2gm1: Difference between revisions

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{{STRUCTURE_2gm1|  PDB=2gm1  |  SCENE=  }}  
{{STRUCTURE_2gm1|  PDB=2gm1  |  SCENE=  }}  


'''Crystal structure of the mitotic kinesin eg5 in complex with mg-adp and n-(3-aminopropyl)-n-((3-benzyl-5-chloro-4-oxo-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)(cyclopropyl)methyl)-4-methylbenzamide'''
===Crystal structure of the mitotic kinesin eg5 in complex with mg-adp and n-(3-aminopropyl)-n-((3-benzyl-5-chloro-4-oxo-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)(cyclopropyl)methyl)-4-methylbenzamide===




==Overview==
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Synthesis and SAR of substituted pyrrolotriazine-4-one analogues as Eg5 inhibitors are described. Many of these analogues displayed potent inhibitory activities in the Eg5 ATPase and A2780 cell proliferation assays. In addition, pyrrolotriazine-4-one analogue 26 demonstrated in vivo efficacy in an iv P388 murine leukemia model. Both NMR and X-ray crystallographic studies revealed that these analogues bind to an allosteric site on the Eg5 protein.
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{{ABSTRACT_PUBMED_16730979}}


==About this Structure==
==About this Structure==
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[[Category: Sheriff, S.]]
[[Category: Sheriff, S.]]
[[Category: Eg5 mg-adp complex inhibitor]]
[[Category: Eg5 mg-adp complex inhibitor]]
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