Literature DB >> 22691797

On-column ligand exchange for structure-based drug design: a case study with human 11β-hydroxysteroid dehydrogenase type 1.

Wenying Qin1, Russell A Judge, Kenton L Longenecker, Larry R Solomon, John E Harlan.   

Abstract

Successfully forming ligand-protein complexes with specific compounds can be a significant challenge in supporting structure-based drug design for a given protein target. In this respect, an on-column ligand- and detergent-exchange method was developed to obtain ligand-protein complexes of an adamantane series of compounds with 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) after a variety of other complexation methods had failed. This report describes the on-column exchange method and an unexpected byproduct of the method in which artificial trimers were observed in the structures.

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Year:  2012        PMID： 22691797      PMCID： PMC3374522          DOI： 10.1107/S1744309112010172

Source DB:  PubMed          Journal:  Acta Crystallogr Sect F Struct Biol Cryst Commun        ISSN： 1744-3091


  26 in total

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4.  A transgenic model of visceral obesity and the metabolic syndrome.

Authors:  H Masuzaki; J Paterson; H Shinyama; N M Morton; J J Mullins; J R Seckl; J S Flier
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5.  Selective inhibition of 11beta-hydroxysteroid dehydrogenase type 1 decreases blood glucose concentrations in hyperglycaemic mice.

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6.  Improved lipid and lipoprotein profile, hepatic insulin sensitivity, and glucose tolerance in 11beta-hydroxysteroid dehydrogenase type 1 null mice.

Authors:  N M Morton; M C Holmes; C Fiévet; B Staels; A Tailleux; J J Mullins; J R Seckl
Journal:  J Biol Chem       Date:  2001-08-23       Impact factor: 5.157

7.  Conformational flexibility in crystal structures of human 11beta-hydroxysteroid dehydrogenase type I provide insights into glucocorticoid interconversion and enzyme regulation.

Authors:  David J Hosfield; Yiqin Wu; Robert J Skene; Mark Hilgers; Andy Jennings; Gyorgy P Snell; Kathleen Aertgeerts
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8.  Selective inhibition of 11 beta-hydroxysteroid dehydrogenase type 1 improves hepatic insulin sensitivity in hyperglycemic mice strains.

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Journal:  Endocrinology       Date:  2003-07-31       Impact factor: 4.736

Review 9.  11beta-hydroxysteroid dehydrogenase type 1: a tissue-specific regulator of glucocorticoid response.

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