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==Bacterial cereblon homologue in complex with (R)-3-(4-methoxyphenyl)piperidine-2,6-dione== | ==Bacterial cereblon homologue in complex with (R)-3-(4-methoxyphenyl)piperidine-2,6-dione== | ||
<StructureSection load='7shh' size='340' side='right'caption='[[7shh]]' scene=''> | <StructureSection load='7shh' size='340' side='right'caption='[[7shh]], [[Resolution|resolution]] 1.90Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7SHH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7SHH FirstGlance]. <br> | <table><tr><td colspan='2'>[[7shh]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Magnetospirillum_gryphiswaldense Magnetospirillum gryphiswaldense]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7SHH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7SHH FirstGlance]. <br> | ||
</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=7shh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7shh OCA], [https://pdbe.org/7shh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7shh RCSB], [https://www.ebi.ac.uk/pdbsum/7shh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7shh ProSAT]</span></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]] 1.9Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=9FT:(3R)-3-(4-methoxyphenyl)piperidine-2,6-dione'>9FT</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=7shh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7shh OCA], [https://pdbe.org/7shh PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7shh RCSB], [https://www.ebi.ac.uk/pdbsum/7shh PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7shh ProSAT]</span></td></tr> | |||
</table> | </table> | ||
== Function == | |||
[https://www.uniprot.org/uniprot/A4TVL0_9PROT A4TVL0_9PROT] | |||
<div style="background-color:#fffaf0;"> | |||
== Publication Abstract from PubMed == | |||
Aberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs utilizing a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ10542 displayed high selectivity over GSPT1 and other members of the JAK family and potency in patient-derived ALL cells containing both JAK2 fusions and CRLF2 rearrangements. | |||
Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.,Alcock LJ, Chang Y, Jarusiewicz JA, Actis M, Nithianantham S, Mayasundari A, Min J, Maxwell D, Hunt J, Smart B, Yang JJ, Nishiguchi G, Fischer M, Mullighan CG, Rankovic Z ACS Med Chem Lett. 2022 Feb 21;13(3):475-482. doi:, 10.1021/acsmedchemlett.1c00650. eCollection 2022 Mar 10. PMID:35300081<ref>PMID:35300081</ref> | |||
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |||
</div> | |||
<div class="pdbe-citations 7shh" style="background-color:#fffaf0;"></div> | |||
== References == | |||
<references/> | |||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: Magnetospirillum gryphiswaldense]] | |||
[[Category: Fischer M]] | [[Category: Fischer M]] | ||
[[Category: Nithianantham S]] | [[Category: Nithianantham S]] | ||
Latest revision as of 13:43, 22 May 2024
Bacterial cereblon homologue in complex with (R)-3-(4-methoxyphenyl)piperidine-2,6-dioneBacterial cereblon homologue in complex with (R)-3-(4-methoxyphenyl)piperidine-2,6-dione
Structural highlights
FunctionPublication Abstract from PubMedAberrant activation of the JAK-STAT signaling pathway has been implicated in the pathogenesis of a range of hematological malignancies and autoimmune disorders. Here we describe the design, synthesis, and characterization of JAK2/3 PROTACs utilizing a phenyl glutarimide (PG) ligand as the cereblon (CRBN) recruiter. SJ10542 displayed high selectivity over GSPT1 and other members of the JAK family and potency in patient-derived ALL cells containing both JAK2 fusions and CRLF2 rearrangements. Development of Potent and Selective Janus Kinase 2/3 Directing PG-PROTACs.,Alcock LJ, Chang Y, Jarusiewicz JA, Actis M, Nithianantham S, Mayasundari A, Min J, Maxwell D, Hunt J, Smart B, Yang JJ, Nishiguchi G, Fischer M, Mullighan CG, Rankovic Z ACS Med Chem Lett. 2022 Feb 21;13(3):475-482. doi:, 10.1021/acsmedchemlett.1c00650. eCollection 2022 Mar 10. PMID:35300081[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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