1.Synthesis and biological evaluation of tetrahydro-beta-carline derivatives.
Xiu-Qin RUAN ; Qi-Dong YOU ; Lei YANG ; Wu-Tong WU
Acta Pharmaceutica Sinica 2008;43(8):828-832
Kinesin spindle protein (KSP/Eg5) is essential for the formation and maintenance of bipolar spindles during mitosis. Inhibition of this protein leads to cell cycle arrest and apoptosis without interfering other microtubule-dependent processes. Therefore, it is a potential target in cancer therapy. Here, a series of tetrahydro-beta-carboline derivatives 5a - k were synthesized as kinesin spindle protein inhibitor. Their structures were confirmed with 1H NMR, ESI-MS and elemental analysis. The synthesized compounds were evaluated for their inhibition of KSP.
Antineoplastic Agents
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chemical synthesis
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chemistry
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pharmacology
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Carbolines
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chemical synthesis
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chemistry
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pharmacology
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Kinesin
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antagonists & inhibitors
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metabolism
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Molecular Structure
2.Molecular Motor Proteins of the Kinesin Superfamily Proteins (KIFs): Structure, Cargo and Disease.
Dae Hyun SEOG ; Dae Ho LEE ; Sang Kyoung LEE
Journal of Korean Medical Science 2004;19(1):1-7
Intracellular organelle transport is essential for morphogenesis and functioning of the cell. Kinesins and kinesin-related proteins make up a large superfamily of molecular motors that transport cargoes such as vesicles, organelles (e.g. mitochondria, peroxisomes, lysosomes), protein complexes (e.g. elements of the cytoskeleton, virus particles), and mRNAs in a microtubule- and ATP-dependent manner in neuronal and non-neuronal cells. Until now, more than 45 kinesin superfamily proteins (KIFs) have been identified in the mouse and human genomes. Elucidating the transport pathways mediated by kinesins, the identities of the cargoes moved, and the nature of the proteins that link kinesin motors to cargoes are areas of intense investigation. This review focuses on the structure, the binding partners of kinesins and kinesin-based human diseases.
Adenosine Triphosphate/metabolism
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Alzheimer Disease/metabolism
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Animals
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Biological Transport
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Cytoplasm/metabolism
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Diabetes Mellitus/metabolism
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Human
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Kinesin/*chemistry/*metabolism
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Mice
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Microtubule-Associated Proteins/chemistry
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Microtubules/metabolism
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Models, Biological
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Neurons/metabolism
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Protein Binding
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Support, Non-U.S. Gov't
3.Phosphoregulation of the dimerization and functions of end-binding protein 1.
Jie CHEN ; Youguang LUO ; Lixin LI ; Jie RAN ; Xincheng WANG ; Siqi GAO ; Min LIU ; Dengwen LI ; Wenqing SHUI ; Jun ZHOU
Protein & Cell 2014;5(10):795-799
Adenomatous Polyposis Coli Protein
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chemistry
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metabolism
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Amino Acid Sequence
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Chromatography, High Pressure Liquid
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HeLa Cells
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Humans
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Kinesin
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chemistry
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metabolism
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Microtubule-Associated Proteins
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chemistry
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metabolism
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Microtubules
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metabolism
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Molecular Sequence Data
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Phosphopeptides
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analysis
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Phosphorylation
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Protein Multimerization
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Tandem Mass Spectrometry