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PubMed · 7541541

Liquid-phase combinatorial synthesis.

H Han·M M Wolfe·S Brenner·K D Janda
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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.

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Amino Acid SequenceAntibodies, MonoclonalDatabases, FactualEnkephalin, LeucineEnzyme-Linked Immunosorbent AssayEpitopesIndicators and ReagentsMolecular Sequence DataOligopeptidesPolyethylene GlycolsSerum Albumin, BovineStructure-Activity RelationshipSulfonamidesbeta-EndorphinComparative StudyJournal ArticleResearch Support, Non-U.S. Gov't

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H Han, M M Wolfe, S Brenner, K D Janda. 1995-07-03. Liquid-phase combinatorial synthesis.. https://doi.org/10.1073/pnas.92.14.6419

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