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Highly pure DNA-encoded chemical libraries by dual-linker solid-phase synthesis.
Keller M, Petrov D, Gloger A, Dietschi B, Jobin K, Gradinger T, Martinelli A, Plais L, Onda Y, Neri D, Scheuermann J. Keller M, et al. Science. 2024 Jun 14;384(6701):1259-1265. doi: 10.1126/science.adn3412. Epub 2024 Jun 13. Science. 2024. PMID: 38870307
The first drugs discovered using DNA-encoded chemical library (DEL) screens have entered late-stage clinical development. However, DEL technology as a whole still suffers from poor chemical purity resulting in suboptimal performance. In this work, we report a techni …
The first drugs discovered using DNA-encoded chemical library (DEL) screens have entered late-stage clinical development. However, …
Impact of library input on the hit discovery rate in DNA-encoded chemical library selections.
Puglioli S, Oehler S, Prati L, Scheuermann J, Bassi G, Cazzamalli S, Neri D, Favalli N. Puglioli S, et al. Chem Sci. 2023 Oct 17;14(43):12026-12033. doi: 10.1039/d3sc03688j. eCollection 2023 Nov 8. Chem Sci. 2023. PMID: 37969600 Free PMC article.
DNA-encoded chemical libraries (DELs) are powerful drug discovery tools, enabling the parallel screening of millions of DNA-barcoded compounds. We investigated how the DEL input affects the hit discovery rate in DEL screenings. Evaluation of selection fingerprints r …
DNA-encoded chemical libraries (DELs) are powerful drug discovery tools, enabling the parallel screening of millions of DNA-barcoded compoun …
Advancing small-molecule drug discovery by encoded dual-display technologies.
Lessing A, Petrov D, Scheuermann J. Lessing A, et al. Trends Pharmacol Sci. 2023 Nov;44(11):817-831. doi: 10.1016/j.tips.2023.08.006. Epub 2023 Sep 20. Trends Pharmacol Sci. 2023. PMID: 37739829 Review.
DNA-encoded chemical library technology (DECL or DEL) has become an important pillar for small-molecule drug discovery. The technology rapidly identifies small-molecule hits for relevant target proteins at low cost and with a high success rate, including ligands for target …
DNA-encoded chemical library technology (DECL or DEL) has become an important pillar for small-molecule drug discovery. The technolog …
A DNA-encoded chemical library based on chiral 4-amino-proline enables stereospecific isozyme-selective protein recognition.
Oehler S, Lucaroni L, Migliorini F, Elsayed A, Prati L, Puglioli S, Matasci M, Schira K, Scheuermann J, Yudin D, Jia M, Ban N, Bushnell D, Kornberg R, Cazzamalli S, Neri D, Favalli N, Bassi G. Oehler S, et al. Nat Chem. 2023 Oct;15(10):1431-1443. doi: 10.1038/s41557-023-01257-3. Epub 2023 Jul 3. Nat Chem. 2023. PMID: 37400597
Here we postulated that the use of rigid, compact and stereo-defined central scaffolds for DEL synthesis may facilitate the discovery of very specific ligands capable of discriminating between closely related protein targets. We synthesized a DEL comprising 3,735,93 …
Here we postulated that the use of rigid, compact and stereo-defined central scaffolds for DEL synthesis may facilitate the discovery …
Isolation of a Natural Killer Group 2D Small-Molecule Ligand from DNA-Encoded Chemical Libraries.
Dakhel S, Galbiati A, Migliorini F, Comacchio C, Oehler S, Prati L, Scheuermann J, Cazzamalli S, Neri D, Bassi G, Favalli N. Dakhel S, et al. ChemMedChem. 2022 Nov 4;17(21):e202200350. doi: 10.1002/cmdc.202200350. Epub 2022 Aug 24. ChemMedChem. 2022. PMID: 35929380
In this work, we report the discovery of a novel NKG2D small molecule binder [K(D) =(41060) nM], isolated from a DNA-Encoded Chemical Library (DEL). The discovery of small organic NKG2D ligands may facilitate the generation of fully synthetic bispecific adaptors, which may …
In this work, we report the discovery of a novel NKG2D small molecule binder [K(D) =(41060) nM], isolated from a DNA-Encoded Chemical Librar …
Durable protection against the SARS-CoV-2 Omicron variant is induced by an adjuvanted subunit vaccine.
Arunachalam PS, Feng Y, Ashraf U, Hu M, Walls AC, Edara VV, Zarnitsyna VI, Aye PP, Golden N, Miranda MC, Green KWM, Threeton BM, Maness NJ, Beddingfield BJ, Bohm RP, Scheuermann SE, Goff K, Dufour J, Russell-Lodrigue K, Kepl E, Fiala B, Wrenn S, Ravichandran R, Ellis D, Carter L, Rogers K, Shirreff LM, Ferrell DE, Deb Adhikary NR, Fontenot J, Hammond HL, Frieman M, Grifoni A, Sette A, O'Hagan DT, Van Der Most R, Rappuoli R, Villinger F, Kleanthous H, Rappaport J, Suthar MS, Veesler D, Wang TT, King NP, Pulendran B. Arunachalam PS, et al. Sci Transl Med. 2022 Aug 17;14(658):eabq4130. doi: 10.1126/scitranslmed.abq4130. Epub 2022 Aug 17. Sci Transl Med. 2022. PMID: 35976993 Free PMC article.
Impact of DNA-Encoded Chemical Library Technology on Drug Discovery.
Keller M, Schira K, Scheuermann J. Keller M, et al. Chimia (Aarau). 2022 May 25;76(5):388-395. doi: 10.2533/chimia.2022.388. Chimia (Aarau). 2022. PMID: 38069709 Free article.
With this perspective we would like to summarize the development of DEL technology and present some representative DEL-derived hits which may soon enter the pharmaceutical market....
With this perspective we would like to summarize the development of DEL technology and present some representative DEL-derived …
Universal encoding of next generation DNA-encoded chemical libraries.
Plais L, Lessing A, Keller M, Martinelli A, Oehler S, Bassi G, Neri D, Scheuermann J. Plais L, et al. Chem Sci. 2022 Jan 11;13(4):967-974. doi: 10.1039/d1sc05721a. eCollection 2022 Jan 26. Chem Sci. 2022. PMID: 35211261 Free PMC article.
We experimentally implemented multiple coding regions and we compared the new DNA encoding scheme with previously reported dual-display DEL modalities in terms of amplifiability and performance in test selections against two target proteins. ...
We experimentally implemented multiple coding regions and we compared the new DNA encoding scheme with previously reported dual-display D …
Macrocyclic DNA-encoded chemical libraries: a historical perspective.
Plais L, Scheuermann J. Plais L, et al. RSC Chem Biol. 2021 Oct 29;3(1):7-17. doi: 10.1039/d1cb00161b. eCollection 2022 Jan 5. RSC Chem Biol. 2021. PMID: 35128404 Free PMC article. Review.
Macrocycles with high affinity and potency were identified for diverse classes of proteins, revealing DEL's huge potential. By giving a historical perspective, we would like to review the methods which permitted the rise of macrocyclic peptide DELs, describe the different …
Macrocycles with high affinity and potency were identified for diverse classes of proteins, revealing DEL's huge potential. By giving …
21 results