4p90 - Revision history

OCA at 07:13, 27 September 2023

OCA — Wed, 27 Sep 2023 07:13:06 GMT

←Older revision		Revision as of 07:13, 27 September 2023
Line 4:		Line 4:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4P90 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4P90 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</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]] 2.49Å</td></tr>
		+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [https://pdbe.org/4p90 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [https://www.ebi.ac.uk/pdbsum/4p90 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4p90 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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [https://pdbe.org/4p90 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [https://www.ebi.ac.uk/pdbsum/4p90 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4p90 ProSAT]</span></td></tr>
	</table>		</table>

OCA at 12:47, 1 February 2023

OCA — Wed, 01 Feb 2023 12:47:43 GMT

←Older revision		Revision as of 12:47, 1 February 2023
Line 3:		Line 3:
	<StructureSection load='4p90' size='340' side='right'caption='[[4p90]], [[Resolution\|resolution]] 2.49Å' scene=''>		<StructureSection load='4p90' size='340' side='right'caption='[[4p90]], [[Resolution\|resolution]] 2.49Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4P90 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4P90 FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene~~></td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene></td></tr>
-	~~<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PAK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [https://pdbe.org/4p90 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [https://www.ebi.ac.uk/pdbsum/4p90 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4p90 ProSAT]</span></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [~~http~~://pdbe.org/4p90 PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4p90 PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4p90 ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/PAK1_HUMAN PAK1_HUMAN]] Protein kinase involved in intracellular signaling pathways downstream of integrins and receptor-type kinases that plays an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes. Can directly phosphorylate BAD and protects cells against apoptosis. Activated by interaction with CDC42 and RAC1. Functions as GTPase effector that links the Rho-related GTPases CDC42 and RAC1 to the JNK MAP kinase pathway. Phosphorylates and activates MAP2K1, and thereby mediates activation of downstream MAP kinases. Involved in the reorganization of the actin cytoskeleton, actin stress fibers and of focal adhesion complexes. Phosphorylates the tubulin chaperone TBCB and thereby plays a role in the regulation of microtubule biogenesis and organization of the tubulin cytoskeleton. Plays a role in the regulation of insulin secretion in response to elevated glucose levels. Part of a ternary complex that contains PAK1, DVL1 and MUSK that is important for MUSK-dependent regulation of AChR clustering during the formation of the neuromuscular junction (NMJ). Activity is inhibited in cells undergoing apoptosis, potentially due to binding of CDC2L1 and CDC2L2. Phosphorylates MYL9/MLC2. Phosphorylates RAF1 at 'Ser-338' and 'Ser-339' resulting in: activation of RAF1, stimulation of RAF1 translocation to mitochondria, phosphorylation of BAD by RAF1, and RAF1 binding to BCL2.<ref>PMID:8805275</ref> <ref>PMID:9395435</ref> <ref>PMID:9032240</ref> <ref>PMID:9528787</ref> <ref>PMID:10551809</ref> <ref>PMID:11733498</ref> <ref>PMID:12624090</ref> <ref>PMID:12876277</ref> <ref>PMID:14585966</ref> <ref>PMID:15611088</ref> <ref>PMID:15831477</ref> <ref>PMID:16278681</ref> <ref>PMID:17726028</ref> <ref>PMID:17989089</ref> <ref>PMID:22669945</ref>	+	[https://www.uniprot.org/uniprot/PAK1_HUMAN PAK1_HUMAN] Protein kinase involved in intracellular signaling pathways downstream of integrins and receptor-type kinases that plays an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes. Can directly phosphorylate BAD and protects cells against apoptosis. Activated by interaction with CDC42 and RAC1. Functions as GTPase effector that links the Rho-related GTPases CDC42 and RAC1 to the JNK MAP kinase pathway. Phosphorylates and activates MAP2K1, and thereby mediates activation of downstream MAP kinases. Involved in the reorganization of the actin cytoskeleton, actin stress fibers and of focal adhesion complexes. Phosphorylates the tubulin chaperone TBCB and thereby plays a role in the regulation of microtubule biogenesis and organization of the tubulin cytoskeleton. Plays a role in the regulation of insulin secretion in response to elevated glucose levels. Part of a ternary complex that contains PAK1, DVL1 and MUSK that is important for MUSK-dependent regulation of AChR clustering during the formation of the neuromuscular junction (NMJ). Activity is inhibited in cells undergoing apoptosis, potentially due to binding of CDC2L1 and CDC2L2. Phosphorylates MYL9/MLC2. Phosphorylates RAF1 at 'Ser-338' and 'Ser-339' resulting in: activation of RAF1, stimulation of RAF1 translocation to mitochondria, phosphorylation of BAD by RAF1, and RAF1 binding to BCL2.<ref>PMID:8805275</ref> <ref>PMID:9395435</ref> <ref>PMID:9032240</ref> <ref>PMID:9528787</ref> <ref>PMID:10551809</ref> <ref>PMID:11733498</ref> <ref>PMID:12624090</ref> <ref>PMID:12876277</ref> <ref>PMID:14585966</ref> <ref>PMID:15611088</ref> <ref>PMID:15831477</ref> <ref>PMID:16278681</ref> <ref>PMID:17726028</ref> <ref>PMID:17989089</ref> <ref>PMID:22669945</ref>

	==See Also==		==See Also==
-	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]	+	*[[Serine/threonine protein kinase 3D structures\|Serine/threonine protein kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Non-specific serine/threonine protein kinase]]~~	+	[[Category: Ferguson AD]]
-	[[Category: Ferguson~~, A D]]~~	+
-	~~[[Category: Inhibitor]]~~	+
-	~~[[Category: Kinase]]~~	+
-	~~[[Category: Transferase-transferase inhibitor complex~~]]	+

OCA at 07:35, 17 April 2019

OCA — Wed, 17 Apr 2019 07:35:14 GMT

←Older revision		Revision as of 07:35, 17 April 2019
Line 1:		Line 1:

	==Crystal structure of the kinase domain of human PAK1 in complex with compound 15==		==Crystal structure of the kinase domain of human PAK1 in complex with compound 15==
-	<StructureSection load='4p90' size='340' side='right' caption='[[4p90]], [[Resolution\|resolution]] 2.49Å' scene=''>	+	<StructureSection load='4p90' size='340' side='right'caption='[[4p90]], [[Resolution\|resolution]] 2.49Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4P90 FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4P90 FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PAK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [http://pdbe.org/4p90 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [http://www.ebi.ac.uk/pdbsum/4p90 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4p90 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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [http://pdbe.org/4p90 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [http://www.ebi.ac.uk/pdbsum/4p90 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4p90 ProSAT]</span></td></tr>
Line 17:		Line 18:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
	[[Category: Ferguson, A D]]		[[Category: Ferguson, A D]]

OCA at 10:55, 5 August 2016

OCA — Fri, 05 Aug 2016 10:55:52 GMT

←Older revision		Revision as of 10:55, 5 August 2016
Line 1:		Line 1:
		+
	==Crystal structure of the kinase domain of human PAK1 in complex with compound 15==		==Crystal structure of the kinase domain of human PAK1 in complex with compound 15==
	<StructureSection load='4p90' size='340' side='right' caption='[[4p90]], [[Resolution\|resolution]] 2.49Å' scene=''>		<StructureSection load='4p90' size='340' side='right' caption='[[4p90]], [[Resolution\|resolution]] 2.49Å' scene=''>
Line 5:		Line 6:
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene></td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [http://www.ebi.ac.uk/pdbsum/4p90 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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [http://pdbe.org/4p90 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [http://www.ebi.ac.uk/pdbsum/4p90 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4p90 ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/PAK1_HUMAN PAK1_HUMAN]] Protein kinase involved in intracellular signaling pathways downstream of integrins and receptor-type kinases that plays an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes. Can directly phosphorylate BAD and protects cells against apoptosis. Activated by interaction with CDC42 and RAC1. Functions as GTPase effector that links the Rho-related GTPases CDC42 and RAC1 to the JNK MAP kinase pathway. Phosphorylates and activates MAP2K1, and thereby mediates activation of downstream MAP kinases. Involved in the reorganization of the actin cytoskeleton, actin stress fibers and of focal adhesion complexes. Phosphorylates the tubulin chaperone TBCB and thereby plays a role in the regulation of microtubule biogenesis and organization of the tubulin cytoskeleton. Plays a role in the regulation of insulin secretion in response to elevated glucose levels. Part of a ternary complex that contains PAK1, DVL1 and MUSK that is important for MUSK-dependent regulation of AChR clustering during the formation of the neuromuscular junction (NMJ). Activity is inhibited in cells undergoing apoptosis, potentially due to binding of CDC2L1 and CDC2L2. Phosphorylates MYL9/MLC2. Phosphorylates RAF1 at 'Ser-338' and 'Ser-339' resulting in: activation of RAF1, stimulation of RAF1 translocation to mitochondria, phosphorylation of BAD by RAF1, and RAF1 binding to BCL2.<ref>PMID:8805275</ref> <ref>PMID:9395435</ref> <ref>PMID:9032240</ref> <ref>PMID:9528787</ref> <ref>PMID:10551809</ref> <ref>PMID:11733498</ref> <ref>PMID:12624090</ref> <ref>PMID:12876277</ref> <ref>PMID:14585966</ref> <ref>PMID:15611088</ref> <ref>PMID:15831477</ref> <ref>PMID:16278681</ref> <ref>PMID:17726028</ref> <ref>PMID:17989089</ref> <ref>PMID:22669945</ref>		[[http://www.uniprot.org/uniprot/PAK1_HUMAN PAK1_HUMAN]] Protein kinase involved in intracellular signaling pathways downstream of integrins and receptor-type kinases that plays an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes. Can directly phosphorylate BAD and protects cells against apoptosis. Activated by interaction with CDC42 and RAC1. Functions as GTPase effector that links the Rho-related GTPases CDC42 and RAC1 to the JNK MAP kinase pathway. Phosphorylates and activates MAP2K1, and thereby mediates activation of downstream MAP kinases. Involved in the reorganization of the actin cytoskeleton, actin stress fibers and of focal adhesion complexes. Phosphorylates the tubulin chaperone TBCB and thereby plays a role in the regulation of microtubule biogenesis and organization of the tubulin cytoskeleton. Plays a role in the regulation of insulin secretion in response to elevated glucose levels. Part of a ternary complex that contains PAK1, DVL1 and MUSK that is important for MUSK-dependent regulation of AChR clustering during the formation of the neuromuscular junction (NMJ). Activity is inhibited in cells undergoing apoptosis, potentially due to binding of CDC2L1 and CDC2L2. Phosphorylates MYL9/MLC2. Phosphorylates RAF1 at 'Ser-338' and 'Ser-339' resulting in: activation of RAF1, stimulation of RAF1 translocation to mitochondria, phosphorylation of BAD by RAF1, and RAF1 binding to BCL2.<ref>PMID:8805275</ref> <ref>PMID:9395435</ref> <ref>PMID:9032240</ref> <ref>PMID:9528787</ref> <ref>PMID:10551809</ref> <ref>PMID:11733498</ref> <ref>PMID:12624090</ref> <ref>PMID:12876277</ref> <ref>PMID:14585966</ref> <ref>PMID:15611088</ref> <ref>PMID:15831477</ref> <ref>PMID:16278681</ref> <ref>PMID:17726028</ref> <ref>PMID:17989089</ref> <ref>PMID:22669945</ref>
		+
		+	==See Also==
		+	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 11:26, 24 December 2014

OCA — Wed, 24 Dec 2014 11:26:51 GMT

←Older revision		Revision as of 11:26, 24 December 2014
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4P90 FirstGlance]. <br>		<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4P90 FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene></td></tr>
-	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [http://www.ebi.ac.uk/pdbsum/4p90 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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [http://www.ebi.ac.uk/pdbsum/4p90 PDBsum]</span></td></tr>
-	<table>	+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/PAK1_HUMAN PAK1_HUMAN]] Protein kinase involved in intracellular signaling pathways downstream of integrins and receptor-type kinases that plays an important role in cytoskeleton dynamics, in cell adhesion, migration, proliferation, apoptosis, mitosis, and in vesicle-mediated transport processes. Can directly phosphorylate BAD and protects cells against apoptosis. Activated by interaction with CDC42 and RAC1. Functions as GTPase effector that links the Rho-related GTPases CDC42 and RAC1 to the JNK MAP kinase pathway. Phosphorylates and activates MAP2K1, and thereby mediates activation of downstream MAP kinases. Involved in the reorganization of the actin cytoskeleton, actin stress fibers and of focal adhesion complexes. Phosphorylates the tubulin chaperone TBCB and thereby plays a role in the regulation of microtubule biogenesis and organization of the tubulin cytoskeleton. Plays a role in the regulation of insulin secretion in response to elevated glucose levels. Part of a ternary complex that contains PAK1, DVL1 and MUSK that is important for MUSK-dependent regulation of AChR clustering during the formation of the neuromuscular junction (NMJ). Activity is inhibited in cells undergoing apoptosis, potentially due to binding of CDC2L1 and CDC2L2. Phosphorylates MYL9/MLC2. Phosphorylates RAF1 at 'Ser-338' and 'Ser-339' resulting in: activation of RAF1, stimulation of RAF1 translocation to mitochondria, phosphorylation of BAD by RAF1, and RAF1 binding to BCL2.<ref>PMID:8805275</ref> <ref>PMID:9395435</ref> <ref>PMID:9032240</ref> <ref>PMID:9528787</ref> <ref>PMID:10551809</ref> <ref>PMID:11733498</ref> <ref>PMID:12624090</ref> <ref>PMID:12876277</ref> <ref>PMID:14585966</ref> <ref>PMID:15611088</ref> <ref>PMID:15831477</ref> <ref>PMID:16278681</ref> <ref>PMID:17726028</ref> <ref>PMID:17989089</ref> <ref>PMID:22669945</ref>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
-	[[Category: Ferguson, A D.]]	+	[[Category: Ferguson, A D]]
	[[Category: Inhibitor]]		[[Category: Inhibitor]]
	[[Category: Kinase]]		[[Category: Kinase]]
	[[Category: Transferase-transferase inhibitor complex]]		[[Category: Transferase-transferase inhibitor complex]]

OCA at 10:11, 10 September 2014

OCA — Wed, 10 Sep 2014 10:11:41 GMT

←Older revision		Revision as of 10:11, 10 September 2014
Line 1:		Line 1:
-	'''~~Unreleased structure~~'''	+	==Crystal structure of the kinase domain of human PAK1 in complex with compound 15==
-		+	<StructureSection load='4p90' size='340' side='right' caption='[[4p90]], [[Resolution\|resolution]] 2.49Å' scene=''>
-	~~The entry~~ 4p90 is ~~ON HOLD until Paper Publication~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[4p90]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4P90 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4P90 FirstGlance]. <br>
-	~~Authors~~: Ferguson, A.D.	+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=2K0:[2-CHLORO-5-(HYDROXYMETHYL)PHENYL]{5-[1-(PIPERIDIN-4-YL)-1H-PYRAZOL-4-YL]-1H-PYRROLO[2,3-B]PYRIDIN-3-YL}METHANONE'>2K0</scene><br>
-		+	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Non-specific_serine/threonine_protein_kinase Non-specific serine/threonine protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.1 2.7.11.1] </span></td></tr>
-	~~Description~~: ~~Crystal structure of the kinase domain of human PAK1 in~~ complex ~~with compound 15~~	+	<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=4p90 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4p90 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4p90 RCSB], [http://www.ebi.ac.uk/pdbsum/4p90 PDBsum]</span></td></tr>
		+	<table>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Non-specific serine/threonine protein kinase]]
		+	[[Category: Ferguson, A D.]]
		+	[[Category: Inhibitor]]
		+	[[Category: Kinase]]
		+	[[Category: Transferase-transferase inhibitor complex]]

OCA at 09:03, 16 April 2014

OCA — Wed, 16 Apr 2014 09:03:46 GMT

←Older revision		Revision as of 09:03, 16 April 2014
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 4p90 is ON HOLD	+	The entry 4p90 is ON HOLD until Paper Publication

	Authors: Ferguson, A.D.		Authors: Ferguson, A.D.

	Description: Crystal structure of the kinase domain of human PAK1 in complex with compound 15		Description: Crystal structure of the kinase domain of human PAK1 in complex with compound 15

OCA: Protected "4p90" [edit=sysop:move=sysop]

OCA — Wed, 09 Apr 2014 05:54:30 GMT

Protected "4p90" [edit=sysop:move=sysop]

←Older revision

Revision as of 05:54, 9 April 2014

OCA: New page: '''Unreleased structure''' The entry 4p90 is ON HOLD Authors: Ferguson, A.D. Description: Crystal structure of the kinase domain of human PAK1 in complex with compound 15

OCA — Wed, 09 Apr 2014 05:54:29 GMT

New page: '''Unreleased structure''' The entry 4p90 is ON HOLD Authors: Ferguson, A.D. Description: Crystal structure of the kinase domain of human PAK1 in complex with compound 15

New page

'''Unreleased structure'''

The entry 4p90 is ON HOLD

Authors: Ferguson, A.D.

Description: Crystal structure of the kinase domain of human PAK1 in complex with compound 15