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BRD4-D1 in complex with BET inhibitorBRD4-D1 in complex with BET inhibitor
Structural highlights
Publication Abstract from PubMedBromodomain and extraterminal (BET) proteins, a family of epigenetic regulators, have emerged as important oncology drug targets. BET proteins have not been targeted for molecular imaging of cancer. Here, we report the development of a novel molecule radiolabelled with positron emitting fluorine-18, [(18)F]BiPET-2, and its in vitro and preclinical evaluation in glioblastoma models. Bromodomain and extraterminal protein-targeted probe enables tumour visualisation in vivo using positron emission tomography.,Dickmann CGF, McDonald AF, Huynh N, Rigopoulos A, Liu Z, Guo N, Osellame LD, Gorman MA, Parker MW, Gan HK, Scott AM, Ackermann U, Burvenich IJG, White JM Chem Commun (Camb). 2023 Mar 9;59(21):3126-3129. doi: 10.1039/d2cc04813b. PMID:36809538[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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