2i5x
From Proteopedia
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'''Engineering the PTPbeta catalytic domain with improved crystallization properties''' | '''Engineering the PTPbeta catalytic domain with improved crystallization properties''' | ||
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[[Category: Pokross, M E.]] | [[Category: Pokross, M E.]] | ||
[[Category: Walter, R L.]] | [[Category: Walter, R L.]] | ||
| - | [[Category: | + | [[Category: Drug design]] |
| - | [[Category: | + | [[Category: Protein engineering]] |
| - | [[Category: | + | [[Category: Protein tyrosine phosphatase]] |
| - | [[Category: | + | [[Category: Wpd-loop]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 07:07:00 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 04:07, 4 May 2008
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. 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 Page seeded by OCA on Sun May 4 07:07:00 2008
