Literature DB >> 10814111

Two comparisons of the performance of positional scanning and deletion synthesis for the identification of active constituents in mixture combinatorial libraries.

D L Boger1, J K Lee, J Goldberg, Q Jin.   

Abstract

Two libraries of 120 compounds each were prepared as individual compounds and as full mixtures. The corresponding scanning and deletion synthesis deconvolution libraries were prepared and tested (L-1210, IC(50)) alongside the individual compounds and mixture libraries. This testing, where the properties of each compound in the mixtures were known, was used to compare the performance of scanning and deletion deconvolution libraries. Each has its own intrinsic strengths, with the former being capable of identifying multiple hits at the expense of accurately identifying the most potent library member, while the latter typically is more sensitive to identifying the most potent hit but at the expense of differentiating weaker activities. The protocols complement one another and together more thoroughly identify potent library members.

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Year:  2000        PMID: 10814111     DOI: 10.1021/jo9916481

Source DB:  PubMed          Journal:  J Org Chem        ISSN: 0022-3263            Impact factor:   4.354


  11 in total

1.  Discovery of inhibitors of aberrant gene transcription from Libraries of DNA binding molecules: inhibition of LEF-1-mediated gene transcription and oncogenic transformation.

Authors:  James S Stover; Jin Shi; Wei Jin; Peter K Vogt; Dale L Boger
Journal:  J Am Chem Soc       Date:  2009-03-11       Impact factor: 15.419

2.  Design, synthesis, and validation of a β-turn mimetic library targeting protein-protein and peptide-receptor interactions.

Authors:  Landon R Whitby; Yoshio Ando; Vincent Setola; Peter K Vogt; Bryan L Roth; Dale L Boger
Journal:  J Am Chem Soc       Date:  2011-06-15       Impact factor: 15.419

3.  Therapeutic Targeting of Myc.

Authors:  Edward V Prochownik; Peter K Vogt
Journal:  Genes Cancer       Date:  2010-06

4.  Small-molecule antagonists of Myc/Max dimerization inhibit Myc-induced transformation of chicken embryo fibroblasts.

Authors:  Thorsten Berg; Steven B Cohen; Joel Desharnais; Corinna Sonderegger; Daniel J Maslyar; Joel Goldberg; Dale L Boger; Peter K Vogt
Journal:  Proc Natl Acad Sci U S A       Date:  2002-03-12       Impact factor: 11.205

5.  Assembly of four diverse heterocyclic libraries enabled by Prins cyclization, Au-catalyzed enyne cycloisomerization, and automated amide synthesis.

Authors:  Jiayue Cui; David I Chai; Christopher Miller; Jason Hao; Christopher Thomas; JingQi Wang; Karl A Scheidt; Sergey A Kozmin
Journal:  J Org Chem       Date:  2012-08-16       Impact factor: 4.354

6.  Synthesis of Functionalized Isoindolinones: Addition of In Situ Generated Organoalanes to Acyliminium Ions.

Authors:  Joshua G Pierce; David L Waller; Peter Wipf
Journal:  J Organomet Chem       Date:  2007-10-01       Impact factor: 2.369

7.  Thermodynamics of protein-protein interactions of cMyc, Max, and Mad: effect of polyions on protein dimerization.

Authors:  Anamika Banerjee; Jianzhong Hu; Dixie J Goss
Journal:  Biochemistry       Date:  2006-02-21       Impact factor: 3.162

8.  Pharmacophore identification of c-Myc inhibitor 10074-G5.

Authors:  Jeremy L Yap; Huabo Wang; Angela Hu; Jay Chauhan; Kwan-Young Jung; Robert B Gharavi; Edward V Prochownik; Steven Fletcher
Journal:  Bioorg Med Chem Lett       Date:  2012-10-17       Impact factor: 2.823

9.  Small molecule inhibitors of Myc/Max dimerization and Myc-induced cell transformation.

Authors:  Jin Shi; James S Stover; Landon R Whitby; Peter K Vogt; Dale L Boger
Journal:  Bioorg Med Chem Lett       Date:  2009-09-17       Impact factor: 2.823

10.  Design, synthesis, and evaluation of an alpha-helix mimetic library targeting protein-protein interactions.

Authors:  Alex Shaginian; Landon R Whitby; Sukwon Hong; Inkyu Hwang; Bilal Farooqi; Mark Searcey; Jiandong Chen; Peter K Vogt; Dale L Boger
Journal:  J Am Chem Soc       Date:  2009-04-22       Impact factor: 15.419

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