6iql

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
-
'''Unreleased structure'''
 
-
The entry 6iql is ON HOLD
+
==Crystal structure of dopamine receptor D4 bound to the subtype-selective ligand, L745870==
 +
<StructureSection load='6iql' size='340' side='right'caption='[[6iql]], [[Resolution|resolution]] 3.50&Aring;' scene=''>
 +
== Structural highlights ==
 +
<table><tr><td colspan='2'>[[6iql]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6IQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6IQL FirstGlance]. <br>
 +
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=L74:3-{[4-(4-chlorophenyl)piperazin-1-yl]methyl}-1H-pyrrolo[2,3-b]pyridine'>L74</scene></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=6iql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6iql OCA], [http://pdbe.org/6iql PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6iql RCSB], [http://www.ebi.ac.uk/pdbsum/6iql PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6iql ProSAT]</span></td></tr>
 +
</table>
 +
== Function ==
 +
[[http://www.uniprot.org/uniprot/DRD4_MOUSE DRD4_MOUSE]] Dopamine receptor responsible for neuronal signaling in the mesolimbic system of the brain, an area of the brain that regulates emotion and complex behavior. Activated by dopamine, but also by epinephrine and norepinephrine, and by numerous synthetic agonists and drugs. Agonist binding triggers signaling via G proteins that inhibit adenylyl cyclase (By similarity). Modulates the circadian rhythm of contrast sensitivity by regulating the rhythmic expression of NPAS2 in the retinal ganglion cells (PubMed:24048828).[UniProtKB:P21917]<ref>PMID:24048828</ref>
 +
<div style="background-color:#fffaf0;">
 +
== Publication Abstract from PubMed ==
 +
Multiple subtypes of dopamine receptors within the GPCR superfamily regulate neurological processes through various downstream signaling pathways. A crucial question about the dopamine receptor family is what structural features determine the subtype-selectivity of potential drugs. Here, we report the 3.5-angstrom crystal structure of mouse dopamine receptor D4 (DRD4) complexed with a subtype-selective antagonist, L745870. Our structure reveals a secondary binding pocket extended from the orthosteric ligand-binding pocket to a DRD4-specific crevice located between transmembrane helices 2 and 3. Additional mutagenesis studies suggest that the antagonist L745870 prevents DRD4 activation by blocking the relative movement between transmembrane helices 2 and 3. These results expand our knowledge of the molecular basis for the physiological functions of DRD4 and assist new drug design.
-
Authors: Ye, Z., Can, C., Zhang, X.C.
+
Crystal structure of dopamine receptor D4 bound to the subtype selective ligand, L745870.,Zhou Y, Cao C, He L, Wang X, Zhang XC Elife. 2019 Nov 21;8. pii: 48822. doi: 10.7554/eLife.48822. PMID:31750832<ref>PMID:31750832</ref>
-
Description: Crystal structure of dopamine receptor D4 bound to the subtype-selective ligand, L745870
+
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
-
[[Category: Unreleased Structures]]
+
</div>
-
[[Category: Can, C]]
+
<div class="pdbe-citations 6iql" style="background-color:#fffaf0;"></div>
-
[[Category: Ye, Z]]
+
== References ==
-
[[Category: Zhang, X.C]]
+
<references/>
 +
__TOC__
 +
</StructureSection>
 +
[[Category: Large Structures]]
 +
[[Category: Cao, C]]
 +
[[Category: Zhang, X C]]
 +
[[Category: Zhou, Y]]
 +
[[Category: Dimerization]]
 +
[[Category: Drd4]]
 +
[[Category: Gpcr]]
 +
[[Category: L745870]]
 +
[[Category: Ligand]]
 +
[[Category: Signaling protein]]

Revision as of 07:59, 4 December 2019

Crystal structure of dopamine receptor D4 bound to the subtype-selective ligand, L745870

PDB ID 6iql

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/6iql"
Personal tools