5fzh

From Proteopedia

(Difference between revisions)

Revision as of 22:58, 1 June 2016

Crystal structure of the catalytic domain of human JARID1B in complex with Maybridge fragment 4,5-dihydronaphtho(1,2-b)thiophene-2- carboxylicacid (N11181a) (ligand modelled based on PANDDA event map, SGC - Diamond I04-1 fragment screening)

Structural highlights

5fzh is a 1 chain structure. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	, , , , , ,
Related:	5fyc, 5fyh, 5fyi, 5fym, 5fys, 5fyt, 5fyu, 5fyv, 5fyy, 5fyz, 5fz0, 5fz1, 5fz3, 5fz4, 5fz6, 5fz7, 5fz8, 5fz9, 5fza, 5fzb, 5fzc, 5fzd, 5fze, 5fzf, 5fzg, 5fzi, 5fzk, 5fzl, 5fzm, 5fzo
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum

Function

[KDM5B_HUMAN] Histone demethylase that demethylates 'Lys-4' of histone H3, thereby playing a central role in histone code. Does not demethylate histone H3 'Lys-9' or H3 'Lys-27'. Demethylates trimethylated, dimethylated and monomethylated H3 'Lys-4'. Acts as a transcriptional corepressor for FOXG1B and PAX9. Favors the proliferation of breast cancer cells by repressing tumor suppressor genes such as BRCA1 and HOXA5. In contrast, may act as a tumor suppressor for melanoma.^[1] ^[2] ^[3] ^[4]

References

↑ Tan K, Shaw AL, Madsen B, Jensen K, Taylor-Papadimitriou J, Freemont PS. Human PLU-1 Has transcriptional repression properties and interacts with the developmental transcription factors BF-1 and PAX9. J Biol Chem. 2003 Jun 6;278(23):20507-13. Epub 2003 Mar 25. PMID:12657635 doi:http://dx.doi.org/10.1074/jbc.M301994200
↑ Roesch A, Becker B, Schneider-Brachert W, Hagen I, Landthaler M, Vogt T. Re-expression of the retinoblastoma-binding protein 2-homolog 1 reveals tumor-suppressive functions in highly metastatic melanoma cells. J Invest Dermatol. 2006 Aug;126(8):1850-9. Epub 2006 Apr 27. PMID:16645588 doi:http://dx.doi.org/10.1038/sj.jid.5700324
↑ Christensen J, Agger K, Cloos PA, Pasini D, Rose S, Sennels L, Rappsilber J, Hansen KH, Salcini AE, Helin K. RBP2 belongs to a family of demethylases, specific for tri-and dimethylated lysine 4 on histone 3. Cell. 2007 Mar 23;128(6):1063-76. Epub 2007 Feb 22. PMID:17320161 doi:S0092-8674(07)00182-1
↑ Yamane K, Tateishi K, Klose RJ, Fang J, Fabrizio LA, Erdjument-Bromage H, Taylor-Papadimitriou J, Tempst P, Zhang Y. PLU-1 is an H3K4 demethylase involved in transcriptional repression and breast cancer cell proliferation. Mol Cell. 2007 Mar 23;25(6):801-12. Epub 2007 Mar 15. PMID:17363312 doi:http://dx.doi.org/S1097-2765(07)00146-3

1 Structural highlights
2 Function
3 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/5fzh"

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
-The entry 5fzh is ON HOLD
+==Crystal structure of the catalytic domain of human JARID1B in complex with Maybridge fragment 4,5-dihydronaphtho(1,2-b)thiophene-2- carboxylicacid (N11181a) (ligand modelled based on PANDDA event map, SGC - Diamond I04-1 fragment screening)==
+<StructureSection load='5fzh' size='340' side='right' caption='[[5fzh]], [[Resolution|resolution]] 2.09&Aring;' scene=''>
-Authors: Nowak, R., Krojer, T., Johansson, C., Kupinska, K., Szykowska, A., Pearce, N., Talon, R., Collins, P., Gileadi, C., Strain-Damerell, C., Burgess-Brown, N.A., Arrowsmith, C.H., Bountra, C., Edwards, A.M., Von Delft, F., Brennan, P.E., Oppermann, U.
+== Structural highlights ==
+<table><tr><td colspan='2'>[[5fzh]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5FZH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5FZH FirstGlance]. <br>
-Description: Crystal structure of the catalytic domain of human JARID1B in complex with Maybridge fragment 4,5-dihydronaphtho(1,2-b)thiophene-2-carboxylicacid (N11181a) (ligand modelled based on PANDDA event map, SGC -Diamond I04-1 fragment screening)
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0TI:(3R)-5-FLUORO-3-HYDROXY-1,3-DIHYDRO-2H-INDOL-2-ONE'>0TI</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=EPE:4-(2-HYDROXYETHYL)-1-PIPERAZINE+ETHANESULFONIC+ACID'>EPE</scene>, <scene name='pdbligand=MN:MANGANESE+(II)+ION'>MN</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
-[[Category: Unreleased Structures]]
+<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5fyc|5fyc]], [[5fyh|5fyh]], [[5fyi|5fyi]], [[5fym|5fym]], [[5fys|5fys]], [[5fyt|5fyt]], [[5fyu|5fyu]], [[5fyv|5fyv]], [[5fyy|5fyy]], [[5fyz|5fyz]], [[5fz0|5fz0]], [[5fz1|5fz1]], [[5fz3|5fz3]], [[5fz4|5fz4]], [[5fz6|5fz6]], [[5fz7|5fz7]], [[5fz8|5fz8]], [[5fz9|5fz9]], [[5fza|5fza]], [[5fzb|5fzb]], [[5fzc|5fzc]], [[5fzd|5fzd]], [[5fze|5fze]], [[5fzf|5fzf]], [[5fzg|5fzg]], [[5fzi|5fzi]], [[5fzk|5fzk]], [[5fzl|5fzl]], [[5fzm|5fzm]], [[5fzo|5fzo]]</td></tr>
-[[Category: Nowak, R]]
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5fzh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5fzh OCA], [http://pdbe.org/5fzh PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5fzh RCSB], [http://www.ebi.ac.uk/pdbsum/5fzh PDBsum]</span></td></tr>
-[[Category: Burgess-Brown, N.A]]
+</table>
-[[Category: Krojer, T]]
+== Function ==
+[[http://www.uniprot.org/uniprot/KDM5B_HUMAN KDM5B_HUMAN]] Histone demethylase that demethylates 'Lys-4' of histone H3, thereby playing a central role in histone code. Does not demethylate histone H3 'Lys-9' or H3 'Lys-27'. Demethylates trimethylated, dimethylated and monomethylated H3 'Lys-4'. Acts as a transcriptional corepressor for FOXG1B and PAX9. Favors the proliferation of breast cancer cells by repressing tumor suppressor genes such as BRCA1 and HOXA5. In contrast, may act as a tumor suppressor for melanoma.<ref>PMID:12657635</ref> <ref>PMID:16645588</ref> <ref>PMID:17320161</ref> <ref>PMID:17363312</ref>
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Arrowsmith, C H]]
 [[Category: Bountra, C]]
-[[Category: Kupinska, K]]
+[[Category: Brennan, P E]]
+[[Category: Burgess-Brown, N A]]
 [[Category: Collins, P]]
-[[Category: Arrowsmith, C.H]]
+[[Category: Delft, F Von]]
+[[Category: Edwards, A M]]
 [[Category: Gileadi, C]]
+[[Category: Johansson, C]]
+[[Category: Krojer, T]]
+[[Category: Kupinska, K]]
+[[Category: Nowak, R]]
 [[Category: Oppermann, U]]
+[[Category: Pearce, N]]
+[[Category: Strain-Damerell, C]]
 [[Category: Szykowska, A]]
-[[Category: Von Delft, F]]
-[[Category: Pearce, N]]
-[[Category: Edwards, A.M]]
 [[Category: Talon, R]]
-[[Category: Johansson, C]]
+[[Category: Diamond i04-1]]
-[[Category: Brennan, P.E]]
+[[Category: Fragment screening]]
-[[Category: Strain-Damerell, C]]
+[[Category: Jarid1b]]
+[[Category: Oxidoreductase]]
+[[Category: Pandda]]
+[[Category: Plu1]]
+[[Category: Sgc]]
+[[Category: Structural genomic]]

5fzh

From Proteopedia

Revision as of 22:58, 1 June 2016

Crystal structure of the catalytic domain of human JARID1B in complex with Maybridge fragment 4,5-dihydronaphtho(1,2-b)thiophene-2- carboxylicacid (N11181a) (ligand modelled based on PANDDA event map, SGC - Diamond I04-1 fragment screening)

Structural highlights

Function

References

Contents

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