5tbo - Revision history

OCA at 12:57, 4 October 2023

OCA — Wed, 04 Oct 2023 12:57:26 GMT

←Older revision		Revision as of 12:57, 4 October 2023
Line 3:		Line 3:
	<StructureSection load='5tbo' size='340' side='right'caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>		<StructureSection load='5tbo' size='340' side='right'caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Plaf7 Plaf7~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5TBO FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Plasmodium_falciparum_3D7 Plasmodium falciparum 3D7]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5TBO FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=78Z:2-(1,1-DIFLUOROETHYL)-5-METHYL-N-[6-(TRIFLUOROMETHYL)PYRIDIN-3-YL][1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-AMINE'>78Z</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LDA:LAURYL+DIMETHYLAMINE-N-OXIDE'>LDA</scene>, <scene name='pdbligand=ORO:OROTIC+ACID'>ORO</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]] 2.151Å</td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PFF0160c ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=36329 PLAF7])</td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=78Z:2-(1,1-DIFLUOROETHYL)-5-METHYL-N-[6-(TRIFLUOROMETHYL)PYRIDIN-3-YL][1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-AMINE'>78Z</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LDA:LAURYL+DIMETHYLAMINE-N-OXIDE'>LDA</scene>, <scene name='pdbligand=ORO:OROTIC+ACID'>ORO</scene></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dihydroorotate_dehydrogenase_(quinone) Dihydroorotate dehydrogenase (quinone)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.3.5.2 1.3.5.2] </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=5tbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tbo OCA], [https://pdbe.org/5tbo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5tbo RCSB], [https://www.ebi.ac.uk/pdbsum/5tbo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5tbo 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=5tbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tbo OCA], [~~http~~://pdbe.org/5tbo PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5tbo RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5tbo PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5tbo ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/PYRD_PLAF7 PYRD_PLAF7]] Catalyzes the conversion of dihydroorotate to orotate with quinone as electron acceptor.	+	[https://www.uniprot.org/uniprot/PYRD_PLAF7 PYRD_PLAF7] Catalyzes the conversion of dihydroorotate to orotate with quinone as electron acceptor.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 28:		Line 27:
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Plaf7~~]]	+	[[Category: Plasmodium falciparum 3D7]]
-	[[Category: Deng, X]]	+	[[Category: Deng X]]
-	[[Category: Phillips, M]]	+	[[Category: Phillips M]]
-	~~[[Category: Alpha/beta barrel]]~~	+
-	~~[[Category: Fmn]]~~	+
-	~~[[Category: Mitochondrial membrane]]~~	+
-	~~[[Category: Oxidoreductase]]~~	+
-	~~[[Category: Oxidoreductase-oxidoreductase inhibitor complex~~]]	+

OCA at 08:23, 21 October 2020

OCA — Wed, 21 Oct 2020 08:23:03 GMT

←Older revision		Revision as of 08:23, 21 October 2020
Line 3:		Line 3:
	<StructureSection load='5tbo' size='340' side='right'caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>		<StructureSection load='5tbo' size='340' side='right'caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Plaf7 Plaf7]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5TBO FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Plaf7 Plaf7]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5TBO FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=78Z:2-(1,1-DIFLUOROETHYL)-5-METHYL-N-[6-(TRIFLUOROMETHYL)PYRIDIN-3-YL][1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-AMINE'>78Z</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LDA:LAURYL+DIMETHYLAMINE-N-OXIDE'>LDA</scene>, <scene name='pdbligand=ORO:OROTIC+ACID'>ORO</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=78Z:2-(1,1-DIFLUOROETHYL)-5-METHYL-N-[6-(TRIFLUOROMETHYL)PYRIDIN-3-YL][1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-AMINE'>78Z</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LDA:LAURYL+DIMETHYLAMINE-N-OXIDE'>LDA</scene>, <scene name='pdbligand=ORO:OROTIC+ACID'>ORO</scene></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PFF0160c ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=36329 PLAF7])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PFF0160c ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=36329 PLAF7])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dihydroorotate_dehydrogenase_(quinone) Dihydroorotate dehydrogenase (quinone)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.3.5.2 1.3.5.2] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dihydroorotate_dehydrogenase_(quinone) Dihydroorotate dehydrogenase (quinone)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.3.5.2 1.3.5.2] </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=5tbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tbo OCA], [http://pdbe.org/5tbo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5tbo RCSB], [http://www.ebi.ac.uk/pdbsum/5tbo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5tbo 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=5tbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tbo OCA], [http://pdbe.org/5tbo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5tbo RCSB], [http://www.ebi.ac.uk/pdbsum/5tbo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5tbo ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==

OCA at 12:30, 25 December 2019

OCA — Wed, 25 Dec 2019 12:30:10 GMT

←Older revision		Revision as of 12:30, 25 December 2019
Line 1:		Line 1:

	==Crystal structure of Plasmodium falciparum dihydroorotate dehydrogenase bound with Inhibitor DSM421==		==Crystal structure of Plasmodium falciparum dihydroorotate dehydrogenase bound with Inhibitor DSM421==
-	<StructureSection load='5tbo' size='340' side='right' caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>	+	<StructureSection load='5tbo' size='340' side='right'caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Plaf7 Plaf7]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5TBO FirstGlance]. <br>		<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Plaf7 Plaf7]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5TBO FirstGlance]. <br>
Line 20:		Line 20:
	</div>		</div>
	<div class="pdbe-citations 5tbo" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5tbo" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Dihydroorotate dehydrogenase 3D structures\|Dihydroorotate dehydrogenase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Plaf7]]		[[Category: Plaf7]]
	[[Category: Deng, X]]		[[Category: Deng, X]]

OCA at 19:01, 15 November 2017

OCA — Wed, 15 Nov 2017 19:01:49 GMT

←Older revision		Revision as of 19:01, 15 November 2017
Line 3:		Line 3:
	<StructureSection load='5tbo' size='340' side='right' caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>		<StructureSection load='5tbo' size='340' side='right' caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5TBO FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Plaf7 Plaf7]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5TBO FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=78Z:2-(1,1-DIFLUOROETHYL)-5-METHYL-N-[6-(TRIFLUOROMETHYL)PYRIDIN-3-YL][1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-AMINE'>78Z</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LDA:LAURYL+DIMETHYLAMINE-N-OXIDE'>LDA</scene>, <scene name='pdbligand=ORO:OROTIC+ACID'>ORO</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=78Z:2-(1,1-DIFLUOROETHYL)-5-METHYL-N-[6-(TRIFLUOROMETHYL)PYRIDIN-3-YL][1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-AMINE'>78Z</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LDA:LAURYL+DIMETHYLAMINE-N-OXIDE'>LDA</scene>, <scene name='pdbligand=ORO:OROTIC+ACID'>ORO</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PFF0160c ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=36329 PLAF7])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dihydroorotate_dehydrogenase_(quinone) Dihydroorotate dehydrogenase (quinone)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.3.5.2 1.3.5.2] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dihydroorotate_dehydrogenase_(quinone) Dihydroorotate dehydrogenase (quinone)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.3.5.2 1.3.5.2] </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=5tbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tbo OCA], [http://pdbe.org/5tbo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5tbo RCSB], [http://www.ebi.ac.uk/pdbsum/5tbo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5tbo 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=5tbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tbo OCA], [http://pdbe.org/5tbo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5tbo RCSB], [http://www.ebi.ac.uk/pdbsum/5tbo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5tbo ProSAT]</span></td></tr>
Line 23:		Line 24:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Plaf7]]
	[[Category: Deng, X]]		[[Category: Deng, X]]
	[[Category: Phillips, M]]		[[Category: Phillips, M]]

OCA at 16:57, 3 October 2016

OCA — Mon, 03 Oct 2016 16:57:40 GMT

←Older revision		Revision as of 16:57, 3 October 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5tbo is ~~ON HOLD~~	+	==Crystal structure of Plasmodium falciparum dihydroorotate dehydrogenase bound with Inhibitor DSM421==
		+	<StructureSection load='5tbo' size='340' side='right' caption='[[5tbo]], [[Resolution\|resolution]] 2.15Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5tbo]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5TBO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5TBO FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=78Z:2-(1,1-DIFLUOROETHYL)-5-METHYL-N-[6-(TRIFLUOROMETHYL)PYRIDIN-3-YL][1,2,4]TRIAZOLO[1,5-A]PYRIMIDIN-7-AMINE'>78Z</scene>, <scene name='pdbligand=FMN:FLAVIN+MONONUCLEOTIDE'>FMN</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=LDA:LAURYL+DIMETHYLAMINE-N-OXIDE'>LDA</scene>, <scene name='pdbligand=ORO:OROTIC+ACID'>ORO</scene></td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Dihydroorotate_dehydrogenase_(quinone) Dihydroorotate dehydrogenase (quinone)], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.3.5.2 1.3.5.2] </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=5tbo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5tbo OCA], [http://pdbe.org/5tbo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5tbo RCSB], [http://www.ebi.ac.uk/pdbsum/5tbo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5tbo ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/PYRD_PLAF7 PYRD_PLAF7]] Catalyzes the conversion of dihydroorotate to orotate with quinone as electron acceptor.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The emergence of drug resistant malaria parasites continues to hamper efforts to control this lethal disease. Dihydroorotate dehydrogenase has recently been validated as a new target for the treatment of malaria and a selective inhibitor (DSM265) of the Plasmodium enzyme is currently in clinical development. With the goal of identifying a backup compound to DSM265, we explored replacement of the SF5-aniline moiety of DSM265 with a series of CF3-pyridinyls, while maintaining the core triazolopyrimidine scaffold. This effort led to the identification of DSM421, which has improved solubility, lower intrinsic clearance and increased plasma exposure after oral dosing compared to DSM265, while maintaining a long predicted human half-life. Its improved physical and chemical properties will allow it to be formulated more readily than DSM265. DSM421 showed excellent efficacy in the SCID mouse model of P. falciparum malaria that supports the prediction of a low human dose (<200 mg). Importantly DSM421 showed equal activity against both P. falciparum and P. vivax field isolates, while DSM265 was more active on P. falciparum. DSM421 has the potential to be developed as a single dose cure or once-weekly chemopreventative for both P. falciparum and P. vivax malaria leading to its advancement as a preclinical development candidate.

-	~~Authors: Xiaoyi Deng~~, ~~Margaret~~ Phillips	+	A triazolopyrimidine-based dihydroorotate dehydrogenase inhibitor (DSM421) with improved drug-like properties for treatment and prevention of malaria.,Phillips MA, White KL, Kokkonda S, Deng X, White J, El Mazouni F, Marsh KC, Tomchick DR, Manjalanagara K, Rudra KR, Wirjanata G, Noviyanti R, Price RN, Marfurt J, Shackleford DM, Chiu FC, Campbell M, Jimenez Diaz MB, Ferrer-Bazaga S, Angulo-Barturen I, Martinez-Martinez MS, Lafuente-Monasterio MJ, Kaminsky W, Silue K, Zeeman AM, Kocken C, Leroy D, Blasco B, Rossignol E, Rueckle T, Matthews D, Burrows JN, Waterson D, Palmer MJ, Rathod PK, Charman SA ACS Infect Dis. 2016 Sep 17. PMID:27641613<ref>PMID:27641613</ref>

-	~~Description: Crystal structure~~ of ~~Plasmodium falciparum dihydroorotate dehydrogenase bound with Inhibitor DSM421~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
-	[[Category: ~~Xiaoyi Deng, Margaret~~ Phillips]]	+	<div class="pdbe-citations 5tbo" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Deng, X]]
		+	[[Category: Phillips, M]]
		+	[[Category: Alpha/beta barrel]]
		+	[[Category: Fmn]]
		+	[[Category: Mitochondrial membrane]]
		+	[[Category: Oxidoreductase]]
		+	[[Category: Oxidoreductase-oxidoreductase inhibitor complex]]

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

OCA — Wed, 21 Sep 2016 12:27:55 GMT

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

←Older revision

Revision as of 12:27, 21 September 2016

OCA: New page: '''Unreleased structure''' The entry 5tbo is ON HOLD Authors: Xiaoyi Deng, Margaret Phillips Description: Crystal structure of Plasmodium falciparum dihydroorotate dehydrogenase bound ...

OCA — Wed, 21 Sep 2016 12:27:53 GMT

New page: '''Unreleased structure''' The entry 5tbo is ON HOLD Authors: Xiaoyi Deng, Margaret Phillips Description: Crystal structure of Plasmodium falciparum dihydroorotate dehydrogenase bound ...

New page

'''Unreleased structure'''

The entry 5tbo is ON HOLD

Authors: Xiaoyi Deng, Margaret Phillips

Description: Crystal structure of Plasmodium falciparum dihydroorotate dehydrogenase bound with Inhibitor DSM421
[[Category: Unreleased Structures]]
[[Category: Xiaoyi Deng, Margaret Phillips]]