Literature DB >> 16720270

A robust small-molecule microarray platform for screening cell lysates.

James E Bradner1, Olivia M McPherson, Ralph Mazitschek, David Barnes-Seeman, John P Shen, Jasmeet Dhaliwal, Kristen E Stevenson, Jay L Duffner, Seung Bum Park, Donna S Neuberg, Paul Nghiem, Stuart L Schreiber, Angela N Koehler.   

Abstract

Herein we report the expanded functional group compatibility of small-molecule microarrays to include immobilization of primary alcohols, secondary alcohols, phenols, carboxylic acids, hydroxamic acids, thiols, and amines on a single slide surface. Small-molecule "diversity microarrays" containing nearly 10,000 known bioactive small molecules, natural products, and small molecules originating from several diversity-oriented syntheses were produced by using an isocyanate-mediated covalent capture strategy. Selected printed bioactive compounds were detected with antibodies against compounds of interest. The new surface of the diversity microarrays is highly compatible with approaches involving cellular lysates. This feature has enabled a robust, optimized screening methodology using cellular lysates, allowing the detection of specific interactions with a broad range of binding affinity by using epitope-tagged or chimeric fluorescent proteins without prior purification. We believe that this expanded research capability has considerable promise in biology and medicine.

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Year:  2006        PMID: 16720270     DOI: 10.1016/j.chembiol.2006.03.004

Source DB:  PubMed          Journal:  Chem Biol        ISSN: 1074-5521


  31 in total

1.  Simultaneous measurement of 10,000 protein-ligand affinity constants using microarray-based kinetic constant assays.

Authors:  James P Landry; Yiyan Fei; Xiangdong Zhu
Journal:  Assay Drug Dev Technol       Date:  2011-12-22       Impact factor: 1.738

2.  Small molecules of different origins have distinct distributions of structural complexity that correlate with protein-binding profiles.

Authors:  Paul A Clemons; Nicole E Bodycombe; Hyman A Carrinski; J Anthony Wilson; Alykhan F Shamji; Bridget K Wagner; Angela N Koehler; Stuart L Schreiber
Journal:  Proc Natl Acad Sci U S A       Date:  2010-10-18       Impact factor: 11.205

3.  A versatile method for functionalizing surfaces with bioactive glycans.

Authors:  Fang Cheng; Jing Shang; Daniel M Ratner
Journal:  Bioconjug Chem       Date:  2010-12-10       Impact factor: 4.774

4.  Identification of a peptoid inhibitor of the proteasome 19S regulatory particle.

Authors:  Hyun-Suk Lim; Chase T Archer; Thomas Kodadek
Journal:  J Am Chem Soc       Date:  2007-05-31       Impact factor: 15.419

Review 5.  Chemical probes and drug leads from advances in synthetic planning and methodology.

Authors:  Christopher J Gerry; Stuart L Schreiber
Journal:  Nat Rev Drug Discov       Date:  2018-04-13       Impact factor: 84.694

Review 6.  Small-molecule microarrays as tools in ligand discovery.

Authors:  Arturo J Vegas; Jason H Fuller; Angela N Koehler
Journal:  Chem Soc Rev       Date:  2008-05-20       Impact factor: 54.564

Review 7.  Neurobiological applications of small molecule screening.

Authors:  Andras Bauer; Brent Stockwell
Journal:  Chem Rev       Date:  2008-05-01       Impact factor: 60.622

8.  Fluorous-based small-molecule microarrays for the discovery of histone deacetylase inhibitors.

Authors:  Arturo J Vegas; James E Bradner; Weiping Tang; Olivia M McPherson; Edward F Greenberg; Angela N Koehler; Stuart L Schreiber
Journal:  Angew Chem Int Ed Engl       Date:  2007       Impact factor: 15.336

9.  Proteins from an unevolved library of de novo designed sequences bind a range of small molecules.

Authors:  Izhack Cherny; Maria Korolev; Angela N Koehler; Michael H Hecht
Journal:  ACS Synth Biol       Date:  2012-04-02       Impact factor: 5.110

10.  Macromolecular scaffolds for immobilizing small molecule microarrays in label-free detection of protein-ligand interactions on solid support.

Authors:  Y S Sun; J P Landry; Y Y Fei; X D Zhu; J T Luo; X B Wang; K S Lam
Journal:  Anal Chem       Date:  2009-07-01       Impact factor: 6.986

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