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PEG Based Resins for Protease Drug Discovery Synthesis, Screening and Analysis of Combinatorial On-Bead Libraries

[ Vol. 6 , Issue. 7 ]

Author(s):

Thomas Groth, Manat Renil and Ernst Meinjohanns   Pages 589 - 610 ( 22 )

Abstract:


This review will cover the entire hit identification process performed with biocompatible, aqueous solvated, poly[ethylene glycol] (PEG) based resins - from synthesis, through screening, to analysis. The different types of resins (including their preparation) will be discussed and compared individually. Examples of one-bead-one-compound substrate libraries will be presented, as will one-bead-two-compounds libraries used for the discovery of enzyme inhibitors. The review includes a section covering organic and bio-organic reactions performed on all-PEG resins and discusses on-bead screening of the libraries with biomolecules. Finally, analysis of compounds on single beads, either via investigation by on-bead NMR or by ladder-coding of the combinatorial compound is covered. In general, the review will focus on chemistry, libraries, synthesis, screening, and analysis, using all-PEG based resins.

Keywords:

on-bead, resins, proteases, inhibitors, substrates, synthesis, peg, hr mas nmr

Affiliation:

Department of Medicinal Chemistry, Combio A / S, Gamle Carlsberg Vej 10, DK-2500 Valby,Copenhagen, Denmark.



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