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08.11
Revolutionizing On-DNA C–N Cross-Coupling: Ruthenium-Mediated "Reverse Buchwald" Opens New Chemical Frontiers
For years, a robust and general method for DNA compatible "reverse" Buchwald-Hartwig-type amination – coupling DNA-conjugated amines with external aryl halides – has been long sought, yet this transformation remained elusive due to the prohibitive challenge of DNA nucleobase interference. To overcome this long-standing technical bottleneck, the Ritter group at the Max-Planck-Institut für Kohlenforschung reported an air-stable ruthenium-mediated η6 π-arene activation strategy in the Journal of the American Chemical Society (JACS). This breakthrough finally enables the precise N-arylation of DNA-linked amines, unlocking a vast and previously inaccessible chemical space for drug discovery.
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04.24
DEL Insight | HitGen Introduces CycWeave, a Token-Free Dual-View Graph Framework for Cyclic Peptidomimetics and DEL Modeling
Recently, the Computational Chemistry team at HitGen introduced CycWeave, a token-free dual-view coarse-grained graph neural framework designed for complex modular molecular systems. By adopting a representation strategy that better matches the modular nature of CPMs and DNA-encoded library (DEL) compounds, CycWeave demonstrated robust and competitive performance in both CPM membrane permeability prediction and large-scale DEL enrichment modeling.
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04.10
DEL Insight | Solid-phase DEL: Applications and Future Prospects
As the field of traditional DNA-Encoded Library (DEL) chemistry reaches maturity, expectations for library quality have become increasingly exacting. Beyond conventional optimizations focused on purification protocols and reaction yields, a growing number of research groups have pioneered solid-phase synthesis strategies to enhance peptide library purity. Here, we present and discuss the key insights gleaned from three recent publications on solid-phase DEL derivatives.
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03.31
DEL Insight | DNA-Encoded Libraries (DELs) for Discovering New Molecular Probes: Application to Live-Cell Bioimaging and Personalized Theranostics
A recent review published in Bioconjugate Chemistry by Marinier et al. (2026) shows that DNA-encoded libraries (DELs), long established for therapeutic small-molecule discovery, represent an underutilized yet highly promising platform for the rapid, parallel development of next-generation molecular probes – particularly for live-cell imaging, targeted radioimaging, and personalized theranostics. DEL-derived targeting moieties can be efficiently and modularly converted into high-affinity, high-selectivity optical or radiolabeled probes – including dual-use agents that simultaneously enable precise diagnosis and effective therapy (Figure 1).
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