4ryd - Revision history

OCA at 10:33, 15 March 2023

OCA — Wed, 15 Mar 2023 10:33:53 GMT

←Older revision		Revision as of 10:33, 15 March 2023
Line 3:		Line 3:
	<StructureSection load='4ryd' size='340' side='right'caption='[[4ryd]], [[Resolution\|resolution]] 2.15Å' scene=''>		<StructureSection load='4ryd' size='340' side='right'caption='[[4ryd]], [[Resolution\|resolution]] 2.15Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4ryd]] is a 12 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=4RYD OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4RYD FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4ryd]] is a 12 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=4RYD OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4RYD 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=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>~~	+	</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=2UE:1-[4-(2-OXOETHYL)BENZYL]GUANIDINE'>2UE</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=TBG:3-METHYL-L-VALINE'>TBG</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>, <scene name='pdbligand=2UE:1-[4-(2-OXOETHYL)BENZYL]GUANIDINE'>2UE</scene>, <scene name='pdbligand=~~TBG~~:~~3-METHYL-L-VALINE~~'>~~TBG~~</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=4ryd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ryd OCA], [https://pdbe.org/4ryd PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4ryd RCSB], [https://www.ebi.ac.uk/pdbsum/4ryd PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4ryd ProSAT]</span></td></tr>
-	~~<tr id~~='~~related'><td class~~=~~"sblockLbl"><b>[[Related_structure\|Related~~:~~]]</b~~></td>~~<td class="sblockDat">[[4omc\|4omc]]~~, ~~[[4omd\|4omd]], [[1p8j\|1p8j]]~~<~~/td></tr>~~	+
-	~~<tr id~~='~~gene'><td class~~=~~"sblockLbl"><b>[[Gene\|Gene~~:~~]]</b~~></td>~~<td class="sblockDat">FUR~~, ~~FURIN, 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=4ryd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ryd OCA], [~~http~~://pdbe.org/4ryd PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4ryd RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4ryd PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4ryd 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 22:		Line 18:
	</div>		</div>
	<div class="pdbe-citations 4ryd" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 4ryd" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Furin\|Furin]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Furin]]~~	+	[[Category: Homo sapiens]]
-	~~[[Category: Human~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Dahms~~, S O~~]]	+	[[Category: Dahms SO]]
-	[[Category: Than~~, M E]]~~	+	[[Category: Than ME]]
-	~~[[Category: Competitive inhibitor]]~~	+
-	~~[[Category: Hydrolase-hydrolase inhibitor complex]]~~	+
-	~~[[Category: Pro-protein convertase]]~~	+
-	~~[[Category: Serine protease~~]]	+

OCA at 09:55, 1 May 2019

OCA — Wed, 01 May 2019 09:55:19 GMT

←Older revision		Revision as of 09:55, 1 May 2019
Line 1:		Line 1:

	==X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba==		==X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba==
-	<StructureSection load='4ryd' size='340' side='right' caption='[[4ryd]], [[Resolution\|resolution]] 2.15Å' scene=''>	+	<StructureSection load='4ryd' size='340' side='right'caption='[[4ryd]], [[Resolution\|resolution]] 2.15Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4ryd]] is a 12 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4RYD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4RYD FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4ryd]] is a 12 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=4RYD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4RYD 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=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>		</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=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</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>, <scene name='pdbligand=2UE:1-[4-(2-OXOETHYL)BENZYL]GUANIDINE'>2UE</scene>, <scene name='pdbligand=TBG:3-METHYL-L-VALINE'>TBG</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>, <scene name='pdbligand=2UE:1-[4-(2-OXOETHYL)BENZYL]GUANIDINE'>2UE</scene>, <scene name='pdbligand=TBG:3-METHYL-L-VALINE'>TBG</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4omc\|4omc]], [[4omd\|4omd]], [[1p8j\|1p8j]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4omc\|4omc]], [[4omd\|4omd]], [[1p8j\|1p8j]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">FUR, FURIN, 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='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=4ryd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ryd OCA], [http://pdbe.org/4ryd PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ryd RCSB], [http://www.ebi.ac.uk/pdbsum/4ryd PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ryd 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=4ryd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ryd OCA], [http://pdbe.org/4ryd PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ryd RCSB], [http://www.ebi.ac.uk/pdbsum/4ryd PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ryd ProSAT]</span></td></tr>
Line 26:		Line 27:
	</StructureSection>		</StructureSection>
	[[Category: Furin]]		[[Category: Furin]]
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Dahms, S O]]		[[Category: Dahms, S O]]
	[[Category: Than, M E]]		[[Category: Than, M E]]

OCA at 13:27, 19 April 2017

OCA — Wed, 19 Apr 2017 13:27:40 GMT

←Older revision		Revision as of 13:27, 19 April 2017
Line 1:		Line 1:
		+
	==X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba==		==X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba==
	<StructureSection load='4ryd' size='340' side='right' caption='[[4ryd]], [[Resolution\|resolution]] 2.15Å' scene=''>		<StructureSection load='4ryd' size='340' side='right' caption='[[4ryd]], [[Resolution\|resolution]] 2.15Å' scene=''>
Line 7:		Line 8:
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4omc\|4omc]], [[4omd\|4omd]], [[1p8j\|1p8j]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4omc\|4omc]], [[4omd\|4omd]], [[1p8j\|1p8j]]</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'>[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=4ryd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ryd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ryd RCSB], [http://www.ebi.ac.uk/pdbsum/4ryd 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=4ryd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ryd OCA], [http://pdbe.org/4ryd PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4ryd RCSB], [http://www.ebi.ac.uk/pdbsum/4ryd PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4ryd ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
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	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 4ryd" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 12:36, 1 July 2015

OCA — Wed, 01 Jul 2015 12:36:06 GMT

←Older revision		Revision as of 12:36, 1 July 2015
Line 4:		Line 4:
	<table><tr><td colspan='2'>[[4ryd]] is a 12 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4RYD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4RYD FirstGlance]. <br>		<table><tr><td colspan='2'>[[4ryd]] is a 12 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4RYD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4RYD 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=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>		</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=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</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>, <scene name='pdbligand=~~2UC~~:1-[3-(2-OXOETHYL)BENZYL]GUANIDINE'>~~2UC~~</scene>, <scene name='pdbligand=TBG:3-METHYL-L-VALINE'>TBG</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>, <scene name='pdbligand=2UE:1-[4-(2-OXOETHYL)BENZYL]GUANIDINE'>2UE</scene>, <scene name='pdbligand=TBG:3-METHYL-L-VALINE'>TBG</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4omc\|4omc]], [[4omd\|4omd]], [[1p8j\|1p8j]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4omc\|4omc]], [[4omd\|4omd]], [[1p8j\|1p8j]]</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'>[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>

OCA at 15:51, 27 May 2015

OCA — Wed, 27 May 2015 15:51:51 GMT

←Older revision		Revision as of 15:51, 27 May 2015
Line 1:		Line 1:
-	'''~~Unreleased~~ structure'''	+	==X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba==
		+	<StructureSection load='4ryd' size='340' side='right' caption='[[4ryd]], [[Resolution\|resolution]] 2.15Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[4ryd]] is a 12 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4RYD OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4RYD 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=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</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>, <scene name='pdbligand=2UC:1-[3-(2-OXOETHYL)BENZYL]GUANIDINE'>2UC</scene>, <scene name='pdbligand=TBG:3-METHYL-L-VALINE'>TBG</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4omc\|4omc]], [[4omd\|4omd]], [[1p8j\|1p8j]]</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=4ryd FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4ryd OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4ryd RCSB], [http://www.ebi.ac.uk/pdbsum/4ryd PDBsum]</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 ==
		+	New peptidomimetic furin inhibitors with unnatural amino acid residues in the P3 position were synthesized. The most potent compound 4-guanidinomethyl-phenylacteyl-Arg-Tle-Arg-4-amidinobenzylamide (MI-1148) inhibits furin with a Ki value of 5.5 pM. The derivatives also strongly inhibit PC1/3, whereas PC2 is less affected. Selected inhibitors were tested in cell culture for antibacterial and antiviral activity against infectious agents known to be dependent on furin activity. A significant protective effect against anthrax and diphtheria toxin was observed in the presence of the furin inhibitors. Furthermore, the spread of the highly pathogenic H5N1 and H7N1 avian influenza viruses and propagation of canine distemper virus was strongly inhibited. Inhibitor MI-1148 was crystallized in complex with human furin. Its N-terminal guanidinomethyl group in the para position of the P5 phenyl ring occupies the same position as that found previously for a structurally related inhibitor containing this substitution in the meta position, thereby maintaining all of the important P5 interactions. Our results confirm that the inhibition of furin is a promising strategy for a short-term treatment of acute infectious diseases.

-	~~The entry 4ryd is ON HOLD until Paper Publication~~	+	Novel Furin Inhibitors with Potent Anti-infectious Activity.,Hardes K, Becker GL, Lu Y, Dahms SO, Kohler S, Beyer W, Sandvig K, Yamamoto H, Lindberg I, Walz L, von Messling V, Than ME, Garten W, Steinmetzer T ChemMedChem. 2015 May 14. doi: 10.1002/cmdc.201500103. PMID:25974265<ref>PMID:25974265</ref>

-	~~Authors: Dahms~~, S.~~O., Than, M.E~~.	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~Description: X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba~~	+	== References ==
-	[[Category: ~~Unreleased Structures~~]]	+	<references/>
-	[[Category: Dahms, S.O]]	+	__TOC__
-	[[Category: Than, M.E]]	+	</StructureSection>
		+	[[Category: Furin]]
		+	[[Category: Dahms, S O]]
		+	[[Category: Than, M E]]
		+	[[Category: Competitive inhibitor]]
		+	[[Category: Hydrolase-hydrolase inhibitor complex]]
		+	[[Category: Pro-protein convertase]]
		+	[[Category: Serine protease]]

OCA at 08:39, 12 February 2015

OCA — Thu, 12 Feb 2015 08:39:45 GMT

←Older revision		Revision as of 08:39, 12 February 2015
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors: Dahms, S.O., Than, M.E.		Authors: Dahms, S.O., Than, M.E.

OCA at 17:36, 24 December 2014

OCA — Wed, 24 Dec 2014 17:36:37 GMT

←Older revision		Revision as of 17:36, 24 December 2014
Line 6:		Line 6:

	Description: X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba		Description: X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba
		+	[[Category: Unreleased Structures]]
		+	[[Category: Dahms, S.O]]
		+	[[Category: Than, M.E]]

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

OCA — Wed, 24 Dec 2014 09:32:31 GMT

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

←Older revision

Revision as of 09:32, 24 December 2014

OCA: New page: '''Unreleased structure''' The entry 4ryd is ON HOLD Authors: Dahms, S.O., Than, M.E. Description: X-ray structure of human furin in complex with the competitive inhibitor para-guanidi...

OCA — Wed, 24 Dec 2014 09:32:29 GMT

New page: '''Unreleased structure''' The entry 4ryd is ON HOLD Authors: Dahms, S.O., Than, M.E. Description: X-ray structure of human furin in complex with the competitive inhibitor para-guanidi...

New page

'''Unreleased structure'''

The entry 4ryd is ON HOLD

Authors: Dahms, S.O., Than, M.E.

Description: X-ray structure of human furin in complex with the competitive inhibitor para-guanidinomethyl-Phac-R-Tle-R-Amba