Literature DB >> 21750879

Screening a fragment cocktail library using ultrafiltration.

Sayaka Shibata1, Zhongsheng Zhang, Konstantin V Korotkov, Jaclyn Delarosa, Alberto Napuli, Angela M Kelley, Natasha Mueller, Jennifer Ross, Frank H Zucker, Frederick S Buckner, Ethan A Merritt, Christophe L M J Verlinde, Wesley C Van Voorhis, Wim G J Hol, Erkang Fan.   

Abstract

Ultrafiltration provides a generic method to discover ligands for protein drug targets with millimolar to micromolar K(d), the typical range of fragment-based drug discovery. This method was tailored to a 96-well format, and cocktails of fragment-sized molecules, with molecular masses between 150 and 300 Da, were screened against medical structural genomics target proteins. The validity of the method was confirmed through competitive binding assays in the presence of ligands known to bind the target proteins.

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Year:  2011        PMID： 21750879      PMCID： PMC3166647          DOI： 10.1007/s00216-011-5225-7

Source DB:  PubMed          Journal:  Anal Bioanal Chem        ISSN： 1618-2642            Impact factor:   4.142


  46 in total

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2.  Biosensor analysis of the interaction between immobilized human serum albumin and drug compounds for prediction of human serum albumin binding levels.

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4.  High-resolution and high-throughput protocols for measuring drug/human serum albumin interactions using BIACORE.

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6.  Proposed steady-state kinetic mechanism for Corynebacterium ammoniagenes FAD synthetase produced by Escherichia coli.

Authors:  I Efimov; V Kuusk; X Zhang; W S McIntire
Journal:  Biochemistry       Date:  1998-07-07       Impact factor: 3.162

7.  Group epitope mapping by saturation transfer difference NMR to identify segments of a ligand in direct contact with a protein receptor.

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Journal:  J Am Chem Soc       Date:  2001-06-27       Impact factor: 15.419

8.  Insights into the mechanism of Escherichia coli methionine aminopeptidase from the structural analysis of reaction products and phosphorus-based transition-state analogues.

Authors:  W T Lowther; Y Zhang; P B Sampson; J F Honek; B W Matthews
Journal:  Biochemistry       Date:  1999-11-09       Impact factor: 3.162

9.  Anchor-based design of improved cholera toxin and E. coli heat-labile enterotoxin receptor binding antagonists that display multiple binding modes.

Authors:  Jason C Pickens; Ethan A Merritt; Misol Ahn; Christophe L M J Verlinde; Wim G J Hol; Erkang Fan
Journal:  Chem Biol       Date:  2002-02

10.  Probing hot spots at protein-ligand binding sites: a fragment-based approach using biophysical methods.

Authors:  Alessio Ciulli; Glyn Williams; Alison G Smith; Tom L Blundell; Chris Abell
Journal:  J Med Chem       Date:  2006-08-10       Impact factor: 7.446
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