2fl2: Difference between revisions

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[[Image:2fl2.gif|left|200px]]<br />

[[Image:2fl2.gif|left|200px]]<br /><applet load="2fl2" size="350" color="white" frame="true" align="right" spinBox="true"

<applet load="2fl2" size="~~450~~" color="white" frame="true" align="right" spinBox="true"

caption="2fl2, resolution 2.5Å" />

'''crystal structure of KSP in complex with inhibitor 19'''<br />

==Overview==

The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is, described. Introduction of basic amide and urea moieties to the, dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780, human ovarian carcinoma cells with EC(50)s<10nM. Ancillary hERG activity, was evaluated for this series of inhibitors.

The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is described. Introduction of basic amide and urea moieties to the dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780 human ovarian carcinoma cells with EC(50)s<10nM. Ancillary hERG activity was evaluated for this series of inhibitors.

==About this Structure==

2FL2 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, ADP and N4T as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=2FL2 OCA].

2FL2 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=ADP:'>ADP</scene> and <scene name='pdbligand=N4T:'>N4T</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2FL2 OCA].

==Reference==

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[[Category: ksp-inhibitor complex]]

''Page seeded by [http://~~ispc~~.weizmann.ac.il/oca OCA ] on ~~Mon Nov 12~~ 22:~~06:51 2007~~''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:22:28 2008''

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@@ Line 1: / Line 1: @@
-[[Image:2fl2.gif|left|200px]]<br />
+[[Image:2fl2.gif|left|200px]]<br /><applet load="2fl2" size="350" color="white" frame="true" align="right" spinBox="true"
-<applet load="2fl2" size="450" color="white" frame="true" align="right" spinBox="true"
 caption="2fl2, resolution 2.5&Aring;" />
 '''crystal structure of KSP in complex with inhibitor 19'''<br />
 ==Overview==
-The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is, described. Introduction of basic amide and urea moieties to the, dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780, human ovarian carcinoma cells with EC(50)s&lt;10nM. Ancillary hERG activity, was evaluated for this series of inhibitors.
+The evolution of 2,4-diaryl-2,5-dihydropyrroles as inhibitors of KSP is described. Introduction of basic amide and urea moieties to the dihydropyrrole nucleus enhanced potency and aqueous solubility, simultaneously, and provided compounds that caused mitotic arrest of A2780 human ovarian carcinoma cells with EC(50)s&lt;10nM. Ancillary hERG activity was evaluated for this series of inhibitors.
 ==About this Structure==
-FL2 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, ADP and N4T as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2FL2 OCA].
+FL2 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=ADP:'>ADP</scene> and <scene name='pdbligand=N4T:'>N4T</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2FL2 OCA].
 ==Reference==
@@ Line 21: / Line 20: @@
 [[Category: ksp-inhibitor complex]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Nov 12 22:06:51 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:22:28 2008''