DNA‐encoded chemical libraries – achievements and remaining challenges. Issue 12 (10th May 2018)

• Record Type: Journal Article
• Authors: Favalli, Nicholas; Bassi, Gabriele; Scheuermann, Jörg; Neri, Dario
• Other Names: Just Wilhelm guestEditor.
• Is Part Of: FEBS letters. Volume 592:Issue 12(2018)
• Page Start: 2168
• Page End: 2180
• Publication Date: 2018-05-10
• Subjects: combinatorial chemistry -- DNA -- DNA‐encoded chemical libraries -- drug discovery -- high‐throughput DNA sequencing; Biochemistry -- Periodicals; Biophysics -- Periodicals; Molecular biology -- Periodicals; Biochimie -- Périodiques; Biochemistry; Biophysics; Molecular biology; Periodicals; 572.05
• DOI: 10.1002/1873-3468.13068
• Languages: English
• ISSNs: 0014-5793

Abstract

Abstract : DNA‐encoded chemical libraries (DECLs) are collections of compounds, individually coupled to DNA tags serving as amplifiable identification barcodes. Since individual compounds can be identified by the associated DNA tag, they can be stored as a mixture, allowing the synthesis and screening of combinatorial libraries of unprecedented size, facilitated by the implementation of split‐and‐pool synthetic procedures or other experimental methodologies. In this review, we briefly present relevant concepts and technologies, which are required for the implementation and interpretation of screening procedures with DNA‐encoded chemical libraries. Moreover, we illustrate some success stories, detailing how novel ligands were discovered from encoded libraries. Finally, we critically review what can realistically be achieved with the technology at the present time, highlighting challenges and opportunities for the future. Abstract :