1ajz

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|PDB= 1ajz |SIZE=350|CAPTION= <scene name='initialview01'>1ajz</scene>, resolution 2.00&Aring;
|PDB= 1ajz |SIZE=350|CAPTION= <scene name='initialview01'>1ajz</scene>, resolution 2.00&Aring;
|SITE=
|SITE=
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|LIGAND= <scene name='pdbligand=SO4:SULFATE ION'>SO4</scene>
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|LIGAND= <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>
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|ACTIVITY= [http://en.wikipedia.org/wiki/Dihydropteroate_synthase Dihydropteroate synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.15 2.5.1.15]
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Dihydropteroate_synthase Dihydropteroate synthase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.5.1.15 2.5.1.15] </span>
|GENE=
|GENE=
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|DOMAIN=
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1ajz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1ajz OCA], [http://www.ebi.ac.uk/pdbsum/1ajz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1ajz RCSB]</span>
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[[Category: Somers, D O.]]
[[Category: Somers, D O.]]
[[Category: Stammers, D K.]]
[[Category: Stammers, D K.]]
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[[Category: SO4]]
 
[[Category: antibiotic]]
[[Category: antibiotic]]
[[Category: biosynthesis]]
[[Category: biosynthesis]]
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[[Category: transferase]]
[[Category: transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 09:58:40 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 18:41:54 2008''

Revision as of 15:41, 30 March 2008


PDB ID 1ajz

Drag the structure with the mouse to rotate
, resolution 2.00Å
Ligands:
Activity: Dihydropteroate synthase, with EC number 2.5.1.15
Resources: FirstGlance, OCA, PDBsum, RCSB
Coordinates: save as pdb, mmCIF, xml



STRUCTURE OF DIHYDROPTEROATE PYROPHOSPHORYLASE


Overview

Sulfonamides were amongst the first clinically useful antibacterial agents to be discovered. The identification of sulfanilamide as the active component of the dye Prontosil rubrum led to the synthesis of clinically useful analogues. Today sulfamethoxazole (in combination with trimethoprim), is used to treat urinary tract infections caused by bacteria such as Escherichia coli and is also a first-line treatment for pneumonia caused by the fungus Pneumocystis carinii, a common condition in AIDS patients. The site of action is the de novo folate biosynthesis enzyme dihydropteroate synthase (DHPS) where sulfonamides act as analogues of one of the substrates, para-aminobenzoic acid (pABA). We report here the crystal structure of E.coli DHPS at 2.0 A resolution refined to an R-factor of 0.185. The single domain of 282 residues forms an eight-stranded alpha/beta-barrel. The 7,8-dihydropterin pyrophosphate (DHPPP) substrate binds in a deep cleft in the barrel, whilst sulfanilamide binds closer to the surface. The DHPPP ligand site is highly conserved amongst prokaryotic and eukaryotic DHPSs.

About this Structure

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

Reference

Crystal structure of the anti-bacterial sulfonamide drug target dihydropteroate synthase., Achari A, Somers DO, Champness JN, Bryant PK, Rosemond J, Stammers DK, Nat Struct Biol. 1997 Jun;4(6):490-7. PMID:9187658

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