2gm1: Difference between revisions

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[[Image:2gm1.gif|left|200px]]<br />

[[Image:2gm1.gif|left|200px]]<br /><applet load="2gm1" size="350" color="white" frame="true" align="right" spinBox="true"

<applet load="2gm1" size="~~450~~" color="white" frame="true" align="right" spinBox="true"

caption="2gm1, resolution 2.30Å" />

'''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'''<br />

==Overview==

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.

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.

==About this Structure==

2GM1 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MG, 2AZ and ADP as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=2GM1 OCA].

2GM1 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=2AZ:'>2AZ</scene> and <scene name='pdbligand=ADP:'>ADP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GM1 OCA].

==Reference==

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[[Category: eg5 mg-adp complex inhibitor]]

''Page seeded by [http://~~ispc~~.weizmann.ac.il/oca OCA ] on ~~Mon Nov 12 22~~:20:03 ~~2007~~''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:33:03 2008''

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@@ Line 1: / Line 1: @@
-[[Image:2gm1.gif|left|200px]]<br />
+[[Image:2gm1.gif|left|200px]]<br /><applet load="2gm1" size="350" color="white" frame="true" align="right" spinBox="true"
-<applet load="2gm1" size="450" color="white" frame="true" align="right" spinBox="true"
 caption="2gm1, resolution 2.30&Aring;" />
 '''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'''<br />
 ==Overview==
-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.
+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.
 ==About this Structure==
-GM1 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MG, 2AZ and ADP as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2GM1 OCA].
+GM1 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=2AZ:'>2AZ</scene> and <scene name='pdbligand=ADP:'>ADP</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GM1 OCA].
 ==Reference==
@@ Line 20: / Line 19: @@
 [[Category: eg5 mg-adp complex inhibitor]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:20:03 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:33:03 2008''