2qju

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[[Image:2qju.jpg|left|200px]]<br /><applet load="2qju" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2qju.jpg|left|200px]]
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caption="2qju, resolution 2.90&Aring;" />
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'''Crystal Structure of an NSS Homolog with Bound Antidepressant'''<br />
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{{Structure
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|PDB= 2qju |SIZE=350|CAPTION= <scene name='initialview01'>2qju</scene>, resolution 2.90&Aring;
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|SITE=
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|LIGAND= <scene name='pdbligand=BOG:B-OCTYLGLUCOSIDE'>BOG</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=LEU:LEUCINE'>LEU</scene> and <scene name='pdbligand=DSM:3-(10,11-DIHYDRO-5H-DIBENZO[B,F]AZEPIN-5-YL)-N-METHYLPROPAN-1-AMINE'>DSM</scene>
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|ACTIVITY=
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|GENE= snf ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=63363 Aquifex aeolicus])
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}}
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'''Crystal Structure of an NSS Homolog with Bound Antidepressant'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2QJU is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Aquifex_aeolicus Aquifex aeolicus] with <scene name='pdbligand=BOG:'>BOG</scene>, <scene name='pdbligand=NA:'>NA</scene>, <scene name='pdbligand=CL:'>CL</scene>, <scene name='pdbligand=LEU:'>LEU</scene> and <scene name='pdbligand=DSM:'>DSM</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QJU OCA].
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2QJU is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Aquifex_aeolicus Aquifex aeolicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2QJU OCA].
==Reference==
==Reference==
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LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake., Zhou Z, Zhen J, Karpowich NK, Goetz RM, Law CJ, Reith ME, Wang DN, Science. 2007 Sep 7;317(5843):1390-3. Epub 2007 Aug 9. PMID:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17690258 17690258]
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LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake., Zhou Z, Zhen J, Karpowich NK, Goetz RM, Law CJ, Reith ME, Wang DN, Science. 2007 Sep 7;317(5843):1390-3. Epub 2007 Aug 9. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/17690258 17690258]
[[Category: Aquifex aeolicus]]
[[Category: Aquifex aeolicus]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: transport protein]]
[[Category: transport protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:39:52 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:26:36 2008''

Revision as of 16:26, 20 March 2008

Image:2qju.jpg


PDB ID 2qju

Drag the structure with the mouse to rotate
, resolution 2.90Å
Ligands: , , , and
Gene: snf (Aquifex aeolicus)
Coordinates: save as pdb, mmCIF, xml



Crystal Structure of an NSS Homolog with Bound Antidepressant


Overview

Tricyclic antidepressants exert their pharmacological effect-inhibiting the reuptake of serotonin, norepinephrine, and dopamine-by directly blocking neurotransmitter transporters (SERT, NET, and DAT, respectively) in the presynaptic membrane. The drug-binding site and the mechanism of this inhibition are poorly understood. We determined the crystal structure at 2.9 angstroms of the bacterial leucine transporter (LeuT), a homolog of SERT, NET, and DAT, in complex with leucine and the antidepressant desipramine. Desipramine binds at the inner end of the extracellular cavity of the transporter and is held in place by a hairpin loop and by a salt bridge. This binding site is separated from the leucine-binding site by the extracellular gate of the transporter. By directly locking the gate, desipramine prevents conformational changes and blocks substrate transport. Mutagenesis experiments on human SERT and DAT indicate that both the desipramine-binding site and its inhibition mechanism are probably conserved in the human neurotransmitter transporters.

About this Structure

2QJU is a Single protein structure of sequence from Aquifex aeolicus. Full crystallographic information is available from OCA.

Reference

LeuT-desipramine structure reveals how antidepressants block neurotransmitter reuptake., Zhou Z, Zhen J, Karpowich NK, Goetz RM, Law CJ, Reith ME, Wang DN, Science. 2007 Sep 7;317(5843):1390-3. Epub 2007 Aug 9. PMID:17690258

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