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7sj3

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'''Unreleased structure'''
 
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The entry 7sj3 is ON HOLD until Paper Publication
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==Structure of CDK4-Cyclin D3 bound to abemaciclib==
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<StructureSection load='7sj3' size='340' side='right'caption='[[7sj3]], [[Resolution|resolution]] 2.51&Aring;' scene=''>
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Authors:
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== Structural highlights ==
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<table><tr><td colspan='2'>[[7sj3]] 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=7SJ3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7SJ3 FirstGlance]. <br>
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Description:
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6ZV:N-{5-[(4-ETHYLPIPERAZIN-1-YL)METHYL]PYRIDIN-2-YL}-5-FLUORO-4-[4-FLUORO-2-METHYL-1-(PROPAN-2-YL)-1H-BENZIMIDAZOL-6-YL]PYRIMIDIN-2-AMINE'>6ZV</scene>, <scene name='pdbligand=ACE:ACETYL+GROUP'>ACE</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
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[[Category: Unreleased Structures]]
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7sj3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7sj3 OCA], [https://pdbe.org/7sj3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7sj3 RCSB], [https://www.ebi.ac.uk/pdbsum/7sj3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7sj3 ProSAT]</span></td></tr>
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</table>
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== Disease ==
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[https://www.uniprot.org/uniprot/CDK4_HUMAN CDK4_HUMAN] Defects in CDK4 are a cause of susceptibility to cutaneous malignant melanoma type 3 (CMM3) [MIM:[https://omim.org/entry/609048 609048]. Malignant melanoma is a malignant neoplasm of melanocytes, arising de novo or from a pre-existing benign nevus, which occurs most often in the skin but also may involve other sites.<ref>PMID:7652577</ref> <ref>PMID:8528263</ref> <ref>PMID:9311594</ref> <ref>PMID:9425228</ref>
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== Function ==
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[https://www.uniprot.org/uniprot/CDK4_HUMAN CDK4_HUMAN] Ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G(1)/S transition. Phosphorylation of RB1 allows dissociation of the transcription factor E2F from the RB/E2F complexes and the subsequent transcription of E2F target genes which are responsible for the progression through the G(1) phase. Hypophosphorylates RB1 in early G(1) phase. Cyclin D-CDK4 complexes are major integrators of various mitogenenic and antimitogenic signals. Also phosphorylates SMAD3 in a cell-cycle-dependent manner and represses its transcriptional activity. Component of the ternary complex, cyclin D/CDK4/CDKN1B, required for nuclear translocation and activity of the cyclin D-CDK4 complex.<ref>PMID:9003781</ref> <ref>PMID:15241418</ref> <ref>PMID:18827403</ref>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Hilgers MT]]
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[[Category: Pelletier LA]]

Revision as of 07:14, 3 November 2022

Structure of CDK4-Cyclin D3 bound to abemaciclib

PDB ID 7sj3

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