Fig. 1
From: Development of a high-throughput strategy for discovery of potent analogues of antibiotic lysocin E
Chemical structures of compounds used in this study. a Structures of lysocin E (1), menaquinone-4 (MK-4, 2), menahydroquinone-4 (MKH-4, 2 H), and ubiquinone-10 (UQ-10, 3). Side-chain structures of 1 important for the potent antimicrobial activity are highlighted in orange (hydrophobic acyl chain), magenta (aromatic ring), and cyan (basic group). b Structure of the 1-based one-bead-one-compound (OBOC) library comprising the bead-linked peptides. R1-4 denote randomized side chains at residues-3, -6, -9, and -11 by split-and-mix synthesis. Table: Structures and properties of side chains at residues-3, -6, -9, and -11 of the bead-linked lysocin E analogues. One-letter codes of the amino acids and molecular weight of the residues are displayed in parentheses. The configurations of residues-3, -6, -9, and -11, sites for the bead-linking and macrolactamization, and direction of the chain elongation are also indicated. Hydrophobic, acidic, basic, hydroxy, primary amide, aromatic, and methyl groups are highlighted in orange, red, cyan, yellow, purple, magenta, and pink, respectively. TentaGel MB TentaGel Macrobeads. c Component amino acids for construction of the 1-based OBOC library. Protective groups to be removed on a solid support are indicated in blue. Boc t-butoxycarbonyl; Fmoc 9-fluorenymethoxycarbonyl; Pbf 2,2,4,6,7-pentamethyldihydrobenzofuran-5-sulfonyl; TBS tert-butyldimethylsilyl; t-Bu tert-butyl; Tr triphenylmethyl
