Design, synthesis and in vitro evaluation of novel bivalent S-adenosylmethionine analogues

…, R White, PG Stockley, S Warriner, WB Turnbull…

文献索引：Joce, Catherine; White, Rebecca; Stockley, Peter G.; Warriner, Stuart; Turnbull, W. Bruce; Nelson, Adam Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 1 p. 278 - 284

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被引用次数: 4

摘要

In optimal cases, bivalent ligands can bind with exceptionally high affinity to their protein targets. However, designing optimised linkers, that orient the two binding groups perfectly, is challenging, and yet crucial in both fragment-based ligand design and in the discovery of bisubstrate enzyme inhibitors. To further our understanding of linker design, a series of novel bivalent S-adenosylmethionine (SAM) analogues were designed with the aim of ...