4u90: Difference between revisions

From Proteopedia
Jump to navigationJump to search
← Older editNewer edit →
OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,331,613 edits
No edit summary
OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,331,613 edits
No edit summary
Line 1: Line 1:
'''Unreleased structure'''
==GephE in complex with PEG crosslinked GABA receptor alpha3 subunit derived dimeric peptide==
<StructureSection load='4u90' size='340' side='right' caption='[[4u90]], [[Resolution|resolution]] 2.00&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4u90]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4U90 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4U90 FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3F8:1,1-[ETHANE-1,2-DIYLBIS(OXYETHANE-2,1-DIYL)]BIS(1H-PYRROLE-2,5-DIONE)'>3F8</scene>, <scene name='pdbligand=BU1:1,4-BUTANEDIOL'>BU1</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4u91|4u91]], [[4pd0|4pd0]], [[4pd1|4pd1]], [[4tk1|4tk1]], [[4tk2|4tk2]], [[4tk3|4tk3]], [[4tk4|4tk4]]</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=4u90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4u90 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4u90 RCSB], [http://www.ebi.ac.uk/pdbsum/4u90 PDBsum]</span></td></tr>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Gephyrin is the central scaffolding protein for inhibitory neurotransmitter receptors in the brain. Here we describe the development of dimeric peptides that inhibit the interaction between gephyrin and these receptors, a process which is fundamental to numerous synaptic functions and diseases of the brain. We first identified receptor-derived minimal gephyrin-binding peptides that displayed exclusive binding towards native gephyrin from brain lysates. We then designed and synthesized a series of dimeric ligands, which led to a remarkable 1220-fold enhancement of the gephyrin affinity (KD =6.8 nM). In X-ray crystal structures we visualized the simultaneous dimer-to-dimer binding in atomic detail, revealing compound-specific binding modes. Thus, we defined the molecular basis of the affinity-enhancing effect of multivalent gephyrin inhibitors and provide conceptually novel compounds with therapeutic potential, which will allow further elucidation of the gephyrin-receptor interplay.


The entry 4u90 is ON HOLD  until Paper Publication
Design and Synthesis of High-Affinity Dimeric Inhibitors Targeting the Interactions between Gephyrin and Inhibitory Neurotransmitter Receptors.,Maric HM, Kasaragod VB, Haugaard-Kedstrom L, Hausrat TJ, Kneussel M, Schindelin H, Stromgaard K Angew Chem Int Ed Engl. 2014 Nov 20. doi: 10.1002/anie.201409043. PMID:25413248<ref>PMID:25413248</ref>


Authors: Kasaragod, V.B., Maric, H.M., Schindelin, H.
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 
</div>
Description:
== References ==
<references/>
__TOC__
</StructureSection>
[[Category: Kasaragod, V B]]
[[Category: Maric, H M]]
[[Category: Schindelin, H]]
[[Category: Gaba type a receptor]]
[[Category: Inhibitory synapse]]
[[Category: Scaffolding protein]]
[[Category: Transfer protein - structural protein complex]]
[[Category: Transferase]]
Retrieved from "https://proteopedia.org/4u90"