Noncellular screening for the discovery of protein-protein interaction modulators.

Drug Discovery Today
Charline KiefferAnne Sophie Voisin-Chiret

Abstract

Protein-protein interactions (PPIs) constitute many potential therapeutic targets for the discovery of new drugs. Given their specificity, PPIs are more challenging to target than other ligands. Thus, finding the best screening process can be difficult. Moreover, PPIs often have no direct accessible activity readout. Therefore, it can be unclear which test to choose for the screening of small molecules targeting PPIs. Given that noncellular assays are the most suitable both as first screening assays and for high-throughput screening (HTS), here we focus on noncellular screening assays. For each assay, we discuss the principles and advantages/drawbacks and provide a recent example. We also highlight the crucial parameters to take into account to select the most suitable assays to screen PPI modulators.

References

Jan 20, 1995·Science·T Clackson, J A Wells
Jan 15, 2002·Journal of Biomolecular Screening·M W PantolianoF R Salemme
Mar 9, 2002·Journal of Biomolecular NMR·Maurizio PellecchiaDaniel S Sem
Jul 26, 2002·Analytical Biochemistry·Haichao ZhangMary Joseph
Feb 13, 2003·Current Topics in Medicinal Chemistry·Edward R ZartlerMichael J Shapiro
Apr 8, 2003·Current Medicinal Chemistry. Anti-cancer Agents·S K SharmaK W Bair
Aug 25, 2004·Analytical Biochemistry·Zaneta Nikolovska-ColeskaShaomeng Wang
Jun 2, 2005·Journal of the American Chemical Society·Paul Schanda, Bernhard Brutscher
Jul 5, 2005·Current Opinion in Structural Biology·Daniel P Ryan, Jacqueline M Matthews
Nov 12, 2005·Journal of Molecular Medicine : Official Organ of the Gesellschaft Deutscher Naturforscher Und Ärzte·David C Fry, Lyubomir T Vassilev
May 16, 2006·Journal of Biomolecular Screening·Yuhong DuHaian Fu
Jun 24, 2006·Drug Discovery Today·Brian K Shoichet
Aug 8, 2006·Proceedings of the National Academy of Sciences of the United States of America·Barbara BecattiniMaurizio Pellecchia
Sep 1, 2006·Journal of Biomolecular Screening·Maxwell D CummingsMarina I Nelen
Jan 28, 2009·Nature Reviews. Drug Discovery·Maurizio PellecchiaGregg Siegal
Feb 13, 2009·Journal of Biomolecular Screening·Fang YiLynne Regan
Jun 18, 2009·Combinatorial Chemistry & High Throughput Screening·William B PetersRichard K Brown
Aug 29, 2009·Cell Cycle·Arumugam MadhumalarChandra Verma
Sep 18, 2009·Combinatorial Chemistry & High Throughput Screening·Joy ConcepcionHong Tan
Jan 1, 2008·Current Chemical Genomics·Richard M EglenMartina Bielefeld
Apr 27, 2010·Current Opinion in Chemical Biology·Natasha ThorneJames Inglese
Sep 2, 2010·Proteins·Howook HwangZhiping Weng
Oct 29, 2010·Nature Communications·Christoph J WienkenStefan Duhr
Mar 4, 2011·Methods in Molecular Biology·Michael Schäferling, Stefan Nagl
Mar 5, 2011·Nature Protocols·Ana M Rossi, Colin W Taylor
Jun 11, 2011·Journal of Computer-aided Molecular Design·Charles A WartchowKuo-Sen Huang
Jun 21, 2011·Current Opinion in Chemical Biology·Xavier MorelliPhilippe Roche
Aug 5, 2011·Assay and Drug Development Technologies·Moran Jerabek-WillemsenStefan Duhr
Nov 10, 2011·Assay and Drug Development Technologies·Guillermo SenisterraMasoud Vedadi
Feb 14, 2012·Expert Opinion on Drug Discovery·Wendy A Lea, Anton Simeonov
Mar 31, 2012·Expert Opinion on Drug Discovery·Nichola C Garbett, Jonathan B Chaires
Jun 2, 2012·Current Pharmaceutical Design·B O VilloutreixO Sperandio
Jan 29, 2013·Chemistry & Biology·Bainan WuMaurizio Pellecchia
Feb 21, 2013·Nature Chemistry·Valeria AzzaritoAndrew J Wilson
Apr 26, 2013·Organic & Biomolecular Chemistry·Rowena HancockGeoff Wells
Jun 5, 2013·Methods in Molecular Biology·Luminita Damian
Jun 5, 2013·Methods in Molecular Biology·Alessio Ciulli

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Citations

Jun 1, 2021·Signal Transduction and Targeted Therapy·Lei ZhongShengyong Yang

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