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1yrs

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[[Image:1yrs.jpg|left|200px]]
[[Image:1yrs.jpg|left|200px]]
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{{Structure
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|PDB= 1yrs |SIZE=350|CAPTION= <scene name='initialview01'>1yrs</scene>, resolution 2.5&Aring;
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The line below this paragraph, containing "STRUCTURE_1yrs", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=ADP:ADENOSINE-5&#39;-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=L47:3-[(5S)-1-ACETYL-3-(2-CHLOROPHENYL)-4,5-DIHYDRO-1H-PYRAZOL-5-YL]PHENOL'>L47</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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|GENE= KIF11, EG5, KNSL1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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|DOMAIN=
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{{STRUCTURE_1yrs| PDB=1yrs | SCENE= }}
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1yrs FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1yrs OCA], [http://www.ebi.ac.uk/pdbsum/1yrs PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1yrs RCSB]</span>
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'''Crystal structure of KSP in complex with inhibitor 1'''
'''Crystal structure of KSP in complex with inhibitor 1'''
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[[Category: Walsh, E S.]]
[[Category: Walsh, E S.]]
[[Category: Yan, Y.]]
[[Category: Yan, Y.]]
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[[Category: cell cycle]]
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[[Category: Cell cycle]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:41:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 01:19:35 2008''
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Revision as of 13:41, 3 May 2008

Image:1yrs.jpg


PDB ID 1yrs

Drag the structure with the mouse to rotate
1yrs, resolution 2.50Å ()
Ligands: , ,
Gene: KIF11, EG5, KNSL1 (Homo sapiens)
Resources: FirstGlance, OCA, RCSB, PDBsum
Coordinates: save as pdb, mmCIF, xml



Crystal structure of KSP in complex with inhibitor 1


Overview

Optimization of high-throughput screening (HTS) hits resulted in the discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of KSP. Dihydropyrazole 15 is a potent, cell-active KSP inhibitor that induces apoptosis and generates aberrant mitotic spindles in human ovarian carcinoma cells at low nanomolar concentrations. X-ray crystallographic evidence is presented which demonstrates that these inhibitors bind in an allosteric pocket of KSP distant from the nucleotide and microtubule binding sites.

About this Structure

1YRS is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Kinesin spindle protein (KSP) inhibitors. Part 1: The discovery of 3,5-diaryl-4,5-dihydropyrazoles as potent and selective inhibitors of the mitotic kinesin KSP., Cox CD, Breslin MJ, Mariano BJ, Coleman PJ, Buser CA, Walsh ES, Hamilton K, Huber HE, Kohl NE, Torrent M, Yan Y, Kuo LC, Hartman GD, Bioorg Med Chem Lett. 2005 Apr 15;15(8):2041-5. PMID:15808464 Page seeded by OCA on Sat May 3 16:41:57 2008

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