8dsd - Revision history

OCA at 10:13, 25 October 2023

2023-10-25T10:13:50Z

← Older revision		Revision as of 10:13, 25 October 2023
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[8dsd]] is a 2 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=8DSD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DSD FirstGlance]. <br>		<table><tr><td colspan='2'>[[8dsd]] is a 2 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=8DSD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DSD FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NCA:NICOTINAMIDE'>NCA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=TIW:(3S)-1-[2-(4-methylphenyl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl]-N-{[4-(methylsulfanyl)phenyl]methyl}piperidine-3-carboxamide'>TIW</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]] 1.429Å</td></tr>
			<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NCA:NICOTINAMIDE'>NCA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=TIW:(3S)-1-[2-(4-methylphenyl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl]-N-{[4-(methylsulfanyl)phenyl]methyl}piperidine-3-carboxamide'>TIW</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=8dsd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dsd OCA], [https://pdbe.org/8dsd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dsd RCSB], [https://www.ebi.ac.uk/pdbsum/8dsd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dsd 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=8dsd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dsd OCA], [https://pdbe.org/8dsd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dsd RCSB], [https://www.ebi.ac.uk/pdbsum/8dsd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dsd ProSAT]</span></td></tr>
	</table>		</table>
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	</div>		</div>
	<div class="pdbe-citations 8dsd" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 8dsd" style="background-color:#fffaf0;"></div>

			==See Also==
			*[[Phosphoribosyltransferase 3D structures\|Phosphoribosyltransferase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 07:35, 8 March 2023

2023-03-08T07:35:02Z

← Older revision		Revision as of 07:35, 8 March 2023
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	~~'''Unreleased structure'''~~

	~~The entry~~ 8dsd is ~~ON HOLD until Paper~~ Publication		==Human NAMPT in complex with substrate NAM and small molecule activator NP-A1-S==
			<StructureSection load='8dsd' size='340' side='right'caption='[[8dsd]], [[Resolution\|resolution]] 1.43Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[8dsd]] is a 2 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=8DSD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8DSD FirstGlance]. <br>
			</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=NCA:NICOTINAMIDE'>NCA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=TIW:(3S)-1-[2-(4-methylphenyl)-2H-pyrazolo[3,4-d]pyrimidin-4-yl]-N-{[4-(methylsulfanyl)phenyl]methyl}piperidine-3-carboxamide'>TIW</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=8dsd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8dsd OCA], [https://pdbe.org/8dsd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8dsd RCSB], [https://www.ebi.ac.uk/pdbsum/8dsd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8dsd ProSAT]</span></td></tr>
			</table>
			== Function ==
			[https://www.uniprot.org/uniprot/NAMPT_HUMAN NAMPT_HUMAN] Catalyzes the condensation of nicotinamide with 5-phosphoribosyl-1-pyrophosphate to yield nicotinamide mononucleotide, an intermediate in the biosynthesis of NAD. It is the rate limiting component in the mammalian NAD biosynthesis pathway (By similarity).
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			In aging and disease, cellular nicotinamide adenine dinucleotide (NAD(+)) is depleted by catabolism to nicotinamide (NAM). NAD(+) supplementation is being pursued to enhance human healthspan and lifespan. Activation of nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting step in NAD(+) biosynthesis, has the potential to increase the salvage of NAM. Novel NAMPT-positive allosteric modulators (N-PAMs) were discovered in addition to the demonstration of NAMPT activation by biogenic phenols. The mechanism of activation was revealed through the synthesis of novel chemical probes, new NAMPT co-crystal structures, and enzyme kinetics. Binding to a rear channel in NAMPT regulates NAM binding and turnover, with biochemical observations being replicated by NAD(+) measurements in human cells. The mechanism of action of N-PAMs identifies, for the first time, the role of the rear channel in the regulation of NAMPT turnover coupled to productive and nonproductive NAM binding. The tight regulation of cellular NAMPT via feedback inhibition by NAM, NAD(+), and adenosine 5'-triphosphate (ATP) is differentially regulated by N-PAMs and other activators, indicating that different classes of pharmacological activators may be engineered to restore or enhance NAD(+) levels in affected tissues.

	~~Authors:~~ Ratia, K., ~~Xiong~~, R., ~~Shen~~, Z., Thatcher, ~~G.R~~.		Mechanism of Allosteric Modulation of Nicotinamide Phosphoribosyltransferase to Elevate Cellular NAD().,Ratia KM, Shen Z, Gordon-Blake J, Lee H, Laham MS, Krider IS, Christie N, Ackerman-Berrier M, Penton C, Knowles NG, Musku SR, Fu J, Velma GR, Xiong R, Thatcher GRJ Biochemistry. 2023 Feb 21;62(4):923-933. doi: 10.1021/acs.biochem.2c00655. Epub , 2023 Feb 6. PMID:36746631<ref>PMID:36746631</ref>

	~~Description: Human NAMPT in complex with substrate NAM and small molecule activator NP~~-A1-S		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	[[Category: ~~Unreleased Structures~~]]		</div>
	[[Category: ~~Thatcher, G.R~~]]		<div class="pdbe-citations 8dsd" style="background-color:#fffaf0;"></div>
	[[Category: Ratia, K]]		== References ==
	[[Category: ~~Xiong, R~~]]		<references/>
	[[Category: ~~Shen, Z~~]]		__TOC__
			</StructureSection>
			[[Category: Homo sapiens]]
			[[Category: Large Structures]]
			[[Category: Ratia K]]
			[[Category: Shen Z]]
			[[Category: Thatcher GR]]
			[[Category: Xiong R]]

OCA at 04:02, 10 August 2022

2022-08-10T04:02:16Z

← Older revision		Revision as of 04:02, 10 August 2022
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	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 8dsd is ON HOLD		The entry 8dsd is ON HOLD until Paper Publication

	Authors: Ratia, K., Xiong, R., Shen, Z., Thatcher, G.R.		Authors: Ratia, K., Xiong, R., Shen, Z., Thatcher, G.R.

OCA: Protected "8dsd" [edit=sysop:move=sysop]

2022-08-03T03:54:52Z

Protected "8dsd" [edit=sysop:move=sysop]

← Older revision	Revision as of 03:54, 3 August 2022
(No difference)

OCA: New page: '''Unreleased structure''' The entry 8dsd is ON HOLD Authors: Ratia, K., Xiong, R., Shen, Z., Thatcher, G.R. Description: Human NAMPT in complex with substrate NAM and small molecule a...

2022-08-03T03:54:52Z

New page: '''Unreleased structure''' The entry 8dsd is ON HOLD Authors: Ratia, K., Xiong, R., Shen, Z., Thatcher, G.R. Description: Human NAMPT in complex with substrate NAM and small molecule a...

New page

'''Unreleased structure'''

The entry 8dsd is ON HOLD

Authors: Ratia, K., Xiong, R., Shen, Z., Thatcher, G.R.

Description: Human NAMPT in complex with substrate NAM and small molecule activator NP-A1-S
[[Category: Unreleased Structures]]
[[Category: Thatcher, G.R]]
[[Category: Ratia, K]]
[[Category: Xiong, R]]
[[Category: Shen, Z]]