2wxj - Revision history

OCA at 10:19, 20 December 2023

OCA — Wed, 20 Dec 2023 10:19:01 GMT

←Older revision		Revision as of 10:19, 20 December 2023
Line 3:		Line 3:
	<StructureSection load='2wxj' size='340' side='right'caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>		<StructureSection load='2wxj' size='340' side='right'caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Lk3_transgenic_mice Lk3 transgenic mice~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</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]] 2.6Å</td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</div></td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [https://pdbe.org/2wxj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [https://www.ebi.ac.uk/pdbsum/2wxj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2wxj 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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [https://pdbe.org/2wxj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [https://www.ebi.ac.uk/pdbsum/2wxj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2wxj ProSAT]</span></td></tr>
	</table>		</table>
		+	== Function ==
		+	[https://www.uniprot.org/uniprot/PK3CD_MOUSE PK3CD_MOUSE] Phosphoinositide-3-kinase (PI3K) that phosphorylates PftdIns(4,5)P2 (Phosphatidylinositol 4,5-bisphosphate) to generate phosphatidylinositol 3,4,5-trisphosphate (PIP3). PIP3 plays a key role by recruiting PH domain-containing proteins to the membrane, including AKT1 and PDPK1, activating signaling cascades involved in cell growth, survival, proliferation, motility and morphology. Mediates immune responses. Plays a role in B-cell development, proliferation, migration, and function. Required for B-cell receptor (BCR) signaling. Mediates B-cell proliferation response to anti-IgM, anti-CD40 and IL4 stimulation. Promotes cytokine production in response to TLR4 and TLR9. Required for antibody class switch mediated by TLR9. Involved in the antigen presentation function of B-cells. Involved in B-cell chemotaxis in response to CXCL13 and sphingosine 1-phosphate (S1P). Required for proliferation, signaling and cytokine production of naive, effector and memory T-cells. Required for T-cell receptor (TCR) signaling. Mediates TCR signaling events at the immune synapse. Activation by TCR leads to antigen-dependent memory T-cell migration and retention to antigenic tissues. Together with PIK3CG participates in T-cell development. Contributes to T-helper cell expansion and differentiation. Required for T-cell migration mediated by homing receptors SELL/CD62L, CCR7 and S1PR1 and antigen dependent recruitment of T-cells. Together with PIK3CG is involved in natural killer (NK) cell development and migration towards the sites of inflammation. Participates in NK cell receptor activation. Have a role in NK cell maturation and cytokine production. Together with PIK3CG is involved in neutrophil chemotaxis and extravasation. Together with PIK3CG participates in neutrophil respiratory burst. Have important roles in mast-cell development and mast cell mediated allergic response. Involved in stem cell factor (SCF)-mediated proliferation, adhesion and migration. Required for allergen-IgE-induced degranulation and cytokine release. The lipid kinase activity is required for its biological function.<ref>PMID:12130661</ref> <ref>PMID:12235209</ref> <ref>PMID:15496927</ref> <ref>PMID:16116162</ref> <ref>PMID:18259608</ref> <ref>PMID:18809712</ref> <ref>PMID:19297623</ref>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 36:		Line 37:
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Lk3 transgenic mice]]~~	+	[[Category: Mus musculus]]
-	~~[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase~~]]	+	[[Category: Berndt A]]
-	[[Category: Berndt, A]]	+	[[Category: Gaillard P]]
-	[[Category: Gaillard, P]]	+	[[Category: Gorrec F]]
-	[[Category: Gorrec, F]]	+	[[Category: Hon W-C]]
-	[[Category: Hon, W C]]	+	[[Category: Houseman BT]]
-	[[Category: Houseman~~, B T~~]]	+	[[Category: Lee DD]]
-	[[Category: Lee~~, D D~~]]	+	[[Category: Liu Y]]
-	[[Category: Liu, Y]]	+	[[Category: Miller S]]
-	[[Category: Miller, S]]	+	[[Category: Pacold JI]]
-	[[Category: Pacold~~, J I~~]]	+	[[Category: Rommel C]]
-	[[Category: Rommel, C]]	+	[[Category: Ruckle T]]
-	[[Category: Ruckle, T]]	+	[[Category: Schwarz MK]]
-	[[Category: Schwarz~~, M K~~]]	+	[[Category: Shaw JP]]
-	[[Category: Shaw~~, J P~~]]	+	[[Category: Shokat KM]]
-	[[Category: Shokat~~, K M~~]]	+	[[Category: Williams O]]
-	[[Category: Williams, O]]	+	[[Category: Williams RL]]
-	[[Category: Williams~~, R L]]~~	+
-	~~[[Category: Cancer]]~~	+
-	~~[[Category: Isoform-specific inhibitor]]~~	+
-	~~[[Category: Nucleotide-binding]]~~	+
-	~~[[Category: Phosphoprotein]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 10:59, 7 July 2021

OCA — Wed, 07 Jul 2021 10:59:21 GMT

←Older revision		Revision as of 10:59, 7 July 2021
Line 3:		Line 3:
	<StructureSection load='2wxj' size='340' side='right'caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>		<StructureSection load='2wxj' size='340' side='right'caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</div></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [~~http~~://pdbe.org/2wxj PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/2wxj PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=2wxj 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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [https://pdbe.org/2wxj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [https://www.ebi.ac.uk/pdbsum/2wxj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2wxj ProSAT]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
Line 30:		Line 30:

	==See Also==		==See Also==
-	*[[Phosphoinositide 3-~~Kinases~~\|Phosphoinositide 3-~~Kinases~~]]	+	*[[Phosphoinositide 3-kinase 3D structures\|Phosphoinositide 3-kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 07:21, 24 April 2019

OCA — Wed, 24 Apr 2019 07:21:38 GMT

←Older revision		Revision as of 07:21, 24 April 2019
Line 1:		Line 1:

	==The crystal structure of the murine class IA PI 3-kinase p110delta in complex with INK654.==		==The crystal structure of the murine class IA PI 3-kinase p110delta in complex with INK654.==
-	<StructureSection load='2wxj' size='340' side='right' caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>	+	<StructureSection load='2wxj' size='340' side='right'caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>		<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>
Line 35:		Line 35:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Lk3 transgenic mice]]		[[Category: Lk3 transgenic mice]]
	[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]		[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]

OCA at 09:46, 3 October 2018

OCA — Wed, 03 Oct 2018 09:46:26 GMT

←Older revision		Revision as of 09:46, 3 October 2018
Line 1:		Line 1:
-	==~~THE CRYSTAL STRUCTURE OF THE MURINE CLASS~~ IA PI 3-~~KINASE P110DELTA IN COMPLEX WITH~~ INK654.==	+
		+	==The crystal structure of the murine class IA PI 3-kinase p110delta in complex with INK654.==
	<StructureSection load='2wxj' size='340' side='right' caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>		<StructureSection load='2wxj' size='340' side='right' caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
Line 6:		Line 7:
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [http://pdbe.org/2wxj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [http://www.ebi.ac.uk/pdbsum/2wxj 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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [http://pdbe.org/2wxj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [http://www.ebi.ac.uk/pdbsum/2wxj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=2wxj ProSAT]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
Line 12:		Line 13:
	Check<jmol>		Check<jmol>
	<jmolCheckbox>		<jmolCheckbox>
-	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/wx/2wxj_consurf.spt"</scriptWhenChecked>	+	<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/wx/2wxj_consurf.spt"</scriptWhenChecked>
	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>		<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>

OCA at 10:13, 8 February 2016

OCA — Mon, 08 Feb 2016 10:13:25 GMT

←Older revision		Revision as of 10:13, 8 February 2016
Line 2:		Line 2:
	<StructureSection load='2wxj' size='340' side='right' caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>		<StructureSection load='2wxj' size='340' side='right' caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Mus_musculus Mus musculus~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Lk3_transgenic_mice Lk3 transgenic mice]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [http://www.ebi.ac.uk/pdbsum/2wxj 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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [http://pdbe.org/2wxj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [http://www.ebi.ac.uk/pdbsum/2wxj PDBsum]</span></td></tr>
	</table>		</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
Line 16:		Line 16:
	<text>to colour the structure by Evolutionary Conservation</text>		<text>to colour the structure by Evolutionary Conservation</text>
	</jmolCheckbox>		</jmolCheckbox>
-	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/~~chain_selection~~.php?pdb_ID=~~2ata~~ ConSurf].	+	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=2wxj ConSurf].
	<div style="clear:both"></div>		<div style="clear:both"></div>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
Line 26:		Line 26:
	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 2wxj" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
Line 33:		Line 34:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Mus musculus~~]]	+	[[Category: Lk3 transgenic mice]]
	[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]		[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]
	[[Category: Berndt, A]]		[[Category: Berndt, A]]

OCA at 08:36, 20 January 2015

OCA — Tue, 20 Jan 2015 08:36:01 GMT

←Older revision		Revision as of 08:36, 20 January 2015
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>		<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>
-	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </span></td></tr>
-	<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [http://www.ebi.ac.uk/pdbsum/2wxj 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=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [http://www.ebi.ac.uk/pdbsum/2wxj PDBsum]</span></td></tr>
-	<table>	+	</table>
	== Evolutionary Conservation ==		== Evolutionary Conservation ==
	[[Image:Consurf_key_small.gif\|200px\|right]]		[[Image:Consurf_key_small.gif\|200px\|right]]
Line 35:		Line 35:
	[[Category: Mus musculus]]		[[Category: Mus musculus]]
	[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]		[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]
-	[[Category: Berndt, A.]]	+	[[Category: Berndt, A]]
-	[[Category: Gaillard, P.]]	+	[[Category: Gaillard, P]]
-	[[Category: Gorrec, F.]]	+	[[Category: Gorrec, F]]
-	[[Category: Hon, W C.]]	+	[[Category: Hon, W C]]
-	[[Category: Houseman, B T.]]	+	[[Category: Houseman, B T]]
-	[[Category: Lee, D D.]]	+	[[Category: Lee, D D]]
-	[[Category: Liu, Y.]]	+	[[Category: Liu, Y]]
-	[[Category: Miller, S.]]	+	[[Category: Miller, S]]
-	[[Category: Pacold, J I.]]	+	[[Category: Pacold, J I]]
-	[[Category: Rommel, C.]]	+	[[Category: Rommel, C]]
-	[[Category: Ruckle, T.]]	+	[[Category: Ruckle, T]]
-	[[Category: Schwarz, M K.]]	+	[[Category: Schwarz, M K]]
-	[[Category: Shaw, J P.]]	+	[[Category: Shaw, J P]]
-	[[Category: Shokat, K M.]]	+	[[Category: Shokat, K M]]
-	[[Category: Williams, O.]]	+	[[Category: Williams, O]]
-	[[Category: Williams, R L.]]	+	[[Category: Williams, R L]]
	[[Category: Cancer]]		[[Category: Cancer]]
	[[Category: Isoform-specific inhibitor]]		[[Category: Isoform-specific inhibitor]]

OCA at 07:06, 29 September 2014

OCA — Mon, 29 Sep 2014 07:06:00 GMT

←Older revision		Revision as of 07:06, 29 September 2014
Line 1:		Line 1:
-	[[~~Image:~~2wxj.~~png~~\|~~left~~\|200px]]	+	==THE CRYSTAL STRUCTURE OF THE MURINE CLASS IA PI 3-KINASE P110DELTA IN COMPLEX WITH INK654.==
		+	<StructureSection load='2wxj' size='340' side='right' caption='[[2wxj]], [[Resolution\|resolution]] 2.60Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2WXJ FirstGlance]. <br>
		+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=RW3:N-[6-(4-AMINO-1-{[2-(4-METHYLPIPERAZIN-1-YL)QUINOLIN-3-YL]METHYL}-1H-PYRAZOLO[3,4-D]PYRIMIDIN-3-YL)-1,3-BENZOTHIAZOL-2-YL]ACETAMIDE'>RW3</scene><br>
		+	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[2wxm\|2wxm]], [[2wxh\|2wxh]], [[2wxk\|2wxk]], [[2wxl\|2wxl]], [[2wxg\|2wxg]], [[2wxi\|2wxi]], [[2wxp\|2wxp]], [[2wxo\|2wxo]], [[2wxf\|2wxf]], [[2wxq\|2wxq]], [[2wxn\|2wxn]], [[2wxe\|2wxe]], [[2wxr\|2wxr]]</td></tr>
		+	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Phosphatidylinositol-4,5-bisphosphate_3-kinase Phosphatidylinositol-4,5-bisphosphate 3-kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.153 2.7.1.153] </span></td></tr>
		+	<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2wxj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2wxj OCA], [http://www.rcsb.org/pdb/explore.do?structureId=2wxj RCSB], [http://www.ebi.ac.uk/pdbsum/2wxj PDBsum]</span></td></tr>
		+	<table>
		+	== Evolutionary Conservation ==
		+	[[Image:Consurf_key_small.gif\|200px\|right]]
		+	Check<jmol>
		+	<jmolCheckbox>
		+	<scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/wx/2wxj_consurf.spt"</scriptWhenChecked>
		+	<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked>
		+	<text>to colour the structure by Evolutionary Conservation</text>
		+	</jmolCheckbox>
		+	</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary\|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf].
		+	<div style="clear:both"></div>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Deregulation of the phosphoinositide-3-OH kinase (PI(3)K) pathway has been implicated in numerous pathologies including cancer, diabetes, thrombosis, rheumatoid arthritis and asthma. Recently, small-molecule and ATP-competitive PI(3)K inhibitors with a wide range of selectivities have entered clinical development. In order to understand the mechanisms underlying the isoform selectivity of these inhibitors, we developed a new expression strategy that enabled us to determine to our knowledge the first crystal structure of the catalytic subunit of the class IA PI(3)K p110 delta. Structures of this enzyme in complex with a broad panel of isoform- and pan-selective class I PI(3)K inhibitors reveal that selectivity toward p110 delta can be achieved by exploiting its conformational flexibility and the sequence diversity of active site residues that do not contact ATP. We have used these observations to rationalize and synthesize highly selective inhibitors for p110 delta with greatly improved potencies.

-	~~{{STRUCTURE_2wxj\| PDB=2wxj \| SCENE= }}~~	+	The p110 delta structure: mechanisms for selectivity and potency of new PI(3)K inhibitors.,Berndt A, Miller S, Williams O, Le DD, Houseman BT, Pacold JI, Gorrec F, Hon WC, Liu Y, Rommel C, Gaillard P, Ruckle T, Schwarz MK, Shokat KM, Shaw JP, Williams RL Nat Chem Biol. 2010 Feb;6(2):117-24. PMID:20081827<ref>PMID:20081827</ref>

-	~~===THE CRYSTAL STRUCTURE OF THE MURINE CLASS IA PI 3-KINASE P110DELTA IN COMPLEX WITH INK654.===~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~{{ABSTRACT_PUBMED_20081827}}~~	+
-		+
-	~~==About this Structure==~~	+
-	~~[[2wxj]] is~~ a ~~1 chain structure with sequence from [http://en~~.~~wikipedia~~.~~org/wiki/Mus_musculus Mus musculus]~~. ~~Full crystallographic information is available from [http:~~/~~/oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA].~~	+

	==See Also==		==See Also==
	*[[Phosphoinositide 3-Kinases\|Phosphoinositide 3-Kinases]]		*[[Phosphoinositide 3-Kinases\|Phosphoinositide 3-Kinases]]
-		+	== References ==
-	==~~Reference~~==	+	<references/>
-	<~~ref group="xtra">PMID:020081827<~~/~~ref~~><~~references group="xtra"~~/>	+	__TOC__
		+	</StructureSection>
	[[Category: Mus musculus]]		[[Category: Mus musculus]]
	[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]		[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]

OCA at 09:49, 20 October 2012

OCA — Sat, 20 Oct 2012 09:49:22 GMT

←Older revision		Revision as of 09:49, 20 October 2012
Line 8:		Line 8:

	==About this Structure==		==About this Structure==
-	[[2wxj]] is a 1 chain structure ~~of [[Phosphoinositide 3-Kinases]]~~ with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA].	+	[[2wxj]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Mus_musculus Mus musculus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2WXJ OCA].

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

OCA at 00:03, 26 July 2012

OCA — Thu, 26 Jul 2012 00:03:52 GMT

←Older revision		Revision as of 00:03, 26 July 2012
Line 1:		Line 1:
	[[Image:2wxj.png\|left\|200px]]		[[Image:2wxj.png\|left\|200px]]

-	<!--
-	The line below this paragraph, containing "STRUCTURE_2wxj", 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_2wxj\| PDB=2wxj \| SCENE= }}		{{STRUCTURE_2wxj\| PDB=2wxj \| SCENE= }}

	===THE CRYSTAL STRUCTURE OF THE MURINE CLASS IA PI 3-KINASE P110DELTA IN COMPLEX WITH INK654.===		===THE CRYSTAL STRUCTURE OF THE MURINE CLASS IA PI 3-KINASE P110DELTA IN COMPLEX WITH INK654.===

-
-	<!--
-	The line below this paragraph, {{ABSTRACT_PUBMED_20081827}}, adds the Publication Abstract to the page
-	(as it appears on PubMed at http://www.pubmed.gov), where 20081827 is the PubMed ID number.
-	-->
	{{ABSTRACT_PUBMED_20081827}}		{{ABSTRACT_PUBMED_20081827}}

Line 22:		Line 11:

	==See Also==		==See Also==
-	*[[Phosphoinositide 3-Kinases]]	+	*[[Phosphoinositide 3-Kinases\|Phosphoinositide 3-Kinases]]

	==Reference==		==Reference==
-	<ref group="xtra">PMID:~~20081827~~</ref><references group="xtra"/>	+	<ref group="xtra">PMID:020081827</ref><references group="xtra"/>
	[[Category: Mus musculus]]		[[Category: Mus musculus]]
	[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]		[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]

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

OCA — Sun, 26 Dec 2010 09:20:09 GMT

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

←Older revision

Revision as of 09:20, 26 December 2010