6hza - Revision history

OCA at 11:42, 24 January 2024

OCA — Wed, 24 Jan 2024 11:42:49 GMT

←Older revision		Revision as of 11:42, 24 January 2024
Line 3:		Line 3:
	<StructureSection load='6hza' size='340' side='right'caption='[[6hza]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='6hza' size='340' side='right'caption='[[6hza]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6hza]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6HZA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6HZA FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6hza]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6HZA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6HZA FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=PTD:PENTANEDIAL'>PTD</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]] 1.9Å</td></tr>
-	~~<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=00S:4-(AMINOMETHYL)BENZENECARBOXIMIDAMIDE'>00S</scene></td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=00S:4-(AMINOMETHYL)BENZENECARBOXIMIDAMIDE'>00S</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=PTD:PENTANEDIAL'>PTD</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">FURIN, FUR, PACE, PCSK3 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>	+
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Furin Furin], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.75 3.4.21.75] </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=6hza FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hza OCA], [https://pdbe.org/6hza PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6hza RCSB], [https://www.ebi.ac.uk/pdbsum/6hza PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6hza 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=6hza FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hza OCA], [https://pdbe.org/6hza PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6hza RCSB], [https://www.ebi.ac.uk/pdbsum/6hza PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6hza ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/FURIN_HUMAN FURIN_HUMAN]] Furin is likely to represent the ubiquitous endoprotease activity within constitutive secretory pathways and capable of cleavage at the RX(K/R)R consensus motif.<ref>PMID:7690548</ref>	+	[https://www.uniprot.org/uniprot/FURIN_HUMAN FURIN_HUMAN] Furin is likely to represent the ubiquitous endoprotease activity within constitutive secretory pathways and capable of cleavage at the RX(K/R)R consensus motif.<ref>PMID:7690548</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 28:		Line 26:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Furin]]~~	+	[[Category: Homo sapiens]]
-	~~[[Category: Human~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Dahms, S O~~]]	+	[[Category: Synthetic construct]]
-	[[Category: ~~Hydrolase]]~~	+	[[Category: Dahms SO]]
-	~~[[Category: Protease proprotein convertase inhibitor complex cyclic peptide~~]]	+

OCA at 10:26, 18 March 2021

OCA — Thu, 18 Mar 2021 10:26:57 GMT

←Older revision		Revision as of 10:26, 18 March 2021
Line 3:		Line 3:
	<StructureSection load='6hza' size='340' side='right'caption='[[6hza]], [[Resolution\|resolution]] 1.90Å' scene=''>		<StructureSection load='6hza' size='340' side='right'caption='[[6hza]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[6hza]] is a 2 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=6HZA OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=6HZA FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[6hza]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6HZA OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6HZA FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=PTD:PENTANEDIAL'>PTD</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=PTD:PENTANEDIAL'>PTD</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=00S:4-(AMINOMETHYL)BENZENECARBOXIMIDAMIDE'>00S</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=00S:4-(AMINOMETHYL)BENZENECARBOXIMIDAMIDE'>00S</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">FURIN, FUR, PACE, PCSK3 ([~~http~~://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">FURIN, FUR, PACE, PCSK3 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/Furin Furin], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.75 3.4.21.75] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Furin Furin], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.75 3.4.21.75] </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=6hza FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hza OCA], [~~http~~://pdbe.org/6hza PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=6hza RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/6hza PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=6hza 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=6hza FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hza OCA], [https://pdbe.org/6hza PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6hza RCSB], [https://www.ebi.ac.uk/pdbsum/6hza PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6hza ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/FURIN_HUMAN FURIN_HUMAN]] Furin is likely to represent the ubiquitous endoprotease activity within constitutive secretory pathways and capable of cleavage at the RX(K/R)R consensus motif.<ref>PMID:7690548</ref>	+	[[https://www.uniprot.org/uniprot/FURIN_HUMAN FURIN_HUMAN]] Furin is likely to represent the ubiquitous endoprotease activity within constitutive secretory pathways and capable of cleavage at the RX(K/R)R consensus motif.<ref>PMID:7690548</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 21:		Line 21:
	</div>		</div>
	<div class="pdbe-citations 6hza" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 6hza" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Furin\|Furin]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 08:17, 3 April 2019

OCA — Wed, 03 Apr 2019 08:17:33 GMT

←Older revision		Revision as of 08:17, 3 April 2019
Line 1:		Line 1:

	==X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-Arg-4-Amba==		==X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-Arg-4-Amba==
-	<StructureSection load='6hza' size='340' side='right' caption='[[6hza]], [[Resolution\|resolution]] 1.90Å' scene=''>	+	<StructureSection load='6hza' size='340' side='right'caption='[[6hza]], [[Resolution\|resolution]] 1.90Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[6hza]] is a 2 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=6HZA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6HZA FirstGlance]. <br>		<table><tr><td colspan='2'>[[6hza]] is a 2 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=6HZA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6HZA FirstGlance]. <br>
Line 27:		Line 27:
	[[Category: Furin]]		[[Category: Furin]]
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Dahms, S O]]		[[Category: Dahms, S O]]
	[[Category: Hydrolase]]		[[Category: Hydrolase]]
	[[Category: Protease proprotein convertase inhibitor complex cyclic peptide]]		[[Category: Protease proprotein convertase inhibitor complex cyclic peptide]]

OCA at 16:00, 27 February 2019

OCA — Wed, 27 Feb 2019 16:00:28 GMT

←Older revision		Revision as of 16:00, 27 February 2019
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 6hza is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-Arg-4-Amba==
		+	<StructureSection load='6hza' size='340' side='right' caption='[[6hza]], [[Resolution\|resolution]] 1.90Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[6hza]] is a 2 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=6HZA OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6HZA FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=PO4:PHOSPHATE+ION'>PO4</scene>, <scene name='pdbligand=PTD:PENTANEDIAL'>PTD</scene></td></tr>
		+	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=00S:4-(AMINOMETHYL)BENZENECARBOXIMIDAMIDE'>00S</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">FURIN, FUR, PACE, PCSK3 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Furin Furin], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.75 3.4.21.75] </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=6hza FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hza OCA], [http://pdbe.org/6hza PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6hza RCSB], [http://www.ebi.ac.uk/pdbsum/6hza PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6hza ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/FURIN_HUMAN FURIN_HUMAN]] Furin is likely to represent the ubiquitous endoprotease activity within constitutive secretory pathways and capable of cleavage at the RX(K/R)R consensus motif.<ref>PMID:7690548</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The activation of viral glycoproteins by the host protease furin is an essential step in the replication of numerous pathogenic viruses. Thus, effective inhibitors of furin could serve as broad-spectrum antiviral drugs. A crystal structure of an inhibitory hexapeptide derivative in complex with furin served as template for the rational design of various types of new cyclic inhibitors. Most of the prepared derivatives are relatively potent furin inhibitors with inhibition constants in the low nanomolar or even sub-nanomolar range. For seven derivatives the crystal structures in complex with furin could be determined. In three complexes, electron density was found for the entire inhibitor. In the other cases the structures could be determined only for the P6/P5-P1 segments, which directly interact with furin. The cyclic derivatives together with two non-cyclic reference compounds were tested as inhibitors of the proteolytic activation and replication of respiratory syncytial virus in cells. Significant antiviral activity was found for both linear reference inhibitors, whereas a negligible efficacy was determined for the cyclic derivatives.

-	~~Authors:~~ Dahms, S.O.	+	Design, Synthesis, and Characterization of Macrocyclic Inhibitors of the Proprotein Convertase Furin.,Lam van TV, Ivanova T, Hardes K, Heindl MR, Morty RE, Bottcher-Friebertshauser E, Lindberg I, Than ME, Dahms SO, Steinmetzer T ChemMedChem. 2019 Jan 25. doi: 10.1002/cmdc.201800807. PMID:30680958<ref>PMID:30680958</ref>

-	~~Description: X-ray structure~~ of ~~furin in complex with~~ the ~~cyclic peptide c[glutaryl~~-~~Arg~~-~~Arg-Lys~~]~~-Arg-4-Amba~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
-	[[Category: Dahms, S.O]]	+	<div class="pdbe-citations 6hza" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Furin]]
		+	[[Category: Human]]
		+	[[Category: Dahms, S O]]
		+	[[Category: Hydrolase]]
		+	[[Category: Protease proprotein convertase inhibitor complex cyclic peptide]]

OCA at 18:29, 2 December 2018

OCA — Sun, 02 Dec 2018 18:29:33 GMT

←Older revision		Revision as of 18:29, 2 December 2018
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors: Dahms, S.O.		Authors: Dahms, S.O.

-	Description: X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-~~Lys~~-4-Amba	+	Description: X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-Arg-4-Amba
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
	[[Category: Dahms, S.O]]		[[Category: Dahms, S.O]]

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

OCA — Wed, 31 Oct 2018 05:13:15 GMT

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

←Older revision

Revision as of 05:13, 31 October 2018

OCA: New page: '''Unreleased structure''' The entry 6hza is ON HOLD Authors: Dahms, S.O. Description: X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-Lys-4-Amba [[...

OCA — Wed, 31 Oct 2018 05:13:13 GMT

New page: '''Unreleased structure''' The entry 6hza is ON HOLD Authors: Dahms, S.O. Description: X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-Lys-4-Amba [[...

New page

'''Unreleased structure'''

The entry 6hza is ON HOLD

Authors: Dahms, S.O.

Description: X-ray structure of furin in complex with the cyclic peptide c[glutaryl-Arg-Arg-Lys]-Lys-4-Amba
[[Category: Unreleased Structures]]
[[Category: Dahms, S.O]]