1tsl: Difference between revisions
New page: left|200px<br /> <applet load="1tsl" size="450" color="white" frame="true" align="right" spinBox="true" caption="1tsl, resolution 2.50Å" /> '''L. CASEI THYMIDYLAT... |
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==About this Structure== | ==About this Structure== | ||
1TSL is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Lactobacillus_casei Lactobacillus casei]] with PO4 and A15 as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.45 2.1.1.45]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1TSL OCA]]. | 1TSL is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Lactobacillus_casei Lactobacillus casei]] with PO4 and A15 as [[http://en.wikipedia.org/wiki/ligands ligands]]. Active as [[http://en.wikipedia.org/wiki/Thymidylate_synthase Thymidylate synthase]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.45 2.1.1.45]]. Structure known Active Site: CAT. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1TSL OCA]]. | ||
==Reference== | ==Reference== | ||
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[[Category: Lactobacillus casei]] | [[Category: Lactobacillus casei]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Thymidylate synthase]] | |||
[[Category: Stout, T.J.]] | [[Category: Stout, T.J.]] | ||
[[Category: Stroud, R.M.]] | [[Category: Stroud, R.M.]] | ||
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[[Category: structure-based drug design]] | [[Category: structure-based drug design]] | ||
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Revision as of 12:43, 30 October 2007
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L. CASEI THYMIDYLATE SYNTHASE WITH SPECIES SPECIFIC INHIBITOR
OverviewOverview
Thymidylate synthase is an attractive target for antiproliferative drug, design because of its key role in the synthesis of DNA. As such, the, enzyme has been widely targeted for anticancer applications. In principle, TS should also be a good target for drugs used to fight infectious, disease. In practice, TS is highly conserved across species, and it has, proven to be difficult to develop inhibitors that are selective for, microbial TS enzymes over the human enzyme. Using the structure of TS from, Lactobacillus casei in complex with the nonsubstrate analogue, phenolphthalein, inhibitors were designed to take advantage of features of, the bacterial enzyme that differ from those of the human enzyme. Upon, synthesis and testing, these inhibitors were found to be up to 40-fold, selective for ... [(full description)]
About this StructureAbout this Structure
1TSL is a [Single protein] structure of sequence from [Lactobacillus casei] with PO4 and A15 as [ligands]. Active as [Thymidylate synthase], with EC number [2.1.1.45]. Structure known Active Site: CAT. Full crystallographic information is available from [OCA].
ReferenceReference
Structure-based design of inhibitors specific for bacterial thymidylate synthase., Stout TJ, Tondi D, Rinaldi M, Barlocco D, Pecorari P, Santi DV, Kuntz ID, Stroud RM, Shoichet BK, Costi MP, Biochemistry. 1999 Feb 2;38(5):1607-17. PMID:9931028
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