2uym: Difference between revisions

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==Overview==
==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.
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==
==About this Structure==
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==Reference==
==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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17498954 17498954]
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 Jul 1;17(13):3562-9. Epub 2007 Apr 29. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17498954 17498954]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Lee, T.T.]]
[[Category: Lee, T T.]]
[[Category: ADP]]
[[Category: ADP]]
[[Category: K03]]
[[Category: K03]]
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[[Category: thiophene]]
[[Category: thiophene]]


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Revision as of 19:51, 21 February 2008

File:2uym.gif


2uym, resolution 2.11Å

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CRYSTAL STRUCTURE OF KSP IN COMPLEX WITH ADP AND THIOPHENE CONTAINING INHIBITOR 37

OverviewOverview

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 StructureAbout this Structure

2UYM is a Single protein structure of sequence from Homo sapiens with , and as ligands. Known structural/functional Site: . Full crystallographic information is available from OCA.

ReferenceReference

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 Jul 1;17(13):3562-9. Epub 2007 Apr 29. PMID:17498954

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