1tsd

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{{STRUCTURE_1tsd| PDB=1tsd | SCENE= }}
{{STRUCTURE_1tsd| PDB=1tsd | SCENE= }}
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'''THYMIDYLATE SYNTHASE COMPLEX WITH 2'-DEOXYURIDINE 5'-MONOPHOSPHATE (DUMP) AND FOLATE ANALOG 1843U89'''
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===THYMIDYLATE SYNTHASE COMPLEX WITH 2'-DEOXYURIDINE 5'-MONOPHOSPHATE (DUMP) AND FOLATE ANALOG 1843U89===
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==Overview==
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The anticancer drug 1843U89 inhibits thymidylate synthase (TS) at sub-nanomolar concentrations and is undergoing clinical trial. The 1.95 A crystal structure of Escherichia coli TS bound to the drug and dUMP reveals that the 1843U89 binding surface includes a hydrophobic patch that is normally buried. To reach this patch, 1843U89 inserts into the wall of the TS active site, resulting in a severe local distortion of the protein. In this new conformation, active-site groups that normally bind to the catalytic cofactor methylene-tetrahydrofolate instead bind to 1843U89 in new ways. This structure provides a rare example of a protein that can bind tightly to distinct substances using a single, flexible, binding surface. This has implications for drug design, as 1843U89 could not have been obtained from current structure-based approaches.
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(as it appears on PubMed at http://www.pubmed.gov), where 8846221 is the PubMed ID number.
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{{ABSTRACT_PUBMED_8846221}}
==About this Structure==
==About this Structure==
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[[Category: 1843u89]]
[[Category: 1843u89]]
[[Category: Dump]]
[[Category: Dump]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 10:18:39 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 00:15:53 2008''

Revision as of 21:15, 27 July 2008

Image:1tsd.png

Template:STRUCTURE 1tsd

THYMIDYLATE SYNTHASE COMPLEX WITH 2'-DEOXYURIDINE 5'-MONOPHOSPHATE (DUMP) AND FOLATE ANALOG 1843U89

Template:ABSTRACT PUBMED 8846221

About this Structure

1TSD is a Single protein structure of sequence from Escherichia coli. Full crystallographic information is available from OCA.

Reference

Ligand-induced distortion of an active site in thymidylate synthase upon binding anticancer drug 1843U89., Weichsel A, Montfort WR, Nat Struct Biol. 1995 Dec;2(12):1095-101. PMID:8846221

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