2biu: Difference between revisions
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|PDB= 2biu |SIZE=350|CAPTION= <scene name='initialview01'>2biu</scene>, resolution 1.71Å | |PDB= 2biu |SIZE=350|CAPTION= <scene name='initialview01'>2biu</scene>, resolution 1.71Å | ||
|SITE= <scene name='pdbsite=AC1:Dms+Binding+Site+For+Chain+X'>AC1</scene> | |SITE= <scene name='pdbsite=AC1:Dms+Binding+Site+For+Chain+X'>AC1</scene> | ||
|LIGAND= <scene name='pdbligand=DMS:DIMETHYL SULFOXIDE'>DMS</scene> | |LIGAND= <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene> | ||
|ACTIVITY= [http://en.wikipedia.org/wiki/Peptidylprolyl_isomerase Peptidylprolyl isomerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=5.2.1.8 5.2.1.8] | |ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Peptidylprolyl_isomerase Peptidylprolyl isomerase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=5.2.1.8 5.2.1.8] </span> | ||
|GENE= | |GENE= | ||
|DOMAIN= | |||
|RELATEDENTRY= | |||
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2biu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2biu OCA], [http://www.ebi.ac.uk/pdbsum/2biu PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2biu RCSB]</span> | |||
}} | }} | ||
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==Overview== | ==Overview== | ||
In the pharmaceutical industry, knowledge of the three-dimensional structure of a specific target facilitates the drug-discovery process. Despite possessing favoured analytical properties such as high purity and monodispersion in light scattering, some proteins are not capable of forming crystals suitable for X-ray analysis. Cyclophilin D, an isoform of cyclophilin that is expressed in the mitochondria, was selected as a drug target for the treatment of cardiac disorders. As the wild-type enzyme defied all attempts at crystallization, protein engineering on the enzyme surface was performed. The K133I mutant gave crystals that diffracted to 1.7 A resolution using in-house X-ray facilities and were suitable for soaking experiments. The crystals were very robust and diffraction was maintained after soaking in 25% DMSO solution: excellent conditions for the rapid analysis of complex structures including crystallographic fragment screening. | In the pharmaceutical industry, knowledge of the three-dimensional structure of a specific target facilitates the drug-discovery process. Despite possessing favoured analytical properties such as high purity and monodispersion in light scattering, some proteins are not capable of forming crystals suitable for X-ray analysis. Cyclophilin D, an isoform of cyclophilin that is expressed in the mitochondria, was selected as a drug target for the treatment of cardiac disorders. As the wild-type enzyme defied all attempts at crystallization, protein engineering on the enzyme surface was performed. The K133I mutant gave crystals that diffracted to 1.7 A resolution using in-house X-ray facilities and were suitable for soaking experiments. The crystals were very robust and diffraction was maintained after soaking in 25% DMSO solution: excellent conditions for the rapid analysis of complex structures including crystallographic fragment screening. | ||
==About this Structure== | ==About this Structure== | ||
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[[Category: Stihle, M.]] | [[Category: Stihle, M.]] | ||
[[Category: Thoma, R.]] | [[Category: Thoma, R.]] | ||
[[Category: cis-tran-isomerization]] | [[Category: cis-tran-isomerization]] | ||
[[Category: crystal engineering]] | [[Category: crystal engineering]] | ||
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[[Category: mitochondrial protein]] | [[Category: mitochondrial protein]] | ||
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 02:07:03 2008'' | ||
