4afz - Revision history

OCA at 07:14, 1 May 2024

OCA — Wed, 01 May 2024 07:14:40 GMT

←Older revision		Revision as of 07:14, 1 May 2024
Line 3:		Line 3:
	<StructureSection load='4afz' size='340' side='right'caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>		<StructureSection load='4afz' size='340' side='right'caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Human Human~~] and [https://en.wikipedia.org/wiki/~~Synthetic_construct_sequences~~ Synthetic construct ~~sequences~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4afz]] is a 4 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=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=TAR:D(~~-~~)-TARTARIC+ACID'>TAR</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]] 2.25Å</td></tr>
-	<tr id='~~related~~'><td class="sblockLbl"><b>[[~~Related_structure~~\|~~Related~~:]]</b></td><td class="sblockDat"~~><div style='overflow: auto; max-height: 3em;'>[[1klt\|1klt]], [[1pjp\|1pjp]], [[1nn6\|1nn6]], [[4afu\|4afu]], [[1t31\|1t31]], [[4afq\|4afq]], [[4afs\|4afs]], [[4ag1\|4ag1]], [[4ag2\|4ag2]]</div></td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=TAR:D(-)-TARTARIC+ACID'>TAR</scene></td></tr>
-	~~<tr~~ id~~='activity'><td class~~="~~sblockLbl~~"><~~b>Activity:</b></td><td class~~=~~"sblockDat"><span class~~=~~'plainlinks~~'>~~[https://en.wikipedia.org/wiki/Chymase Chymase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.39 3.4.21.39]~~ </~~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=4afz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4afz OCA], [https://pdbe.org/4afz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4afz RCSB], [https://www.ebi.ac.uk/pdbsum/4afz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4afz 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=4afz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4afz OCA], [https://pdbe.org/4afz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4afz RCSB], [https://www.ebi.ac.uk/pdbsum/4afz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4afz ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/CMA1_HUMAN CMA1_HUMAN]] Major secreted protease of mast cells with suspected roles in vasoactive peptide generation, extracellular matrix degradation, and regulation of gland secretion.	+	[https://www.uniprot.org/uniprot/CMA1_HUMAN CMA1_HUMAN] Major secreted protease of mast cells with suspected roles in vasoactive peptide generation, extracellular matrix degradation, and regulation of gland secretion.
-	~~<div style="background-color:#fffaf0;">~~	+
-	~~== Publication Abstract from PubMed ==~~	+
-	The serine protease chymase (EC = 3.4.21.39) is expressed in the secretory granules of mast cells, which are important in allergic reactions. Fynomers, which are binding proteins derived from the Fyn SH3 domain, were generated against human chymase to produce binding partners to facilitate crystallization, structure determination and structure-based drug discovery, and to provide inhibitors of chymase for therapeutic applications. The best Fynomer was found to bind chymase with a KD of 0.9 nM and koff of 6.6x10 (-4) s (-1) , and to selectively inhibit chymase activity with an IC 50 value of 2 nM. Three different Fynomers were co-crystallized with chymase in 6 different crystal forms overall, with diffraction quality in the range of 2.25 to 1.4 A resolution, which is suitable for drug design efforts. The X-ray structures show that all Fynomers bind to the active site of chymase. The conserved residues Arg15-Trp16-Thr17 in the RT-loop of the chymase binding Fynomers provide a tight interaction, with Trp16 pointing deep into the S1 pocket of chymase. These results confirm the suitability of Fynomers as research tools to facilitate protein crystallization, as well as for the development of assays to investigate the biological mechanism of targets. Finally, their highly specific inhibitory activity and favorable molecular properties support the use of Fynomers as potential therapeutic agents.	+
-		+
-	Generation, characterization and structural data of chymase binding proteins based on the human Fyn kinase SH3 domain.,Schlatter D, Brack S, Banner DW, Batey S, Benz J, Bertschinger J, Huber W, Joseph C, Rufer A, van der Klooster A, Weber M, Grabulovski D, Hennig M MAbs. 2012 Jul 1;4(4):497-508. Epub 2012 Jul 1. PMID:22653218<ref>PMID:22653218</ref>	+
-		+
-	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~	+
-	~~</div>~~	+
-	~~<div class="pdbe-citations 4afz" style="background-color:#fffaf0;"></div>~~	+
-	~~== References ==~~	+
-	~~<references/>~~	+
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Chymase]]~~	+	[[Category: Homo sapiens]]
-	~~[[Category: Human~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Synthetic construct ~~sequences~~]]	+	[[Category: Synthetic construct]]
-	[[Category: Banner~~, D W~~]]	+	[[Category: Banner DW]]
-	[[Category: Batey, S]]	+	[[Category: Batey S]]
-	[[Category: Benz, J]]	+	[[Category: Benz J]]
-	[[Category: Bertschinger, J]]	+	[[Category: Bertschinger J]]
-	[[Category: Brack, S]]	+	[[Category: Brack S]]
-	[[Category: Grabulovski, D]]	+	[[Category: Grabulovski D]]
-	[[Category: Hennig, M]]	+	[[Category: Hennig M]]
-	[[Category: Huber, W]]	+	[[Category: Huber W]]
-	[[Category: Joseph, C]]	+	[[Category: Joseph C]]
-	~~[[Category: Kloosters, A Van Der~~]]	+	[[Category: Rufer A]]
-	[[Category: Rufer, A]]	+	[[Category: Schlatter D]]
-	[[Category: Schlatter, D]]	+	[[Category: Van Der Kloosters A]]
-	[[Category: ~~Weber, M~~]]	+	[[Category: Weber M]]
-	[[Category: ~~Hydrolase-de novo protein complex]]~~	+
-	~~[[Category: Inhibitor]]~~	+
-	~~[[Category: Serine protease~~]]	+

OCA at 05:32, 25 August 2022

OCA — Thu, 25 Aug 2022 05:32:53 GMT

←Older revision		Revision as of 05:32, 25 August 2022
Line 3:		Line 3:
	<StructureSection load='4afz' size='340' side='right'caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>		<StructureSection load='4afz' size='340' side='right'caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/Human Human] and [~~http~~://en.wikipedia.org/wiki/Synthetic_construct_sequences Synthetic construct sequences]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human] and [https://en.wikipedia.org/wiki/Synthetic_construct_sequences Synthetic construct sequences]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=TAR:D(-)-TARTARIC+ACID'>TAR</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=TAR:D(-)-TARTARIC+ACID'>TAR</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1klt\|1klt]], [[1pjp\|1pjp]], [[1nn6\|1nn6]], [[4afu\|4afu]], [[1t31\|1t31]], [[4afq\|4afq]], [[4afs\|4afs]], [[4ag1\|4ag1]], [[4ag2\|4ag2]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1klt\|1klt]], [[1pjp\|1pjp]], [[1nn6\|1nn6]], [[4afu\|4afu]], [[1t31\|1t31]], [[4afq\|4afq]], [[4afs\|4afs]], [[4ag1\|4ag1]], [[4ag2\|4ag2]]</div></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/Chymase Chymase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.39 3.4.21.39] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Chymase Chymase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.39 3.4.21.39] </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=4afz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4afz OCA], [~~http~~://pdbe.org/4afz PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4afz RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4afz PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4afz 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=4afz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4afz OCA], [https://pdbe.org/4afz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4afz RCSB], [https://www.ebi.ac.uk/pdbsum/4afz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4afz ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/CMA1_HUMAN CMA1_HUMAN]] Major secreted protease of mast cells with suspected roles in vasoactive peptide generation, extracellular matrix degradation, and regulation of gland secretion.	+	[[https://www.uniprot.org/uniprot/CMA1_HUMAN CMA1_HUMAN]] Major secreted protease of mast cells with suspected roles in vasoactive peptide generation, extracellular matrix degradation, and regulation of gland secretion.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 26:		Line 26:
	[[Category: Chymase]]		[[Category: Chymase]]
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Synthetic construct sequences]]		[[Category: Synthetic construct sequences]]
	[[Category: Banner, D W]]		[[Category: Banner, D W]]

OCA at 09:07, 6 March 2019

OCA — Wed, 06 Mar 2019 09:07:53 GMT

←Older revision		Revision as of 09:07, 6 March 2019
Line 1:		Line 1:

	==Human Chymase - Fynomer Complex==		==Human Chymase - Fynomer Complex==
-	<StructureSection load='4afz' size='340' side='right' caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>	+	<StructureSection load='4afz' size='340' side='right'caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human] and [http://en.wikipedia.org/wiki/Synthetic_construct_sequences Synthetic construct sequences]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>		<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human] and [http://en.wikipedia.org/wiki/Synthetic_construct_sequences Synthetic construct sequences]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>

OCA at 12:34, 4 August 2016

OCA — Thu, 04 Aug 2016 12:34:19 GMT

←Older revision		Revision as of 12:34, 4 August 2016
Line 1:		Line 1:
		+
	==Human Chymase - Fynomer Complex==		==Human Chymase - Fynomer Complex==
	<StructureSection load='4afz' size='340' side='right' caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>		<StructureSection load='4afz' size='340' side='right' caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Homo_sapiens Homo sapiens~~] and [http://en.wikipedia.org/wiki/~~Synthetic_construct~~ Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human] and [http://en.wikipedia.org/wiki/Synthetic_construct_sequences Synthetic construct sequences]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=TAR:D(-)-TARTARIC+ACID'>TAR</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=TAR:D(-)-TARTARIC+ACID'>TAR</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1klt\|1klt]], [[1pjp\|1pjp]], [[1nn6\|1nn6]], [[4afu\|4afu]], [[1t31\|1t31]], [[4afq\|4afq]], [[4afs\|4afs]], [[4ag1\|4ag1]], [[4ag2\|4ag2]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1klt\|1klt]], [[1pjp\|1pjp]], [[1nn6\|1nn6]], [[4afu\|4afu]], [[1t31\|1t31]], [[4afq\|4afq]], [[4afs\|4afs]], [[4ag1\|4ag1]], [[4ag2\|4ag2]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Chymase Chymase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.39 3.4.21.39] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Chymase Chymase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.39 3.4.21.39] </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=4afz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4afz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4afz RCSB], [http://www.ebi.ac.uk/pdbsum/4afz 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=4afz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4afz OCA], [http://pdbe.org/4afz PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4afz RCSB], [http://www.ebi.ac.uk/pdbsum/4afz PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4afz ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 18:		Line 19:
	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 4afz" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>
Line 23:		Line 25:
	</StructureSection>		</StructureSection>
	[[Category: Chymase]]		[[Category: Chymase]]
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
-	[[Category: Synthetic construct]]	+	[[Category: Synthetic construct sequences]]
	[[Category: Banner, D W]]		[[Category: Banner, D W]]
	[[Category: Batey, S]]		[[Category: Batey, S]]

OCA at 14:33, 24 December 2014

OCA — Wed, 24 Dec 2014 14:33:22 GMT

←Older revision		Revision as of 14:33, 24 December 2014
Line 1:		Line 1:
-	[[~~Image:~~4afz.~~png~~\|~~left~~\|~~200px~~]]	+	==Human Chymase - Fynomer Complex==
		+	<StructureSection load='4afz' size='340' side='right' caption='[[4afz]], [[Resolution\|resolution]] 2.25Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[4afz]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4AFZ FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=TAR:D(-)-TARTARIC+ACID'>TAR</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1klt\|1klt]], [[1pjp\|1pjp]], [[1nn6\|1nn6]], [[4afu\|4afu]], [[1t31\|1t31]], [[4afq\|4afq]], [[4afs\|4afs]], [[4ag1\|4ag1]], [[4ag2\|4ag2]]</td></tr>
		+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Chymase Chymase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.21.39 3.4.21.39] </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=4afz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4afz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4afz RCSB], [http://www.ebi.ac.uk/pdbsum/4afz PDBsum]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/CMA1_HUMAN CMA1_HUMAN]] Major secreted protease of mast cells with suspected roles in vasoactive peptide generation, extracellular matrix degradation, and regulation of gland secretion.
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	The serine protease chymase (EC = 3.4.21.39) is expressed in the secretory granules of mast cells, which are important in allergic reactions. Fynomers, which are binding proteins derived from the Fyn SH3 domain, were generated against human chymase to produce binding partners to facilitate crystallization, structure determination and structure-based drug discovery, and to provide inhibitors of chymase for therapeutic applications. The best Fynomer was found to bind chymase with a KD of 0.9 nM and koff of 6.6x10 (-4) s (-1) , and to selectively inhibit chymase activity with an IC 50 value of 2 nM. Three different Fynomers were co-crystallized with chymase in 6 different crystal forms overall, with diffraction quality in the range of 2.25 to 1.4 A resolution, which is suitable for drug design efforts. The X-ray structures show that all Fynomers bind to the active site of chymase. The conserved residues Arg15-Trp16-Thr17 in the RT-loop of the chymase binding Fynomers provide a tight interaction, with Trp16 pointing deep into the S1 pocket of chymase. These results confirm the suitability of Fynomers as research tools to facilitate protein crystallization, as well as for the development of assays to investigate the biological mechanism of targets. Finally, their highly specific inhibitory activity and favorable molecular properties support the use of Fynomers as potential therapeutic agents.

-	~~{{STRUCTURE_4afz\| PDB=4afz \| SCENE= }}~~	+	Generation, characterization and structural data of chymase binding proteins based on the human Fyn kinase SH3 domain.,Schlatter D, Brack S, Banner DW, Batey S, Benz J, Bertschinger J, Huber W, Joseph C, Rufer A, van der Klooster A, Weber M, Grabulovski D, Hennig M MAbs. 2012 Jul 1;4(4):497-508. Epub 2012 Jul 1. PMID:22653218<ref>PMID:22653218</ref>

-	~~===Human Chymase - Fynomer Complex===~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~{{ABSTRACT_PUBMED_22653218}}~~	+	== References ==
-		+	<references/>
-	~~==About this Structure==~~	+	__TOC__
-	~~[[4afz]] is~~ a ~~4 chain structure with sequence from [http://en~~.~~wikipedia~~.~~org/wiki/Homo_sapiens Homo sapiens] and [http://en~~.~~wikipedia.org~~/~~wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA].~~	+	</StructureSection>
-		+
-	==~~Reference~~==	+
-	<~~ref group="xtra">PMID:022653218<~~/~~ref~~><~~references group="xtra"~~/>	+
	[[Category: Chymase]]		[[Category: Chymase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
	[[Category: Synthetic construct]]		[[Category: Synthetic construct]]
-	[[Category: Banner, D W.]]	+	[[Category: Banner, D W]]
-	[[Category: Batey, S.]]	+	[[Category: Batey, S]]
-	[[Category: Benz, J.]]	+	[[Category: Benz, J]]
-	[[Category: Bertschinger, J.]]	+	[[Category: Bertschinger, J]]
-	[[Category: Brack, S.]]	+	[[Category: Brack, S]]
-	[[Category: Grabulovski, D.]]	+	[[Category: Grabulovski, D]]
-	[[Category: Hennig, M.]]	+	[[Category: Hennig, M]]
-	[[Category: Huber, W.]]	+	[[Category: Huber, W]]
-	[[Category: Joseph, C.]]	+	[[Category: Joseph, C]]
-	[[Category: Kloosters, A Van Der.]]	+	[[Category: Kloosters, A Van Der]]
-	[[Category: Rufer, A.]]	+	[[Category: Rufer, A]]
-	[[Category: Schlatter, D.]]	+	[[Category: Schlatter, D]]
-	[[Category: Weber, M.]]	+	[[Category: Weber, M]]
	[[Category: Hydrolase-de novo protein complex]]		[[Category: Hydrolase-de novo protein complex]]
	[[Category: Inhibitor]]		[[Category: Inhibitor]]
	[[Category: Serine protease]]		[[Category: Serine protease]]

OCA at 04:55, 15 August 2012

OCA — Wed, 15 Aug 2012 04:55:08 GMT

←Older revision		Revision as of 04:55, 15 August 2012
Line 1:		Line 1:
-	[[Image:4afz.~~jpg~~\|left\|200px]]	+	[[Image:4afz.png\|left\|200px]]

	{{STRUCTURE_4afz\| PDB=4afz \| SCENE= }}		{{STRUCTURE_4afz\| PDB=4afz \| SCENE= }}
Line 25:		Line 25:
	[[Category: Joseph, C.]]		[[Category: Joseph, C.]]
	[[Category: Kloosters, A Van Der.]]		[[Category: Kloosters, A Van Der.]]
-	[[Category: Rudolph, M G.]]
	[[Category: Rufer, A.]]		[[Category: Rufer, A.]]
	[[Category: Schlatter, D.]]		[[Category: Schlatter, D.]]

OCA at 08:13, 11 July 2012

OCA — Wed, 11 Jul 2012 08:13:58 GMT

←Older revision		Revision as of 08:13, 11 July 2012
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	[[Image:4afz.jpg\|left\|200px]]

-	~~The entry~~ 4afz ~~is ON HOLD~~ ~~until Paper Publication~~	+	{{STRUCTURE_4afz\| PDB=4afz \| SCENE= }}

-	~~Authors: SCHLATTER, D., BRACK, S., BANNER, D.W., BATEY, S., BENZ, J., BERTSCHINGER, J., HUBER, W., JOSEPH, C., RUDOLPH, M.G., RUFER, A., VAN DER KLOOSTERS, A., WEBER, M., GRABULOVSKI, D., HENNIG, M.~~	+	===Human Chymase - Fynomer Complex===

-	~~Description~~: ~~Human~~ Chymase -~~Fynomer Complex~~	+	{{ABSTRACT_PUBMED_22653218}}
		+
		+	==About this Structure==
		+	[[4afz]] is a 4 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [http://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4AFZ OCA].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:022653218</ref><references group="xtra"/>
		+	[[Category: Chymase]]
		+	[[Category: Homo sapiens]]
		+	[[Category: Synthetic construct]]
		+	[[Category: Banner, D W.]]
		+	[[Category: Batey, S.]]
		+	[[Category: Benz, J.]]
		+	[[Category: Bertschinger, J.]]
		+	[[Category: Brack, S.]]
		+	[[Category: Grabulovski, D.]]
		+	[[Category: Hennig, M.]]
		+	[[Category: Huber, W.]]
		+	[[Category: Joseph, C.]]
		+	[[Category: Kloosters, A Van Der.]]
		+	[[Category: Rudolph, M G.]]
		+	[[Category: Rufer, A.]]
		+	[[Category: Schlatter, D.]]
		+	[[Category: Weber, M.]]
		+	[[Category: Hydrolase-de novo protein complex]]
		+	[[Category: Inhibitor]]
		+	[[Category: Serine protease]]

OCA at 08:19, 29 February 2012

OCA — Wed, 29 Feb 2012 08:19:04 GMT

←Older revision		Revision as of 08:19, 29 February 2012
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

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

	Authors: SCHLATTER, D., BRACK, S., BANNER, D.W., BATEY, S., BENZ, J., BERTSCHINGER, J., HUBER, W., JOSEPH, C., RUDOLPH, M.G., RUFER, A., VAN DER KLOOSTERS, A., WEBER, M., GRABULOVSKI, D., HENNIG, M.		Authors: SCHLATTER, D., BRACK, S., BANNER, D.W., BATEY, S., BENZ, J., BERTSCHINGER, J., HUBER, W., JOSEPH, C., RUDOLPH, M.G., RUFER, A., VAN DER KLOOSTERS, A., WEBER, M., GRABULOVSKI, D., HENNIG, M.

	Description: Human Chymase -Fynomer Complex		Description: Human Chymase -Fynomer Complex

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

OCA — Wed, 01 Feb 2012 06:57:35 GMT

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

←Older revision

Revision as of 06:57, 1 February 2012

OCA: New page: '''Unreleased structure''' The entry 4afz is ON HOLD Authors: SCHLATTER, D., BRACK, S., BANNER, D.W., BATEY, S., BENZ, J., BERTSCHINGER, J., HUBER, W., JOSEPH, C., RUDOLPH, M.G., RUFER,...

OCA — Wed, 01 Feb 2012 06:57:34 GMT

New page: '''Unreleased structure''' The entry 4afz is ON HOLD Authors: SCHLATTER, D., BRACK, S., BANNER, D.W., BATEY, S., BENZ, J., BERTSCHINGER, J., HUBER, W., JOSEPH, C., RUDOLPH, M.G., RUFER,...

New page

'''Unreleased structure'''

The entry 4afz is ON HOLD

Authors: SCHLATTER, D., BRACK, S., BANNER, D.W., BATEY, S., BENZ, J., BERTSCHINGER, J., HUBER, W., JOSEPH, C., RUDOLPH, M.G., RUFER, A., VAN DER KLOOSTERS, A., WEBER, M., GRABULOVSKI, D., HENNIG, M.

Description: Human Chymase -Fynomer Complex