2pg2
From Proteopedia
(New page: 200px<br /> <applet load="2pg2" size="450" color="white" frame="true" align="right" spinBox="true" caption="2pg2, resolution 1.849Å" /> '''Crystal structure ...) |
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| - | [[Image:2pg2. | + | [[Image:2pg2.jpg|left|200px]]<br /><applet load="2pg2" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="2pg2, resolution 1.849Å" /> | caption="2pg2, resolution 1.849Å" /> | ||
'''Crystal structure of KSP in complex with ADP and thiophene containing inhibitor 15'''<br /> | '''Crystal structure of KSP in complex with ADP and thiophene containing inhibitor 15'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2PG2 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 K01 as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 2PG2 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=K01:'>K01</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2PG2 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: kinesin spindle protein; ksp; eg5; complex; inhibitor; thiophene]] | [[Category: kinesin spindle protein; ksp; eg5; complex; inhibitor; thiophene]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 12:04:49 2008'' |
Revision as of 10:04, 23 January 2008
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Crystal structure of KSP in complex with ADP and thiophene containing inhibitor 15
Overview
We have identified and synthesized a series of thiophene containing, inhibitors of kinesin spindle protein. SAR studies led to the synthesis of, 33, which was co-crystallized with KSP and determined to bind to an, allosteric pocket previously described for other known KSP inhibitors.
About this Structure
2PG2 is a Single protein structure of sequence from Homo sapiens with , and as ligands. Full crystallographic information is available from OCA.
Reference
Synthesis and SAR of thiophene containing kinesin spindle protein (KSP) inhibitors., Pinkerton AB, Lee TT, Hoffman TZ, Wang Y, Kahraman M, Cook TG, Severance D, Gahman TC, Noble SA, Shiau AK, Davis RL, Bioorg Med Chem Lett. 2007 Apr 29;. PMID:17498954
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