4oth - Revision history

OCA at 07:45, 25 January 2023

OCA — Wed, 25 Jan 2023 07:45:03 GMT

←Older revision		Revision as of 07:45, 25 January 2023
Line 1:		Line 1:

	==Crystal Structure of PRK1 Catalytic Domain in Complex with Ro-31-8220==		==Crystal Structure of PRK1 Catalytic Domain in Complex with Ro-31-8220==
-	<StructureSection load='4oth' size='340' side='right' caption='[[4oth]], [[Resolution\|resolution]] 1.80Å' scene=''>	+	<StructureSection load='4oth' size='340' side='right'caption='[[4oth]], [[Resolution\|resolution]] 1.80Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4oth]] is a 1 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=4OTH OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=4OTH FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4oth]] is a 1 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=4OTH OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4OTH FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DRN:BISINDOLYLMALEIMIDE+IX'>DRN</scene>~~</td></tr>~~	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=DRN:BISINDOLYLMALEIMIDE+IX'>DRN</scene>, <scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
-	~~<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat">~~<scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [https://pdbe.org/4oth PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [https://www.ebi.ac.uk/pdbsum/4oth PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4oth ProSAT]</span></td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>~~	+
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PKN1, PAK1, PKN, PRK1, PRKCL1 ([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/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [~~http~~://pdbe.org/4oth PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/4oth PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=4oth ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/PKN1_HUMAN PKN1_HUMAN]] PKC-related serine/threonine-protein kinase involved in various processes such as regulation of the intermediate filaments of the actin cytoskeleton, cell migration, tumor cell invasion and transcription regulation. Regulates the cytoskeletal network by phosphorylating proteins such as VIM and neurofilament proteins NEFH, NEFL and NEFM, leading to inhibit their polymerization. Phosphorylates 'Ser-575', 'Ser-637' and 'Ser-669' of MAPT/Tau, lowering its ability to bind to microtubules, resulting in disruption of tubulin assembly. Acts as a key coactivator of androgen receptor (ANDR)-dependent transcription, by being recruited to ANDR target genes and specifically mediating phosphorylation of 'Thr-11' of histone H3 (H3T11ph), a specific tag for epigenetic transcriptional activation that promotes demethylation of histone H3 'Lys-9' (H3K9me) by KDM4C/JMJD2C. Phosphorylates HDAC5, HDAC7 and HDAC9, leading to impair their import in the nucleus. Phosphorylates 'Thr-38' of PPP1R14A, 'Ser-159', 'Ser-163' and 'Ser-170' of MARCKS, and GFAP. Able to phosphorylate RPS6 in vitro.<ref>PMID:8557118</ref> <ref>PMID:8621664</ref> <ref>PMID:9175763</ref> <ref>PMID:11104762</ref> <ref>PMID:12514133</ref> <ref>PMID:17332740</ref> <ref>PMID:18066052</ref> <ref>PMID:20188095</ref> <ref>PMID:21754995</ref>	+	[https://www.uniprot.org/uniprot/PKN1_HUMAN PKN1_HUMAN] PKC-related serine/threonine-protein kinase involved in various processes such as regulation of the intermediate filaments of the actin cytoskeleton, cell migration, tumor cell invasion and transcription regulation. Regulates the cytoskeletal network by phosphorylating proteins such as VIM and neurofilament proteins NEFH, NEFL and NEFM, leading to inhibit their polymerization. Phosphorylates 'Ser-575', 'Ser-637' and 'Ser-669' of MAPT/Tau, lowering its ability to bind to microtubules, resulting in disruption of tubulin assembly. Acts as a key coactivator of androgen receptor (ANDR)-dependent transcription, by being recruited to ANDR target genes and specifically mediating phosphorylation of 'Thr-11' of histone H3 (H3T11ph), a specific tag for epigenetic transcriptional activation that promotes demethylation of histone H3 'Lys-9' (H3K9me) by KDM4C/JMJD2C. Phosphorylates HDAC5, HDAC7 and HDAC9, leading to impair their import in the nucleus. Phosphorylates 'Thr-38' of PPP1R14A, 'Ser-159', 'Ser-163' and 'Ser-170' of MARCKS, and GFAP. Able to phosphorylate RPS6 in vitro.<ref>PMID:8557118</ref> <ref>PMID:8621664</ref> <ref>PMID:9175763</ref> <ref>PMID:11104762</ref> <ref>PMID:12514133</ref> <ref>PMID:17332740</ref> <ref>PMID:18066052</ref> <ref>PMID:20188095</ref> <ref>PMID:21754995</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 24:		Line 20:

	==See Also==		==See Also==
-	*[[~~Student Project 1 for UMass Chemistry 423 Spring 2015~~\|~~Student Project 1 for UMass Chemistry 423 Spring 2015~~]]	+	*[[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: ~~Protein kinase C~~]]	+	[[Category: Large Structures]]
-	[[Category: Abbassian, M]]	+	[[Category: Abbassian M]]
-	[[Category: Cathers, B]]	+	[[Category: Cathers B]]
-	[[Category: Chamberlain~~, P P~~]]	+	[[Category: Chamberlain PP]]
-	[[Category: Delker, S]]	+	[[Category: Delker S]]
-	[[Category: Jackson, P]]	+	[[Category: Jackson P]]
-	[[Category: Mahmoudi, A]]	+	[[Category: Mahmoudi A]]
-	[[Category: Muir, J]]	+	[[Category: Muir J]]
-	[[Category: Pagarigan, B]]	+	[[Category: Pagarigan B]]
-	[[Category: Raheja, N]]	+	[[Category: Raheja N]]
-	~~[[Category: Atp binding]]~~	+
-	~~[[Category: Kinase]]~~	+
-	~~[[Category: Phosphorylation]]~~	+
-	~~[[Category: Pkn1]]~~	+
-	~~[[Category: Prk1]]~~	+
-	~~[[Category: Protein kinase]]~~	+
-	~~[[Category: Protein kinase c related kinase 1]]~~	+
-	~~[[Category: Transferase-transferase inhibitor complex~~]]	+

OCA at 20:16, 24 January 2018

OCA — Wed, 24 Jan 2018 20:16:07 GMT

←Older revision		Revision as of 20:16, 24 January 2018
Line 3:		Line 3:
	<StructureSection load='4oth' size='340' side='right' caption='[[4oth]], [[Resolution\|resolution]] 1.80Å' scene=''>		<StructureSection load='4oth' size='340' side='right' caption='[[4oth]], [[Resolution\|resolution]] 1.80Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[4oth]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OTH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4OTH FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[4oth]] is a 1 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=4OTH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4OTH FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DRN:BISINDOLYLMALEIMIDE+IX'>DRN</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DRN:BISINDOLYLMALEIMIDE+IX'>DRN</scene></td></tr>
	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>		<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">PKN1, PAK1, PKN, PRK1, PRKCL1 ([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/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [http://pdbe.org/4oth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [http://www.ebi.ac.uk/pdbsum/4oth PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4oth 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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [http://pdbe.org/4oth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [http://www.ebi.ac.uk/pdbsum/4oth PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4oth ProSAT]</span></td></tr>
Line 23:		Line 24:

	==See Also==		==See Also==
-	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]
	*[[Student Project 1 for UMass Chemistry 423 Spring 2015\|Student Project 1 for UMass Chemistry 423 Spring 2015]]		*[[Student Project 1 for UMass Chemistry 423 Spring 2015\|Student Project 1 for UMass Chemistry 423 Spring 2015]]
	== References ==		== References ==
Line 29:		Line 29:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Protein kinase C]]		[[Category: Protein kinase C]]
	[[Category: Abbassian, M]]		[[Category: Abbassian, M]]
-	[[Category: B., Pagarigan]]
	[[Category: Cathers, B]]		[[Category: Cathers, B]]
	[[Category: Chamberlain, P P]]		[[Category: Chamberlain, P P]]
Line 38:		Line 38:
	[[Category: Mahmoudi, A]]		[[Category: Mahmoudi, A]]
	[[Category: Muir, J]]		[[Category: Muir, J]]
		+	[[Category: Pagarigan, B]]
	[[Category: Raheja, N]]		[[Category: Raheja, N]]
	[[Category: Atp binding]]		[[Category: Atp binding]]

OCA at 10:16, 5 August 2016

OCA — Fri, 05 Aug 2016 10:16:28 GMT

←Older revision		Revision as of 10:16, 5 August 2016
Line 1:		Line 1:
		+
	==Crystal Structure of PRK1 Catalytic Domain in Complex with Ro-31-8220==		==Crystal Structure of PRK1 Catalytic Domain in Complex with Ro-31-8220==
	<StructureSection load='4oth' size='340' side='right' caption='[[4oth]], [[Resolution\|resolution]] 1.80Å' scene=''>		<StructureSection load='4oth' size='340' side='right' caption='[[4oth]], [[Resolution\|resolution]] 1.80Å' scene=''>
Line 7:		Line 8:
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [http://www.ebi.ac.uk/pdbsum/4oth 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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [http://pdbe.org/4oth PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [http://www.ebi.ac.uk/pdbsum/4oth PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4oth ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 19:		Line 20:
	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 4oth" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Serine/threonine protein kinase\|Serine/threonine protein kinase]]
		+	*[[Student Project 1 for UMass Chemistry 423 Spring 2015\|Student Project 1 for UMass Chemistry 423 Spring 2015]]
	== References ==		== References ==
	<references/>		<references/>

OCA at 01:32, 25 December 2014

OCA — Thu, 25 Dec 2014 01:32:02 GMT

←Older revision		Revision as of 01:32, 25 December 2014
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[4oth]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OTH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4OTH FirstGlance]. <br>		<table><tr><td colspan='2'>[[4oth]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OTH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4OTH FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DRN:BISINDOLYLMALEIMIDE+IX'>DRN</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DRN:BISINDOLYLMALEIMIDE+IX'>DRN</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>	+	<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>
-	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [http://www.ebi.ac.uk/pdbsum/4oth 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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [http://www.ebi.ac.uk/pdbsum/4oth PDBsum]</span></td></tr>
-	<table>	+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/PKN1_HUMAN PKN1_HUMAN]] PKC-related serine/threonine-protein kinase involved in various processes such as regulation of the intermediate filaments of the actin cytoskeleton, cell migration, tumor cell invasion and transcription regulation. Regulates the cytoskeletal network by phosphorylating proteins such as VIM and neurofilament proteins NEFH, NEFL and NEFM, leading to inhibit their polymerization. Phosphorylates 'Ser-575', 'Ser-637' and 'Ser-669' of MAPT/Tau, lowering its ability to bind to microtubules, resulting in disruption of tubulin assembly. Acts as a key coactivator of androgen receptor (ANDR)-dependent transcription, by being recruited to ANDR target genes and specifically mediating phosphorylation of 'Thr-11' of histone H3 (H3T11ph), a specific tag for epigenetic transcriptional activation that promotes demethylation of histone H3 'Lys-9' (H3K9me) by KDM4C/JMJD2C. Phosphorylates HDAC5, HDAC7 and HDAC9, leading to impair their import in the nucleus. Phosphorylates 'Thr-38' of PPP1R14A, 'Ser-159', 'Ser-163' and 'Ser-170' of MARCKS, and GFAP. Able to phosphorylate RPS6 in vitro.<ref>PMID:8557118</ref> <ref>PMID:8621664</ref> <ref>PMID:9175763</ref> <ref>PMID:11104762</ref> <ref>PMID:12514133</ref> <ref>PMID:17332740</ref> <ref>PMID:18066052</ref> <ref>PMID:20188095</ref> <ref>PMID:21754995</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 22:		Line 24:
	</StructureSection>		</StructureSection>
	[[Category: Protein kinase C]]		[[Category: Protein kinase C]]
-	[[Category: Abbassian, M.]]	+	[[Category: Abbassian, M]]
-	[[Category: B., Pagarigan.]]	+	[[Category: B., Pagarigan]]
-	[[Category: Cathers, B.]]	+	[[Category: Cathers, B]]
-	[[Category: Chamberlain, P P.]]	+	[[Category: Chamberlain, P P]]
-	[[Category: Delker, S.]]	+	[[Category: Delker, S]]
-	[[Category: Jackson, P.]]	+	[[Category: Jackson, P]]
-	[[Category: Mahmoudi, A.]]	+	[[Category: Mahmoudi, A]]
-	[[Category: Muir, J.]]	+	[[Category: Muir, J]]
-	[[Category: Raheja, N.]]	+	[[Category: Raheja, N]]
	[[Category: Atp binding]]		[[Category: Atp binding]]
	[[Category: Kinase]]		[[Category: Kinase]]

OCA at 08:37, 27 August 2014

OCA — Wed, 27 Aug 2014 08:37:33 GMT

←Older revision		Revision as of 08:37, 27 August 2014
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-	'''~~Unreleased~~ structure'''	+	==Crystal Structure of PRK1 Catalytic Domain in Complex with Ro-31-8220==
		+	<StructureSection load='4oth' size='340' side='right' caption='[[4oth]], [[Resolution\|resolution]] 1.80Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[4oth]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4OTH OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4OTH FirstGlance]. <br>
		+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DRN:BISINDOLYLMALEIMIDE+IX'>DRN</scene><br>
		+	<tr><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=SEP:PHOSPHOSERINE'>SEP</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
		+	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[4otd\|4otd]], [[4otg\|4otg]], [[4oti\|4oti]]</td></tr>
		+	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Protein_kinase_C Protein kinase C], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.13 2.7.11.13] </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=4oth FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4oth OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4oth RCSB], [http://www.ebi.ac.uk/pdbsum/4oth PDBsum]</span></td></tr>
		+	<table>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Protein kinase C related kinase 1 (PRK1) is a component of Rho-GTPase, androgen receptor, histone demethylase and histone deacetylase signaling pathways implicated in prostate and ovarian cancer. Herein we describe the crystal structure of PRK1 in apo form, and also in complex with a panel of literature inhibitors including the clinical candidates lestaurtinib and tofacitinib, as well as the staurosporine analog Ro-31-8220. PRK1 is a member of the AGC-kinase class, and as such exhibits the characteristic regulatory sequence at the C-terminus of the catalytic domain - the 'C-tail'. The C-tail fully encircles the catalytic domain placing a phenylalanine in the ATP-binding site. Our inhibitor structures include examples of molecules which both interact with, and displace the C-tail from the active site. This information may assist in the design of inhibitors targeting both PRK and other members of the AGC kinase family.

-	~~The entry 4oth is ON HOLD~~	+	Crystal Structures of PRK1 in Complex with the Clinical Compounds Lestaurtinib and Tofacitinib Reveal Ligand Induced Conformational Changes.,Chamberlain P, Delker S, Pagarigan B, Mahmoudi A, Jackson P, Abbasian M, Muir J, Raheja N, Cathers B PLoS One. 2014 Aug 11;9(8):e103638. doi: 10.1371/journal.pone.0103638., eCollection 2014. PMID:25111382<ref>PMID:25111382</ref>

-	~~Authors: Chamberlain~~, P.P., ~~Delker, S~~., Pagarigan B., ~~Mahmoudi, A~~., Jackson, P., ~~Abbassian, M~~., Muir, J., Raheja, N.~~, Cathers, B.~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-		+	</div>
-	~~Description~~: ~~Crystal Structure of PRK1 Catalytic Domain in Complex with Ro-31~~-~~8220~~	+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Protein kinase C]]
		+	[[Category: Abbassian, M.]]
		+	[[Category: B., Pagarigan.]]
		+	[[Category: Cathers, B.]]
		+	[[Category: Chamberlain, P P.]]
		+	[[Category: Delker, S.]]
		+	[[Category: Jackson, P.]]
		+	[[Category: Mahmoudi, A.]]
		+	[[Category: Muir, J.]]
		+	[[Category: Raheja, N.]]
		+	[[Category: Atp binding]]
		+	[[Category: Kinase]]
		+	[[Category: Phosphorylation]]
		+	[[Category: Pkn1]]
		+	[[Category: Prk1]]
		+	[[Category: Protein kinase]]
		+	[[Category: Protein kinase c related kinase 1]]
		+	[[Category: Transferase-transferase inhibitor complex]]

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

OCA — Wed, 19 Feb 2014 16:23:58 GMT

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

←Older revision

Revision as of 16:23, 19 February 2014

OCA: New page: '''Unreleased structure''' The entry 4oth is ON HOLD Authors: Chamberlain, P.P., Delker, S., Pagarigan B., Mahmoudi, A., Jackson, P., Abbassian, M., Muir, J., Raheja, N., Cathers, B. D...

OCA — Wed, 19 Feb 2014 16:23:57 GMT

New page: '''Unreleased structure''' The entry 4oth is ON HOLD Authors: Chamberlain, P.P., Delker, S., Pagarigan B., Mahmoudi, A., Jackson, P., Abbassian, M., Muir, J., Raheja, N., Cathers, B. D...

New page

'''Unreleased structure'''

The entry 4oth is ON HOLD

Authors: Chamberlain, P.P., Delker, S., Pagarigan B., Mahmoudi, A., Jackson, P., Abbassian, M., Muir, J., Raheja, N., Cathers, B.

Description: Crystal Structure of PRK1 Catalytic Domain in Complex with Ro-31-8220