4lce

From Proteopedia

(Difference between revisions)

Revision as of 19:33, 25 December 2014

CtBP1 in complex with substrate MTOB

Structural highlights

4lce is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Related:	4lcj
Gene:	CTBP, CTBP1 (HUMAN)
Resources:	FirstGlance, OCA, RCSB, PDBsum

Function

[CTBP1_HUMAN] Involved in controlling the equilibrium between tubular and stacked structures in the Golgi complex. Functions in brown adipose tissue (BAT) differentiation. Corepressor targeting diverse transcription regulators such as GLIS2. Has dehydrogenase activity.^[1] ^[2] ^[3] ^[4]

Publication Abstract from PubMed

The oncogenic corepressors C-terminal Binding Protein (CtBP) 1 and 2 harbor regulatory d-isomer specific 2-hydroxyacid dehydrogenase (d2-HDH) domains. 4-Methylthio 2-oxobutyric acid (MTOB) exhibits substrate inhibition and can interfere with CtBP oncogenic activity in cell culture and mice. Crystal structures of human CtBP1 and CtBP2 in complex with MTOB and NAD+ revealed two key features: a conserved tryptophan that likely contributes to substrate specificity and a hydrophilic cavity that links MTOB with an NAD+ phosphate. Neither feature is present in other d2-HDH enzymes. These structures thus offer key opportunities for the development of highly selective anti-neoplastic CtBP inhibitors.

Crystal structures of human CtBP in complex with substrate MTOB reveal active site features useful for inhibitor design.,Hilbert BJ, Grossman SR, Schiffer CA, Royer WE Jr FEBS Lett. 2014 Mar 19. pii: S0014-5793(14)00231-2. doi:, 10.1016/j.febslet.2014.03.026. PMID:24657618^[5]

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

References

↑ Sewalt RG, Gunster MJ, van der Vlag J, Satijn DP, Otte AP. C-Terminal binding protein is a transcriptional repressor that interacts with a specific class of vertebrate Polycomb proteins. Mol Cell Biol. 1999 Jan;19(1):777-87. PMID:9858600
↑ Alpatov R, Munguba GC, Caton P, Joo JH, Shi Y, Shi Y, Hunt ME, Sugrue SP. Nuclear speckle-associated protein Pnn/DRS binds to the transcriptional corepressor CtBP and relieves CtBP-mediated repression of the E-cadherin gene. Mol Cell Biol. 2004 Dec;24(23):10223-35. PMID:15542832 doi:http://dx.doi.org/10.1128/MCB.24.23.10223-10235.2004
↑ Purbey PK, Singh S, Notani D, Kumar PP, Limaye AS, Galande S. Acetylation-dependent interaction of SATB1 and CtBP1 mediates transcriptional repression by SATB1. Mol Cell Biol. 2009 Mar;29(5):1321-37. doi: 10.1128/MCB.00822-08. Epub 2008 Dec, 22. PMID:19103759 doi:10.1128/MCB.00822-08
↑ Kumar V, Carlson JE, Ohgi KA, Edwards TA, Rose DW, Escalante CR, Rosenfeld MG, Aggarwal AK. Transcription corepressor CtBP is an NAD(+)-regulated dehydrogenase. Mol Cell. 2002 Oct;10(4):857-69. PMID:12419229
↑ Hilbert BJ, Grossman SR, Schiffer CA, Royer WE Jr. Crystal structures of human CtBP in complex with substrate MTOB reveal active site features useful for inhibitor design. FEBS Lett. 2014 Mar 19. pii: S0014-5793(14)00231-2. doi:, 10.1016/j.febslet.2014.03.026. PMID:24657618 doi:http://dx.doi.org/10.1016/j.febslet.2014.03.026

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

Proteopedia Page Contributors and Editors (what is this?)

OCA

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

@@ Line 2: / Line 2: @@
 <StructureSection load='4lce' size='340' side='right' caption='[[4lce]], [[Resolution|resolution]] 2.38&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[4lce]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LCE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4LCE FirstGlance]. <br>
+<table><tr><td colspan='2'>[[4lce]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4LCE OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4LCE FirstGlance]. <br>
 </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=KMT:4-(METHYLSULFANYL)-2-OXOBUTANOIC+ACID'>KMT</scene>, <scene name='pdbligand=NAD:NICOTINAMIDE-ADENINE-DINUCLEOTIDE'>NAD</scene></td></tr>
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lcj|4lcj]]</td></tr>
+<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CTBP, CTBP1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
 <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=4lce FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lce OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4lce RCSB], [http://www.ebi.ac.uk/pdbsum/4lce PDBsum]</span></td></tr>
 </table>
+== Function ==
+[[http://www.uniprot.org/uniprot/CTBP1_HUMAN CTBP1_HUMAN]] Involved in controlling the equilibrium between tubular and stacked structures in the Golgi complex. Functions in brown adipose tissue (BAT) differentiation. Corepressor targeting diverse transcription regulators such as GLIS2. Has dehydrogenase activity.<ref>PMID:9858600</ref> <ref>PMID:15542832</ref> <ref>PMID:19103759</ref> <ref>PMID:12419229</ref>
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==
@@ Line 19: / Line 22: @@
 __TOC__
 </StructureSection>
+[[Category: Human]]
 [[Category: Hilbert, B J]]
 [[Category: Royer, W E]]

4lce

From Proteopedia

Revision as of 19:33, 25 December 2014

CtBP1 in complex with substrate MTOB

Structural highlights

Function

Publication Abstract from PubMed

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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