2i5x
From Proteopedia
(New page: 200px<br /> <applet load="2i5x" size="450" color="white" frame="true" align="right" spinBox="true" caption="2i5x, resolution 1.700Å" /> '''Engineering the PT...) |
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| - | [[Image:2i5x.gif|left|200px]]<br /> | + | [[Image:2i5x.gif|left|200px]]<br /><applet load="2i5x" size="350" color="white" frame="true" align="right" spinBox="true" |
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caption="2i5x, resolution 1.700Å" /> | caption="2i5x, resolution 1.700Å" /> | ||
'''Engineering the PTPbeta catalytic domain with improved crystallization properties'''<br /> | '''Engineering the PTPbeta catalytic domain with improved crystallization properties'''<br /> | ||
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==About this Structure== | ==About this Structure== | ||
| - | 2I5X is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with MG, CL and UA5 as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] Full crystallographic information is available from [http:// | + | 2I5X is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=MG:'>MG</scene>, <scene name='pdbligand=CL:'>CL</scene> and <scene name='pdbligand=UA5:'>UA5</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Active as [http://en.wikipedia.org/wiki/Protein-tyrosine-phosphatase Protein-tyrosine-phosphatase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.1.3.48 3.1.3.48] Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2I5X OCA]. |
==Reference== | ==Reference== | ||
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[[Category: wpd-loop]] | [[Category: wpd-loop]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 15:30:48 2008'' |
Revision as of 13:30, 23 January 2008
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Engineering the PTPbeta catalytic domain with improved crystallization properties
Overview
Protein tyrosine phosphatases (PTPs) play roles in many biological, processes and are considered to be important targets for drug discovery., As inhibitor development has proven challenging, crystal structure-based, design will be very helpful to advance inhibitor potency and selectivity., Successful application of protein crystallography to drug discovery, heavily relies on high-quality crystal structures of the protein of, interest complexed with pharmaceutically interesting ligands. It is very, important to be able to produce protein-ligand crystals rapidly and, reproducibly for as many ligands as necessary. This study details our, efforts to engineer the catalytic domain of human protein tyrosine, phosphatase beta (HPTPbeta-CD) with properties suitable for, rapid-turnaround crystallography. Structures of apo HPTPbeta-CD and its, complexes with several novel small-molecule inhibitors are presented here, for the first time.
About this Structure
2I5X is a Single protein structure of sequence from Homo sapiens with , and as ligands. Active as Protein-tyrosine-phosphatase, with EC number 3.1.3.48 Full crystallographic information is available from OCA.
Reference
Engineering the catalytic domain of human protein tyrosine phosphatase beta for structure-based drug discovery., Evdokimov AG, Pokross M, Walter R, Mekel M, Cox B, Li C, Bechard R, Genbauffe F, Andrews R, Diven C, Howard B, Rastogi V, Gray J, Maier M, Peters KG, Acta Crystallogr D Biol Crystallogr. 2006 Dec;62(Pt 12):1435-45. Epub 2006, Nov 23. PMID:17139078
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