7s7v: 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 3: Line 3:
<StructureSection load='7s7v' size='340' side='right'caption='[[7s7v]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
<StructureSection load='7s7v' size='340' side='right'caption='[[7s7v]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[7s7v]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7S7V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7S7V FirstGlance]. <br>
<table><tr><td colspan='2'>[[7s7v]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Thermoanaerobacter_sp._X513 Thermoanaerobacter sp. X513]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7S7V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7S7V FirstGlance]. <br>
</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CRO:{2-[(1R,2R)-1-AMINO-2-HYDROXYPROPYL]-4-(4-HYDROXYBENZYLIDENE)-5-OXO-4,5-DIHYDRO-1H-IMIDAZOL-1-YL}ACETIC+ACID'>CRO</scene></td></tr>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CRO:{2-[(1R,2R)-1-AMINO-2-HYDROXYPROPYL]-4-(4-HYDROXYBENZYLIDENE)-5-OXO-4,5-DIHYDRO-1H-IMIDAZOL-1-YL}ACETIC+ACID'>CRO</scene></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7s7v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7s7v OCA], [https://pdbe.org/7s7v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7s7v RCSB], [https://www.ebi.ac.uk/pdbsum/7s7v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7s7v ProSAT]</span></td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7s7v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7s7v OCA], [https://pdbe.org/7s7v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7s7v RCSB], [https://www.ebi.ac.uk/pdbsum/7s7v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7s7v ProSAT]</span></td></tr>
</table>
</table>
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
Nicotinic partial agonists provide an accepted aid for smoking cessation and thus contribute to decreasing tobacco-related disease. Improved drugs constitute a continued area of study. However, there remains no reductionist method to examine the cellular and subcellular pharmacokinetic properties of these compounds in living cells. Here, we developed new intensity-based drug-sensing fluorescent reporters (iDrugSnFRs) for the nicotinic partial agonists dianicline, cytisine, and two cytisine derivatives - 10-fluorocytisine and 9-bromo-10-ethylcytisine. We report the first atomic-scale structures of liganded periplasmic binding protein-based biosensors, accelerating development of iDrugSnFRs and also explaining the activation mechanism. The nicotinic iDrugSnFRs detect their drug partners in solution, as well as at the plasma membrane (PM) and in the endoplasmic reticulum (ER) of cell lines and mouse hippocampal neurons. At the PM, the speed of solution changes limits the growth and decay rates of the fluorescence response in almost all cases. In contrast, we found that rates of membrane crossing differ among these nicotinic drugs by &gt;30-fold. The new nicotinic iDrugSnFRs provide insight into the real-time pharmacokinetic properties of nicotinic agonists and provide a methodology whereby iDrugSnFRs can inform both pharmaceutical neuroscience and addiction neuroscience.
Fluorescence activation mechanism and imaging of drug permeation with new sensors for smoking-cessation ligands.,Nichols AL, Blumenfeld Z, Fan C, Luebbert L, Blom AEM, Cohen BN, Marvin JS, Borden PM, Kim CH, Muthusamy AK, Shivange AV, Knox HJ, Campello HR, Wang JH, Dougherty DA, Looger LL, Gallagher T, Rees DC, Lester HA Elife. 2022 Jan 4;11. pii: 74648. doi: 10.7554/eLife.74648. PMID:34982029<ref>PMID:34982029</ref>
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
<div class="pdbe-citations 7s7v" style="background-color:#fffaf0;"></div>
== References ==
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
[[Category: Large Structures]]
[[Category: Large Structures]]
[[Category: Fan, C]]
[[Category: Thermoanaerobacter sp. X513]]
[[Category: Lester, H A]]
[[Category: Fan C]]
[[Category: Looger, L L]]
[[Category: Lester HA]]
[[Category: Rees, D C]]
[[Category: Looger LL]]
[[Category: Shivange, A V]]
[[Category: Rees DC]]
[[Category: Choline-binding protein]]
[[Category: Shivange AV]]
[[Category: Fluorescent protein]]
[[Category: Fluorescent sensor]]
[[Category: Gfp]]
[[Category: Nicotine]]
[[Category: Nicotine-binding protein]]
[[Category: Periplasmic binding protein]]
[[Category: Pharmacokinetic sensor]]

Revision as of 06:56, 8 February 2023

Crystal structure of iNicSnFR3a Fluorescent Nicotine Sensor

7s7v, resolution 2.50Å

Drag the structure with the mouse to rotate

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "https://proteopedia.org/index.php?title=7s7v&oldid=3712485"