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9q1g
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Blimp-1 with compound 5== | |
| + | <StructureSection load='9q1g' size='340' side='right'caption='[[9q1g]], [[Resolution|resolution]] 3.70Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[9q1g]] is a 8 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=9Q1G OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=9Q1G 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]] 3.703Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=A1CNQ:(2S)-2-(4-bromophenyl)-2-(5,8-dihydropyrido[3,4-d]pyrimidin-7(6H)-yl)acetamide'>A1CNQ</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=9q1g FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=9q1g OCA], [https://pdbe.org/9q1g PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=9q1g RCSB], [https://www.ebi.ac.uk/pdbsum/9q1g PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=9q1g ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/PRDM1_HUMAN PRDM1_HUMAN] Transcriptional repressor that binds specifically to the PRDI element in the promoter of the beta-interferon gene. Drives the maturation of B-lymphocytes into Ig secreting cells. | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | B-lymphocyte-induced maturation protein 1 (BLIMP-1/PRDM1) is a master transcriptional repressor essential for terminal differentiation of activated B-cells into bone-marrow resident plasma cells. Multiple myeloma (MM) is a plasma cell malignancy wherein the BLIMP-1 regulon remains critical to support basal cell functions, such as an elevated metabolic state and immunoglobulin production that underlie disease manifestation and tumor cell proliferation. It is predicted that perturbation of BLIMP-1 will significantly impact tumor cell homeostasis and ultimately reduce MM cell survival. Herein, we describe the discovery and optimization of the first orally bioavailable BLIMP-1 heterobifunctional ligand-directed degrader (LDD) and demonstration of the expected antitumor response and immunomodulatory biology following BLIMP-1 degradation using preclinical in vivo MM models. | ||
| - | + | Discovery and Characterization of Novel BLIMP-1 Heterobifunctional Ligand-Directed Degraders.,Simmons BJ, Groocock L, Moreno J, Peters DS, Hughes ME, Veeravalli V, Crawford JM, Chalkley M, Griffith M, Plooster M, Hu B, Gamez J, Leisten J, Barnes MJ, Chinn J, Deb G, Modi H, Katepalli M, Weiss D, Won W, Sun Z, Yu S, Reid C, Donnell AF, Li L, Watson ER, Perrin-Ninkovic S, Shi L, Narla RK, Zapf CW, Bence N, Lopez-Girona A, Riggs JR J Med Chem. 2025 Dec 11;68(23):25385-25402. doi: 10.1021/acs.jmedchem.5c02363. , Epub 2025 Nov 24. PMID:41284831<ref>PMID:41284831</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| + | <div class="pdbe-citations 9q1g" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Watson ER]] | ||
Current revision
Blimp-1 with compound 5
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