Design and Application of a DNA-Encoded Macrocyclic Peptide Library

A DNA-encoded macrocyclic peptide library was designed and synthesized with 2.4 × 1012 members composed of 4–20 natural and non-natural amino acids. Affinity-based selection was performed against two therapeutic targets, VHL and RSV N protein. On the basis of selection data, some peptides were selec...

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Veröffentlicht in:	ACS chemical biology 2018-01, Vol.13 (1), p.53-59
Hauptverfasser:	Zhu, Zhengrong, Shaginian, Alex, Grady, LaShadric C, O’Keeffe, Thomas, Shi, Xiangguo E, Davie, Christopher P, Simpson, Graham L, Messer, Jeffrey A, Evindar, Ghotas, Bream, Robert N, Thansandote, Praew P, Prentice, Naomi R, Mason, Andrew M, Pal, Sandeep
Format:	Artikel
Sprache:	eng
Schlagworte:	Amino Acids - chemistry DNA - chemistry Drug Evaluation, Preclinical - methods Molecular Targeted Therapy Peptide Library Peptides, Cyclic - chemistry Peptides, Cyclic - genetics Peptides, Cyclic - pharmacology Polymerase Chain Reaction Respiratory Syncytial Viruses Viral Proteins - antagonists & inhibitors Viral Proteins - chemistry Viral Proteins - metabolism Von Hippel-Lindau Tumor Suppressor Protein - chemistry Von Hippel-Lindau Tumor Suppressor Protein - metabolism
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Beschreibung
Zusammenfassung:	A DNA-encoded macrocyclic peptide library was designed and synthesized with 2.4 × 1012 members composed of 4–20 natural and non-natural amino acids. Affinity-based selection was performed against two therapeutic targets, VHL and RSV N protein. On the basis of selection data, some peptides were selected for resynthesis without a DNA tag, and their activity was confirmed.
ISSN:	1554-8929 1554-8937
DOI:	10.1021/acschembio.7b00852