5yz3 - Revision history

OCA at 08:41, 22 November 2023

OCA — Wed, 22 Nov 2023 08:41:15 GMT

←Older revision		Revision as of 08:41, 22 November 2023
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	==Crystal structure of T2R-TTL-28 complex==		==Crystal structure of T2R-TTL-28 complex==
-	<StructureSection load='5yz3' size='340' side='right' caption='[[5yz3]], [[Resolution\|resolution]] 2.54Å' scene=''>	+	<StructureSection load='5yz3' size='340' side='right'caption='[[5yz3]], [[Resolution\|resolution]] 2.54Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5yz3]] is a 6 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [~~http~~://en.wikipedia.org/wiki/~~Buffalo_rat Buffalo rat~~] and [~~http~~://en.wikipedia.org/wiki/~~Chick Chick~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YZ3 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5YZ3 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5yz3]] is a 6 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [https://en.wikipedia.org/wiki/Gallus_gallus Gallus gallus] and [https://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YZ3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5YZ3 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=94U:N-[4-(diethylamino)phenyl]-4H-pyrrolo[2,3-d][1,3]thiazole-5-carboxamide'>94U</scene>, <scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</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]] 2.545Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Stmn4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat]), TTL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9031 CHICK])</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=94U:N-[4-(diethylamino)phenyl]-4H-pyrrolo[2,3-d][1,3]thiazole-5-carboxamide'>94U</scene>, <scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5yz3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5yz3 OCA], [~~http~~://pdbe.org/5yz3 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5yz3 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5yz3 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5yz3 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=5yz3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5yz3 OCA], [https://pdbe.org/5yz3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5yz3 RCSB], [https://www.ebi.ac.uk/pdbsum/5yz3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5yz3 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/TBA1B_BOVIN TBA1B_BOVIN]] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain. [[http://www.uniprot.org/uniprot/STMN4_RAT STMN4_RAT]] Exhibits microtubule-destabilizing activity.<ref>PMID:15039434</ref> <ref>PMID:12111843</ref> <ref>PMID:15014504</ref> [[http://www.uniprot.org/uniprot/TBB2B_BOVIN TBB2B_BOVIN]] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain ~~(By similarity)~~.	+	[https://www.uniprot.org/uniprot/TBA1B_BOVIN TBA1B_BOVIN] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</div>		</div>
	<div class="pdbe-citations 5yz3" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5yz3" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Stathmin-4 3D structures\|Stathmin-4 3D structures]]
		+	*[[Tubulin 3D Structures\|Tubulin 3D Structures]]
		+	*[[Tubulin tyrosine ligase\|Tubulin tyrosine ligase]]
	== References ==		== References ==
	<references/>		<references/>
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	</StructureSection>		</StructureSection>
	[[Category: Bos taurus]]		[[Category: Bos taurus]]
-	[[Category: ~~Buffalo rat~~]]	+	[[Category: Gallus gallus]]
-	[[Category: ~~Chick~~]]	+	[[Category: Large Structures]]
-	[[Category: ~~Chen, Q~~]]	+	[[Category: Rattus norvegicus]]
-	[[Category: ~~Yu, Y~~]]	+	[[Category: Chen Q]]
-	[[Category: ~~Cell cycle]]~~	+	[[Category: Yu Y]]
-	~~[[Category: Complex]]~~	+
-	~~[[Category: Structural protein]]~~	+
-	~~[[Category: Structural protein-inhibitor complex]]~~	+
-	~~[[Category: Tubulin~~]]	+

OCA at 07:08, 31 October 2018

OCA — Wed, 31 Oct 2018 07:08:32 GMT

←Older revision		Revision as of 07:08, 31 October 2018
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	<StructureSection load='5yz3' size='340' side='right' caption='[[5yz3]], [[Resolution\|resolution]] 2.54Å' scene=''>		<StructureSection load='5yz3' size='340' side='right' caption='[[5yz3]], [[Resolution\|resolution]] 2.54Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5yz3]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/ ] and [http://en.wikipedia.org/wiki/~~Bos_taurus Bos taurus~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YZ3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5YZ3 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5yz3]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus], [http://en.wikipedia.org/wiki/Buffalo_rat Buffalo rat] and [http://en.wikipedia.org/wiki/Chick Chick]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YZ3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5YZ3 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=94U:N-[4-(diethylamino)phenyl]-4H-pyrrolo[2,3-d][1,3]thiazole-5-carboxamide'>94U</scene>, <scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</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=94U:N-[4-(diethylamino)phenyl]-4H-pyrrolo[2,3-d][1,3]thiazole-5-carboxamide'>94U</scene>, <scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Stmn4 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10116 Buffalo rat]), TTL ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9031 CHICK])</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=5yz3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5yz3 OCA], [http://pdbe.org/5yz3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5yz3 RCSB], [http://www.ebi.ac.uk/pdbsum/5yz3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5yz3 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=5yz3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5yz3 OCA], [http://pdbe.org/5yz3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5yz3 RCSB], [http://www.ebi.ac.uk/pdbsum/5yz3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5yz3 ProSAT]</span></td></tr>
	</table>		</table>
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	</StructureSection>		</StructureSection>
	[[Category: Bos taurus]]		[[Category: Bos taurus]]
		+	[[Category: Buffalo rat]]
		+	[[Category: Chick]]
	[[Category: Chen, Q]]		[[Category: Chen, Q]]
	[[Category: Yu, Y]]		[[Category: Yu, Y]]

OCA at 05:46, 24 October 2018

OCA — Wed, 24 Oct 2018 05:46:57 GMT

←Older revision		Revision as of 05:46, 24 October 2018
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5yz3 is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==Crystal structure of T2R-TTL-28 complex==
		+	<StructureSection load='5yz3' size='340' side='right' caption='[[5yz3]], [[Resolution\|resolution]] 2.54Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5yz3]] is a 6 chain structure with sequence from [http://en.wikipedia.org/wiki/ ] and [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5YZ3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5YZ3 FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=94U:N-[4-(diethylamino)phenyl]-4H-pyrrolo[2,3-d][1,3]thiazole-5-carboxamide'>94U</scene>, <scene name='pdbligand=ACP:PHOSPHOMETHYLPHOSPHONIC+ACID+ADENYLATE+ESTER'>ACP</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=GDP:GUANOSINE-5-DIPHOSPHATE'>GDP</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=GTP:GUANOSINE-5-TRIPHOSPHATE'>GTP</scene>, <scene name='pdbligand=MES:2-(N-MORPHOLINO)-ETHANESULFONIC+ACID'>MES</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr>
		+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5yz3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5yz3 OCA], [http://pdbe.org/5yz3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5yz3 RCSB], [http://www.ebi.ac.uk/pdbsum/5yz3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5yz3 ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/TBA1B_BOVIN TBA1B_BOVIN]] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain. [[http://www.uniprot.org/uniprot/STMN4_RAT STMN4_RAT]] Exhibits microtubule-destabilizing activity.<ref>PMID:15039434</ref> <ref>PMID:12111843</ref> <ref>PMID:15014504</ref> [[http://www.uniprot.org/uniprot/TBB2B_BOVIN TBB2B_BOVIN]] Tubulin is the major constituent of microtubules. It binds two moles of GTP, one at an exchangeable site on the beta chain and one at a non-exchangeable site on the alpha chain (By similarity).
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Microtubule inhibitors as chemotherapeutic drugs are widely used for cancer treatment. However, the development of multidrug resistance (MDR) in cancer is a major challenge for microtubule inhibitors in their clinical implementation. From a high-throughput drug screen using cells transformed by oncogenic RAS, we identify a lead heteroaryl amide compound that blocks cell proliferation. Analysis of the structure-activity relationship indicated that this series of scaffolds (exemplified by MP-HJ-1b) represents a potent inhibitor of tumor cell growth. MP-HJ-1b showed activities against a panel of more than 1,000 human cancer cell lines with a wide variety of tissue origins. This compound depolymerized microtubules and affected spindle formation. It also induced the spike-like conformation of microtubules in vitro and in vivo, which is different from typical microtubule modulators. Structural analysis revealed that this series of compounds bound the colchicine pocket at the intra-dimer interface, although mostly not overlapping with colchicine binding. MP-HJ-1b displayed favorable pharmacological properties for overcoming tumor MDR, both in vitro and in vivo Taken together, our data reveal a novel scaffold represented by MP-HJ-1b that can be developed as a cancer therapeutic against tumors with MDR.Significance: Paclitaxel is a widely used chemotherapeutic drug in patients with multiple types of cancer. However, resistance to paclitaxel is a challenge. This study describes a novel class of microtubule inhibitors with the ability to circumvent multidrug resistance across multiple tumor cell lines. Cancer Res; 78(20); 5949-57. (c)2018 AACR.

-	~~Authors~~:	+	A Novel Microtubule Inhibitor Overcomes Multidrug Resistance in Tumors.,Ning N, Yu Y, Wu M, Zhang R, Zhang T, Zhu C, Huang L, Yun CH, Benes CH, Zhang J, Deng X, Chen Q, Ren R Cancer Res. 2018 Oct 15;78(20):5949-5957. doi: 10.1158/0008-5472.CAN-18-0455., Epub 2018 Aug 22. PMID:30135190<ref>PMID:30135190</ref>

-	~~Description~~:	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	[[Category: ~~Unreleased Structures~~]]	+	</div>
		+	<div class="pdbe-citations 5yz3" style="background-color:#fffaf0;"></div>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Bos taurus]]
		+	[[Category: Chen, Q]]
		+	[[Category: Yu, Y]]
		+	[[Category: Cell cycle]]
		+	[[Category: Complex]]
		+	[[Category: Structural protein]]
		+	[[Category: Structural protein-inhibitor complex]]
		+	[[Category: Tubulin]]

OCA at 04:50, 3 January 2018

OCA — Wed, 03 Jan 2018 04:50:37 GMT

←Older revision		Revision as of 04:50, 3 January 2018
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 5yz3 is ON HOLD	+	The entry 5yz3 is ON HOLD until Paper Publication

	Authors:		Authors:

OCA: Protected "5yz3" [edit=sysop:move=sysop]

OCA — Wed, 20 Dec 2017 04:52:36 GMT

Protected "5yz3" [edit=sysop:move=sysop]

←Older revision

Revision as of 04:52, 20 December 2017

OCA: New page: '''Unreleased structure''' The entry 5yz3 is ON HOLD Authors: Description: Category: Unreleased Structures

OCA — Wed, 20 Dec 2017 04:52:35 GMT

New page: '''Unreleased structure''' The entry 5yz3 is ON HOLD Authors: Description: Category: Unreleased Structures

New page

'''Unreleased structure'''

The entry 5yz3 is ON HOLD

Authors:

Description:
[[Category: Unreleased Structures]]