Structural diversity in de novo cyclic peptide ligands from genetically encoded library technologies
Sign Up to like & getrecommendations! Published in 2020 at "Peptide Science"
DOI: 10.1002/pep2.24204
Abstract: Cyclic peptides discovered by genetically encoded library technologies have emerged as a class of promising molecules in chemical biology and drug discovery. Here we review the cyclic peptides identified through these techniques reported in the… read more here.
Keywords: library technologies; cyclic peptide; encoded library; genetically encoded ... See more keywords
Photochemical Methods Applied to DNA Encoded Library (DEL) Synthesis.
Sign Up to like & getrecommendations! Published in 2023 at "Accounts of chemical research"
DOI: 10.1021/acs.accounts.2c00778
Abstract: ConspectusDNA-encoded library technology (DELT) is a new screening modality that allows efficient, cost-effective, and rapid identification of small molecules with potential biological activity. This emerging technique represents an enormous advancement that, in combination with other… read more here.
Keywords: dna; encoded library; reaction; del synthesis ... See more keywords
Building Block-Centric Approach to DNA-Encoded Library Design
Sign Up to like & getrecommendations! Published in 2024 at "Journal of Chemical Information and Modeling"
DOI: 10.1021/acs.jcim.4c00232
Abstract: DNA-encoded library technology grants access to nearly infinite opportunities to explore the chemical structure space for drug discovery. Successful navigation depends on the design and synthesis of libraries with appropriate physicochemical properties (PCPs) and structural… read more here.
Keywords: library design; space; encoded library; dna encoded ... See more keywords
Development and Validation of an Automated DNA-Encoded Library Screening Data Analysis Platform: PB-DEL Autoscreening Analysis (PB-DELASA)
Sign Up to like & getrecommendations! Published in 2025 at "Journal of chemical information and modeling"
DOI: 10.1021/acs.jcim.5c00816
Abstract: Tools available for analyzing next-generation sequencing (NGS) data produced from DNA-encoded library (DEL) screening campaigns are often constrained to customized methods developed internally by individual institutes, which usually generate data specifically focusing on protein-ligand interactions… read more here.
Keywords: del; analysis; development validation; encoded library ... See more keywords
Discovery and Optimization of WDR5 Inhibitors via Cascade Deoxyribonucleic Acid-Encoded Library Selection Approach.
Sign Up to like & getrecommendations! Published in 2024 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.3c01463
Abstract: The DNA-encoded library (DEL) is a powerful hit generation tool for chemical biology and drug discovery; however, the optimization of DEL hits remained a daunting challenge for the medicinal chemistry community. In this study, hit… read more here.
Keywords: wdr5 inhibitors; chemistry; del; encoded library ... See more keywords
From DNA-Encoded Library Screening to AM-9747: An MTA-Cooperative PRMT5 Inhibitor with Potent Oral In Vivo Efficacy
Sign Up to like & getrecommendations! Published in 2025 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.4c03101
Abstract: Inhibition of the methyltransferase enzyme PRMT5 by MTA accumulation is a vulnerability of MTAP-deleted cancers. Herein, we report the discovery and optimization of a quinolin-2-amine DEL hit that cooperatively binds PRMT5:MEP50 and MTA to generate… read more here.
Keywords: library screening; mta; dna encoded; prmt5 ... See more keywords
Copper(I/II)-Promoted Diverse Imidazo[1,2-α]pyridine Synthesis on Solid-Phase Bound DNA Oligonucleotides for Encoded Library Design.
Sign Up to like & getrecommendations! Published in 2021 at "Organic letters"
DOI: 10.1021/acs.orglett.1c01834
Abstract: DNA-encoded libraries designed around heterocyclic scaffolds have proven highly productive in target-based screening. Here, we show the synthesis of imidazopyridines on a controlled pore glass-coupled DNA oligonucleotide for solid phase-initiated encoded library synthesis. The target… read more here.
Keywords: dna; library design; encoded library; solid phase ... See more keywords
Reagent-Based Scaffold Diversity for DNA-Encoded Library Design: Solid Phase Synthesis of DNA-Tagged sp3-Rich Heterocycles by SnAP Chemistry.
Sign Up to like & getrecommendations! Published in 2022 at "Organic letters"
DOI: 10.1021/acs.orglett.2c00228
Abstract: Reactions that require strictly dry conditions are challenging to translate to a DNA-encoded library format. Controlled pore glass solid support-connected DNA oligonucleotide-aldehyde conjugates could be condensed with SnAP reagents and cyclized to various sp3-rich heterocycles.… read more here.
Keywords: dna; encoded library; chemistry; sp3 rich ... See more keywords
Multifunctional Building Blocks Compatible with Photoredox-Mediated Alkylation for DNA-Encoded Library Synthesis.
Sign Up to like & getrecommendations! Published in 2020 at "Organic letters"
DOI: 10.1021/acs.orglett.9b04568
Abstract: DNA-encoded library (DEL) technology has emerged as a novel interrogation modality for ligand discovery in the pharmaceutical industry. Given the increasing demand for a higher proportion of C(sp3)-hybridized centers in DEL platforms, a photoredox-mediated cross-coupling… read more here.
Keywords: multifunctional building; dna encoded; encoded library; photoredox mediated ... See more keywords
DNA-Encoded Library Technology─A Catalyst for Covalent Ligand Discovery.
Sign Up to like & getrecommendations! Published in 2024 at "ACS chemical biology"
DOI: 10.1021/acschembio.3c00803
Abstract: The identification of novel covalent ligands for therapeutic purposes has long depended on serendipity, with dedicated hit finding techniques emerging only in the early 2000s. Advances in chemoproteomics have enabled robust characterization of putative drugs… read more here.
Keywords: technology; covalent; covalent ligand; encoded library ... See more keywords
Activity-Based DNA-Encoded Library Screening.
Sign Up to like & getrecommendations! Published in 2019 at "ACS combinatorial science"
DOI: 10.1021/acscombsci.9b00037
Abstract: Robotic high-throughput compound screening (HTS) and, increasingly, DNA-encoded library (DEL) screening are driving bioactive chemical matter discovery in the postgenomic era. HTS enables activity-based investigation of highly complex targets using static compound libraries. Conversely, DEL… read more here.
Keywords: screening; activity based; dna encoded; encoded library ... See more keywords