3rkz - Revision history

OCA at 12:28, 14 March 2024

OCA — Thu, 14 Mar 2024 12:28:19 GMT

←Older revision		Revision as of 12:28, 14 March 2024
Line 3:		Line 3:
	<StructureSection load='3rkz' size='340' side='right'caption='[[3rkz]], [[Resolution\|resolution]] 1.57Å' scene=''>		<StructureSection load='3rkz' size='340' side='right'caption='[[3rkz]], [[Resolution\|resolution]] 1.57Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3rkz]] is a 1 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=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3rkz]] is a 1 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=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</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]] 1.5693Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">HSP90A, HSP90AA1, HSPC1, HSPCA ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [https://pdbe.org/3rkz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [https://www.ebi.ac.uk/pdbsum/3rkz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rkz 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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [https://pdbe.org/3rkz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [https://www.ebi.ac.uk/pdbsum/3rkz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rkz ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/HS90A_HUMAN HS90A_HUMAN]] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.<ref>PMID:15937123</ref> <ref>PMID:11274138</ref>	+	[https://www.uniprot.org/uniprot/HS90A_HUMAN HS90A_HUMAN] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.<ref>PMID:15937123</ref> <ref>PMID:11274138</ref>
-	~~<div style="background-color:#fffaf0;">~~	+
-	~~== Publication Abstract from PubMed ==~~	+
-	An extension of our previously reported series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. Addition of a second methyl group to the tether provided analogs that show increased potency in binding as well as cell-proliferation assays and, more importantly, are stable toward microsomes. We wish to disclose the discovery of a macrocycle which showed impressive biomarker activity 24-h post dosing and which demonstrated prolonged exposure in tumors. When studied in a lung cancer xenograft model, the compound demonstrated significant tumor size reduction.	+
-		+
-	Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.,Zapf CW, Bloom JD, Li Z, Dushin RG, Nittoli T, Otteng M, Nikitenko A, Golas JM, Liu H, Lucas J, Boschelli F, Vogan E, Olland A, Johnson M, Levin JI Bioorg Med Chem Lett. 2011 Jun 27. PMID:21715165<ref>PMID:21715165</ref>	+
-		+
-	~~From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>~~	+
-	~~</div>~~	+
-	~~<div class="pdbe-citations 3rkz" style="background-color:#fffaf0;"></div~~>	+

	==See Also==		==See Also==
Line 26:		Line 17:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Bloom~~, J D~~]]	+	[[Category: Bloom JD]]
-	[[Category: Boschelli, F]]	+	[[Category: Boschelli F]]
-	[[Category: Dushin~~, R G~~]]	+	[[Category: Dushin RG]]
-	[[Category: Golas~~, J M~~]]	+	[[Category: Golas JM]]
-	[[Category: Johnson, M]]	+	[[Category: Johnson M]]
-	[[Category: Levin~~, J I~~]]	+	[[Category: Levin JI]]
-	[[Category: Li, Z]]	+	[[Category: Li Z]]
-	[[Category: Liu, H]]	+	[[Category: Liu H]]
-	[[Category: Lucas, J]]	+	[[Category: Lucas J]]
-	[[Category: Nikitenko, A]]	+	[[Category: Nikitenko A]]
-	[[Category: Nittoli, T]]	+	[[Category: Nittoli T]]
-	[[Category: Olland, A]]	+	[[Category: Olland A]]
-	[[Category: Otteng, M]]	+	[[Category: Otteng M]]
-	[[Category: Vogan, E]]	+	[[Category: Vogan E]]
-	[[Category: Zapf~~, C W]]~~	+	[[Category: Zapf CW]]
-	~~[[Category: Atp binding domain]]~~	+
-	~~[[Category: Atp-binding]]~~	+
-	~~[[Category: Chaperone]]~~	+
-	~~[[Category: Chaperone-chaperone inhibitor complex]]~~	+
-	~~[[Category: Nucleotide-binding]]~~	+
-	~~[[Category: Phosphoprotein]]~~	+
-	~~[[Category: Stress response~~]]	+

OCA at 10:15, 22 June 2022

OCA — Wed, 22 Jun 2022 10:15:12 GMT

←Older revision		Revision as of 10:15, 22 June 2022
Line 1:		Line 1:

	==Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.==		==Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.==
-	<StructureSection load='3rkz' size='340' side='right' caption='[[3rkz]], [[Resolution\|resolution]] 1.57Å' scene=''>	+	<StructureSection load='3rkz' size='340' side='right'caption='[[3rkz]], [[Resolution\|resolution]] 1.57Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3rkz]] is a 1 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=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3rkz]] is a 1 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=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">HSP90A, HSP90AA1, HSPC1, HSPCA ([~~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">HSP90A, HSP90AA1, HSPC1, HSPCA ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [~~http~~://pdbe.org/3rkz PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3rkz PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3rkz 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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [https://pdbe.org/3rkz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [https://www.ebi.ac.uk/pdbsum/3rkz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3rkz ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/HS90A_HUMAN HS90A_HUMAN]] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.<ref>PMID:15937123</ref> <ref>PMID:11274138</ref>	+	[[https://www.uniprot.org/uniprot/HS90A_HUMAN HS90A_HUMAN]] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.<ref>PMID:15937123</ref> <ref>PMID:11274138</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 21:		Line 21:

	==See Also==		==See Also==
-	*[[Heat Shock ~~Proteins~~\|Heat Shock ~~Proteins~~]]	+	*[[Heat Shock Protein structures\|Heat Shock Protein structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 27:		Line 27:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Bloom, J D]]		[[Category: Bloom, J D]]
	[[Category: Boschelli, F]]		[[Category: Boschelli, F]]

OCA at 09:24, 5 August 2016

OCA — Fri, 05 Aug 2016 09:24:37 GMT

←Older revision		Revision as of 09:24, 5 August 2016
Line 1:		Line 1:
		+
	==Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.==		==Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.==
	<StructureSection load='3rkz' size='340' side='right' caption='[[3rkz]], [[Resolution\|resolution]] 1.57Å' scene=''>		<StructureSection load='3rkz' size='340' side='right' caption='[[3rkz]], [[Resolution\|resolution]] 1.57Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3rkz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Homo_sapiens Homo sapiens~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3rkz]] is a 1 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=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">HSP90A, HSP90AA1, HSPC1, HSPCA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">HSP90A, HSP90AA1, HSPC1, HSPCA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [http://www.ebi.ac.uk/pdbsum/3rkz 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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [http://pdbe.org/3rkz PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [http://www.ebi.ac.uk/pdbsum/3rkz PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3rkz ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 17:		Line 18:
	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 3rkz" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 24:		Line 26:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Bloom, J D]]		[[Category: Bloom, J D]]
	[[Category: Boschelli, F]]		[[Category: Boschelli, F]]

OCA at 17:38, 25 December 2014

OCA — Thu, 25 Dec 2014 17:38:48 GMT

←Older revision		Revision as of 17:38, 25 December 2014
Line 7:		Line 7:
	<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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [http://www.ebi.ac.uk/pdbsum/3rkz 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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [http://www.ebi.ac.uk/pdbsum/3rkz PDBsum]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/HS90A_HUMAN HS90A_HUMAN]] Molecular chaperone that promotes the maturation, structural maintenance and proper regulation of specific target proteins involved for instance in cell cycle control and signal transduction. Undergoes a functional cycle that is linked to its ATPase activity. This cycle probably induces conformational changes in the client proteins, thereby causing their activation. Interacts dynamically with various co-chaperones that modulate its substrate recognition, ATPase cycle and chaperone function.<ref>PMID:15937123</ref> <ref>PMID:11274138</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==

OCA at 12:34, 9 December 2014

OCA — Tue, 09 Dec 2014 12:34:31 GMT

←Older revision		Revision as of 12:34, 9 December 2014
Line 1:		Line 1:
-	[[~~Image:~~3rkz.~~png~~\|~~left~~\|~~200px~~]]	+	==Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.==
		+	<StructureSection load='3rkz' size='340' side='right' caption='[[3rkz]], [[Resolution\|resolution]] 1.57Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[3rkz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3RKZ FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=06T:(5R,6S)-3-(L-ALANYL)-5,6,15,15,18-PENTAMETHYL-17-OXO-2,3,4,5,6,7,14,15,16,17-DECAHYDRO-1H-12,8-(METHENO)[1,5,9]TRIAZACYCLOTETRADECINO[1,2-A]INDOLE-9-CARBOXAMIDE'>06T</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">HSP90A, HSP90AA1, HSPC1, HSPCA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</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=3rkz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3rkz OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3rkz RCSB], [http://www.ebi.ac.uk/pdbsum/3rkz PDBsum]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	An extension of our previously reported series of macrocyclic ortho-aminobenzamide Hsp90 inhibitors is reported. Addition of a second methyl group to the tether provided analogs that show increased potency in binding as well as cell-proliferation assays and, more importantly, are stable toward microsomes. We wish to disclose the discovery of a macrocycle which showed impressive biomarker activity 24-h post dosing and which demonstrated prolonged exposure in tumors. When studied in a lung cancer xenograft model, the compound demonstrated significant tumor size reduction.

-	~~{{STRUCTURE_3rkz\| PDB=3rkz \| SCENE= }}~~	+	Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.,Zapf CW, Bloom JD, Li Z, Dushin RG, Nittoli T, Otteng M, Nikitenko A, Golas JM, Liu H, Lucas J, Boschelli F, Vogan E, Olland A, Johnson M, Levin JI Bioorg Med Chem Lett. 2011 Jun 27. PMID:21715165<ref>PMID:21715165</ref>

-	~~===Discovery of~~ a ~~stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable~~ of ~~significantly decreasing tumor volume in a mouse xenograft model~~.~~===~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~{{ABSTRACT_PUBMED_21715165}}~~	+
-		+
-	~~==About this Structure==~~	+
-	~~[[3rkz]] is a 1 chain structure with sequence from [http://en~~.~~wikipedia~~.~~org~~/~~wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA].~~	+

	==See Also==		==See Also==
	*[[Heat Shock Proteins\|Heat Shock Proteins]]		*[[Heat Shock Proteins\|Heat Shock Proteins]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	<~~ref group="xtra">PMID:021715165<~~/~~ref~~><~~references group="xtra"~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Bloom, J D.]]	+	[[Category: Bloom, J D]]
-	[[Category: Boschelli, F.]]	+	[[Category: Boschelli, F]]
-	[[Category: Dushin, R G.]]	+	[[Category: Dushin, R G]]
-	[[Category: Golas, J M.]]	+	[[Category: Golas, J M]]
-	[[Category: Johnson, M.]]	+	[[Category: Johnson, M]]
-	[[Category: Levin, J I.]]	+	[[Category: Levin, J I]]
-	[[Category: Li, Z.]]	+	[[Category: Li, Z]]
-	[[Category: Liu, H.]]	+	[[Category: Liu, H]]
-	[[Category: Lucas, J.]]	+	[[Category: Lucas, J]]
-	[[Category: Nikitenko, A.]]	+	[[Category: Nikitenko, A]]
-	[[Category: Nittoli, T.]]	+	[[Category: Nittoli, T]]
-	[[Category: Olland, A.]]	+	[[Category: Olland, A]]
-	[[Category: Otteng, M.]]	+	[[Category: Otteng, M]]
-	[[Category: Vogan, E.]]	+	[[Category: Vogan, E]]
-	[[Category: Zapf, C W.]]	+	[[Category: Zapf, C W]]
	[[Category: Atp binding domain]]		[[Category: Atp binding domain]]
	[[Category: Atp-binding]]		[[Category: Atp-binding]]

OCA at 19:33, 20 October 2012

OCA — Sat, 20 Oct 2012 19:33:08 GMT

←Older revision		Revision as of 19:33, 20 October 2012
Line 8:		Line 8:

	==About this Structure==		==About this Structure==
-	[[3rkz]] is a 1 chain structure ~~of [[Heat Shock Proteins]]~~ with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA].	+	[[3rkz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA].

	==See Also==		==See Also==

OCA at 07:43, 27 July 2012

OCA — Fri, 27 Jul 2012 07:43:12 GMT

←Older revision		Revision as of 07:43, 27 July 2012
Line 1:		Line 1:
	[[Image:3rkz.png\|left\|200px]]		[[Image:3rkz.png\|left\|200px]]

-	<!--
-	The line below this paragraph, containing "STRUCTURE_3rkz", creates the "Structure Box" on the page.
-	You may change the PDB parameter (which sets the PDB file loaded into the applet)
-	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-	or leave the SCENE parameter empty for the default display.
-	-->
	{{STRUCTURE_3rkz\| PDB=3rkz \| SCENE= }}		{{STRUCTURE_3rkz\| PDB=3rkz \| SCENE= }}

	===Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.===		===Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.===

-
-	<!--
-	The line below this paragraph, {{ABSTRACT_PUBMED_21715165}}, adds the Publication Abstract to the page
-	(as it appears on PubMed at http://www.pubmed.gov), where 21715165 is the PubMed ID number.
-	-->
	{{ABSTRACT_PUBMED_21715165}}		{{ABSTRACT_PUBMED_21715165}}

	==About this Structure==		==About this Structure==
-	[[3rkz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA].	+	[[3rkz]] is a 1 chain structure of [[Heat Shock Proteins]] with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA].
		+
		+	==See Also==
		+	*[[Heat Shock Proteins\|Heat Shock Proteins]]

	==Reference==		==Reference==

OCA at 07:59, 3 August 2011

OCA — Wed, 03 Aug 2011 07:59:44 GMT

←Older revision		Revision as of 07:59, 3 August 2011
Line 1:		Line 1:
-	[[Image:3rkz.~~jpg~~\|left\|200px]]	+	[[Image:3rkz.png\|left\|200px]]

	<!--		<!--

OCA at 07:35, 13 July 2011

OCA — Wed, 13 Jul 2011 07:35:23 GMT

←Older revision		Revision as of 07:35, 13 July 2011
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	[[Image:3rkz.jpg\|left\|200px]]

-	The ~~entry 3rkz~~ is ~~ON HOLD~~ ~~until Paper Publication~~	+	<!--
		+	The line below this paragraph, containing "STRUCTURE_3rkz", creates the "Structure Box" on the page.
		+	You may change the PDB parameter (which sets the PDB file loaded into the applet)
		+	or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
		+	or leave the SCENE parameter empty for the default display.
		+	-->
		+	{{STRUCTURE_3rkz\| PDB=3rkz \| SCENE= }}

-	~~Authors: Zapf, C.W., Bloom, J.D., Li, Z., Dushin, R.G., Nittoli, T., Otteng, M., Nikitenko, A., Golas, J.M., Liu, H., Lucas, J., Boschelli, F., Vogan, E., Olland, A., Johnson, M., Levin, J.I~~.	+	===Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.===

-	~~Description~~: ~~Discovery of a stable macrocyclic o~~-~~aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in~~ a ~~mouse xenograft model~~.	+
		+	<!--
		+	The line below this paragraph, {{ABSTRACT_PUBMED_21715165}}, adds the Publication Abstract to the page
		+	(as it appears on PubMed at http://www.pubmed.gov), where 21715165 is the PubMed ID number.
		+	-->
		+	{{ABSTRACT_PUBMED_21715165}}
		+
		+	==About this Structure==
		+	[[3rkz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3RKZ OCA].
		+
		+	==Reference==
		+	<ref group="xtra">PMID:021715165</ref><references group="xtra"/>
		+	[[Category: Homo sapiens]]
		+	[[Category: Bloom, J D.]]
		+	[[Category: Boschelli, F.]]
		+	[[Category: Dushin, R G.]]
		+	[[Category: Golas, J M.]]
		+	[[Category: Johnson, M.]]
		+	[[Category: Levin, J I.]]
		+	[[Category: Li, Z.]]
		+	[[Category: Liu, H.]]
		+	[[Category: Lucas, J.]]
		+	[[Category: Nikitenko, A.]]
		+	[[Category: Nittoli, T.]]
		+	[[Category: Olland, A.]]
		+	[[Category: Otteng, M.]]
		+	[[Category: Vogan, E.]]
		+	[[Category: Zapf, C W.]]
		+	[[Category: Atp binding domain]]
		+	[[Category: Atp-binding]]
		+	[[Category: Chaperone]]
		+	[[Category: Chaperone-chaperone inhibitor complex]]
		+	[[Category: Nucleotide-binding]]
		+	[[Category: Phosphoprotein]]
		+	[[Category: Stress response]]

OCA at 05:21, 1 June 2011

OCA — Wed, 01 Jun 2011 05:21:44 GMT

←Older revision		Revision as of 05:21, 1 June 2011
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3rkz is ON HOLD	+	The entry 3rkz is ON HOLD until Paper Publication

	Authors: Zapf, C.W., Bloom, J.D., Li, Z., Dushin, R.G., Nittoli, T., Otteng, M., Nikitenko, A., Golas, J.M., Liu, H., Lucas, J., Boschelli, F., Vogan, E., Olland, A., Johnson, M., Levin, J.I.		Authors: Zapf, C.W., Bloom, J.D., Li, Z., Dushin, R.G., Nittoli, T., Otteng, M., Nikitenko, A., Golas, J.M., Liu, H., Lucas, J., Boschelli, F., Vogan, E., Olland, A., Johnson, M., Levin, J.I.

	Description: Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.		Description: Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.