2p5h

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
m (Protected "2p5h" [edit=sysop:move=sysop])
Line 1: Line 1:
-
[[Image:2p5h.png|left|200px]]
+
==sPLA2 inhibitor 9==
 +
<StructureSection load='2p5h' size='340' side='right' caption='[[2p5h]], [[NMR_Ensembles_of_Models | 20 NMR models]]' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[2p5h]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2P5H OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2P5H FirstGlance]. <br>
 +
</td></tr><tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2p5j|2p5j]], [[2p60|2p60]]</td></tr>
 +
<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2p5h FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2p5h OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2p5h RCSB], [http://www.ebi.ac.uk/pdbsum/2p5h PDBsum]</span></td></tr>
 +
<table>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
Secretory phospholipase A2 (sPLA2) and matrix metallopreoteinases (MMPs) are key enzymes involved in rheumatoid arthritis (RA), and their modulation thus represents a potential therapeutic option. On the basis of Escherichia coli radioassay, synthetic peptides were designed and screened for sPLA2 inhibition. The linear peptide, 10f (PIP-18), inhibited the recombinant human synovial sPLA2 activity with an IC50 of 1.19 microM. Not only did the peptide interfere with the function of sPLA2, but it also appeared to inhibit mRNA expression of sPLA2 and various MMPs in IL-1beta-stimulated RA synovial fibroblast (RASF) cultures and thereby the production of the corresponding proteins (&gt;80% inhibition). Nuclear magnetic resonance (NMR), modeling, and docking studies indicate that in solution the peptide exhibits a beta-turn at residues Trp-Asp-Gly-Val and possibly binds to the hydrophobic channel of sPLA2. The results strongly suggest that the modulatory action of peptide 10f may play a major role in counteracting the development of RA.
-
{{STRUCTURE_2p5h| PDB=2p5h | SCENE= }}
+
Novel peptide inhibitors of human secretory phospholipase A2 with antiinflammatory activity: solution structure and molecular modeling.,Thwin MM, Satyanarayanajois SD, Nagarajarao LM, Sato K, Arjunan P, Ramapatna SL, Kumar PV, Gopalakrishnakone P J Med Chem. 2007 Nov 29;50(24):5938-50. Epub 2007 Nov 1. PMID:17973469<ref>PMID:17973469</ref>
-
===sPLA2 inhibitor 9===
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-
 
+
</div>
-
{{ABSTRACT_PUBMED_17973469}}
+
== References ==
-
 
+
<references/>
-
==About this Structure==
+
__TOC__
-
[[2p5h]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2P5H OCA].
+
</StructureSection>
-
 
+
-
==Reference==
+
-
<ref group="xtra">PMID:017973469</ref><references group="xtra"/>
+
[[Category: Arjunan, P.]]
[[Category: Arjunan, P.]]
[[Category: Gopalakrishnakone, P P.]]
[[Category: Gopalakrishnakone, P P.]]

Revision as of 07:05, 9 June 2014

sPLA2 inhibitor 9

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/2p5h"
Views
Personal tools
Navigation
Toolbox