2biu: Difference between revisions
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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 | 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== | ||
2BIU is a | 2BIU 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 DMS as [http://en.wikipedia.org/wiki/ligand ligand]. Active as [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] Structure known Active Site: AC1. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2BIU OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: mitochondrial protein]] | [[Category: mitochondrial protein]] | ||
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Revision as of 13:16, 5 November 2007
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CRYSTAL STRUCTURE OF HUMAN CYCLOPHILIN D AT 1.7 A RESOLUTION, DMSO COMPLEX
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.
About this Structure
2BIU is a Single protein structure of sequence from Homo sapiens with DMS as ligand. Active as Peptidylprolyl isomerase, with EC number 5.2.1.8 Structure known Active Site: AC1. Full crystallographic information is available from OCA.
Reference
Crystal engineering yields crystals of cyclophilin D diffracting to 1.7 A resolution., Schlatter D, Thoma R, Kung E, Stihle M, Muller F, Borroni E, Cesura A, Hennig M, Acta Crystallogr D Biol Crystallogr. 2005 May;61(Pt 5):513-9. Epub 2005, Apr 20. PMID:15858260
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