4uwi - Revision history

OCA at 11:24, 9 May 2024

OCA — Thu, 09 May 2024 11:24:04 GMT

←Older revision		Revision as of 11:24, 9 May 2024
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Aspergillus_fumigatus Aspergillus fumigatus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4UWI FirstGlance]. <br>		<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Aspergillus_fumigatus Aspergillus fumigatus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4UWI FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=XMQ:2,6-DICHLORO-4-[3-(4-METHYLPIPERAZIN-1-YL)PROPYL]-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE'>XMQ</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]] 1.8Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=XMQ:2,6-DICHLORO-4-[3-(4-METHYLPIPERAZIN-1-YL)PROPYL]-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE'>XMQ</scene></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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [https://pdbe.org/4uwi PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [https://www.ebi.ac.uk/pdbsum/4uwi PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4uwi 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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [https://pdbe.org/4uwi PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [https://www.ebi.ac.uk/pdbsum/4uwi PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4uwi ProSAT]</span></td></tr>
	</table>		</table>

OCA at 07:46, 29 March 2023

OCA — Wed, 29 Mar 2023 07:46:06 GMT

←Older revision		Revision as of 07:46, 29 March 2023
Line 3:		Line 3:
	<StructureSection load='4uwi' size='340' side='right'caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>		<StructureSection load='4uwi' size='340' side='right'caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Aspfm Aspfm~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4UWI FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Aspergillus_fumigatus Aspergillus fumigatus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4UWI FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=XMQ:2,6-DICHLORO-4-[3-(4-METHYLPIPERAZIN-1-YL)PROPYL]-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE'>XMQ</scene~~></td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=XMQ:2,6-DICHLORO-4-[3-(4-METHYLPIPERAZIN-1-YL)PROPYL]-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE'>XMQ</scene></td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4uwj\|4uwj]]</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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [https://pdbe.org/4uwi PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [https://www.ebi.ac.uk/pdbsum/4uwi PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4uwi ProSAT]</span></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glycylpeptide_N-tetradecanoyltransferase Glycylpeptide N-tetradecanoyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.97 2.3.1.97] </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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [~~http~~://pdbe.org/4uwi PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4uwi PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4uwi ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/NMT_ASPFU NMT_ASPFU]] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins.	+	[https://www.uniprot.org/uniprot/NMT_ASPFU NMT_ASPFU] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 24:		Line 22:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Aspfm]]~~	+	[[Category: Aspergillus fumigatus]]
-	~~[[Category: Glycylpeptide N-tetradecanoyltransferase~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Brand, S]]	+	[[Category: Brand S]]
-	[[Category: Brenk, R]]	+	[[Category: Brenk R]]
-	[[Category: Fairlamb~~, A H~~]]	+	[[Category: Fairlamb AH]]
-	[[Category: Ferguson~~, M A.J~~]]	+	[[Category: Ferguson MAJ]]
-	[[Category: Frearson~~, J A~~]]	+	[[Category: Frearson JA]]
-	[[Category: Gilbert~~, I H~~]]	+	[[Category: Gilbert IH]]
-	[[Category: Hallyburton, I]]	+	[[Category: Hallyburton I]]
-	[[Category: Harrison~~, J R~~]]	+	[[Category: Harrison JR]]
-	[[Category: McElroy~~, S P~~]]	+	[[Category: McElroy SP]]
-	[[Category: Norcross~~, N R~~]]	+	[[Category: Norcross NR]]
-	[[Category: Norval, S]]	+	[[Category: Norval S]]
-	[[Category: Read~~, K D~~]]	+	[[Category: Read KD]]
-	[[Category: Robinson~~, D A~~]]	+	[[Category: Robinson DA]]
-	[[Category: Simeons~~, F R.C~~]]	+	[[Category: Simeons FRC]]
-	[[Category: Smith~~, V C~~]]	+	[[Category: Smith VC]]
-	[[Category: Stojanovski, L]]	+	[[Category: Stojanovski L]]
-	[[Category: Thompson, S]]	+	[[Category: Thompson S]]
-	[[Category: Torrie~~, L S~~]]	+	[[Category: Torrie LS]]
-	[[Category: Wyatt~~, P G]]~~	+	[[Category: Wyatt PG]]
-	~~[[Category: Drug discovery]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 11:05, 26 February 2020

OCA — Wed, 26 Feb 2020 11:05:59 GMT

←Older revision		Revision as of 11:05, 26 February 2020
Line 1:		Line 1:

	==Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand==		==Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand==
-	<StructureSection load='4uwi' size='340' side='right' caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>	+	<StructureSection load='4uwi' size='340' side='right'caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Aspfm Aspfm]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UWI FirstGlance]. <br>		<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Aspfm Aspfm]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UWI FirstGlance]. <br>
Line 26:		Line 26:
	[[Category: Aspfm]]		[[Category: Aspfm]]
	[[Category: Glycylpeptide N-tetradecanoyltransferase]]		[[Category: Glycylpeptide N-tetradecanoyltransferase]]
		+	[[Category: Large Structures]]
	[[Category: Brand, S]]		[[Category: Brand, S]]
	[[Category: Brenk, R]]		[[Category: Brenk, R]]

OCA at 06:52, 15 February 2018

OCA — Thu, 15 Feb 2018 06:52:34 GMT

←Older revision		Revision as of 06:52, 15 February 2018
Line 3:		Line 3:
	<StructureSection load='4uwi' size='340' side='right' caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>		<StructureSection load='4uwi' size='340' side='right' caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UWI FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Aspfm Aspfm]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UWI FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=XMQ:2,6-DICHLORO-4-[3-(4-METHYLPIPERAZIN-1-YL)PROPYL]-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE'>XMQ</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=XMQ:2,6-DICHLORO-4-[3-(4-METHYLPIPERAZIN-1-YL)PROPYL]-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE'>XMQ</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4uwj\|4uwj]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4uwj\|4uwj]]</td></tr>
Line 24:		Line 24:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Aspfm]]
	[[Category: Glycylpeptide N-tetradecanoyltransferase]]		[[Category: Glycylpeptide N-tetradecanoyltransferase]]
	[[Category: Brand, S]]		[[Category: Brand, S]]

OCA at 10:25, 11 August 2016

OCA — Thu, 11 Aug 2016 10:25:37 GMT

←Older revision		Revision as of 10:25, 11 August 2016
Line 1:		Line 1:
		+
	==Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand==		==Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand==
	<StructureSection load='4uwi' size='340' side='right' caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>		<StructureSection load='4uwi' size='340' side='right' caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>
Line 6:		Line 7:
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4uwj\|4uwj]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4uwj\|4uwj]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glycylpeptide_N-tetradecanoyltransferase Glycylpeptide N-tetradecanoyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.97 2.3.1.97] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glycylpeptide_N-tetradecanoyltransferase Glycylpeptide N-tetradecanoyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.97 2.3.1.97] </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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [http://www.ebi.ac.uk/pdbsum/4uwi 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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [http://pdbe.org/4uwi PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [http://www.ebi.ac.uk/pdbsum/4uwi PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4uwi ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 18:		Line 19:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 4uwi" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 16:54, 25 December 2014

OCA — Thu, 25 Dec 2014 16:54:23 GMT

←Older revision		Revision as of 16:54, 25 December 2014
Line 8:		Line 8:
	<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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [http://www.ebi.ac.uk/pdbsum/4uwi 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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [http://www.ebi.ac.uk/pdbsum/4uwi PDBsum]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/NMT_ASPFU NMT_ASPFU]] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==

OCA at 09:30, 3 December 2014

OCA — Wed, 03 Dec 2014 09:30:24 GMT

←Older revision		Revision as of 09:30, 3 December 2014
Line 1:		Line 1:
-	'''~~Unreleased~~ structure'''	+	==Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand==
		+	<StructureSection load='4uwi' size='340' side='right' caption='[[4uwi]], [[Resolution\|resolution]] 1.80Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[4uwi]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UWI OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UWI FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=XMQ:2,6-DICHLORO-4-[3-(4-METHYLPIPERAZIN-1-YL)PROPYL]-N-(1,3,5-TRIMETHYL-1H-PYRAZOL-4-YL)BENZENESULFONAMIDE'>XMQ</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4uwj\|4uwj]]</td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glycylpeptide_N-tetradecanoyltransferase Glycylpeptide N-tetradecanoyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.3.1.97 2.3.1.97] </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=4uwi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4uwi OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4uwi RCSB], [http://www.ebi.ac.uk/pdbsum/4uwi PDBsum]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatment of human African trypanosomiasis (HAT). From previous studies, we identified pyrazole sulfonamide, DDD85646 (1), a potent inhibitor of TbNMT. Although this compound represents an excellent lead, poor central nervous system (CNS) exposure restricts its use to the hemolymphatic form (stage 1) of the disease. With a clear clinical need for new drug treatments for HAT that address both the hemolymphatic and CNS stages of the disease, a chemistry campaign was initiated to address the shortfalls of this series. This paper describes modifications to the pyrazole sulfonamides which markedly improved blood-brain barrier permeability, achieved by reducing polar surface area and capping the sulfonamide. Moreover, replacing the core aromatic with a flexible linker significantly improved selectivity. This led to the discovery of DDD100097 (40) which demonstrated partial efficacy in a stage 2 (CNS) mouse model of HAT.

-	~~The entry 4uwi is ON HOLD until Paper Publication~~	+	Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma brucei N-Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis.,Brand S, Norcross NR, Thompson S, Harrison JR, Smith VC, Robinson DA, Torrie LS, McElroy SP, Hallyburton I, Norval S, Scullion P, Stojanovski L, Simeons FR, van Aalten D, Frearson JA, Brenk R, Fairlamb AH, Ferguson MA, Wyatt PG, Gilbert IH, Read KD J Med Chem. 2014 Nov 20. PMID:25412409<ref>PMID:25412409</ref>

-	~~Authors: Robinson~~, D.A., Brand, S., ~~Norcross, N.~~R., ~~Thompson~~, S.~~, Harrison~~, J~~.R.~~, ~~Smith~~, ~~V.C., Torrie, L.S.~~, McElroy, S.P~~., Hallyburton, I.~~, Norval, S., ~~Stojanovski, L.~~, Simeons, F.R.C., ~~Frearson~~, ~~J.A.~~, ~~Brenk, R., Fairlamb, A.H., Ferguson, M.A.J.~~, Wyatt, P.G~~., Gilbert, I.H., Read, K.D.~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~Description~~: ~~Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand~~	+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Glycylpeptide N-tetradecanoyltransferase]]
		+	[[Category: Brand, S]]
		+	[[Category: Brenk, R]]
		+	[[Category: Fairlamb, A H]]
		+	[[Category: Ferguson, M A.J]]
		+	[[Category: Frearson, J A]]
		+	[[Category: Gilbert, I H]]
		+	[[Category: Hallyburton, I]]
		+	[[Category: Harrison, J R]]
		+	[[Category: McElroy, S P]]
		+	[[Category: Norcross, N R]]
		+	[[Category: Norval, S]]
		+	[[Category: Read, K D]]
		+	[[Category: Robinson, D A]]
		+	[[Category: Simeons, F R.C]]
		+	[[Category: Smith, V C]]
		+	[[Category: Stojanovski, L]]
		+	[[Category: Thompson, S]]
		+	[[Category: Torrie, L S]]
		+	[[Category: Wyatt, P G]]
		+	[[Category: Drug discovery]]
		+	[[Category: Transferase]]

OCA at 11:43, 19 November 2014

OCA — Wed, 19 Nov 2014 11:43:25 GMT

←Older revision		Revision as of 11:43, 19 November 2014
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4uwi is ON HOLD	+	The entry 4uwi is ON HOLD until Paper Publication

	Authors: Robinson, D.A., Brand, S., Norcross, N.R., Thompson, S., Harrison, J.R., Smith, V.C., Torrie, L.S., McElroy, S.P., Hallyburton, I., Norval, S., Stojanovski, L., Simeons, F.R.C., Frearson, J.A., Brenk, R., Fairlamb, A.H., Ferguson, M.A.J., Wyatt, P.G., Gilbert, I.H., Read, K.D.		Authors: Robinson, D.A., Brand, S., Norcross, N.R., Thompson, S., Harrison, J.R., Smith, V.C., Torrie, L.S., McElroy, S.P., Hallyburton, I., Norval, S., Stojanovski, L., Simeons, F.R.C., Frearson, J.A., Brenk, R., Fairlamb, A.H., Ferguson, M.A.J., Wyatt, P.G., Gilbert, I.H., Read, K.D.

	Description: Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand		Description: Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand

OCA: Protected "4uwi" [edit=sysop:move=sysop]

OCA — Wed, 20 Aug 2014 15:14:27 GMT

Protected "4uwi" [edit=sysop:move=sysop]

←Older revision

Revision as of 15:14, 20 August 2014

OCA: New page: '''Unreleased structure''' The entry 4uwi is ON HOLD Authors: Robinson, D.A., Brand, S., Norcross, N.R., Thompson, S., Harrison, J.R., Smith, V.C., Torrie, L.S., McElroy, S.P., Hallybur...

OCA — Wed, 20 Aug 2014 15:14:25 GMT

New page: '''Unreleased structure''' The entry 4uwi is ON HOLD Authors: Robinson, D.A., Brand, S., Norcross, N.R., Thompson, S., Harrison, J.R., Smith, V.C., Torrie, L.S., McElroy, S.P., Hallybur...

New page

'''Unreleased structure'''

The entry 4uwi is ON HOLD

Authors: Robinson, D.A., Brand, S., Norcross, N.R., Thompson, S., Harrison, J.R., Smith, V.C., Torrie, L.S., McElroy, S.P., Hallyburton, I., Norval, S., Stojanovski, L., Simeons, F.R.C., Frearson, J.A., Brenk, R., Fairlamb, A.H., Ferguson, M.A.J., Wyatt, P.G., Gilbert, I.H., Read, K.D.

Description: Crystal structure of Aspergillus fumigatus N-myristoyl transferase in complex with myristoyl CoA and a pyrazole sulphonamide ligand