2bkk

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[[Image:2bkk.gif|left|200px]]
[[Image:2bkk.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2bkk |SIZE=350|CAPTION= <scene name='initialview01'>2bkk</scene>, resolution 2.15&Aring;
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The line below this paragraph, containing "STRUCTURE_2bkk", creates the "Structure Box" on the page.
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|SITE= <scene name='pdbsite=AC1:Mg+Binding+Site+For+Chain+C'>AC1</scene>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=ADP:ADENOSINE-5&#39;-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Kanamycin_kinase Kanamycin kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.95 2.7.1.95] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE=
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-->
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|DOMAIN=
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{{STRUCTURE_2bkk| PDB=2bkk | SCENE= }}
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|RELATEDENTRY=
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2bkk FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2bkk OCA], [http://www.ebi.ac.uk/pdbsum/2bkk PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2bkk RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF AMINOGLYCOSIDE PHOSPHOTRANSFERASE APH (3')-IIIA IN COMPLEX WITH THE INHIBITOR AR_3A'''
'''CRYSTAL STRUCTURE OF AMINOGLYCOSIDE PHOSPHOTRANSFERASE APH (3')-IIIA IN COMPLEX WITH THE INHIBITOR AR_3A'''
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[[Category: Parizek, P.]]
[[Category: Parizek, P.]]
[[Category: Pluckthun, A.]]
[[Category: Pluckthun, A.]]
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[[Category: ankyrin repeat]]
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[[Category: Ankyrin repeat]]
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[[Category: antibiotic resistance]]
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[[Category: Antibiotic resistance]]
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[[Category: atp-binding]]
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[[Category: Atp-binding]]
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[[Category: co-crystallization]]
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[[Category: Co-crystallization]]
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[[Category: designed repeat protein]]
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[[Category: Designed repeat protein]]
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[[Category: drug design]]
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[[Category: Drug design]]
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[[Category: enzyme inhibition]]
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[[Category: Enzyme inhibition]]
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[[Category: inhibitor design]]
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[[Category: Inhibitor design]]
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[[Category: kinase]]
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[[Category: Kinase]]
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[[Category: kinase inhibition]]
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[[Category: Kinase inhibition]]
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[[Category: plasmid]]
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[[Category: Plasmid]]
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[[Category: transferase]]
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[[Category: Transferase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 20:25:01 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:07:47 2008''
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Revision as of 17:25, 3 May 2008

Image:2bkk.gif

Template:STRUCTURE 2bkk

CRYSTAL STRUCTURE OF AMINOGLYCOSIDE PHOSPHOTRANSFERASE APH (3')-IIIA IN COMPLEX WITH THE INHIBITOR AR_3A


Overview

Aminoglycoside phosphotransferase (3')-IIIa (APH) is a bacterial kinase that confers antibiotic resistance to many pathogenic bacteria and shares structural homology with eukaryotic protein kinases. We report here the crystal structure of APH, trapped in an inactive conformation by a tailor-made inhibitory ankyrin repeat (AR) protein, at 2.15 A resolution. The inhibitor was selected from a combinatorial library of designed AR proteins. The AR protein binds the C-terminal lobe of APH and thereby stabilizes three alpha helices, which are necessary for substrate binding, in a significantly displaced conformation. BIAcore analysis and kinetic enzyme inhibition experiments are consistent with the proposed allosteric inhibition mechanism. In contrast to most small-molecule kinase inhibitors, the AR proteins are not restricted to active site binding, allowing for higher specificity. Inactive conformations of pharmaceutically relevant enzymes, as can be elucidated with the approach presented here, represent powerful starting points for rational drug design.

About this Structure

2BKK is a Protein complex structure of sequences from Enterococcus faecalis. Full crystallographic information is available from OCA.

Reference

Allosteric inhibition of aminoglycoside phosphotransferase by a designed ankyrin repeat protein., Kohl A, Amstutz P, Parizek P, Binz HK, Briand C, Capitani G, Forrer P, Pluckthun A, Grutter MG, Structure. 2005 Aug;13(8):1131-41. PMID:16084385 Page seeded by OCA on Sat May 3 20:25:01 2008

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