6cgw - Revision history

OCA at 10:17, 15 November 2023

OCA — Wed, 15 Nov 2023 10:17:51 GMT

←Older revision		Revision as of 10:17, 15 November 2023
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[6cgw]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Chilobrachys_guangxiensis Chilobrachys guangxiensis]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CGW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6CGW FirstGlance]. <br>		<table><tr><td colspan='2'>[[6cgw]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Chilobrachys_guangxiensis Chilobrachys guangxiensis]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CGW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6CGW FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NLE:NORLEUCINE'>NLE</scene></td></tr>	+	</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NLE:NORLEUCINE'>NLE</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=6cgw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6cgw OCA], [https://pdbe.org/6cgw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6cgw RCSB], [https://www.ebi.ac.uk/pdbsum/6cgw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6cgw 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=6cgw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6cgw OCA], [https://pdbe.org/6cgw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6cgw RCSB], [https://www.ebi.ac.uk/pdbsum/6cgw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6cgw ProSAT]</span></td></tr>
	</table>		</table>

OCA at 10:39, 14 June 2023

OCA — Wed, 14 Jun 2023 10:39:54 GMT

←Older revision		Revision as of 10:39, 14 June 2023
Line 1:		Line 1:

	==Solution NMR structure of JzTx-V, a Nav 1.7 inhibitory peptide==		==Solution NMR structure of JzTx-V, a Nav 1.7 inhibitory peptide==
-	<StructureSection load='6cgw' size='340' side='right'caption='[[6cgw~~]], [[NMR_Ensembles_of_Models \| 8 NMR models~~]]' scene=''>	+	<StructureSection load='6cgw' size='340' side='right'caption='[[6cgw]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6cgw]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CGW OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=6CGW FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6cgw]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Chilobrachys_guangxiensis Chilobrachys guangxiensis]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CGW OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6CGW FirstGlance]. <br>
-	</td></tr><tr id='~~NonStdRes~~'><td class="sblockLbl"><b>[[~~Non-Standard_Residue~~\|~~NonStd Res~~:]]</b></td><td class="sblockDat"><scene name='pdbligand=NLE:NORLEUCINE'>NLE</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NLE:NORLEUCINE'>NLE</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=6cgw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6cgw OCA], [~~http~~://pdbe.org/6cgw PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6cgw RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6cgw PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6cgw 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=6cgw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6cgw OCA], [https://pdbe.org/6cgw PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6cgw RCSB], [https://www.ebi.ac.uk/pdbsum/6cgw PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6cgw ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/JZTX5_CHIGU JZTX5_CHIGU]] Inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium channels (Nav) in rat dorsal root ganglion neurons. Highly inhibits Kv4.2/KCND2 and Kv4.3/KCND3 potassium channels and weakly inhibits Kv2.1/KCNB1 potassium channels. The toxin shifts the activation curves to more depolarized potentials. Also binds to phospholipid membranes.<ref>PMID:17150181</ref> <ref>PMID:17157888</ref> <ref>PMID:18581053</ref> <ref>PMID:20571743</ref>	+	[https://www.uniprot.org/uniprot/JZTX5_CHIGU JZTX5_CHIGU] Inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium channels (Nav) in rat dorsal root ganglion neurons. Highly inhibits Kv4.2/KCND2 and Kv4.3/KCND3 potassium channels and weakly inhibits Kv2.1/KCNB1 potassium channels. The toxin shifts the activation curves to more depolarized potentials. Also binds to phospholipid membranes.<ref>PMID:17150181</ref> <ref>PMID:17157888</ref> <ref>PMID:18581053</ref> <ref>PMID:20571743</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 22:		Line 22:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Chilobrachys guangxiensis]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Andrews, K]]	+	[[Category: Andrews K]]
-	[[Category: Jordan~~, J B]]~~	+	[[Category: Jordan JB]]
-	~~[[Category: Fractionated tarantula venom]]~~	+
-	~~[[Category: Nav 1 7 inhibitor]]~~	+
-	~~[[Category: Toxin~~]]	+

OCA at 08:57, 11 November 2020

OCA — Wed, 11 Nov 2020 08:57:06 GMT

←Older revision		Revision as of 08:57, 11 November 2020
Line 1:		Line 1:

	==Solution NMR structure of JzTx-V, a Nav 1.7 inhibitory peptide==		==Solution NMR structure of JzTx-V, a Nav 1.7 inhibitory peptide==
-	<StructureSection load='6cgw' size='340' side='right' caption='[[6cgw]], [[NMR_Ensembles_of_Models \| 8 NMR models]]' scene=''>	+	<StructureSection load='6cgw' size='340' side='right'caption='[[6cgw]], [[NMR_Ensembles_of_Models \| 8 NMR models]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6cgw]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CGW OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6CGW FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6cgw]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CGW OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=6CGW FirstGlance]. <br>
	</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=NLE:NORLEUCINE'>NLE</scene></td></tr>		</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=NLE:NORLEUCINE'>NLE</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=6cgw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6cgw OCA], [http://pdbe.org/6cgw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6cgw RCSB], [http://www.ebi.ac.uk/pdbsum/6cgw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6cgw 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=6cgw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6cgw OCA], [http://pdbe.org/6cgw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6cgw RCSB], [http://www.ebi.ac.uk/pdbsum/6cgw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6cgw ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 22:		Line 22:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Andrews, K]]		[[Category: Andrews, K]]
	[[Category: Jordan, J B]]		[[Category: Jordan, J B]]

OCA at 05:59, 16 May 2018

OCA — Wed, 16 May 2018 05:59:14 GMT

←Older revision		Revision as of 05:59, 16 May 2018
Line 9:		Line 9:
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/JZTX5_CHIGU JZTX5_CHIGU]] Inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium channels (Nav) in rat dorsal root ganglion neurons. Highly inhibits Kv4.2/KCND2 and Kv4.3/KCND3 potassium channels and weakly inhibits Kv2.1/KCNB1 potassium channels. The toxin shifts the activation curves to more depolarized potentials. Also binds to phospholipid membranes.<ref>PMID:17150181</ref> <ref>PMID:17157888</ref> <ref>PMID:18581053</ref> <ref>PMID:20571743</ref>		[[http://www.uniprot.org/uniprot/JZTX5_CHIGU JZTX5_CHIGU]] Inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium channels (Nav) in rat dorsal root ganglion neurons. Highly inhibits Kv4.2/KCND2 and Kv4.3/KCND3 potassium channels and weakly inhibits Kv2.1/KCNB1 potassium channels. The toxin shifts the activation curves to more depolarized potentials. Also binds to phospholipid membranes.<ref>PMID:17150181</ref> <ref>PMID:17157888</ref> <ref>PMID:18581053</ref> <ref>PMID:20571743</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Identification of voltage-gated sodium channel NaV1.7 inhibitors for chronic pain therapeutic development is an area of vigorous pursuit. In an effort to identify more potent leads compared to our previously reported GpTx-1 peptide series, electrophysiology screening of fractionated tarantula venom discovered the NaV1.7 inhibitory peptide JzTx-V from the Chinese earth tiger tarantula Chilobrachys jingzhao. The parent peptide displayed nominal selectivity over the skeletal muscle NaV1.4 channel. Attribute-based positional scan analoging identified a key Ile28Glu mutation that improved NaV1.4 selectivity over 100-fold, and further optimization yielded the potent and selective peptide leads AM-8145 and AM-0422. NMR analyses revealed that the Ile28Glu substitution changed peptide conformation, pointing to a structural rationale for the selectivity gains. AM-8145 and AM-0422 as well as GpTx-1 and HwTx-IV competed for ProTx-II binding in HEK293 cells expressing human NaV1.7, suggesting that these NaV1.7 inhibitory peptides interact with a similar binding site. AM-8145 potently blocked native tetrodotoxin-sensitive (TTX-S) channels in mouse dorsal root ganglia (DRG) neurons, exhibited 30- to 120-fold selectivity over other human TTX-S channels and exhibited over 1,000-fold selectivity over other human tetrodotoxin-resistant (TTX-R) channels. Leveraging NaV1.7-NaV1.5 chimeras containing various voltage-sensor and pore regions, AM-8145 mapped to the second voltage-sensor domain of NaV1.7. AM-0422, but not the inactive peptide analog AM-8374, dose-dependently blocked capsaicin-induced DRG neuron action potential firing using a multi-electrode array readout and mechanically-induced C-fiber spiking in a saphenous skin-nerve preparation. Collectively, AM-8145 and AM-0422 represent potent, new engineered NaV1.7 inhibitory peptides derived from the JzTx-V scaffold with improved NaV selectivity and biological activity in blocking action potential firing in both DRG neurons and C-fibers.
		+
		+	Pharmacological characterization of potent and selective NaV1.7 inhibitors engineered from Chilobrachys jingzhao tarantula venom peptide JzTx-V.,Moyer BD, Murray JK, Ligutti J, Andrews K, Favreau P, Jordan JB, Lee JH, Liu D, Long J, Sham K, Shi L, Stocklin R, Wu B, Yin R, Yu V, Zou A, Biswas K, Miranda LP PLoS One. 2018 May 3;13(5):e0196791. doi: 10.1371/journal.pone.0196791., eCollection 2018. PMID:29723257<ref>PMID:29723257</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 6cgw" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 08:09, 2 May 2018

OCA — Wed, 02 May 2018 08:09:44 GMT

←Older revision		Revision as of 08:09, 2 May 2018
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6cgw is ~~ON HOLD~~	+	==Solution NMR structure of JzTx-V, a Nav 1.7 inhibitory peptide==
-		+	<StructureSection load='6cgw' size='340' side='right' caption='[[6cgw]], [[NMR_Ensembles_of_Models \| 8 NMR models]]' scene=''>
-	~~Authors~~:	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[6cgw]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6CGW OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6CGW FirstGlance]. <br>
-	~~Description~~:	+	</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=NLE:NORLEUCINE'>NLE</scene></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	<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=6cgw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6cgw OCA], [http://pdbe.org/6cgw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6cgw RCSB], [http://www.ebi.ac.uk/pdbsum/6cgw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6cgw ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/JZTX5_CHIGU JZTX5_CHIGU]] Inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium channels (Nav) in rat dorsal root ganglion neurons. Highly inhibits Kv4.2/KCND2 and Kv4.3/KCND3 potassium channels and weakly inhibits Kv2.1/KCNB1 potassium channels. The toxin shifts the activation curves to more depolarized potentials. Also binds to phospholipid membranes.<ref>PMID:17150181</ref> <ref>PMID:17157888</ref> <ref>PMID:18581053</ref> <ref>PMID:20571743</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Andrews, K]]
		+	[[Category: Jordan, J B]]
		+	[[Category: Fractionated tarantula venom]]
		+	[[Category: Nav 1 7 inhibitor]]
		+	[[Category: Toxin]]

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

OCA — Wed, 28 Feb 2018 05:04:30 GMT

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

←Older revision

Revision as of 05:04, 28 February 2018

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

OCA — Wed, 28 Feb 2018 05:04:29 GMT

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

New page

'''Unreleased structure'''

The entry 6cgw is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]