PMID: 7541541Jul 3, 1995Paper

Liquid-phase combinatorial synthesis

Proceedings of the National Academy of Sciences of the United States of America
H HanK D Janda

Abstract

A concept termed liquid-phase combinatorial synthesis (LPCS) is described. The central feature of this methodology is that it combines the advantages that classic organic synthesis in solution offers with those that solid-phase synthesis can provide, through the application of a linear homogeneous polymer. To validate this concept two libraries were prepared, one of peptide and the second of nonpeptide origin. The peptide-based library was synthesized by a recursive deconvolution strategy [Erb, E., Janda, K. D. & Brenner, S. (1994) Proc. Natl. Acad. Sci. USA 91, 11422-11426] and several ligands were found within this library to bind a monoclonal antibody elicited against beta-endorphin. The non-peptide molecules synthesized were arylsulfonamides, a class of compounds of known clinical bactericidal efficacy. The results indicate that the reaction scope of LPCS should be general, and its value to multiple, high-throughput screening assays could be of particular merit, since multimilligram quantities of each library member can readily be attained.

Citations

May 27, 2004·Organic & Biomolecular Chemistry·Katerina CernovskáBurkhard König
Jul 23, 2013·Angewandte Chemie·Christian SiltanenAlexander Revzin
Oct 1, 1996·Molecular Diversity·A M VandersteenK D Janda
Aug 29, 2002·Chemical Communications : Chem Comm·Kazuhiro ChibaMasahiro Tada
Jun 29, 2004·PLoS Biology·David R HalpinPehr B Harbury
Jan 16, 2002·Journal of Receptor and Signal Transduction Research·D W Hobbs, T Guo
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Sep 22, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yunkyung JeongJae-Sang Ryu
Jul 4, 2009·Langmuir : the ACS Journal of Surfaces and Colloids·Motoyuki IijimaKazuhiro Chiba
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Oct 10, 2002·Chemical Reviews·Jun-Ichi Yoshida, Kenichiro Itami
Nov 1, 2007·Journal of Combinatorial Chemistry·Chuan-Xin ZhangChao-Guo Yan
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Apr 1, 1997·Chemical Reviews·Dennis J. Gravert, Kim D. Janda
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Dec 6, 2003·The Journal of Organic Chemistry·Alexander FishmanEdward Lee-Ruff

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