5eqi - Revision history

OCA at 08:16, 12 July 2023

OCA — Wed, 12 Jul 2023 08:16:30 GMT

←Older revision		Revision as of 08:16, 12 July 2023
Line 3:		Line 3:
	<StructureSection load='5eqi' size='340' side='right'caption='[[5eqi]], [[Resolution\|resolution]] 3.00Å' scene=''>		<StructureSection load='5eqi' size='340' side='right'caption='[[5eqi]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5eqi]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EQI OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5EQI FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5eqi]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EQI OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5EQI FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat"~~><scene name='pdbligand=5RH:CYTOCHALASIN+B'>5RH</scene></td></tr>~~	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution\|Resolution]] 3.002Å</td></tr>
-	~~<tr~~ id~~='related'><td class~~="~~sblockLbl~~">~~<b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5eqg\|5eqg]]~~, [[~~5eqh~~\|~~5eqh~~]]</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5RH:CYTOCHALASIN+B'>5RH</scene></td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat">~~SLC2A1, GLUT1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode~~=~~Info&srchmode~~=~~5&id=9606 HUMAN])~~</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=5eqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eqi OCA], [https://pdbe.org/5eqi PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5eqi RCSB], [https://www.ebi.ac.uk/pdbsum/5eqi PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5eqi ProSAT]</span></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=5eqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eqi OCA], [~~http~~://pdbe.org/5eqi PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5eqi RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5eqi PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5eqi ProSAT]</span></td></tr>	+
	</table>		</table>
	== Disease ==		== Disease ==
-	[~~[http~~://www.uniprot.org/uniprot/GTR1_HUMAN GTR1_HUMAN]] Hereditary cryohydrocytosis with reduced stomatin;Paroxysmal exertion-induced dyskinesia;Encephalopathy due to GLUT1 deficiency;Paroxysmal dystonic choreathetosis with episodic ataxia and spasticity;Childhood absence epilepsy;Epilepsy with myoclonic-astatic seizures. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry.	+	[https://www.uniprot.org/uniprot/GTR1_HUMAN GTR1_HUMAN] Hereditary cryohydrocytosis with reduced stomatin;Paroxysmal exertion-induced dyskinesia;Encephalopathy due to GLUT1 deficiency;Paroxysmal dystonic choreathetosis with episodic ataxia and spasticity;Childhood absence epilepsy;Epilepsy with myoclonic-astatic seizures. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry.
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/GTR1_HUMAN GTR1_HUMAN]] Facilitative glucose transporter. This isoform may be responsible for constitutive or basal glucose uptake. Has a very broad substrate specificity; can transport a wide range of aldoses including both pentoses and hexoses.	+	[https://www.uniprot.org/uniprot/GTR1_HUMAN GTR1_HUMAN] Facilitative glucose transporter. This isoform may be responsible for constitutive or basal glucose uptake. Has a very broad substrate specificity; can transport a wide range of aldoses including both pentoses and hexoses.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 26:		Line 25:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Bringmann, P]]	+	[[Category: Bringmann P]]
-	[[Category: Caboni, L]]	+	[[Category: Caboni L]]
-	[[Category: Finer-Moore, J]]	+	[[Category: Finer-Moore J]]
-	[[Category: Heisler, I]]	+	[[Category: Heisler I]]
-	[[Category: Hillig, R]]	+	[[Category: Hillig R]]
-	[[Category: Kapoor, K]]	+	[[Category: Kapoor K]]
-	[[Category: Muller, T]]	+	[[Category: Muller T]]
-	[[Category: Pedersen~~, B P~~]]	+	[[Category: Pedersen BP]]
-	[[Category: Siebeneicher, H]]	+	[[Category: Siebeneicher H]]
-	[[Category: Stroud~~, R M~~]]	+	[[Category: Stroud RM]]
-	[[Category: Waight~~, A B]]~~	+	[[Category: Waight AB]]
-	~~[[Category: Glucose transporter]]~~	+
-	~~[[Category: Mfs transporter]]~~	+
-	~~[[Category: Transport protein-inhibitor complex~~]]	+

OCA at 08:51, 5 February 2020

OCA — Wed, 05 Feb 2020 08:51:08 GMT

←Older revision		Revision as of 08:51, 5 February 2020
Line 1:		Line 1:

-	==~~MFS transporter~~ in complex with Cytochalasin B==	+	==Human GLUT1 in complex with Cytochalasin B==
	<StructureSection load='5eqi' size='340' side='right'caption='[[5eqi]], [[Resolution\|resolution]] 3.00Å' scene=''>		<StructureSection load='5eqi' size='340' side='right'caption='[[5eqi]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==

OCA at 11:34, 25 December 2019

OCA — Wed, 25 Dec 2019 11:34:47 GMT

←Older revision		Revision as of 11:34, 25 December 2019
Line 1:		Line 1:

	==MFS transporter in complex with Cytochalasin B==		==MFS transporter in complex with Cytochalasin B==
-	<StructureSection load='5eqi' size='340' side='right' caption='[[5eqi]], [[Resolution\|resolution]] 3.00Å' scene=''>	+	<StructureSection load='5eqi' size='340' side='right'caption='[[5eqi]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5eqi]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EQI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5EQI FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5eqi]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EQI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5EQI FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5RH:CYTOCHALASIN+B'>5RH</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5RH:CYTOCHALASIN+B'>5RH</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5eqg\|5eqg]], [[5eqh\|5eqh]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5eqg\|5eqg]], [[5eqh\|5eqh]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">SLC2A1, GLUT1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=5eqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eqi OCA], [http://pdbe.org/5eqi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eqi RCSB], [http://www.ebi.ac.uk/pdbsum/5eqi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5eqi ProSAT]</span></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=5eqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eqi OCA], [http://pdbe.org/5eqi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eqi RCSB], [http://www.ebi.ac.uk/pdbsum/5eqi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5eqi ProSAT]</span></td></tr>
	</table>		</table>
Line 25:		Line 26:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Bringmann, P]]		[[Category: Bringmann, P]]
	[[Category: Caboni, L]]		[[Category: Caboni, L]]

OCA at 06:48, 6 October 2017

OCA — Fri, 06 Oct 2017 06:48:47 GMT

←Older revision		Revision as of 06:48, 6 October 2017
Line 6:		Line 6:
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5RH:CYTOCHALASIN+B'>5RH</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5RH:CYTOCHALASIN+B'>5RH</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5eqg\|5eqg]], [[5eqh\|5eqh]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5eqg\|5eqg]], [[5eqh\|5eqh]]</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=5eqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eqi OCA], [http://pdbe.org/5eqi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eqi RCSB], [http://www.ebi.ac.uk/pdbsum/5eqi PDBsum]</span></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=5eqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eqi OCA], [http://pdbe.org/5eqi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eqi RCSB], [http://www.ebi.ac.uk/pdbsum/5eqi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5eqi ProSAT]</span></td></tr>
	</table>		</table>
	== Disease ==		== Disease ==

OCA at 16:39, 10 May 2016

OCA — Tue, 10 May 2016 16:39:52 GMT

←Older revision		Revision as of 16:39, 10 May 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	The entry ~~5eqi~~ is ~~ON HOLD~~	+	==MFS transporter in complex with Cytochalasin B==
		+	<StructureSection load='5eqi' size='340' side='right' caption='[[5eqi]], [[Resolution\|resolution]] 3.00Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5eqi]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5EQI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5EQI FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=5RH:CYTOCHALASIN+B'>5RH</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5eqg\|5eqg]], [[5eqh\|5eqh]]</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=5eqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5eqi OCA], [http://pdbe.org/5eqi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5eqi RCSB], [http://www.ebi.ac.uk/pdbsum/5eqi PDBsum]</span></td></tr>
		+	</table>
		+	== Disease ==
		+	[[http://www.uniprot.org/uniprot/GTR1_HUMAN GTR1_HUMAN]] Hereditary cryohydrocytosis with reduced stomatin;Paroxysmal exertion-induced dyskinesia;Encephalopathy due to GLUT1 deficiency;Paroxysmal dystonic choreathetosis with episodic ataxia and spasticity;Childhood absence epilepsy;Epilepsy with myoclonic-astatic seizures. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry. The disease is caused by mutations affecting the gene represented in this entry.
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/GTR1_HUMAN GTR1_HUMAN]] Facilitative glucose transporter. This isoform may be responsible for constitutive or basal glucose uptake. Has a very broad substrate specificity; can transport a wide range of aldoses including both pentoses and hexoses.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Cancerous cells have an acutely increased demand for energy, leading to increased levels of human glucose transporter 1 (hGLUT1). This up-regulation suggests hGLUT1 as a target for therapeutic inhibitors addressing a multitude of cancer types. Here, we present three inhibitor-bound, inward-open structures of WT-hGLUT1 crystallized with three different inhibitors: cytochalasin B, a nine-membered bicyclic ring fused to a 14-membered macrocycle, which has been described extensively in the literature of hGLUTs, and two previously undescribed Phe amide-derived inhibitors. Despite very different chemical backbones, all three compounds bind in the central cavity of the inward-open state of hGLUT1, and all binding sites overlap the glucose-binding site. The inhibitory action of the compounds was determined for hGLUT family members, hGLUT1-4, using cell-based assays, and compared with homology models for these hGLUT members. This comparison uncovered a probable basis for the observed differences in inhibition between family members. We pinpoint regions of the hGLUT proteins that can be targeted to achieve isoform selectivity, and show that these same regions are used for inhibitors with very distinct structural backbones. The inhibitor cocomplex structures of hGLUT1 provide an important structural insight for the design of more selective inhibitors for hGLUTs and hGLUT1 in particular.

-	~~Authors: Kapoor~~, K., Finer-Moore~~, J.~~, Pedersen, ~~B.P.~~, Waight, A~~.B., Caboni, L.~~, Hillig~~, R.~~, Bringmann, P., Heisler, I., Muller, T., Siebeneicher, H., Stroud, R.M.	+	Mechanism of inhibition of human glucose transporter GLUT1 is conserved between cytochalasin B and phenylalanine amides.,Kapoor K, Finer-Moore JS, Pedersen BP, Caboni L, Waight A, Hillig RC, Bringmann P, Heisler I, Muller T, Siebeneicher H, Stroud RM Proc Natl Acad Sci U S A. 2016 Apr 26;113(17):4711-6. doi:, 10.1073/pnas.1603735113. Epub 2016 Apr 12. PMID:27078104<ref>PMID:27078104</ref>

-	~~Description:~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[Category: Unreleased Structures]]~~	+	</div>
-	~~[[Category~~: ~~Hillig, R]]~~	+	<div class="pdbe-citations 5eqi" style="background-color:#fffaf0;"></div>
-	~~[[Category: Muller, T]]~~	+	== References ==
-	~~[[Category: Caboni, L]]~~	+	<references/>
-	~~[[Category: Pedersen, B.P]]~~	+	__TOC__
-	~~[[Category: Siebeneicher, H]]~~	+	</StructureSection>
	[[Category: Bringmann, P]]		[[Category: Bringmann, P]]
-	[[Category: ~~Kapoor~~, K]]	+	[[Category: Caboni, L]]
	[[Category: Finer-Moore, J]]		[[Category: Finer-Moore, J]]
	[[Category: Heisler, I]]		[[Category: Heisler, I]]
-	[[Category: Stroud, R.M]]	+	[[Category: Hillig, R]]
-	[[Category: Waight, A.B]]	+	[[Category: Kapoor, K]]
		+	[[Category: Muller, T]]
		+	[[Category: Pedersen, B P]]
		+	[[Category: Siebeneicher, H]]
		+	[[Category: Stroud, R M]]
		+	[[Category: Waight, A B]]
		+	[[Category: Glucose transporter]]
		+	[[Category: Mfs transporter]]
		+	[[Category: Transport protein-inhibitor complex]]

OCA: Protected "5eqi" [edit=sysop:move=sysop]

OCA — Tue, 01 Dec 2015 03:14:05 GMT

Protected "5eqi" [edit=sysop:move=sysop]

←Older revision

Revision as of 03:14, 1 December 2015

OCA: New page: '''Unreleased structure''' The entry 5eqi is ON HOLD Authors: Kapoor, K., Finer-Moore, J., Pedersen, B.P., Waight, A.B., Caboni, L., Hillig, R., Bringmann, P., Heisler, I., Muller, T., ...

OCA — Tue, 01 Dec 2015 03:14:04 GMT

New page: '''Unreleased structure''' The entry 5eqi is ON HOLD Authors: Kapoor, K., Finer-Moore, J., Pedersen, B.P., Waight, A.B., Caboni, L., Hillig, R., Bringmann, P., Heisler, I., Muller, T., ...

New page

'''Unreleased structure'''

The entry 5eqi is ON HOLD

Authors: Kapoor, K., Finer-Moore, J., Pedersen, B.P., Waight, A.B., Caboni, L., Hillig, R., Bringmann, P., Heisler, I., Muller, T., Siebeneicher, H., Stroud, R.M.

Description:
[[Category: Unreleased Structures]]
[[Category: Hillig, R]]
[[Category: Muller, T]]
[[Category: Caboni, L]]
[[Category: Pedersen, B.P]]
[[Category: Siebeneicher, H]]
[[Category: Bringmann, P]]
[[Category: Kapoor, K]]
[[Category: Finer-Moore, J]]
[[Category: Heisler, I]]
[[Category: Stroud, R.M]]
[[Category: Waight, A.B]]