Proximity Labeling: DEL Selection Without Capturing the Target - X-Chem

DNA-encoded library (DEL) selections typically use affinity pulldown to enrich compounds that bind targets of interest. While it is highly effective at identifying hits for numerous targets, affinity...

Strategy for Engineering High Photolysis Efficiency of Photocleavable Protecting Groups through...

Photolabile protecting groups (PPGs) enable the precise activation of molecular function with light in many research areas, such as photopharmacology, where remote spatiotemporal control over the...

Lysine-Targeted Reversible Covalent Ligand Discovery for Proteins via Phage Display

Binding via reversible covalent bond formation presents a novel and powerful mechanism to enhance the potency of synthetic inhibitors for therapeutically important proteins. Work on this front has...

Trio-pharmacophore DNA-encoded chemical library for simultaneous selection of fragments and linkers

Nature Communications - Dual-pharmacophore DNA-Encoded Libraries (DELs) can generate large libraries, but linker optimisation is challenging. Here, the authors report a trio-pharmacophore DEL...

A Visible and Near-Infrared Light Activatable Diazocoumarin Probe for Fluorogenic Protein Labeling...

Chemical modification of proteins in living cells permits valuable glimpses into the molecular interactions that underpin dynamic cellular events. While genetic engineering methods are often prefer...

Converting Double-Stranded DNA-Encoded Libraries (DELs) to Single-Stranded Libraries for More...

DNA-encoded library (DEL) is an efficient high-throughput screening technology platform in drug discovery and is also gaining momentum in academic research. Today, the majority of DELs are assembled...

Direct Selection of DNA-Encoded Libraries for Biased Agonists of GPCRs on Live Cells

G protein-coupled receptors (GPCRs) are the largest superfamily of human membrane target proteins for approved drugs. GPCR ligands can have a complex array of pharmacological activities. Among these...

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Selection methods for proximity-dependent enrichment of ligands from DNA-encoded libraries using...

Herein, we report a selection approach to enrich ligands from DNA-encoded libraries (DELs) based on proximity to an enzymatic tag on the target protein. This method involves uncaging or installation...