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A Fragment‐Based In Situ Combinatorial Approach To Identify High‐Affinity Ligands for Unknown Binding Sites

2010; Wiley; Volume: 49; Issue: 33 Linguagem: Inglês

10.1002/anie.200907254

1521-3773

Sachin V. Shelke, Brian Cutting, Xiaohua Jiang, Hendrik Koliwer‐Brandl, Daniel S. Strasser, Oliver Schwardt, Sørge Kelm, Beat Ernst,

HER2/EGFR in Cancer Research

In the lead: The title method for the identification of ligands is particularly useful for binding sites where little or no structural information is available. In a fragment-based approach, a suitable pair of first- and second-site ligands is identified by NMR experiments. By applying a receptor-mediated in situ combinatorial approach, the two ligands are then linked to generate a new high-affinity lead structure (see picture).