2mt8 - Revision history

OCA at 05:21, 17 October 2024

2024-10-17T05:21:52Z

← Older revision		Revision as of 05:21, 17 October 2024
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	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>
	</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [https://pdbe.org/2mt8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [https://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>		</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models\|Method:]]</b></td><td class="sblockDat" id="methodDat">Solution NMR, 20 models</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [https://pdbe.org/2mt8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [https://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==

OCA at 09:44, 14 June 2023

2023-06-14T09:44:50Z

← Older revision		Revision as of 09:44, 14 June 2023
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	==Solution structure MTAbl13, a grafted MCoTI-II==		==Solution structure MTAbl13, a grafted MCoTI-II==
	<StructureSection load='2mt8' size='340' side='right'caption='[[2mt8~~]], [[NMR_Ensembles_of_Models \| 20 NMR models~~]]' scene=''>		<StructureSection load='2mt8' size='340' side='right'caption='[[2mt8]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Synthetic_construct Synthetic construct]. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>
	</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [https://pdbe.org/2mt8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [https://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>		</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [https://pdbe.org/2mt8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [https://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>
	</table>		</table>
			== Function ==
			[https://www.uniprot.org/uniprot/ITR2_MOMCO ITR2_MOMCO]
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
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	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: ~~Craik, D~~]]		[[Category: Synthetic construct]]
	[[Category: ~~Huang, Y~~]]		[[Category: Craik D]]
	[[Category: ~~Wang, C~~]]		[[Category: Huang Y]]
	[[Category: ~~Cyclotide]]~~		[[Category: Wang C]]
	~~[[Category: Hydrolase inhibitor]]~~
	~~[[Category: Trypsin inhibitor~~]]

OCA at 09:02, 23 February 2022

2022-02-23T09:02:58Z

← Older revision		Revision as of 09:02, 23 February 2022
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	<StructureSection load='2mt8' size='340' side='right'caption='[[2mt8]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>		<StructureSection load='2mt8' size='340' side='right'caption='[[2mt8]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>
	</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://proteopedia.org/fgij/fg.htm?mol=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [~~http~~://pdbe.org/2mt8 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>		</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [https://pdbe.org/2mt8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [https://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>
	</table>		</table>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">

OCA at 06:27, 20 May 2020

2020-05-20T06:27:59Z

← Older revision		Revision as of 06:27, 20 May 2020
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	==Solution structure MTAbl13, a grafted MCoTI-II==		==Solution structure MTAbl13, a grafted MCoTI-II==
	<StructureSection load='2mt8' size='340' side='right' caption='[[2mt8]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>		<StructureSection load='2mt8' size='340' side='right'caption='[[2mt8]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>
	</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [http://pdbe.org/2mt8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [http://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>		</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [http://pdbe.org/2mt8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [http://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>
	</table>		</table>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
			[[Category: Large Structures]]
	[[Category: Craik, D]]		[[Category: Craik, D]]
	[[Category: Huang, Y]]		[[Category: Huang, Y]]

OCA at 16:50, 15 August 2018

2018-08-15T16:50:06Z

← Older revision		Revision as of 16:50, 15 August 2018
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	==Solution structure MTAbl13, a grafted MCoTI-II==		==Solution structure MTAbl13, a grafted MCoTI-II==
	<StructureSection load='2mt8' size='340' side='right' caption='[[2mt8]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>		<StructureSection load='2mt8' size='340' side='right' caption='[[2mt8]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>		<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>
	</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [http://pdbe.org/2mt8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [http://www.ebi.ac.uk/pdbsum/2mt8 PDBsum]</span></td></tr>		</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [http://pdbe.org/2mt8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [http://www.ebi.ac.uk/pdbsum/2mt8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2mt8 ProSAT]</span></td></tr>
	</table>		</table>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">

OCA at 03:50, 16 October 2015

2015-10-16T03:50:33Z

← Older revision		Revision as of 03:50, 16 October 2015
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	'''~~Unreleased~~ structure'''		==Solution structure MTAbl13, a grafted MCoTI-II==
			<StructureSection load='2mt8' size='340' side='right' caption='[[2mt8]], [[NMR_Ensembles_of_Models \| 20 NMR models]]' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[2mt8]] is a 1 chain structure. Full experimental information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2MT8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2MT8 FirstGlance]. <br>
			</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=2mt8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2mt8 OCA], [http://pdbe.org/2mt8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2mt8 RCSB], [http://www.ebi.ac.uk/pdbsum/2mt8 PDBsum]</span></td></tr>
			</table>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			The constitutively active tyrosine kinase BCR-ABL is the underlying cause of chronic myeloid leukemia (CML). Current CML treatments rely on the long-term use of tyrosine kinase inhibitors (TKIs), which target the ATP binding site of BCR-ABL. Over the course of treatment, 20-30% of CML patients develop TKI resistance, which is commonly attributed to point mutations in the drug-binding region. We design a new class of peptide inhibitors that target the substrate-binding site of BCR-ABL by grafting sequences derived from abltide, the optimal substrate of Abl kinase, onto a cell-penetrating cyclotide MCoTI-II. Three grafted cyclotides show significant Abl kinase inhibition in vitro in the low micromolar range using a novel kinase inhibition assay. Our work also demonstrates that a reengineered MCoTI-II with abltide sequences grafted in both loop 1 and 6 inhibits the activity of [T315I]Abl in vitro, a mutant Abl kinase harboring the "gatekeeper" mutation which is notorious for being multidrug resistant. Results from serum stability and cell internalization studies confirm that the MCoTI-II scaffold provides enzymatic stability and cell-penetrating properties to the lead molecules. Taken together, our study highlights that reengineered cyclotides incorporating abltide-derived sequences are promising substrate-competitive inhibitors for Abl kinase and the T315I mutant.

	~~The entry 2mt8 is ON HOLD until Paper Publication~~		Design of substrate-based BCR-ABL kinase inhibitors using the cyclotide scaffold.,Huang YH, Henriques ST, Wang CK, Thorstholm L, Daly NL, Kaas Q, Craik DJ Sci Rep. 2015 Aug 12;5:12974. doi: 10.1038/srep12974. PMID:26264857<ref>PMID:26264857</ref>

	~~Authors: Huang~~, Y.~~, Wang, C~~.~~, Craik, D~~.		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
			</div>
	~~Description~~: ~~Solution structure MTAbl13, a grafted MCoTI-II~~		<div class="pdbe-citations 2mt8" style="background-color:#fffaf0;"></div>
	~~[[Category: Unreleased Structures]]~~		== References ==
			<references/>
			__TOC__
			</StructureSection>
	[[Category: Craik, D]]		[[Category: Craik, D]]
			[[Category: Huang, Y]]
	[[Category: Wang, C]]		[[Category: Wang, C]]
	[[Category: ~~Huang, Y~~]]		[[Category: Cyclotide]]
			[[Category: Hydrolase inhibitor]]
			[[Category: Trypsin inhibitor]]

OCA at 13:57, 5 August 2015

2015-08-05T13:57:31Z

← Older revision		Revision as of 13:57, 5 August 2015
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	Description: Solution structure MTAbl13, a grafted MCoTI-II		Description: Solution structure MTAbl13, a grafted MCoTI-II
	[[Category: Unreleased Structures]]		[[Category: Unreleased Structures]]
	~~[[Category: Huang, Y]]~~
	[[Category: Craik, D]]		[[Category: Craik, D]]
	[[Category: Wang, C]]		[[Category: Wang, C]]
			[[Category: Huang, Y]]

OCA at 12:22, 24 December 2014

2014-12-24T12:22:46Z

← Older revision		Revision as of 12:22, 24 December 2014
Line 6:		Line 6:

	Description: Solution structure MTAbl13, a grafted MCoTI-II		Description: Solution structure MTAbl13, a grafted MCoTI-II
			[[Category: Unreleased Structures]]
			[[Category: Huang, Y]]
			[[Category: Craik, D]]
			[[Category: Wang, C]]

OCA at 12:43, 10 December 2014

2014-12-10T12:43:20Z

← Older revision		Revision as of 12:43, 10 December 2014
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 2mt8 is ON HOLD		The entry 2mt8 is ON HOLD until Paper Publication

	Authors: Huang, Y., Wang, C., Craik, D.		Authors: Huang, Y., Wang, C., Craik, D.

	Description: Solution structure MTAbl13, a grafted MCoTI-II		Description: Solution structure MTAbl13, a grafted MCoTI-II

OCA: Protected "2mt8" [edit=sysop:move=sysop]

2014-08-27T06:05:58Z

Protected "2mt8" [edit=sysop:move=sysop]

← Older revision	Revision as of 06:05, 27 August 2014
(No difference)