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| [[Image:1ypv.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_1ypv| PDB=1ypv | SCENE= }} | | {{STRUCTURE_1ypv| PDB=1ypv | SCENE= }} |
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| '''Structure of human thymidylate synthase at low salt conditions'''
| | ===Structure of human thymidylate synthase at low salt conditions=== |
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| ==Overview==
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| Human thymidylate synthase, a target in cancer chemotherapy, was crystallized from PEG 3350 with 30 mM ammonium sulfate (AS) in the crystallization medium. The crystals are isomorphous with the high-salt crystals ( approximately 2.0 M AS) and the structure has been solved and refined (R = 22.6%, R(free) = 24.3%) at 1.8 A resolution. The high- and low-AS-concentration structures are quite similar, with loop 181-197 is in the inactive conformation. Also, residues 95-106 and 129-135 (eukaryotic inserts region) show high mobility as assessed by poor electron density and high values of crystallographic temperature factors (residues 1-25 and 108-129 are disordered in both structures). The high mobility of this region may reflect the situation at physiological ionic strength. Of the four sulfate ions observed bound at 2.0 M AS, only two are present at 30 mM AS. The inactive conformation appears to be stabilized by the side chain of Val3 or a leucine residue from the disordered regions. The low-salt conditions of these crystals should be much more suitable for the study of thymidylate synthase inhibitors, especially those that utilize sulfate-binding sites to stabilize the inactive conformation of loop 181-197.
| | The line below this paragraph, {{ABSTRACT_PUBMED_15858273}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 15858273 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_15858273}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Methyltransferase]] | | [[Category: Methyltransferase]] |
| [[Category: Thymidylate synthase]] | | [[Category: Thymidylate synthase]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 16:37:45 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 05:12:08 2008'' |
