8e17

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BRD4-D1 in complex with BET inhibitor

Structural highlights

8e17 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:X-ray diffraction, Resolution 1.47Å
Ligands:EDO, U7R
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Publication Abstract from PubMed

Bromodomain 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.

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References

  1. 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. Bromodomain and extraterminal protein-targeted probe enables tumour visualisation in vivo using positron emission tomography. Chem Commun (Camb). 2023 Mar 9;59(21):3126-3129. PMID:36809538 doi:10.1039/d2cc04813b

Contents


PDB ID 8e17

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