Abstract
DNA-encoded library technology (ELT) is a cutting-edge enabling technology platform for drug discovery. Here we describe how to design and synthesize a macrocyclic DNA-encoded library; how to perform selection, sequencing, and data analysis to identify potential active peptides; and how to synthesize off-DNA peptides to confirm activity. This approach provides an effective tool for pharmaceutical research based on peptides.
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References
Goodnow RA, Dumelin CE, Keefe AD (2017) DNA-encoded chemistry: enabling the deeper sampling of chemical space. Nat Rev Drug Discov 16:131–147
Yuen LH, Franzini RM (2017) Achievements, Challenges, and Opportunities in DNA-Encoded Library Research: An Academic Point of View. Chembiochem 18:829–836
Arico-Muendel C (2016) From haystack to needle: finding value with DNA encoded library technology at GSK. Med Chem Commun 7:1898–1909
Zimmermann G, Neri D (2016) DNA-encoded chemical libraries: foundations and applications in lead discovery. Drug Discov Today 21:1828–1834
Zhu Z, Shaginian A, Grady LC, O’Keeffe T, Shi XE, Davie CP, Simpson GL, Messer JA, Evindar G, Bream RN, Thansandote PP, Prentice NR, Mason AM, Pal S (2018) Design and Application of a DNA-Encoded Macrocyclic Peptide Library. ACS Chem Biol 13:53–59
Kleiner RE, Dumelin CE, Liu DR (2011) Small-molecule discovery from DNA-encoded chemical libraries. Chem Soc Rev 40:5707–5717
Thansandote P, Harris RM, Dexter HL, Simpson GL, Pal S, Upton RJ, Valko K (2015) Improving the passive permeability of macrocyclic peptides: Balancing permeability with other physicochemical properties. Bioorg Med Chem 23:322–327
Johnson TW, Dress KR, Edwards M (2009) Using the Golden Triangle to optimize clearance and oral absorption. Bioorg Med Chem Lett 19:5560–5564
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Zhu, Z. et al. (2019). DNA-Encoded Macrocyclic Peptide Library. In: Goetz, G. (eds) Cyclic Peptide Design. Methods in Molecular Biology, vol 2001. Humana, New York, NY. https://doi.org/10.1007/978-1-4939-9504-2_12
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DOI: https://doi.org/10.1007/978-1-4939-9504-2_12
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Publisher Name: Humana, New York, NY
Print ISBN: 978-1-4939-9503-5
Online ISBN: 978-1-4939-9504-2
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