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Article

Highly specific, bisubstrate-competitive Src inhibitors from DNA-templated macrocycles.

Nature chemical biology - 19 Feb 2012

Georghiou George, Kleiner Ralph E, Pulkoski-Gross Michael, Liu David R, Seeliger Markus A

Abstract excerpt

Protein kinases are attractive therapeutic targets, but their high sequence and structural conservation complicates the development of specific inhibitors. We recently identified, in a DNA-templated macrocycle library, inhibitors with unusually high selectivity among Src-family kinases. Starting from these compounds, we developed and characterized in molecular detail potent macrocyclic inhibitors of Src kinase...

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Identifiers

PMID: 22344177
DOI: 10.1038/nchembio.792
PMCID: PMC3307835

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 6 Sept 2026. Manifest publication-graph-cohort-2026-09-06.1.

Source receipt: pubmed, retrieved 6 Sept 2026.

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