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. 2018 Apr 17;9(5):408-410.
doi: 10.1021/acsmedchemlett.8b00128. eCollection 2018 May 10.

What Do You Get from DNA-Encoded Libraries?

Affiliations

What Do You Get from DNA-Encoded Libraries?

Alexander L Satz. ACS Med Chem Lett. .

Abstract

Use of DNA-encoded libraries (DELs) in the pharmaceutical industry has rapidly increased. We discuss what to expect when you run a DEL screen and contemplate guidelines for library design. Additionally, we consider some visionary work and extrapolate to the future.

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Conflict of interest statement

The author declares no competing financial interest.

Figures

Figure 1
Figure 1
Molecules in the clinic are similar to their original DNA-encoded library (DEL) hits.
Figure 2
Figure 2
Molecular weights of all DEL-derived Roche hits.

References

    1. Goodnow R. A. Jr; Dumelin C. E.; Keefe A. D. DNA-encoded chemistry: enabling the deeper sampling of chemical space. Nat. Rev. Drug Discovery 2017, 16, 131–147. 10.1038/nrd.2016.213. - DOI - PubMed
    1. Harris P. A.; Berger S. B.; Jeong J. U.; Nagilla R.; Bandyopadhyay D.; Campobasso N.; Capriotti C. A.; Cox J. A.; Dare L.; Dong X.; Eidam P. M.; Finger J. N.; Hoffman S. J.; Kang J.; Kasparcova V.; King B. W.; Lehr R.; Lan Y.; Leister L. K.; Lich J. D.; MacDonald T. T.; Miller N. A.; Ouellette M. T.; Pao C. S.; Rahman A.; Reilly M. A.; Rendina A. R.; Rivera E. J.; Schaeffer M. C.; Sehon C. A.; Singhaus R. R.; Sun H. H.; Swift B. A.; Totoritis R. D.; Vossenkämper A.; Ward P.; Wisnoski D. D.; Zhang D.; Marquis R. W.; Gough P. J.; Bertin J. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J. Med. Chem. 2017, 60, 1247–1261. 10.1021/acs.jmedchem.6b01751. - DOI - PubMed
    1. Belyanskaya S. L.; Ding Y.; Callahan J. F.; Lazaar A. L.; Israel D. I. Discovering Drugs with DNA-Encoded Library Technology: From Concept to Clinic with an Inhibitor of Soluble Epoxide Hydrolase. ChemBioChem 2017, 18, 837–842. 10.1002/cbic.201700014. - DOI - PubMed
    1. Clark M. A.; Acharya R. A.; Arico-Muendel C. C.; Belyanskaya S. L.; Benjamin D. R.; Carlson N. R.; Centrella P. A.; Chiu C. H.; Creaser S. P.; Cuozzo J. W.; Davie C. P.; Ding Y.; Franklin G. J.; Franzen K. D.; Gefter M. L.; Hale S. P.; Hansen N. J. V.; Israel D. I.; Jiang J.; Kavarana M. J.; Kelley M. S.; Kollmann C. S.; Li F.; Lind K.; Mataruse S.; Medeiros P. F.; Messer J. A.; Myers P.; O’Keefe H.; Oliff M. C.; Rise C. E.; Satz A. L.; Skinner S. R.; Svendsen J. L.; Tang L.; van Vloten K.; Wagner R. W.; Yao G.; Zhao B.; Morgan B. A. Design, synthesis and selection of DNA-encoded small molecule libraries. Nat. Chem. Biol. 2009, 5, 647–654. 10.1038/nchembio.211. - DOI - PubMed
    1. Eidam O.; Satz A. L. Analysis of the Productivity of DNA Encoded Libraries. MedChemComm 2016, 7, 1323–1331. 10.1039/C6MD00221H. - DOI