Discovery of dual-target ligands binding to beta2-adrenoceptor and cysteinyl-leukotriene receptor for the potential treatment of asthma from natural products derived DNA-encoded library

Liang, Qi; Zuo, Haiyue; Yang, Tian; Yin, Jiatai; Huang, Xiaomin; Wang, Jing; Li, Qian; Yin, Guowei; Zhao, Xinfeng

doi:10.1016/j.ejmech.2022.114212

Cited by 11 publications

(1 citation statement)

References 42 publications

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“…Practically, dual-display DELs permit the discovery of synergistic pairs of ligands, in a fashion comparable to fragment based drug discovery (FBDD). , However, it is necessary to engineer linkers between the binding moieties after selection experiments, as it is the case with FBDD approaches. − While new methodologies have been developed to transition from double-stranded to single-stranded DELs, rendering the libraries more modular and versatile for synthesis and selections, − dual-display DELs enable innovative strategies for affinity-based selections such as affinity maturation of known hits and (photo)cross-linking to biological targets in solution or on cell surfaces . Thanks to its continued optimization, the field of dual-display DELs now offers a panel of options for starting drug discovery projects. ,− …”

Section: Introductionmentioning

confidence: 99%

Asymmetry of Dual-Display DNA-Encoded Chemical Libraries

Plais,

Trachsel,

Scheuermann

2024

Bioconjugate Chem.

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While dual-display DNA-encoded chemical libraries (DELs) are increasingly employed for ligand discovery, some of their fundamental properties have not yet been studied in-depth. Aided with fluorescence polarization experiments, we demonstrate that dual-display DELs are intrinsically asymmetrical entities, and we deduce practical guidelines to perform better-informed on-DNA hit validation from these libraries.

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