8dyr: Difference between revisions
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[8dyr]] 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=8DYR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DYR FirstGlance]. <br> | <table><tr><td colspan='2'>[[8dyr]] 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=8DYR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DYR FirstGlance]. <br> | ||
</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=U59:(4P,6P)-4-[2-(cyclopropylmethoxy)-5-(methanesulfonyl)phenyl]-6-[1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl]-2-methylisoquinolin-1(2H)-one'>U59</scene></td></tr> | </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=U59:(4P,6P)-4-[2-(cyclopropylmethoxy)-5-(methanesulfonyl)phenyl]-6-[1-(2-fluoroethyl)-1H-1,2,3-triazol-4-yl]-2-methylisoquinolin-1(2H)-one'>U59</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=8dyr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dyr OCA], [https://pdbe.org/8dyr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dyr RCSB], [https://www.ebi.ac.uk/pdbsum/8dyr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dyr ProSAT]</span></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=8dyr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dyr OCA], [https://pdbe.org/8dyr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dyr RCSB], [https://www.ebi.ac.uk/pdbsum/8dyr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dyr ProSAT]</span></td></tr> | ||
</table> | </table> | ||
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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