2e94
From Proteopedia
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| - | [[Image:2e94.jpg|left|200px]] | + | [[Image:2e94.jpg|left|200px]] |
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| - | '''S. cerevisiae geranylgeranyl pyrophosphate synthase in complex with magnesium and BPH-364''' | + | {{Structure |
| + | |PDB= 2e94 |SIZE=350|CAPTION= <scene name='initialview01'>2e94</scene>, resolution 2.18Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene> and <scene name='pdbligand=364:3-BIPHENYL-3-YL-1-(2-HYDROXY-2,2-DIPHOSPHONOETHYL)PYRIDINIUM'>364</scene> | ||
| + | |ACTIVITY= [http://en.wikipedia.org/wiki/Trans-hexaprenyltranstransferase Trans-hexaprenyltranstransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.30 2.5.1.30] | ||
| + | |GENE= | ||
| + | }} | ||
| + | |||
| + | '''S. cerevisiae geranylgeranyl pyrophosphate synthase in complex with magnesium and BPH-364''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2E94 is a [ | + | 2E94 is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Saccharomyces_cerevisiae Saccharomyces cerevisiae]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2E94 OCA]. |
==Reference== | ==Reference== | ||
| - | Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases., Guo RT, Cao R, Liang PH, Ko TP, Chang TH, Hudock MP, Jeng WY, Chen CK, Zhang Y, Song Y, Kuo CJ, Yin F, Oldfield E, Wang AH, Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7. Epub 2007 May 29. PMID:[http:// | + | Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases., Guo RT, Cao R, Liang PH, Ko TP, Chang TH, Hudock MP, Jeng WY, Chen CK, Zhang Y, Song Y, Kuo CJ, Yin F, Oldfield E, Wang AH, Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7. Epub 2007 May 29. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17535895 17535895] |
[[Category: Saccharomyces cerevisiae]] | [[Category: Saccharomyces cerevisiae]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
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[[Category: prenyltransferase]] | [[Category: prenyltransferase]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 16:37:01 2008'' |
Revision as of 14:37, 20 March 2008
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| , resolution 2.18Å | |||||||
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| Ligands: | and | ||||||
| Activity: | Trans-hexaprenyltranstransferase, with EC number 2.5.1.30 | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
S. cerevisiae geranylgeranyl pyrophosphate synthase in complex with magnesium and BPH-364
Overview
Bisphosphonate drugs (e.g., Fosamax and Zometa) are thought to act primarily by inhibiting farnesyl diphosphate synthase (FPPS), resulting in decreased prenylation of small GTPases. Here, we show that some bisphosphonates can also inhibit geranylgeranyl diphosphate synthase (GGPPS), as well as undecaprenyl diphosphate synthase (UPPS), a cis-prenyltransferase of interest as a target for antibacterial therapy. Our results on GGPPS (10 structures) show that there are three bisphosphonate-binding sites, consisting of FPP or isopentenyl diphosphate substrate-binding sites together with a GGPP product- or inhibitor-binding site. In UPPS, there are a total of four binding sites (in five structures). These results are of general interest because they provide the first structures of GGPPS- and UPPS-inhibitor complexes, potentially important drug targets, in addition to revealing a remarkably broad spectrum of binding modes not seen in FPPS inhibition.
About this Structure
2E94 is a Single protein structure of sequence from Saccharomyces cerevisiae. Full crystallographic information is available from OCA.
Reference
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases., Guo RT, Cao R, Liang PH, Ko TP, Chang TH, Hudock MP, Jeng WY, Chen CK, Zhang Y, Song Y, Kuo CJ, Yin F, Oldfield E, Wang AH, Proc Natl Acad Sci U S A. 2007 Jun 12;104(24):10022-7. Epub 2007 May 29. PMID:17535895
Page seeded by OCA on Thu Mar 20 16:37:01 2008
