1rqi

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[[Image:1rqi.gif|left|200px]]<br /><applet load="1rqi" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:1rqi.gif|left|200px]]
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caption="1rqi, resolution 2.42&Aring;" />
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'''Active Conformation of Farnesyl Pyrophosphate Synthase Bound to Isopentyl Pyrophosphate and Dimethylallyl S-Thiolodiphosphate'''<br />
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{{Structure
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|PDB= 1rqi |SIZE=350|CAPTION= <scene name='initialview01'>1rqi</scene>, resolution 2.42&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=DST:DIMETHYLALLYL+S-THIOLODIPHOSPHATE'>DST</scene>, <scene name='pdbligand=IPR:ISOPENTYL+PYROPHOSPHATE'>IPR</scene> and <scene name='pdbligand=DPO:DIPHOSPHATE'>DPO</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Geranyltranstransferase Geranyltranstransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.10 2.5.1.10]
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|GENE= ISPA, B0421 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=562 Escherichia coli])
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}}
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'''Active Conformation of Farnesyl Pyrophosphate Synthase Bound to Isopentyl Pyrophosphate and Dimethylallyl S-Thiolodiphosphate'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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1RQI is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=DST:'>DST</scene>, <scene name='pdbligand=IPR:'>IPR</scene> and <scene name='pdbligand=DPO:'>DPO</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Geranyltranstransferase Geranyltranstransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.10 2.5.1.10] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RQI OCA].
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1RQI is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Escherichia_coli Escherichia coli]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1RQI OCA].
==Reference==
==Reference==
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Structural basis for bisphosphonate-mediated inhibition of isoprenoid biosynthesis., Hosfield DJ, Zhang Y, Dougan DR, Broun A, Tari LW, Swanson RV, Finn J, J Biol Chem. 2004 Mar 5;279(10):8526-9. Epub 2003 Dec 12. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=14672944 14672944]
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Structural basis for bisphosphonate-mediated inhibition of isoprenoid biosynthesis., Hosfield DJ, Zhang Y, Dougan DR, Broun A, Tari LW, Swanson RV, Finn J, J Biol Chem. 2004 Mar 5;279(10):8526-9. Epub 2003 Dec 12. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/14672944 14672944]
[[Category: Escherichia coli]]
[[Category: Escherichia coli]]
[[Category: Geranyltranstransferase]]
[[Category: Geranyltranstransferase]]
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[[Category: isoprenyl synthase]]
[[Category: isoprenyl synthase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:53:34 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 13:54:58 2008''

Revision as of 11:55, 20 March 2008

Image:1rqi.gif


PDB ID 1rqi

Drag the structure with the mouse to rotate
, resolution 2.42Å
Ligands: , , and
Gene: ISPA, B0421 (Escherichia coli)
Activity: Geranyltranstransferase, with EC number 2.5.1.10
Coordinates: save as pdb, mmCIF, xml



Active Conformation of Farnesyl Pyrophosphate Synthase Bound to Isopentyl Pyrophosphate and Dimethylallyl S-Thiolodiphosphate


Overview

Farnesyl pyrophosphate synthetase (FPPS) synthesizes farnesyl pyrophosphate through successive condensations of isopentyl pyrophosphate with dimethylallyl pyrophosphate and geranyl pyrophosphate. Nitrogen-containing bisphosphonate drugs used to treat osteoclast-mediated bone resorption and tumor-induced hypercalcemia are potent inhibitors of the enzyme. Here we present crystal structures of substrate and bisphosphonate complexes of FPPS. The structures reveal how enzyme conformational changes organize conserved active site residues to exploit metal-induced ionization and substrate positioning for catalysis. The structures further demonstrate how nitrogen-containing bisphosphonates mimic a carbocation intermediate to inhibit the enzyme. Together, these FPPS complexes provide a structural template for the design of novel inhibitors that may prove useful for the treatment of osteoporosis and other clinical indications including cancer.

About this Structure

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

Reference

Structural basis for bisphosphonate-mediated inhibition of isoprenoid biosynthesis., Hosfield DJ, Zhang Y, Dougan DR, Broun A, Tari LW, Swanson RV, Finn J, J Biol Chem. 2004 Mar 5;279(10):8526-9. Epub 2003 Dec 12. PMID:14672944

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