1rts

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(New page: 200px<br /> <applet load="1rts" size="450" color="white" frame="true" align="right" spinBox="true" caption="1rts, resolution 3.30&Aring;" /> '''THYMIDYLATE SYNTHAS...)
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==About this Structure==
==About this Structure==
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1RTS is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]] with UMP and D16 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=1RTS OCA]].
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1RTS is a [[http://en.wikipedia.org/wiki/Single_protein Single protein]] structure of sequence from [[http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]] with UMP and D16 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: NUL. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1RTS OCA]].
==Reference==
==Reference==
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[[Category: Rattus norvegicus]]
[[Category: Rattus norvegicus]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: Thymidylate synthase]]
[[Category: Ciesla, J.]]
[[Category: Ciesla, J.]]
[[Category: Dzik, J.M.]]
[[Category: Dzik, J.M.]]
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[[Category: tomudex]]
[[Category: tomudex]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Mon Oct 29 20:48:47 2007''
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 13:34:56 2007''

Revision as of 11:30, 30 October 2007


1rts, resolution 3.30Å

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THYMIDYLATE SYNTHASE FROM RAT IN TERNARY COMPLEX WITH DUMP AND TOMUDEX

Overview

Two crystal structures of rat thymidylate synthase (TS) complexed with, dUMP and the anticancer drug Tomudex (ZD1694) have been determined to, resolutions of 3.3 and 2.6 A. Tomudex is one of several new antifolates, targeted to TS and the first to be approved for clinical use. The, structures represent the first views of any mammalian TS bound to ligands, and suggest that the rat protein undergoes a ligand-induced conformational, change similar to that of the Escherichia coli protein. Surprisingly, Tomudex does not induce the "closed" conformation in rat TS that is seen, on binding to E. coli TS, resulting in inhibitor atoms that differ in, position by more than 1.5 A. Several species-specific differences in, sequence may be the reason for this. Phe 74 shifts to a new position in, the rat ... [(full description)]

About this Structure

1RTS is a [Single protein] structure of sequence from [Rattus norvegicus] with UMP and D16 as [ligands]. Active as [Thymidylate synthase], with EC number [2.1.1.45]. Structure known Active Site: NUL. Full crystallographic information is available from [OCA].

Reference

Crystal structures of rat thymidylate synthase inhibited by Tomudex, a potent anticancer drug., Sotelo-Mundo RR, Ciesla J, Dzik JM, Rode W, Maley F, Maley GF, Hardy LW, Montfort WR, Biochemistry. 1999 Jan 19;38(3):1087-94. PMID:9894005

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