6dna - Revision history

OCA at 06:10, 11 October 2023

OCA — Wed, 11 Oct 2023 06:10:14 GMT

←Older revision		Revision as of 06:10, 11 October 2023
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	==Crystal structure of T110A mutant human Glutamate oxaloacetate transaminase 1 (GOT1)==		==Crystal structure of T110A mutant human Glutamate oxaloacetate transaminase 1 (GOT1)==
-	<StructureSection load='6dna' size='340' side='right' caption='[[6dna]], [[Resolution\|resolution]] 3.00Å' scene=''>	+	<StructureSection load='6dna' size='340' side='right'caption='[[6dna]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6dna]] is a 6 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=6DNA OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6DNA FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6dna]] is a 6 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=6DNA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6DNA FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat"~~><scene name~~=~~'pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene~~>, ~~<scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</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]] 3Å</td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat">~~GOT1 ([http~~:/~~/www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode~~=~~Info&srchmode~~=5~~&id=9606 HUMAN])~~</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</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=6dna FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dna OCA], [~~http~~://pdbe.org/6dna PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6dna RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6dna PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6dna 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=6dna FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dna OCA], [https://pdbe.org/6dna PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6dna RCSB], [https://www.ebi.ac.uk/pdbsum/6dna PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6dna ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/AATC_HUMAN AATC_HUMAN]] Plays a key role in amino acid metabolism (By similarity).	+	[https://www.uniprot.org/uniprot/AATC_HUMAN AATC_HUMAN] Plays a key role in amino acid metabolism (By similarity).
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</div>		</div>
	<div class="pdbe-citations 6dna" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 6dna" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Aspartate aminotransferase 3D structures\|Aspartate aminotransferase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
-	[[Category: Assar, Z]]	+	[[Category: Large Structures]]
-	[[Category: Holt~~, M C~~]]	+	[[Category: Assar Z]]
-	[[Category: Lairson, L]]	+	[[Category: Holt MC]]
-	[[Category: Lyssiotis~~, C A~~]]	+	[[Category: Lairson L]]
-	[[Category: Stein~~, A J]]~~	+	[[Category: Lyssiotis CA]]
-	~~[[Category: Aspartate aminotransferase]]~~	+	[[Category: Stein AJ]]
-	~~[[Category: Glutamate oxaloacetate transaminase 1]]~~	+
-	~~[[Category: Got1]]~~	+
-	~~[[Category: Plp]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 07:03, 5 December 2018

OCA — Wed, 05 Dec 2018 07:03:14 GMT

←Older revision		Revision as of 07:03, 5 December 2018
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	<StructureSection load='6dna' size='340' side='right' caption='[[6dna]], [[Resolution\|resolution]] 3.00Å' scene=''>		<StructureSection load='6dna' size='340' side='right' caption='[[6dna]], [[Resolution\|resolution]] 3.00Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6dna]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6DNA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6DNA FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6dna]] is a 6 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=6DNA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6DNA FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">GOT1 ([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=6dna FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dna OCA], [http://pdbe.org/6dna PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6dna RCSB], [http://www.ebi.ac.uk/pdbsum/6dna PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6dna 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=6dna FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dna OCA], [http://pdbe.org/6dna PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6dna RCSB], [http://www.ebi.ac.uk/pdbsum/6dna PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6dna ProSAT]</span></td></tr>
	</table>		</table>
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Assar, Z]]		[[Category: Assar, Z]]
	[[Category: Holt, M C]]		[[Category: Holt, M C]]

OCA at 08:15, 14 November 2018

OCA — Wed, 14 Nov 2018 08:15:41 GMT

←Older revision		Revision as of 08:15, 14 November 2018
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-	'''Unreleased structure'''

-	~~The entry~~ 6dna is ~~ON HOLD until Paper~~ Publication	+	==Crystal structure of T110A mutant human Glutamate oxaloacetate transaminase 1 (GOT1)==
		+	<StructureSection load='6dna' size='340' side='right' caption='[[6dna]], [[Resolution\|resolution]] 3.00Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6dna]] is a 6 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6DNA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6DNA FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=PG4:TETRAETHYLENE+GLYCOL'>PG4</scene>, <scene name='pdbligand=PLP:PYRIDOXAL-5-PHOSPHATE'>PLP</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=6dna FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dna OCA], [http://pdbe.org/6dna PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6dna RCSB], [http://www.ebi.ac.uk/pdbsum/6dna PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6dna ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/AATC_HUMAN AATC_HUMAN]] Plays a key role in amino acid metabolism (By similarity).
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Pancreatic cancer cells are characterized by deregulated metabolic programs that facilitate growth and resistance to oxidative stress. Among these programs, pancreatic cancers preferentially utilize a metabolic pathway through the enzyme aspartate aminotransferase 1 [also known as glutamate oxaloacetate transaminase 1 (GOT1)] to support cellular redox homeostasis. As such, small molecule inhibitors that target GOT1 could serve as starting points for the development of new therapies for pancreatic cancer. We ran a high-throughput screen for inhibitors of GOT1 and identified a small molecule, iGOT1-01, with in vitro GOT1 inhibitor activity. Application in pancreatic cancer cells revealed metabolic and growth inhibitory activity reflecting a promiscuous inhibitory profile. We then performed an in silico docking analysis to study inhibitor-GOT1 interactions with iGOT1-01 analogues that possess improved solubility and potency properties. These results suggested that the GOT1 inhibitor competed for binding to the pyridoxal 5-phosphate (PLP) cofactor site of GOT1. To analyze how the GOT1 inhibitor bound to GOT1, a series of GOT1 mutant enzymes that abolished PLP binding were generated. Application of the mutants in X-ray crystallography and thermal shift assays again suggested but were unable to formally conclude that the GOT1 inhibitor bound to the PLP site. Mutational studies revealed the relationship between PLP binding and the thermal stability of GOT1 while highlighting the essential nature of several residues for GOT1 catalytic activity. Insight into the mode of action of GOT1 inhibitors may provide leads to the development of drugs that target redox balance in pancreatic cancer.

-	~~Authors~~:	+	Biochemical Characterization and Structure-Based Mutational Analysis Provide Insight into the Binding and Mechanism of Action of Novel Aspartate Aminotransferase Inhibitors.,Holt MC, Assar Z, Beheshti Zavareh R, Lin L, Anglin J, Mashadova O, Haldar D, Mullarky E, Kremer DM, Cantley LC, Kimmelman AC, Stein AJ, Lairson LL, Lyssiotis CA Biochemistry. 2018 Nov 12. doi: 10.1021/acs.biochem.8b00914. PMID:30365304<ref>PMID:30365304</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 6dna" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Assar, Z]]
		+	[[Category: Holt, M C]]
		+	[[Category: Lairson, L]]
		+	[[Category: Lyssiotis, C A]]
		+	[[Category: Stein, A J]]
		+	[[Category: Aspartate aminotransferase]]
		+	[[Category: Glutamate oxaloacetate transaminase 1]]
		+	[[Category: Got1]]
		+	[[Category: Plp]]
		+	[[Category: Transferase]]

OCA at 04:02, 11 July 2018

OCA — Wed, 11 Jul 2018 04:02:51 GMT

←Older revision		Revision as of 04:02, 11 July 2018
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	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors:		Authors:

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

OCA — Thu, 14 Jun 2018 05:47:00 GMT

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

←Older revision

Revision as of 05:47, 14 June 2018

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

OCA — Thu, 14 Jun 2018 05:46:58 GMT

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

New page

'''Unreleased structure'''

The entry 6dna is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]