2uym: Difference between revisions
No edit summary |
No edit summary |
||
Line 4: | Line 4: | ||
==Overview== | ==Overview== | ||
We have identified and synthesized a series of thiophene containing | 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== | ||
Line 10: | Line 10: | ||
==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 | 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 | [[Category: Lee, T T.]] | ||
[[Category: ADP]] | [[Category: ADP]] | ||
[[Category: K03]] | [[Category: K03]] | ||
Line 33: | Line 33: | ||
[[Category: thiophene]] | [[Category: thiophene]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:51:35 2008'' |
Revision as of 19:51, 21 February 2008
|
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
Page seeded by OCA on Thu Feb 21 18:51:35 2008