8r07
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==C-terminal Rel-homology Domain of NFAT1== | |
| + | <StructureSection load='8r07' size='340' side='right'caption='[[8r07]], [[Resolution|resolution]] 1.74Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[8r07]] is a 2 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=8R07 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8R07 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]] 1.74Å</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=8r07 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8r07 OCA], [https://pdbe.org/8r07 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8r07 RCSB], [https://www.ebi.ac.uk/pdbsum/8r07 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8r07 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Transcription factors are generally considered challenging, if not "undruggable", targets but they promise new therapeutic options due to their fundamental involvement in many diseases. In this study, we aim to assess the ligandability of the C-terminal Rel-homology domain of nuclear factor of activated T cells 1 (NFAT1), a TF implicated in T-cell regulation. Using a combination of experimental and computational approaches, we demonstrate that small molecule fragments can indeed bind to this protein domain. The newly identified binder is the first small molecule binder to NFAT1 validated with biophysical methods and an elucidated binding mode by X-ray crystallography. The reported eutomer/distomer pair provides a strong basis for potential exploration of higher potency binders on the path toward degrader or glue modalities. | ||
| - | + | Ligandability assessment of the C-terminal Rel-homology domain of NFAT1.,Bottcher J, Fuchs JE, Mayer M, Kahmann J, Zak KM, Wunberg T, Woehrle S, Kessler D Arch Pharm (Weinheim). 2024 Jun;357(6):e2300649. doi: 10.1002/ardp.202300649. , Epub 2024 Feb 23. PMID:38396281<ref>PMID:38396281</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 8r07" style="background-color:#fffaf0;"></div> |
| - | [[Category: Boettcher | + | == References == |
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Boettcher J]] | ||
| + | [[Category: Zak KM]] | ||
Current revision
C-terminal Rel-homology Domain of NFAT1
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