8e17: Difference between revisions
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==BRD4-D1 in complex with BET inhibitor== | |||
<StructureSection load='8e17' size='340' side='right'caption='[[8e17]], [[Resolution|resolution]] 1.47Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[8e17]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=8E17 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8E17 FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.47Å</td></tr> | |||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=U7R:(4P,6M)-6-[1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl]-4-[5-(methanesulfonyl)-2-methoxyphenyl]-2-methylisoquinolin-1(2H)-one'>U7R</scene></td></tr> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=8e17 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8e17 OCA], [https://pdbe.org/8e17 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8e17 RCSB], [https://www.ebi.ac.uk/pdbsum/8e17 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8e17 ProSAT]</span></td></tr> | |||
</table> | |||
<div style="background-color:#fffaf0;"> | |||
== 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<ref>PMID:36809538</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
[[Category: | </div> | ||
[[Category: | <div class="pdbe-citations 8e17" style="background-color:#fffaf0;"></div> | ||
[[Category: | == References == | ||
[[Category: | <references/> | ||
[[Category: White | __TOC__ | ||
</StructureSection> | |||
[[Category: Homo sapiens]] | |||
[[Category: Large Structures]] | |||
[[Category: Fitzgerald CGD]] | |||
[[Category: Gorman MA]] | |||
[[Category: Parker MW]] | |||
[[Category: White JM]] | |||
Latest revision as of 13:16, 25 October 2023
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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