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A DNA-encoded library for the identification of natural product binders that modulate poly (ADP-ribose) polymerase 1, a validated anti-cancer target

Biochem Biophys Res Commun. 2020; 
Jie Li, Yu Li, Fengping Lu, Lili Liu, Qun Ji, Ke Song, Qianqian Yin, Richard A Lerner, Guang Yang, Hongtao Xu, Peixiang Ma
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Recombinant Antibody Expression … visualization. 2.2. nDEL panning. The panning procedure was performed as previously described [21,22]. In brief, 5 μg His-tagged recombinant human PARP-1 was mixed with Ni-charged MagBeads (GenScript, Cat. #L00295 … Get A Quote

摘要

Natural products have been an invaluable source of drug discovery, but their targets remain largely unknown. Natural products enriched DNA-encoded chemical libraries (nDELs) empower the researchers to rapidly and economically screen numerous natural products against various protein targets, and therefore promote the elucidation of the molecular mechanisms. In this work, we used poly (ADP-ribose) polymerase 1 (PARP1), as an example to explore the usage of nDEL for the functional natural products selection. We used late-stage modification approach to label three positive binders with unique DNA barcodes, whose dissociation constants range from sub-micromolar to micromolar. The selection criterion was set up accor... More

关键词

DNA-Encoded library, Drug discovery, Luteolin, Natural products, PARP1