5mpj - Revision history

OCA at 17:43, 8 November 2023

OCA — Wed, 08 Nov 2023 17:43:10 GMT

←Older revision		Revision as of 17:43, 8 November 2023
Line 3:		Line 3:
	<StructureSection load='5mpj' size='340' side='right'caption='[[5mpj]], [[Resolution\|resolution]] 2.14Å' scene=''>		<StructureSection load='5mpj' size='340' side='right'caption='[[5mpj]], [[Resolution\|resolution]] 2.14Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5mpj]] 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=5MPJ OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5MPJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5mpj]] 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=5MPJ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5MPJ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=IHP:INOSITOL+HEXAKISPHOSPHATE'>IHP</scene>, <scene name='pdbligand=J2P:(3-CHLORANYL-4-PHENYL-PHENYL)METHYL-ETHYL-AZANIUM'>J2P</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]] 2.14Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CSNK2A1, CK2A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=IHP:INOSITOL+HEXAKISPHOSPHATE'>IHP</scene>, <scene name='pdbligand=J2P:(3-CHLORANYL-4-PHENYL-PHENYL)METHYL-ETHYL-AZANIUM'>J2P</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='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5mpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mpj OCA], [https://pdbe.org/5mpj PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5mpj RCSB], [https://www.ebi.ac.uk/pdbsum/5mpj PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5mpj ProSAT]</span></td></tr>
-	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://proteopedia.org/fgij/fg.htm?mol=5mpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mpj OCA], [~~http~~://pdbe.org/5mpj PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5mpj RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5mpj PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5mpj ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/CSK21_HUMAN CSK21_HUMAN]] Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine. Regulates numerous cellular processes, such as cell cycle progression, apoptosis and transcription, as well as viral infection. May act as a regulatory node which integrates and coordinates numerous signals leading to an appropriate cellular response. During mitosis, functions as a component of the p53/TP53-dependent spindle assembly checkpoint (SAC) that maintains cyclin-B-CDK1 activity and G2 arrest in response to spindle damage. Also required for p53/TP53-mediated apoptosis, phosphorylating 'Ser-392' of p53/TP53 following UV irradiation. Can also negatively regulate apoptosis. Phosphorylates the caspases CASP9 and CASP2 and the apoptotic regulator NOL3. Phosphorylation protects CASP9 from cleavage and activation by CASP8, and inhibits the dimerization of CASP2 and activation of CASP8. Regulates transcription by direct phosphorylation of RNA polymerases I, II, III and IV. Also phosphorylates and regulates numerous transcription factors including NF-kappa-B, STAT1, CREB1, IRF1, IRF2, ATF1, SRF, MAX, JUN, FOS, MYC and MYB. Phosphorylates Hsp90 and its co-chaperones FKBP4 and CDC37, which is essential for chaperone function. Regulates Wnt signaling by phosphorylating CTNNB1 and the transcription factor LEF1. Acts as an ectokinase that phosphorylates several extracellular proteins. During viral infection, phosphorylates various proteins involved in the viral life cycles of EBV, HSV, HBV, HCV, HIV, CMV and HPV.<ref>PMID:11239457</ref> <ref>PMID:11704824</ref> <ref>PMID:16193064</ref> <ref>PMID:19188443</ref>	+	[https://www.uniprot.org/uniprot/CSK21_HUMAN CSK21_HUMAN] Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine. Regulates numerous cellular processes, such as cell cycle progression, apoptosis and transcription, as well as viral infection. May act as a regulatory node which integrates and coordinates numerous signals leading to an appropriate cellular response. During mitosis, functions as a component of the p53/TP53-dependent spindle assembly checkpoint (SAC) that maintains cyclin-B-CDK1 activity and G2 arrest in response to spindle damage. Also required for p53/TP53-mediated apoptosis, phosphorylating 'Ser-392' of p53/TP53 following UV irradiation. Can also negatively regulate apoptosis. Phosphorylates the caspases CASP9 and CASP2 and the apoptotic regulator NOL3. Phosphorylation protects CASP9 from cleavage and activation by CASP8, and inhibits the dimerization of CASP2 and activation of CASP8. Regulates transcription by direct phosphorylation of RNA polymerases I, II, III and IV. Also phosphorylates and regulates numerous transcription factors including NF-kappa-B, STAT1, CREB1, IRF1, IRF2, ATF1, SRF, MAX, JUN, FOS, MYC and MYB. Phosphorylates Hsp90 and its co-chaperones FKBP4 and CDC37, which is essential for chaperone function. Regulates Wnt signaling by phosphorylating CTNNB1 and the transcription factor LEF1. Acts as an ectokinase that phosphorylates several extracellular proteins. During viral infection, phosphorylates various proteins involved in the viral life cycles of EBV, HSV, HBV, HCV, HIV, CMV and HPV.<ref>PMID:11239457</ref> <ref>PMID:11704824</ref> <ref>PMID:16193064</ref> <ref>PMID:19188443</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 27:		Line 26:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	~~[[Category: Non-specific serine/threonine protein kinase]]~~	+	[[Category: Brear P]]
-	[[Category: Brear, P]]	+	[[Category: De Fusco C]]
-	[[Category: Fusco, C De]]	+	[[Category: Georgiou K]]
-	[[Category: Georgiou, K]]	+	[[Category: Hyvonen M]]
-	[[Category: Hyvonen, M]]	+	[[Category: Iegre J]]
-	[[Category: Iegre, J]]	+	[[Category: Sore H]]
-	[[Category: Sore, H]]	+	[[Category: Spring D]]
-	[[Category: Spring, D]]	+
-	~~[[Category: Ck2a]]~~	+
-	~~[[Category: Ck2alpha]]~~	+
-	~~[[Category: Fragment based drug discovery]]~~	+
-	~~[[Category: High concentration screening]]~~	+
-	~~[[Category: Selective atp competitive inhibitor]]~~	+
-	~~[[Category: Surface entrophy reduction]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 06:25, 7 October 2020

OCA — Wed, 07 Oct 2020 06:25:04 GMT

←Older revision		Revision as of 06:25, 7 October 2020
Line 1:		Line 1:

	==1-(2-chloro-[1,1'-biphenyl]-4-yl)-N-methylethanamine==		==1-(2-chloro-[1,1'-biphenyl]-4-yl)-N-methylethanamine==
-	<StructureSection load='5mpj' size='340' side='right' caption='[[5mpj]], [[Resolution\|resolution]] 2.14Å' scene=''>	+	<StructureSection load='5mpj' size='340' side='right'caption='[[5mpj]], [[Resolution\|resolution]] 2.14Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5mpj]] 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=5MPJ OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5MPJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5mpj]] 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=5MPJ OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5MPJ FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=~~I6P~~:INOSITOL+~~1,2,3,4,5,6-~~HEXAKISPHOSPHATE'>~~I6P~~</scene>, <scene name='pdbligand=J2P:(3-CHLORANYL-4-PHENYL-PHENYL)METHYL-ETHYL-AZANIUM'>J2P</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=IHP:INOSITOL+HEXAKISPHOSPHATE'>IHP</scene>, <scene name='pdbligand=J2P:(3-CHLORANYL-4-PHENYL-PHENYL)METHYL-ETHYL-AZANIUM'>J2P</scene></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CSNK2A1, CK2A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CSNK2A1, CK2A1 ([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=5mpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mpj OCA], [http://pdbe.org/5mpj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5mpj RCSB], [http://www.ebi.ac.uk/pdbsum/5mpj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5mpj ProSAT]</span></td></tr>	+	<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5mpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mpj OCA], [http://pdbe.org/5mpj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5mpj RCSB], [http://www.ebi.ac.uk/pdbsum/5mpj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5mpj ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 20:		Line 20:
	</div>		</div>
	<div class="pdbe-citations 5mpj" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5mpj" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Casein kinase 3D structures\|Casein kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 25:		Line 28:
	</StructureSection>		</StructureSection>
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
	[[Category: Brear, P]]		[[Category: Brear, P]]

OCA at 23:17, 15 November 2017

OCA — Wed, 15 Nov 2017 23:17:24 GMT

←Older revision		Revision as of 23:17, 15 November 2017
Line 3:		Line 3:
	<StructureSection load='5mpj' size='340' side='right' caption='[[5mpj]], [[Resolution\|resolution]] 2.14Å' scene=''>		<StructureSection load='5mpj' size='340' side='right' caption='[[5mpj]], [[Resolution\|resolution]] 2.14Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5mpj]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5MPJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5MPJ FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5mpj]] 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=5MPJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5MPJ FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=I6P:INOSITOL+1,2,3,4,5,6-HEXAKISPHOSPHATE'>I6P</scene>, <scene name='pdbligand=J2P:(3-CHLORANYL-4-PHENYL-PHENYL)METHYL-ETHYL-AZANIUM'>J2P</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=I6P:INOSITOL+1,2,3,4,5,6-HEXAKISPHOSPHATE'>I6P</scene>, <scene name='pdbligand=J2P:(3-CHLORANYL-4-PHENYL-PHENYL)METHYL-ETHYL-AZANIUM'>J2P</scene></td></tr>
		+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CSNK2A1, CK2A1 ([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=5mpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mpj OCA], [http://pdbe.org/5mpj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5mpj RCSB], [http://www.ebi.ac.uk/pdbsum/5mpj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5mpj 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=5mpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mpj OCA], [http://pdbe.org/5mpj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5mpj RCSB], [http://www.ebi.ac.uk/pdbsum/5mpj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5mpj ProSAT]</span></td></tr>
Line 23:		Line 24:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
	[[Category: Non-specific serine/threonine protein kinase]]		[[Category: Non-specific serine/threonine protein kinase]]
	[[Category: Brear, P]]		[[Category: Brear, P]]

OCA at 13:41, 24 May 2017

OCA — Wed, 24 May 2017 13:41:32 GMT

←Older revision		Revision as of 13:41, 24 May 2017
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry~~ 5mpj is ~~ON HOLD~~ ~~until Paper~~ Publication	+	==1-(2-chloro-[1,1'-biphenyl]-4-yl)-N-methylethanamine==
		+	<StructureSection load='5mpj' size='340' side='right' caption='[[5mpj]], [[Resolution\|resolution]] 2.14Å' scene=''>
		+	== Structural highlights ==
		+	<table><tr><td colspan='2'>[[5mpj]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5MPJ OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5MPJ FirstGlance]. <br>
		+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=ADP:ADENOSINE-5-DIPHOSPHATE'>ADP</scene>, <scene name='pdbligand=I6P:INOSITOL+1,2,3,4,5,6-HEXAKISPHOSPHATE'>I6P</scene>, <scene name='pdbligand=J2P:(3-CHLORANYL-4-PHENYL-PHENYL)METHYL-ETHYL-AZANIUM'>J2P</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='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=5mpj FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5mpj OCA], [http://pdbe.org/5mpj PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5mpj RCSB], [http://www.ebi.ac.uk/pdbsum/5mpj PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5mpj ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/CSK21_HUMAN CSK21_HUMAN]] Catalytic subunit of a constitutively active serine/threonine-protein kinase complex that phosphorylates a large number of substrates containing acidic residues C-terminal to the phosphorylated serine or threonine. Regulates numerous cellular processes, such as cell cycle progression, apoptosis and transcription, as well as viral infection. May act as a regulatory node which integrates and coordinates numerous signals leading to an appropriate cellular response. During mitosis, functions as a component of the p53/TP53-dependent spindle assembly checkpoint (SAC) that maintains cyclin-B-CDK1 activity and G2 arrest in response to spindle damage. Also required for p53/TP53-mediated apoptosis, phosphorylating 'Ser-392' of p53/TP53 following UV irradiation. Can also negatively regulate apoptosis. Phosphorylates the caspases CASP9 and CASP2 and the apoptotic regulator NOL3. Phosphorylation protects CASP9 from cleavage and activation by CASP8, and inhibits the dimerization of CASP2 and activation of CASP8. Regulates transcription by direct phosphorylation of RNA polymerases I, II, III and IV. Also phosphorylates and regulates numerous transcription factors including NF-kappa-B, STAT1, CREB1, IRF1, IRF2, ATF1, SRF, MAX, JUN, FOS, MYC and MYB. Phosphorylates Hsp90 and its co-chaperones FKBP4 and CDC37, which is essential for chaperone function. Regulates Wnt signaling by phosphorylating CTNNB1 and the transcription factor LEF1. Acts as an ectokinase that phosphorylates several extracellular proteins. During viral infection, phosphorylates various proteins involved in the viral life cycles of EBV, HSV, HBV, HCV, HIV, CMV and HPV.<ref>PMID:11239457</ref> <ref>PMID:11704824</ref> <ref>PMID:16193064</ref> <ref>PMID:19188443</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	Recently we reported the discovery of a potent and selective CK2alpha inhibitor CAM4066. This compound inhibits CK2 activity by exploiting a pocket located outside the ATP binding site (alphaD pocket). Here we describe in detail the journey that led to the discovery of CAM4066 using the challenging fragment linking strategy. Specifically, we aimed to develop inhibitors by linking a high-affinity fragment anchored in the alphaD site to a weakly binding warhead fragment occupying the ATP site. Moreover, we describe the remarkable impact that molecular modelling had on the development of this novel chemical tool. The work described herein shows potential for the development of a novel class of CK2 inhibitors.

-	~~Authors: Brear, P~~., De Fusco, C., ~~Georgiou, K.~~, Iegre, J., ~~Sore~~, H., Hyvonen, M., Spring, D.	+	A fragment-based approach leading to the discovery of a novel binding site and the selective CK2 inhibitor CAM4066.,De Fusco C, Brear P, Iegre J, Georgiou KH, Sore HF, Hyvonen M, Spring DR Bioorg Med Chem. 2017 Apr 30. pii: S0968-0896(16)31479-1. doi:, 10.1016/j.bmc.2017.04.037. PMID:28495381<ref>PMID:28495381</ref>

-	~~Description: 1-(2-chloro-[1~~,1'-~~biphenyl]~~-~~4-yl)-N-methylethanamine~~	+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
-	~~[[Category~~: ~~Unreleased Structures]]~~	+	</div>
-	~~[[Category: Hyvonen, M]]~~	+	<div class="pdbe-citations 5mpj" style="background-color:#fffaf0;"></div>
-	[[Category: ~~Georgiou, K~~]]	+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Non-specific serine/threonine protein kinase]]
	[[Category: Brear, P]]		[[Category: Brear, P]]
-	[[Category: ~~Spring~~, D]]	+	[[Category: Fusco, C De]]
-	[[Category: ~~Sore~~, H]]	+	[[Category: Georgiou, K]]
		+	[[Category: Hyvonen, M]]
	[[Category: Iegre, J]]		[[Category: Iegre, J]]
-	[[Category: ~~De Fusco~~, C]]	+	[[Category: Sore, H]]
		+	[[Category: Spring, D]]
		+	[[Category: Ck2a]]
		+	[[Category: Ck2alpha]]
		+	[[Category: Fragment based drug discovery]]
		+	[[Category: High concentration screening]]
		+	[[Category: Selective atp competitive inhibitor]]
		+	[[Category: Surface entrophy reduction]]
		+	[[Category: Transferase]]

OCA at 11:31, 9 March 2017

OCA — Thu, 09 Mar 2017 11:31:44 GMT

←Older revision		Revision as of 11:31, 9 March 2017
Line 9:		Line 9:
	[[Category: Hyvonen, M]]		[[Category: Hyvonen, M]]
	[[Category: Georgiou, K]]		[[Category: Georgiou, K]]
		+	[[Category: Brear, P]]
	[[Category: Spring, D]]		[[Category: Spring, D]]
		+	[[Category: Sore, H]]
	[[Category: Iegre, J]]		[[Category: Iegre, J]]
	[[Category: De Fusco, C]]		[[Category: De Fusco, C]]
-	[[Category: Brear, P]]
-	[[Category: Sore, H]]

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

OCA — Mon, 02 Jan 2017 13:49:50 GMT

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

←Older revision

Revision as of 13:49, 2 January 2017

OCA: New page: '''Unreleased structure''' The entry 5mpj is ON HOLD until Paper Publication Authors: Brear, P., De Fusco, C., Georgiou, K., Iegre, J., Sore, H., Hyvonen, M., Spring, D. Description: 1...

OCA — Mon, 02 Jan 2017 13:49:49 GMT

New page: '''Unreleased structure''' The entry 5mpj is ON HOLD until Paper Publication Authors: Brear, P., De Fusco, C., Georgiou, K., Iegre, J., Sore, H., Hyvonen, M., Spring, D. Description: 1...

New page

'''Unreleased structure'''

The entry 5mpj is ON HOLD until Paper Publication

Authors: Brear, P., De Fusco, C., Georgiou, K., Iegre, J., Sore, H., Hyvonen, M., Spring, D.

Description: 1-(2-chloro-[1,1'-biphenyl]-4-yl)-N-methylethanamine
[[Category: Unreleased Structures]]
[[Category: Hyvonen, M]]
[[Category: Georgiou, K]]
[[Category: Spring, D]]
[[Category: Iegre, J]]
[[Category: De Fusco, C]]
[[Category: Brear, P]]
[[Category: Sore, H]]