4b9k

From Proteopedia

(Difference between revisions)

Current revision

pVHL-ELOB-ELOC complex_(2S,4R)-1-(3-amino-2-methylbenzoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide bound

Structural highlights

4b9k is a 12 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2Å
Ligands:	, ,
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

ELOC_HUMAN SIII, also known as elongin, is a general transcription elongation factor that increases the RNA polymerase II transcription elongation past template-encoded arresting sites. Subunit A is transcriptionally active and its transcription activity is strongly enhanced by binding to the dimeric complex of the SIII regulatory subunits B and C (elongin BC complex).^[1] The elongin BC complex seems to be involved as an adapter protein in the proteasomal degradation of target proteins via different E3 ubiquitin ligase complexes, including the von Hippel-Lindau ubiquitination complex CBC(VHL). By binding to BC-box motifs it seems to link target recruitment subunits, like VHL and members of the SOCS box family, to Cullin/RBX1 modules that activate E2 ubiquitination enzymes.^[2]

Publication Abstract from PubMed

By design: Novel small-molecule inhibitors of the interaction between the von Hippel-Lindau ligase (VHL) and its molecular target HIF1alpha, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC(50) value of 0.9 microM and is thus the first sub-micromolar inhibitor of the VHL-HIF1alpha interaction.

Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1alpha,Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM Angew Chem Int Ed Engl. 2012 Oct 12. doi: 10.1002/anie.201206231. PMID:23065727^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Kario E, Marmor MD, Adamsky K, Citri A, Amit I, Amariglio N, Rechavi G, Yarden Y. Suppressors of cytokine signaling 4 and 5 regulate epidermal growth factor receptor signaling. J Biol Chem. 2005 Feb 25;280(8):7038-48. Epub 2004 Dec 7. PMID:15590694 doi:10.1074/jbc.M408575200
↑ Kario E, Marmor MD, Adamsky K, Citri A, Amit I, Amariglio N, Rechavi G, Yarden Y. Suppressors of cytokine signaling 4 and 5 regulate epidermal growth factor receptor signaling. J Biol Chem. 2005 Feb 25;280(8):7038-48. Epub 2004 Dec 7. PMID:15590694 doi:10.1074/jbc.M408575200
↑ Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM. Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1alpha Angew Chem Int Ed Engl. 2012 Oct 12. doi: 10.1002/anie.201206231. PMID:23065727 doi:http://dx.doi.org/10.1002/anie.201206231

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 See Also
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4b9k"

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
-The entry 4b9k is ON HOLD
+==pVHL-ELOB-ELOC complex_(2S,4R)-1-(3-amino-2-methylbenzoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide bound==
+<StructureSection load='4b9k' size='340' side='right'caption='[[4b9k]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
+== Structural highlights ==
+<table><tr><td colspan='2'>[[4b9k]] is a 12 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=4B9K OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4B9K 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]] 2&#8491;</td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ACT:ACETATE+ION'>ACT</scene>, <scene name='pdbligand=CAS:S-(DIMETHYLARSENIC)CYSTEINE'>CAS</scene>, <scene name='pdbligand=TG0:(2S,4R)-1-(3-AMINO-2-METHYLBENZOYL)-4-HYDROXY-N-(4-(4-METHYLTHIAZOL-5-YL)BENZYL)PYRROLIDINE-2-CARBOXAMIDE'>TG0</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=4b9k FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4b9k OCA], [https://pdbe.org/4b9k PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4b9k RCSB], [https://www.ebi.ac.uk/pdbsum/4b9k PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4b9k ProSAT]</span></td></tr>
+</table>
+== Function ==
+[https://www.uniprot.org/uniprot/ELOC_HUMAN ELOC_HUMAN] SIII, also known as elongin, is a general transcription elongation factor that increases the RNA polymerase II transcription elongation past template-encoded arresting sites. Subunit A is transcriptionally active and its transcription activity is strongly enhanced by binding to the dimeric complex of the SIII regulatory subunits B and C (elongin BC complex).<ref>PMID:15590694</ref>   The elongin BC complex seems to be involved as an adapter protein in the proteasomal degradation of target proteins via different E3 ubiquitin ligase complexes, including the von Hippel-Lindau ubiquitination complex CBC(VHL). By binding to BC-box motifs it seems to link target recruitment subunits, like VHL and members of the SOCS box family, to Cullin/RBX1 modules that activate E2 ubiquitination enzymes.<ref>PMID:15590694</ref>
+<div style="background-color:#fffaf0;">
+== Publication Abstract from PubMed ==
+By design: Novel small-molecule inhibitors of the interaction between the von Hippel-Lindau ligase (VHL) and its molecular target HIF1alpha, a transcription factor involved in oxygen sensing, have been developed and studied. The most potent inhibitor binds with an IC(50) value of 0.9 microM and is thus the first sub-micromolar inhibitor of the VHL-HIF1alpha interaction.
-Authors: Buckley, D.L., Gustafson, J.L., VanMolle, I., Roth, A.G., SeopTae, H., Gareiss, P.C., Jorgensen, W.L., Ciulli, A., Crews, C.M.
+Small-Molecule Inhibitors of the Interaction between the E3 Ligase VHL and HIF1alpha,Buckley DL, Gustafson JL, Van Molle I, Roth AG, Tae HS, Gareiss PC, Jorgensen WL, Ciulli A, Crews CM Angew Chem Int Ed Engl. 2012 Oct 12. doi: 10.1002/anie.201206231. PMID:23065727<ref>PMID:23065727</ref>
-Description: pVHL:ElonginB:ElonginC complex_3-PYRIDIN-4-YL-2,4-DIHYDRO-INDENO1,2-. C.PYRAZOLEbound
+From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
+</div>
+<div class="pdbe-citations 4b9k" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[Elongation factor 3D structures|Elongation factor 3D structures]]
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Homo sapiens]]
+[[Category: Large Structures]]
+[[Category: Buckley DL]]
+[[Category: Ciulli A]]
+[[Category: Crews CM]]
+[[Category: Gareiss PC]]
+[[Category: Gustafson JL]]
+[[Category: Jorgensen WL]]
+[[Category: Roth AG]]
+[[Category: SeopTae H]]
+[[Category: VanMolle I]]

4b9k

From Proteopedia

Current revision

pVHL-ELOB-ELOC complex_(2S,4R)-1-(3-amino-2-methylbenzoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide bound

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

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