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

Santos, RG, Appel, JR, Giulianotti, MA et al. (2013). The mathematics of a successful deconvolution: A quantitative assessment of mixture-based combinatorial libraries screened against two formylpeptide receptors . 18(6), 6408-6424. 10.3390/molecules18066408

cited authors

  • Santos, RG; Appel, JR; Giulianotti, MA; Edwards, BS; Sklar, LA; Houghten, RA; Pinilla, C

abstract

  • In the past 20 years, synthetic combinatorial methods have fundamentally advanced the ability to synthesize and screen large numbers of compounds for drug discovery and basic research. Mixture-based libraries and positional scanning deconvolution combine two approaches for the rapid identification of specific scaffolds and active ligands. Here we present a quantitative assessment of the screening of 32 positional scanning libraries in the identification of highly specific and selective ligands for two formylpeptide receptors. We also compare and contrast two mixture-based library approaches using a mathematical model to facilitate the selection of active scaffolds and libraries to be pursued for further evaluation. The flexibility demonstrated in the differently formatted mixture-based libraries allows for their screening in a wide range of assays. © 2013 by the authors.

publication date

  • June 1, 2013

Digital Object Identifier (DOI)

start page

  • 6408

end page

  • 6424

volume

  • 18

issue

  • 6