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Article

Chemical biology. A bump-and-hole approach to engineer controlled selectivity of BET bromodomain chemical probes.

Science (New York, N.Y.) - 31 Oct 2014

Baud Matthias G J, Lin-Shiao Enrique, Cardote Teresa, Tallant Cynthia, Pschibul Annica, Chan Kwok-Ho, Zengerle Michael, Garcia Jordi R, Kwan Terence T-L, Ferguson Fleur M, Ciulli Alessio

Abstract excerpt

Small molecules are useful tools for probing the biological function and therapeutic potential of individual proteins, but achieving selectivity is challenging when the target protein shares structural domains with other proteins. The Bromo and Extra-Terminal (BET) proteins have attracted interest because of their roles in transcriptional regulation, epigenetics, and cancer. The BET bromodomains (protein...

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Identifiers

PMID: 25323695
DOI: 10.1126/science.1249830
PMCID: PMC4458378

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PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 7 Sept 2026. Manifest publication-graph-cohort-2026-09-07.1.

Source receipt: pubmed, retrieved 7 Sept 2026.

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