6bh8

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
m (Protected "6bh8" [edit=sysop:move=sysop])
Line 1: Line 1:
-
'''Unreleased structure'''
 
-
The entry 6bh8 is ON HOLD until Paper Publication
+
==Crystal structure of ZMPSTE24 in complex with phosphoramidon==
 +
<StructureSection load='6bh8' size='340' side='right' caption='[[6bh8]], [[Resolution|resolution]] 3.85&Aring;' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[6bh8]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6BH8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6BH8 FirstGlance]. <br>
 +
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=C8E:(HYDROXYETHYLOXY)TRI(ETHYLOXY)OCTANE'>C8E</scene>, <scene name='pdbligand=RDF:N-ALPHA-L-RHAMNOPYRANOSYLOXY(HYDROXYPHOSPHINYL)-L-LEUCYL-L-TRYPTOPHAN'>RDF</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
 +
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5syt|5syt]], [[4aw6|4aw6]], [[2ypt|2ypt]]</td></tr>
 +
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Ste24_endopeptidase Ste24 endopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.84 3.4.24.84] </span></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=6bh8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6bh8 OCA], [http://pdbe.org/6bh8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6bh8 RCSB], [http://www.ebi.ac.uk/pdbsum/6bh8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6bh8 ProSAT]</span></td></tr>
 +
</table>
 +
== Disease ==
 +
[[http://www.uniprot.org/uniprot/FACE1_HUMAN FACE1_HUMAN]] Mandibuloacral dysplasia with type B lipodystrophy;Hutchinson-Gilford progeria syndrome;Lethal restrictive dermopathy. Mandibuloacral dysplasia with type B lipodystrophy (MADB) [MIM:[http://omim.org/entry/608612 608612]]: A disorder characterized by mandibular and clavicular hypoplasia, acroosteolysis, delayed closure of the cranial suture, joint contractures, and generalized lipodystrophy with loss of subcutaneous fat from the extremities, face, neck and trunk. Note=The disease is caused by mutations affecting the gene represented in this entry.<ref>PMID:12913070</ref> <ref>PMID:17152860</ref> <ref>PMID:18435794</ref> <ref>PMID:20814950</ref> Lethal tight skin contracture syndrome (LTSCS) [MIM:[http://omim.org/entry/275210 275210]]: Rare disorder mainly characterized by intrauterine growth retardation, tight and rigid skin with erosions, prominent superficial vasculature and epidermal hyperkeratosis, facial features (small mouth, small pinched nose and micrognathia), sparse/absent eyelashes and eyebrows, mineralization defects of the skull, thin dysplastic clavicles, pulmonary hypoplasia, multiple joint contractures and an early neonatal lethal course. Liveborn children usually die within the first week of life. The overall prevalence of consanguineous cases suggested an autosomal recessive inheritance. Note=The disease is caused by mutations affecting the gene represented in this entry.<ref>PMID:15317753</ref>
 +
== Function ==
 +
[[http://www.uniprot.org/uniprot/FACE1_HUMAN FACE1_HUMAN]] Proteolytically removes the C-terminal three residues of farnesylated proteins. Acts on lamin A/C.
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
The integral membrane protein zinc metalloprotease ZMPSTE24 possesses a completely novel structure, comprising seven long kinked transmembrane helices that encircle a voluminous 14 000 A(3) cavity within the membrane. Functionally conserved soluble zinc metalloprotease residues are contained within this cavity. As part of an effort to understand the structural and functional relationships between ZMPSTE24 and soluble zinc metalloproteases, the inhibition of ZMPSTE24 by phosphoramidon [N-(alpha-rhamnopyranosyl-oxyhydroxyphosphinyl)-Leu-Trp], a transition-state analog and competitive inhibitor of multiple soluble zinc metalloproteases, especially gluzincins, has been characterized functionally and structurally. The functional results, the determination of preliminary IC50 values by the use of an intramolecular quenched-fluorescence fluorogenic peptide assay, indicate that phosphoramidon inhibits ZMPSTE24 in a manner consistent with competitive inhibition. The structural results, a 3.85 A resolution X-ray crystal structure of a ZMPSTE24-phosphoramidon complex, indicate that the overall binding mode observed between phosphoramidon and soluble gluzincins is conserved. Based on the structural data, a significantly lower potency than that observed for soluble gluzincins such as thermolysin and neprilysin is predicted. These results strongly suggest a close relationship between soluble gluzincins and the integral membrane protein zinc metalloprotease ZMPSTE24.
-
Authors: Goblirsch, B.R., Arachea, B.T., Wiener, M.C.
+
Phosphoramidon inhibits the integral membrane protein zinc metalloprotease ZMPSTE24.,Goblirsch BR, Arachea BT, Councell DJ, Wiener MC Acta Crystallogr D Struct Biol. 2018 Aug 1;74(Pt 8):739-747. doi:, 10.1107/S2059798318003431. Epub 2018 Jul 24. PMID:30082509<ref>PMID:30082509</ref>
-
Description: Crystal structure of ZMPSTE24 in complex with phosphoramidon
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-
[[Category: Unreleased Structures]]
+
</div>
-
[[Category: Wiener, M.C]]
+
<div class="pdbe-citations 6bh8" style="background-color:#fffaf0;"></div>
-
[[Category: Arachea, B.T]]
+
== References ==
-
[[Category: Goblirsch, B.R]]
+
<references/>
 +
__TOC__
 +
</StructureSection>
 +
[[Category: Ste24 endopeptidase]]
 +
[[Category: Arachea, B T]]
 +
[[Category: Goblirsch, B R]]
 +
[[Category: Wiener, M C]]
 +
[[Category: Hydrolase]]
 +
[[Category: Inhibitor complex]]
 +
[[Category: Integral membrane protein]]
 +
[[Category: Zinc metalloprotease]]

Revision as of 16:11, 15 August 2018

Crystal structure of ZMPSTE24 in complex with phosphoramidon

6bh8, resolution 3.85Å

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/6bh8"
Personal tools