Literature DB >> 22913403

A novel method for the determination of isokinetic ratios and its application in the synthesis of two new positional scanning libraries.

Marc A Giulianotti1, Ginamarie Debevec, Radleigh G Santos, Laura E Maida, Wenteng Chen, Lili Ou, Yongping Yu, Colette T Dooley, Richard A Houghten.   

Abstract

A novel method for the direct evaluation of the equimolarity of the compounds contained in a mixture is presented. We applied the method toward calculating isokinetic ratios for the reaction between the amine termini of a resin bound peptide fragment and a sulfonyl chloride to produce equal molar mixtures of sulfonamides. The results of this study and the application of the method to the synthesis of two new positional scanning synthetic combinatorial libraries (PS-SCL) are discussed.

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Year:  2012        PMID： 22913403      PMCID： PMC3825827          DOI： 10.1021/co300060s

Source DB:  PubMed          Journal:  ACS Comb Sci        ISSN： 2156-8944            Impact factor:   3.784


  17 in total

1.  Parallel solid-phase synthesis of disubstituted 1,6-piperazine-2-ones.

Authors:  Adel Nefzi; Richard A Mimna; Richard A Houghten
Journal:  J Comb Chem       Date:  2002 Nov-Dec

Review 2.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

3.  Advances in the use of synthetic combinatorial chemistry: mixture-based libraries.

Authors:  Clemencia Pinilla; Jon R Appel; Eva Borràs; Richard A Houghten
Journal:  Nat Med       Date:  2003-01       Impact factor: 53.440

4.  Strategies for the use of mixture-based synthetic combinatorial libraries: scaffold ranking, direct testing in vivo, and enhanced deconvolution by computational methods.

Authors:  Richard A Houghten; Clemencia Pinilla; Marc A Giulianotti; Jon R Appel; Colette T Dooley; Adel Nefzi; John M Ostresh; Yongping Yu; Gerald M Maggiora; Jose L Medina-Franco; Daniela Brunner; Jeff Schneider
Journal:  J Comb Chem       Date:  2007-12-08

5.  Identification of two novel, potent, low-liability antinociceptive compounds from the direct in vivo screening of a large mixture-based combinatorial library.

Authors:  Kate J Reilley; Marc Giulianotti; Colette T Dooley; Adel Nefzi; Jay P McLaughlin; Richard A Houghten
Journal:  AAPS J       Date:  2010-04-27       Impact factor: 4.009

6.  Positional scanning peptide libraries for kinase substrate specificity determinations: straightforward and reproducible synthesis using pentafluorophenyl esters.

Authors:  Thomas Ljungdahl; Jenny Veide-Vilg; Fredrik Wallner; Markus J Tamás; Morten Grøtli
Journal:  J Comb Chem       Date:  2010-09-13

7.  Use and implications of the harmonic mean model on mixtures for basic research and drug discovery.

Authors:  Radleigh G Santos; Marc A Giulianotti; Colette T Dooley; Clemencia Pinilla; Jon R Appel; Richard A Houghten
Journal:  ACS Comb Sci       Date:  2011-03-11       Impact factor: 3.784

8.  Determination of isokinetic ratios necessary for equimolar incorporation of carboxylic acids in the solid-phase synthesis of mixture-based combinatorial libraries.

Authors:  Achyuta N Acharya; John M Ostresh; Richard A Houghten
Journal:  Biopolymers       Date:  2002-10-05       Impact factor: 2.505

9.  Rapidly measuring reactivities of carboxylic acids to generate equireactive building block mixtures: a spectrometric assay.

Authors:  Kendra L Dombi; Ulrich E Steiner; Clemens Richert
Journal:  J Comb Chem       Date:  2003 Jan-Feb

10.  GM-CSF production allows the identification of immunoprevalent antigens recognized by human CD4+ T cells following smallpox vaccination.

Authors:  Valeria Judkowski; Alcinette Bunying; Feng Ge; Jon R Appel; Kingyee Law; Atima Sharma; Claudia Raja-Gabaglia; Patricia Norori; Radleigh G Santos; Marc A Giulianotti; Mark K Slifka; Daniel C Douek; Barney S Graham; Clemencia Pinilla
Journal:  PLoS One       Date:  2011-09-09       Impact factor: 3.240
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  5 in total

1.  Selective agonists and antagonists of formylpeptide receptors: duplex flow cytometry and mixture-based positional scanning libraries.

Authors:  Clemencia Pinilla; Bruce S Edwards; Jon R Appel; Tina Yates-Gibbins; Marc A Giulianotti; Jose L Medina-Franco; Susan M Young; Radleigh G Santos; Larry A Sklar; Richard A Houghten
Journal:  Mol Pharmacol       Date:  2013-06-20       Impact factor: 4.436

2.  Libraries from Libraries: A Series of Sulfonamide Linked Heterocycles Derived from the Same Scaffold.

Authors:  Ginamarie Debevec; Wenteng Chen; Yongping Yu; Richard A Houghten; Marc A Giulianotti
Journal:  Tetrahedron Lett       Date:  2013-08-07       Impact factor: 2.415

3.  Dissecting MMP P10' and P11' subsite sequence preferences, utilizing a positional scanning, combinatorial triple-helical peptide library.

Authors:  Michal Tokmina-Roszyk; Gregg B Fields
Journal:  J Biol Chem       Date:  2018-09-05       Impact factor: 5.157

4.  The mathematics of a successful deconvolution: a quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors.

Authors:  Radleigh G Santos; Jon R Appel; Marc A Giulianotti; Bruce S Edwards; Larry A Sklar; Richard A Houghten; Clemencia Pinilla
Journal:  Molecules       Date:  2013-05-30       Impact factor: 4.411

5.  Positional Scanning MUC1 Glycopeptide Library Reveals the Importance of PDTR Epitope Glycosylation for Lectin Binding.

Authors:  YashoNandini Singh; Maria C Rodriguez Benavente; Mohammed H Al-Huniti; Donella Beckwith; Ramya Ayyalasomayajula; Eric Patino; William S Miranda; Alex Wade; Maré Cudic
Journal:  J Org Chem       Date:  2019-12-18       Impact factor: 4.354
  5 in total

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