5ae8 - Revision history

OCA at 06:08, 5 July 2023

OCA — Wed, 05 Jul 2023 06:08:20 GMT

←Older revision		Revision as of 06:08, 5 July 2023
Line 3:		Line 3:
	<StructureSection load='5ae8' size='340' side='right'caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>		<StructureSection load='5ae8' size='340' side='right'caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5ae8]] 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=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5ae8]] 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=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=VVX:6-(1H-INDOL-4-YL)-4-(5-{[4-(1-METHYLETHYL)-1-PIPERAZINYL]METHYL}-1,3-OXAZOL-2-YL)-1H-INDAZOLE'>VVX</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]] 2.42Å</td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[5ae9\|5ae9]]</div></td></tr>~~	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=VVX:6-(1H-INDOL-4-YL)-4-(5-{[4-(1-METHYLETHYL)-1-PIPERAZINYL]METHYL}-1,3-OXAZOL-2-YL)-1H-INDAZOLE'>VVX</scene></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Pik3cd ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 LK3 transgenic mice])</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=5ae8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ae8 OCA], [https://pdbe.org/5ae8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ae8 RCSB], [https://www.ebi.ac.uk/pdbsum/5ae8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ae8 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=5ae8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ae8 OCA], [https://pdbe.org/5ae8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ae8 RCSB], [https://www.ebi.ac.uk/pdbsum/5ae8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ae8 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== 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>	+	[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>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 25:		Line 24:
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Lk3 transgenic mice~~]]	+	[[Category: Mus musculus]]
-	[[Category: Amour, A]]	+	[[Category: Amour A]]
-	[[Category: Baldwin~~, I R~~]]	+	[[Category: Baldwin IR]]
-	[[Category: Cooper~~, A W.J~~]]	+	[[Category: Cooper AWJ]]
-	[[Category: Deakin~~, A M~~]]	+	[[Category: Deakin AM]]
-	[[Category: Down~~, K D~~]]	+	[[Category: Down KD]]
-	[[Category: Felton~~, L M~~]]	+	[[Category: Felton LM]]
-	[[Category: Guntrip~~, S B~~]]	+	[[Category: Guntrip SB]]
-	[[Category: Hamblin, N]]	+	[[Category: Hamblin N]]
-	[[Category: Hardy, C]]	+	[[Category: Hardy C]]
-	[[Category: Harrison~~, Z A~~]]	+	[[Category: Harrison ZA]]
-	[[Category: Jones~~, K L~~]]	+	[[Category: Jones KL]]
-	[[Category: Jones, P]]	+	[[Category: Jones P]]
-	[[Category: Keeling~~, S E~~]]	+	[[Category: Keeling SE]]
-	[[Category: Le, J]]	+	[[Category: Le J]]
-	[[Category: Livia, S]]	+	[[Category: Livia S]]
-	[[Category: Lucas, F]]	+	[[Category: Lucas F]]
-	[[Category: Lunniss~~, C J~~]]	+	[[Category: Lunniss CJ]]
-	[[Category: Parr~~, N J~~]]	+	[[Category: Parr NJ]]
-	[[Category: Robinson, E]]	+	[[Category: Robinson E]]
-	[[Category: Rowland, P]]	+	[[Category: Rowland P]]
-	[[Category: Smith, S]]	+	[[Category: Smith S]]
-	[[Category: Thomas~~, D A~~]]	+	[[Category: Thomas DA]]
-	[[Category: Vitulli, G]]	+	[[Category: Vitulli G]]
-	[[Category: Washio, Y]]	+	[[Category: Washio Y]]
-	~~[[Category: Pi3 kinase delta]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 08:53, 29 September 2021

OCA — Wed, 29 Sep 2021 08:53:06 GMT

←Older revision		Revision as of 08:53, 29 September 2021
Line 3:		Line 3:
	<StructureSection load='5ae8' size='340' side='right'caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>		<StructureSection load='5ae8' size='340' side='right'caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5ae8]] 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=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5ae8]] 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=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VVX:6-(1H-INDOL-4-YL)-4-(5-{[4-(1-METHYLETHYL)-1-PIPERAZINYL]METHYL}-1,3-OXAZOL-2-YL)-1H-INDAZOLE'>VVX</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=VVX:6-(1H-INDOL-4-YL)-4-(5-{[4-(1-METHYLETHYL)-1-PIPERAZINYL]METHYL}-1,3-OXAZOL-2-YL)-1H-INDAZOLE'>VVX</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5ae9\|5ae9]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[5ae9\|5ae9]]</div></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=5ae8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ae8 OCA], [~~http~~://pdbe.org/5ae8 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5ae8 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5ae8 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5ae8 ProSAT]</span></td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">Pik3cd ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=10090 LK3 transgenic mice])</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=5ae8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ae8 OCA], [https://pdbe.org/5ae8 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5ae8 RCSB], [https://www.ebi.ac.uk/pdbsum/5ae8 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5ae8 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>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==

OCA at 07:58, 4 March 2020

OCA — Wed, 04 Mar 2020 07:58:43 GMT

←Older revision		Revision as of 07:58, 4 March 2020
Line 1:		Line 1:

	==Crystal structure of mouse PI3 kinase delta in complex with GSK2269557==		==Crystal structure of mouse PI3 kinase delta in complex with GSK2269557==
-	<StructureSection load='5ae8' size='340' side='right' caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>	+	<StructureSection load='5ae8' size='340' side='right'caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[5ae8]] 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=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>		<table><tr><td colspan='2'>[[5ae8]] 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=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>
Line 21:		Line 21:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Lk3 transgenic mice]]		[[Category: Lk3 transgenic mice]]
	[[Category: Amour, A]]		[[Category: Amour, A]]

OCA at 17:10, 16 November 2017

OCA — Thu, 16 Nov 2017 17:10:32 GMT

←Older revision		Revision as of 17:10, 16 November 2017
Line 1:		Line 1:
		+
	==Crystal structure of mouse PI3 kinase delta in complex with GSK2269557==		==Crystal structure of mouse PI3 kinase delta in complex with GSK2269557==
	<StructureSection load='5ae8' size='340' side='right' caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>		<StructureSection load='5ae8' size='340' side='right' caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5ae8]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5ae8]] 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=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VVX:6-(1H-INDOL-4-YL)-4-(5-{[4-(1-METHYLETHYL)-1-PIPERAZINYL]METHYL}-1,3-OXAZOL-2-YL)-1H-INDAZOLE'>VVX</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VVX:6-(1H-INDOL-4-YL)-4-(5-{[4-(1-METHYLETHYL)-1-PIPERAZINYL]METHYL}-1,3-OXAZOL-2-YL)-1H-INDAZOLE'>VVX</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5ae9\|5ae9]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5ae9\|5ae9]]</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=5ae8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ae8 OCA], [http://pdbe.org/5ae8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ae8 RCSB], [http://www.ebi.ac.uk/pdbsum/5ae8 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=5ae8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ae8 OCA], [http://pdbe.org/5ae8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ae8 RCSB], [http://www.ebi.ac.uk/pdbsum/5ae8 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5ae8 ProSAT]</span></td></tr>
	</table>		</table>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
Line 20:		Line 21:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Lk3 transgenic mice]]
	[[Category: Amour, A]]		[[Category: Amour, A]]
	[[Category: Baldwin, I R]]		[[Category: Baldwin, I R]]

OCA at 07:39, 7 October 2015

OCA — Wed, 07 Oct 2015 07:39:58 GMT

←Older revision		Revision as of 07:39, 7 October 2015
Line 1:		Line 1:
-	'''~~Unreleased~~ structure'''	+	==Crystal structure of mouse PI3 kinase delta in complex with GSK2269557==
		+	<StructureSection load='5ae8' size='340' side='right' caption='[[5ae8]], [[Resolution\|resolution]] 2.42Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5ae8]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5AE8 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5AE8 FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=VVX:6-(1H-INDOL-4-YL)-4-(5-{[4-(1-METHYLETHYL)-1-PIPERAZINYL]METHYL}-1,3-OXAZOL-2-YL)-1H-INDAZOLE'>VVX</scene></td></tr>
		+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[5ae9\|5ae9]]</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=5ae8 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5ae8 OCA], [http://pdbe.org/5ae8 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5ae8 RCSB], [http://www.ebi.ac.uk/pdbsum/5ae8 PDBsum]</span></td></tr>
		+	</table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Optimization of lead compound 1, through extensive use of structure-based design and a focus on PI3Kdelta potency, isoform selectivity, and inhaled PK properties, led to the discovery of clinical candidates 2 (GSK2269557) and 3 (GSK2292767) for the treatment of respiratory indications via inhalation. Compounds 2 and 3 are both highly selective for PI3Kdelta over the closely related isoforms and are active in a disease relevant brown Norway rat acute OVA model of Th2-driven lung inflammation.

-	~~The entry 5ae8 is ON HOLD~~	+	Optimization of Novel Indazoles as Highly Potent and Selective Inhibitors of Phosphoinositide 3-Kinase delta for the Treatment of Respiratory Disease.,Down K, Amour A, Baldwin IR, Cooper AW, Deakin AM, Felton LM, Guntrip SB, Hardy C, Harrison ZA, Jones KL, Jones P, Keeling SE, Le J, Livia S, Lucas F, Lunniss CJ, Parr NJ, Robinson E, Rowland P, Smith S, Thomas DA, Vitulli G, Washio Y, Hamblin JN J Med Chem. 2015 Sep 24;58(18):7381-99. doi: 10.1021/acs.jmedchem.5b00767. Epub, 2015 Sep 3. PMID:26301626<ref>PMID:26301626</ref>

-	~~Authors: Down~~, K.D., Amour, A., Baldwin, I.R., Cooper, A.W.J., Deakin, A.M., Felton, L.M., Guntrip, S.B., Hardy, C., Harrison, Z.A., Jones, K.L~~., Jones, P., Keeling, S.E., Le, J., Livia, S., Lucas, F., Lunniss, C.J., Parr, N.J., Robinson, E., Rowland, P., Smith, S., Thomas, D.A., Vitulli, G., Washio, Y., Hamblin, N.~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~Description: Crystal structure of mouse PI3 kinase delta in complex with GSK2269557~~	+	<div class="pdbe-citations 5ae8" style="background-color:#fffaf0;"></div>
-	[[Category: ~~Unreleased Structures~~]]	+	== References ==
-	[[Category: ~~Guntrip~~, S.B]]	+	<references/>
-	[[Category: ~~Cooper~~, ~~A.W.~~J]]	+	__TOC__
-	[[Category: ~~Washio~~, Y]]	+	</StructureSection>
		+	[[Category: Amour, A]]
		+	[[Category: Baldwin, I R]]
		+	[[Category: Cooper, A W.J]]
		+	[[Category: Deakin, A M]]
		+	[[Category: Down, K D]]
		+	[[Category: Felton, L M]]
		+	[[Category: Guntrip, S B]]
		+	[[Category: Hamblin, N]]
		+	[[Category: Hardy, C]]
		+	[[Category: Harrison, Z A]]
		+	[[Category: Jones, K L]]
		+	[[Category: Jones, P]]
		+	[[Category: Keeling, S E]]
		+	[[Category: Le, J]]
		+	[[Category: Livia, S]]
	[[Category: Lucas, F]]		[[Category: Lucas, F]]
-	[[Category: ~~Down~~, ~~K.D~~]]	+	[[Category: Lunniss, C J]]
-	[[Category: ~~Harrison~~, ~~Z.A~~]]	+	[[Category: Parr, N J]]
		+	[[Category: Robinson, E]]
		+	[[Category: Rowland, P]]
	[[Category: Smith, S]]		[[Category: Smith, S]]
-	~~[[Category: Jones, K.L]]~~	+	[[Category: Thomas, D A]]
-	~~[[Category: Robinson, E]]~~	+
-	~~[[Category: Livia, S]]~~	+
-	~~[[Category: Baldwin, I.R]]~~	+
-	[[Category: Thomas, D.A]]	+
-	~~[[Category: Jones, P~~]]	+
	[[Category: Vitulli, G]]		[[Category: Vitulli, G]]
-	[[Category: ~~Keeling~~, ~~S.E~~]]	+	[[Category: Washio, Y]]
-	[[Category: ~~Lunniss, C.J~~]]	+	[[Category: Pi3 kinase delta]]
-	[[Category: ~~Felton, L.M]]~~	+	[[Category: Transferase]]
-	~~[[Category: Parr, N.J]]~~	+
-	~~[[Category: Hardy, C]]~~	+
-	~~[[Category: Hamblin, N]]~~	+
-	~~[[Category: Rowland, P]]~~	+
-	~~[[Category: Amour, A]]~~	+
-	~~[[Category: Deakin, A.M]]~~	+
-	~~[[Category: Le, J~~]]	+

OCA: Protected "5ae8" [edit=sysop:move=sysop]

OCA — Wed, 02 Sep 2015 09:49:46 GMT

Protected "5ae8" [edit=sysop:move=sysop]

←Older revision

Revision as of 09:49, 2 September 2015

OCA: New page: '''Unreleased structure''' The entry 5ae8 is ON HOLD Authors: Down, K.D., Amour, A., Baldwin, I.R., Cooper, A.W.J., Deakin, A.M., Felton, L.M., Guntrip, S.B., Hardy, C., Harrison, Z.A.,...

OCA — Wed, 02 Sep 2015 09:49:45 GMT

New page: '''Unreleased structure''' The entry 5ae8 is ON HOLD Authors: Down, K.D., Amour, A., Baldwin, I.R., Cooper, A.W.J., Deakin, A.M., Felton, L.M., Guntrip, S.B., Hardy, C., Harrison, Z.A.,...

New page

'''Unreleased structure'''

The entry 5ae8 is ON HOLD

Authors: Down, K.D., Amour, A., Baldwin, I.R., Cooper, A.W.J., Deakin, A.M., Felton, L.M., Guntrip, S.B., Hardy, C., Harrison, Z.A., Jones, K.L., Jones, P., Keeling, S.E., Le, J., Livia, S., Lucas, F., Lunniss, C.J., Parr, N.J., Robinson, E., Rowland, P., Smith, S., Thomas, D.A., Vitulli, G., Washio, Y., Hamblin, N.

Description: Crystal structure of mouse PI3 kinase delta in complex with GSK2269557
[[Category: Unreleased Structures]]
[[Category: Guntrip, S.B]]
[[Category: Cooper, A.W.J]]
[[Category: Washio, Y]]
[[Category: Lucas, F]]
[[Category: Down, K.D]]
[[Category: Harrison, Z.A]]
[[Category: Smith, S]]
[[Category: Jones, K.L]]
[[Category: Robinson, E]]
[[Category: Livia, S]]
[[Category: Baldwin, I.R]]
[[Category: Thomas, D.A]]
[[Category: Jones, P]]
[[Category: Vitulli, G]]
[[Category: Keeling, S.E]]
[[Category: Lunniss, C.J]]
[[Category: Felton, L.M]]
[[Category: Parr, N.J]]
[[Category: Hardy, C]]
[[Category: Hamblin, N]]
[[Category: Rowland, P]]
[[Category: Amour, A]]
[[Category: Deakin, A.M]]
[[Category: Le, J]]