cells becomes evident when they fail to fulfill their function. For example, kinesin deficiencies have ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GABAA Receptor Positive Allosteric Modulators
In pharmacology, GABAA receptor positive allosteric modulators are positive allosteric modulator (PAM) molecules that increase the activity of the GABAA receptor protein in the vertebrate central nervous system. GABA is a major inhibitory neurotransmitter in the central nervous system. Upon binding, it triggers the GABAA receptor to open its chloride channel to allow chloride ions into the neuron, making the cell hyperpolarized and less likely to fire. GABAA PAMs increase the effect of GABA by making the channel open more frequently or for longer periods. However, they have no effect if GABA or another agonist is not present. Unlike GABAA receptor agonists, GABAA PAMs do not bind at the same active site as the γ-Aminobutyric acid (GABA) neurotransmitter molecule: they affect the receptor by binding at a different site on the protein. This is called allosteric modulation. In psychopharmacology, GABAA receptor PAMs used as drugs have mainly sedative and anxiolytic effects. ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
GHB Receptor Agonists
''gamma''-Hydroxybutyric acid (or γ-hydroxybutyric acid (GHB), also known as 4-hydroxybutanoic acid) is a naturally occurring neurotransmitter and a depressant drug. It is a precursor to GABA, glutamate, and glycine in certain brain areas. It acts on the GHB receptor and is a weak agonist at the GABAB receptor. GHB has been used in the medical setting as a general anesthetic and as treatment for cataplexy, narcolepsy, and alcoholism. It is also used illegally as an intoxicant, as an athletic-performance enhancer, as a date-rape drug, and as a recreational drug. It is commonly used in the form of a salt, such as sodium γ-hydroxybutyrate (NaGHB, sodium oxybate, or Xyrem) or potassium γ-hydroxybutyrate (KGHB, potassium oxybate). GHB is also produced as a result of fermentation, and is found in small quantities in some beers and wines, beef, and small citrus fruits. Succinic semialdehyde dehydrogenase deficiency is a disease that causes GHB to accumulate in the blood. Medic ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Thioureas
In organic chemistry, thioureas are members of a family of organosulfur compounds with the formula and structure . The parent member of this class of compounds is thiourea (). The thiourea functional group has a planar core. Structure and bonding Thioureas have planar core. The bond distance is near 1.71 Å, which is 0.1 Å longer than in normal ketones (). The C–N bond distances are short. Thioureas occurs in two tautomeric forms. For the parent thiourea, the thione form predominates in aqueous solutions. The thiol form, known as an isothiourea, can be encountered in substituted compounds such as isothiouronium salts. : Synthesis ''N'',''N''′-unsubstituted thioureas can be prepared by treating the corresponding cyanamide with hydrogen sulfide or similar sulfide sources. Organic ammonium salts react with potassium thiocyanate as the source of the thiocarbonyl (). Alternatively, ''N'',''N''′-disubstituted thioureas can be prepared by coupling two amines ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
