6ar9 - Revision history

OCA at 14:23, 4 October 2023

OCA — Wed, 04 Oct 2023 14:23:34 GMT

←Older revision		Revision as of 14:23, 4 October 2023
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	<StructureSection load='6ar9' size='340' side='right'caption='[[6ar9]], [[Resolution\|resolution]] 2.28Å' scene=''>		<StructureSection load='6ar9' size='340' side='right'caption='[[6ar9]], [[Resolution\|resolution]] 2.28Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6ar9]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6AR9 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=6AR9 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6ar9]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Trypanosoma_brucei_brucei_TREU927 Trypanosoma brucei brucei TREU927]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6AR9 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6AR9 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3L4:[(2-{[2-(2-AMINO-6-OXO-1,6-DIHYDRO-9H-PURIN-9-YL)ETHYL][(E)-2-PHOSPHONOETHENYL]AMINO}ETHOXY)METHYL]PHOSPHONIC+ACID'>3L4</scene>, <scene name='pdbligand=MG:~~MAGNESIUM+ION~~'>MG</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]] 2.28Å</td></tr>
-	~~<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat">~~<scene name='pdbligand=~~CSO~~:~~S-HYDROXYCYSTEINE~~'>~~CSO~~</scene></td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3L4:[(2-{[2-(2-AMINO-6-OXO-1,6-DIHYDRO-9H-PURIN-9-YL)ETHYL][(E)-2-PHOSPHONOETHENYL]AMINO}ETHOXY)METHYL]PHOSPHONIC+ACID'>3L4</scene>, <scene name='pdbligand=CSO:S-HYDROXYCYSTEINE'>CSO</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></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=6ar9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ar9 OCA], [~~http~~://pdbe.org/6ar9 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6ar9 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6ar9 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6ar9 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=6ar9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ar9 OCA], [https://pdbe.org/6ar9 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6ar9 RCSB], [https://www.ebi.ac.uk/pdbsum/6ar9 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6ar9 ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/Q38CA1_TRYB2 Q38CA1_TRYB2]
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Gudday, L W~~]]	+	[[Category: Trypanosoma brucei brucei TREU927]]
-	[[Category: ~~Teran, D~~]]	+	[[Category: Gudday LW]]
-	[[Category: ~~Acyclic nucleoside phosphonate]]~~	+	[[Category: Teran D]]
-	~~[[Category: Purine salvage]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 21:30, 28 October 2020

OCA — Wed, 28 Oct 2020 21:30:59 GMT

←Older revision		Revision as of 21:30, 28 October 2020
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	==Crystal structure of hypoxanthine-guanine-xanthine phosphorybosyltranferase in complex with [(2-{[2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)ethyl][(E)-2-phosphonoethenyl]amino}ethoxy)methyl]phosphonic acid==		==Crystal structure of hypoxanthine-guanine-xanthine phosphorybosyltranferase in complex with [(2-{[2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)ethyl][(E)-2-phosphonoethenyl]amino}ethoxy)methyl]phosphonic acid==
-	<StructureSection load='6ar9' size='340' side='right' caption='[[6ar9]], [[Resolution\|resolution]] 2.28Å' scene=''>	+	<StructureSection load='6ar9' size='340' side='right'caption='[[6ar9]], [[Resolution\|resolution]] 2.28Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6ar9]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6AR9 OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6AR9 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6ar9]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6AR9 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6AR9 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3L4:[(2-{[2-(2-AMINO-6-OXO-1,6-DIHYDRO-9H-PURIN-9-YL)ETHYL][(E)-2-PHOSPHONOETHENYL]AMINO}ETHOXY)METHYL]PHOSPHONIC+ACID'>3L4</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=3L4:[(2-{[2-(2-AMINO-6-OXO-1,6-DIHYDRO-9H-PURIN-9-YL)ETHYL][(E)-2-PHOSPHONOETHENYL]AMINO}ETHOXY)METHYL]PHOSPHONIC+ACID'>3L4</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CSO:S-HYDROXYCYSTEINE'>CSO</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CSO:S-HYDROXYCYSTEINE'>CSO</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=6ar9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ar9 OCA], [http://pdbe.org/6ar9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6ar9 RCSB], [http://www.ebi.ac.uk/pdbsum/6ar9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6ar9 ProSAT]</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=6ar9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ar9 OCA], [http://pdbe.org/6ar9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6ar9 RCSB], [http://www.ebi.ac.uk/pdbsum/6ar9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6ar9 ProSAT]</span></td></tr>
	</table>		</table>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
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	</div>		</div>
	<div class="pdbe-citations 6ar9" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 6ar9" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Phosphoribosyltransferase 3D structures\|Phosphoribosyltransferase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Gudday, L W]]		[[Category: Gudday, L W]]
	[[Category: Teran, D]]		[[Category: Teran, D]]

OCA at 06:29, 14 March 2018

OCA — Wed, 14 Mar 2018 06:29:06 GMT

←Older revision		Revision as of 06:29, 14 March 2018
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-	'''Unreleased structure'''

-	~~The entry~~ 6ar9 is ~~ON HOLD until Paper~~ Publication	+	==Crystal structure of hypoxanthine-guanine-xanthine phosphorybosyltranferase in complex with [(2-{[2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)ethyl][(E)-2-phosphonoethenyl]amino}ethoxy)methyl]phosphonic acid==
		+	<StructureSection load='6ar9' size='340' side='right' caption='[[6ar9]], [[Resolution\|resolution]] 2.28Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6ar9]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6AR9 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6AR9 FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3L4:[(2-{[2-(2-AMINO-6-OXO-1,6-DIHYDRO-9H-PURIN-9-YL)ETHYL][(E)-2-PHOSPHONOETHENYL]AMINO}ETHOXY)METHYL]PHOSPHONIC+ACID'>3L4</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
		+	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CSO:S-HYDROXYCYSTEINE'>CSO</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=6ar9 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6ar9 OCA], [http://pdbe.org/6ar9 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6ar9 RCSB], [http://www.ebi.ac.uk/pdbsum/6ar9 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6ar9 ProSAT]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Due to toxicity and compliance issues and the emergence of resistance to current medications new drugs for the treatment of Human African Trypanosomiasis are needed. A potential approach to developing novel anti-trypanosomal drugs is by inhibition of the 6-oxopurine salvage pathways which synthesise the nucleoside monophosphates required for DNA/RNA production. This is in view of the fact that trypanosomes lack the machinery for de novo synthesis of the purine ring. To provide validation for this approach as a drug target, we have RNAi silenced the three 6-oxopurine phosphoribosyltransferase (PRTase) isoforms in the infectious stage of Trypanosoma brucei demonstrating that the combined activity of these enzymes is critical for the parasites' viability. Furthermore, we have determined crystal structures of two of these isoforms in complex with several acyclic nucleoside phosphonates (ANPs), a class of compound previously shown to inhibit 6-oxopurine PRTases from several species including Plasmodium falciparum. The most potent of these compounds have Ki values as low as 60 nM, and IC50 values in cell based assays as low as 4 muM. This data provides a solid platform for further investigations into the use of this pathway as a target for anti-trypanosomal drug discovery.

-	~~Authors:~~ Teran, D., ~~Gudday~~, L.W.	+	Evaluation of the Trypanosoma brucei 6-oxopurine salvage pathway as a potential target for drug discovery.,Dolezelova E, Teran D, Gahura O, Kotrbova Z, Prochazkova M, Keough D, Spacek P, Hockova D, Guddat L, Zikova A PLoS Negl Trop Dis. 2018 Feb 26;12(2):e0006301. doi:, 10.1371/journal.pntd.0006301. eCollection 2018 Feb. PMID:29481567<ref>PMID:29481567</ref>

-	~~Description: Crystal structure~~ of ~~hypoxanthine~~-~~guanine~~-~~xanthine phosphorybosyltranferase in complex with [(2-{[2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)ethyl][(E)-2-phosphonoethenyl]amino}ethoxy)methyl]phosphonic acid~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[Category~~: ~~Unreleased Structures]]~~	+	</div>
-	[[Category: Gudday, L.W]]	+	<div class="pdbe-citations 6ar9" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Gudday, L W]]
	[[Category: Teran, D]]		[[Category: Teran, D]]
		+	[[Category: Acyclic nucleoside phosphonate]]
		+	[[Category: Purine salvage]]
		+	[[Category: Transferase]]

OCA at 08:08, 4 October 2017

OCA — Wed, 04 Oct 2017 08:08:33 GMT

←Older revision		Revision as of 08:08, 4 October 2017
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 6ar9 is ON HOLD	+	The entry 6ar9 is ON HOLD until Paper Publication

	Authors: Teran, D., Gudday, L.W.		Authors: Teran, D., Gudday, L.W.

OCA: Protected "6ar9" [edit=sysop:move=sysop]

OCA — Wed, 27 Sep 2017 16:42:05 GMT

Protected "6ar9" [edit=sysop:move=sysop]

←Older revision

Revision as of 16:42, 27 September 2017

OCA: New page: '''Unreleased structure''' The entry 6ar9 is ON HOLD Authors: Teran, D., Gudday, L.W. Description: Crystal structure of hypoxanthine-guanine-xanthine phosphorybosyltranferase in comple...

OCA — Wed, 27 Sep 2017 16:42:04 GMT

New page: '''Unreleased structure''' The entry 6ar9 is ON HOLD Authors: Teran, D., Gudday, L.W. Description: Crystal structure of hypoxanthine-guanine-xanthine phosphorybosyltranferase in comple...

New page

'''Unreleased structure'''

The entry 6ar9 is ON HOLD

Authors: Teran, D., Gudday, L.W.

Description: Crystal structure of hypoxanthine-guanine-xanthine phosphorybosyltranferase in complex with [(2-{[2-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)ethyl][(E)-2-phosphonoethenyl]amino}ethoxy)methyl]phosphonic acid
[[Category: Unreleased Structures]]
[[Category: Gudday, L.W]]
[[Category: Teran, D]]