4xe0 - Revision history

OCA at 07:44, 27 September 2023

OCA — Wed, 27 Sep 2023 07:44:33 GMT

←Older revision		Revision as of 07:44, 27 September 2023
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4xe0]] 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=4XE0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4XE0 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4xe0]] 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=4XE0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4XE0 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=40L:5-FLUORO-3-PHENYL-2-[(1S)-1-(7H-PURIN-6-YLAMINO)PROPYL]QUINAZOLIN-4(3H)-ONE'>40L</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]] 2.434Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=40L:5-FLUORO-3-PHENYL-2-[(1S)-1-(7H-PURIN-6-YLAMINO)PROPYL]QUINAZOLIN-4(3H)-ONE'>40L</scene></td></tr>
	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4xe0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xe0 OCA], [https://pdbe.org/4xe0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4xe0 RCSB], [https://www.ebi.ac.uk/pdbsum/4xe0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4xe0 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=4xe0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xe0 OCA], [https://pdbe.org/4xe0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4xe0 RCSB], [https://www.ebi.ac.uk/pdbsum/4xe0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4xe0 ProSAT]</span></td></tr>
	</table>		</table>

OCA at 21:24, 12 April 2023

OCA — Wed, 12 Apr 2023 21:24:50 GMT

←Older revision		Revision as of 21:24, 12 April 2023
Line 3:		Line 3:
	<StructureSection load='4xe0' size='340' side='right'caption='[[4xe0]], [[Resolution\|resolution]] 2.43Å' scene=''>		<StructureSection load='4xe0' size='340' side='right'caption='[[4xe0]], [[Resolution\|resolution]] 2.43Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4xe0]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XE0 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4XE0 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4xe0]] 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=4XE0 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4XE0 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=40L:5-FLUORO-3-PHENYL-2-[(1S)-1-(7H-PURIN-6-YLAMINO)PROPYL]QUINAZOLIN-4(3H)-ONE'>40L</scene~~></td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=40L:5-FLUORO-3-PHENYL-2-[(1S)-1-(7H-PURIN-6-YLAMINO)PROPYL]QUINAZOLIN-4(3H)-ONE'>40L</scene></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'>[https://proteopedia.org/fgij/fg.htm?mol=4xe0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xe0 OCA], [https://pdbe.org/4xe0 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4xe0 RCSB], [https://www.ebi.ac.uk/pdbsum/4xe0 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4xe0 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=4xe0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xe0 OCA], [~~http~~://pdbe.org/4xe0 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4xe0 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4xe0 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4xe0 ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://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 24:		Line 23:
	</StructureSection>		</StructureSection>
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: ~~Phosphatidylinositol-4,5-bisphosphate 3-kinase~~]]	+	[[Category: Mus musculus]]
-	[[Category: Somoza~~, J R~~]]	+	[[Category: Somoza JR]]
-	[[Category: Villasenor, A]]	+	[[Category: Villasenor A]]
-	~~[[Category: Kinase]]~~	+
-	~~[[Category: Pi3k]]~~	+
-	~~[[Category: Transferase-transferase inhibitor complex]]~~	+
-	~~[[Category: Zydelig~~]]	+

OCA at 06:49, 10 July 2019

OCA — Wed, 10 Jul 2019 06:49:56 GMT

←Older revision		Revision as of 06:49, 10 July 2019
Line 1:		Line 1:

	==Idelalisib bound to the p110 subunit of PI3K delta==		==Idelalisib bound to the p110 subunit of PI3K delta==
-	<StructureSection load='4xe0' size='340' side='right' caption='[[4xe0]], [[Resolution\|resolution]] 2.43Å' scene=''>	+	<StructureSection load='4xe0' size='340' side='right'caption='[[4xe0]], [[Resolution\|resolution]] 2.43Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4xe0]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XE0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XE0 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4xe0]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XE0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XE0 FirstGlance]. <br>
Line 23:		Line 23:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Large Structures]]
	[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]		[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]
	[[Category: Somoza, J R]]		[[Category: Somoza, J R]]

OCA at 00:07, 26 January 2017

OCA — Thu, 26 Jan 2017 00:07:45 GMT

←Older revision		Revision as of 00:07, 26 January 2017
Line 1:		Line 1:
		+
	==Idelalisib bound to the p110 subunit of PI3K delta==		==Idelalisib bound to the p110 subunit of PI3K delta==
	<StructureSection load='4xe0' size='340' side='right' caption='[[4xe0]], [[Resolution\|resolution]] 2.43Å' scene=''>		<StructureSection load='4xe0' size='340' side='right' caption='[[4xe0]], [[Resolution\|resolution]] 2.43Å' scene=''>
Line 5:		Line 6:
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=40L:5-FLUORO-3-PHENYL-2-[(1S)-1-(7H-PURIN-6-YLAMINO)PROPYL]QUINAZOLIN-4(3H)-ONE'>40L</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=40L:5-FLUORO-3-PHENYL-2-[(1S)-1-(7H-PURIN-6-YLAMINO)PROPYL]QUINAZOLIN-4(3H)-ONE'>40L</scene></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=4xe0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xe0 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4xe0 RCSB], [http://www.ebi.ac.uk/pdbsum/4xe0 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=4xe0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xe0 OCA], [http://pdbe.org/4xe0 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4xe0 RCSB], [http://www.ebi.ac.uk/pdbsum/4xe0 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4xe0 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 17:		Line 18:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
		+	<div class="pdbe-citations 4xe0" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 05:49, 12 February 2015

OCA — Thu, 12 Feb 2015 05:49:17 GMT

←Older revision		Revision as of 05:49, 12 February 2015
Line 9:		Line 9:
	== Function ==		== Function ==
	[[http://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>		[[http://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;">
		+	== Publication Abstract from PubMed ==
		+	Idelalisib (also known as GS-1101, CAL-101, IC489666 and Zydelig) is a phosphoinositide 3-kinase delta (PI3Kdelta) inhibitor that has recently been approved for the treatment of several hematological malignancies. Given its use in human diseases, we needed a clear picture of how idelalisib binds to and inhibits PI3Kdelta. Our data showed that idelalisib is a potent and selective inhibitor of the kinase activity of PI3Kdelta. A kinetic characterization clearly demonstrated ATP-competitive inhibition, and several additional biochemical and biophysical assays showed that the compound binds reversibly and non-covalently to the kinase. A crystal structure of idelalisib bound to the p110delta subunit of PI3Kdelta furthers our understanding of the binding interactions that confer the potency and selectivity of idelalisib.
		+
		+	Structural, Biochemical and Biophysical Characterization of Idelalisib Binding to Phosphoinositide 3-kinase Delta.,Somoza JR, Koditek D, Villasenor AG, Novikov N, Wong MH, Liclican A, Xing W, Lagpacan L, Wang R, Schultz BE, Papalia GA, Samuel D, Lad L, McGrath ME J Biol Chem. 2015 Jan 28. pii: jbc.M114.634683. PMID:25631052<ref>PMID:25631052</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 16:01, 7 February 2015

OCA — Sat, 07 Feb 2015 16:01:59 GMT

←Older revision		Revision as of 16:01, 7 February 2015
Line 1:		Line 1:
-	'''~~Unreleased structure~~'''	+	==Idelalisib bound to the p110 subunit of PI3K delta==
-		+	<StructureSection load='4xe0' size='340' side='right' caption='[[4xe0]], [[Resolution\|resolution]] 2.43Å' scene=''>
-	~~The entry~~ 4xe0 is ~~ON HOLD~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[4xe0]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4XE0 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4XE0 FirstGlance]. <br>
-	~~Authors~~: ~~Somoza~~, J.R., ~~Villasenor~~, A	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=40L:5-FLUORO-3-PHENYL-2-[(1S)-1-(7H-PURIN-6-YLAMINO)PROPYL]QUINAZOLIN-4(3H)-ONE'>40L</scene></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>
-	~~Description~~: ~~Idelalisib bound to~~ PI3K ~~delta~~	+	<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=4xe0 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4xe0 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4xe0 RCSB], [http://www.ebi.ac.uk/pdbsum/4xe0 PDBsum]</span></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	</table>
		+	== Function ==
		+	[[http://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>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Phosphatidylinositol-4,5-bisphosphate 3-kinase]]
		+	[[Category: Somoza, J R]]
	[[Category: Villasenor, A]]		[[Category: Villasenor, A]]
-	[[Category: ~~Somoza, J.R~~]]	+	[[Category: Kinase]]
		+	[[Category: Pi3k]]
		+	[[Category: Transferase-transferase inhibitor complex]]
		+	[[Category: Zydelig]]

OCA at 15:20, 28 January 2015

OCA — Wed, 28 Jan 2015 15:20:01 GMT

←Older revision		Revision as of 15:20, 28 January 2015
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	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4xe0 is ON HOLD ~~until sometime in the future~~	+	The entry 4xe0 is ON HOLD

	Authors: Somoza, J.R., Villasenor, A		Authors: Somoza, J.R., Villasenor, A

OCA at 12:36, 14 January 2015

OCA — Wed, 14 Jan 2015 12:36:46 GMT

←Older revision		Revision as of 12:36, 14 January 2015
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4xe0 is ON HOLD	+	The entry 4xe0 is ON HOLD until sometime in the future

	Authors: Somoza, J.R., Villasenor, A		Authors: Somoza, J.R., Villasenor, A

OCA: Protected "4xe0" [edit=sysop:move=sysop]

OCA — Wed, 31 Dec 2014 14:02:27 GMT

Protected "4xe0" [edit=sysop:move=sysop]

←Older revision

Revision as of 14:02, 31 December 2014

OCA: New page: '''Unreleased structure''' The entry 4xe0 is ON HOLD Authors: Somoza, J.R., Villasenor, A Description: Idelalisib bound to PI3K delta Category: Unreleased Structures [[Category: Vi...

OCA — Wed, 31 Dec 2014 14:02:26 GMT

New page: '''Unreleased structure''' The entry 4xe0 is ON HOLD Authors: Somoza, J.R., Villasenor, A Description: Idelalisib bound to PI3K delta Category: Unreleased Structures [[Category: Vi...

New page

'''Unreleased structure'''

The entry 4xe0 is ON HOLD

Authors: Somoza, J.R., Villasenor, A

Description: Idelalisib bound to PI3K delta
[[Category: Unreleased Structures]]
[[Category: Villasenor, A]]
[[Category: Somoza, J.R]]