OCA at 06:13, 20 May 2020

2020-05-20T06:13:22Z

←Older revision		Revision as of 06:13, 20 May 2020
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	==Structure of ABCG2 bound to mitoxantrone==		==Structure of ABCG2 bound to mitoxantrone==
-	<StructureSection load='6vxi' size='340' side='right'caption='[[6vxi]]' scene=''>	+	<StructureSection load='6vxi' size='340' side='right'caption='[[6vxi]], [[Resolution\|resolution]] 3.70Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6VXI OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6VXI FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6vxi]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6VXI OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6VXI FirstGlance]. <br>
-	</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6vxi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vxi OCA], [http://pdbe.org/6vxi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6vxi RCSB], [http://www.ebi.ac.uk/pdbsum/6vxi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6vxi ProSAT]</span></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CLR:CHOLESTEROL'>CLR</scene>, <scene name='pdbligand=MIX:1,4-DIHYDROXY-5,8-BIS({2-[(2-HYDROXYETHYL)AMINO]ETHYL}AMINO)-9,10-ANTHRACENEDIONE'>MIX</scene></td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/ABC-type_xenobiotic_transporter ABC-type xenobiotic transporter], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=7.6.2.2 7.6.2.2] </span></td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6vxi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vxi OCA], [http://pdbe.org/6vxi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6vxi RCSB], [http://www.ebi.ac.uk/pdbsum/6vxi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6vxi ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/ABCG2_HUMAN ABCG2_HUMAN]] High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from the brain. Appears to play a major role in the multidrug resistance phenotype of several cancer cell lines. Implicated in the efflux of numerous drugs and xenobiotics: mitoxantrone, the photosensitizer pheophorbide, camptothecin, methotrexate, azidothymidine (AZT), and the anthracyclines daunorubicin and doxorubicin.<ref>PMID:12958161</ref> <ref>PMID:20705604</ref> <ref>PMID:22132962</ref> <ref>PMID:23189181</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	ABCG2 is an ABC transporter that extrudes a variety of compounds from cells, and presents an obstacle in treating chemotherapy-resistant cancers. Despite recent structural insights, no anticancer drug bound to ABCG2 has been resolved, and the mechanisms of multidrug transport remain obscure. Such a gap of knowledge limits the development of novel compounds that block or evade this critical molecular pump. Here we present single-particle cryo-EM studies of ABCG2 in the apo state, and bound to the three structurally distinct chemotherapeutics. Without the binding of conformation-selective antibody fragments or inhibitors, the resting ABCG2 adopts a closed conformation. Our cryo-EM, biochemical, and functional analyses reveal the binding mode of three chemotherapeutic compounds, demonstrate how these molecules open the closed conformation of the transporter, and establish that imatinib is particularly effective in stabilizing the inward facing conformation of ABCG2. Together these studies reveal the previously unrecognized conformational cycle of ABCG2.
		+
		+	ABCG2 transports anticancer drugs via a closed-to-open switch.,Orlando BJ, Liao M Nat Commun. 2020 May 8;11(1):2264. doi: 10.1038/s41467-020-16155-2. PMID:32385283<ref>PMID:32385283</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6vxi" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: ABC-type xenobiotic transporter]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Liao M]]	+	[[Category: Liao, M]]
-	[[Category: Orlando BJ]]	+	[[Category: Orlando, B J]]
		+	[[Category: Abc transporter]]
		+	[[Category: Abcg2]]
		+	[[Category: Mitoxantrone]]
		+	[[Category: Translocase]]

OCA at 05:35, 13 May 2020

2020-05-13T05:35:04Z

←Older revision		Revision as of 05:35, 13 May 2020
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-	'''Unreleased structure'''

-	~~The entry~~ 6vxi ~~is ON HOLD until Paper Publication~~	+	==Structure of ABCG2 bound to mitoxantrone==
-		+	<StructureSection load='6vxi' size='340' side='right'caption='[[6vxi]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6VXI OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6VXI FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=6vxi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6vxi OCA], [http://pdbe.org/6vxi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6vxi RCSB], [http://www.ebi.ac.uk/pdbsum/6vxi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6vxi ProSAT]</span></td></tr>
-	[[Category: ~~Unreleased~~ Structures]]	+	</table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Large Structures]]
		+	[[Category: Liao M]]
		+	[[Category: Orlando BJ]]

OCA at 08:28, 18 March 2020

2020-03-18T08:28:52Z

←Older revision		Revision as of 08:28, 18 March 2020
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6vxi is ON HOLD	+	The entry 6vxi is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "6vxi" [edit=sysop:move=sysop]

2020-03-04T05:37:59Z

Protected "6vxi" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:37, 4 March 2020

OCA: New page: '''Unreleased structure''' The entry 6vxi is ON HOLD Authors: Description: Category: Unreleased Structures

2020-03-04T05:37:58Z

New page: '''Unreleased structure''' The entry 6vxi is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 6vxi is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]

6vxi - Revision history

OCA at 06:13, 20 May 2020

OCA at 05:35, 13 May 2020

OCA at 08:28, 18 March 2020

OCA: Protected "6vxi" [edit=sysop:move=sysop]

OCA: New page: '''Unreleased structure''' The entry 6vxi is ON HOLD Authors: Description: Category: Unreleased Structures