5i5z - Revision history

OCA at 08:24, 23 August 2023

2023-08-23T08:24:16Z

←Older revision		Revision as of 08:24, 23 August 2023
Line 3:		Line 3:
	<StructureSection load='5i5z' size='340' side='right'caption='[[5i5z]], [[Resolution\|resolution]] 2.60Å' scene=''>		<StructureSection load='5i5z' size='340' side='right'caption='[[5i5z]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5i5z]] 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=5I5Z OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://proteopedia.org/fgij/fg.htm?mol=5I5Z FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5i5z]] 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=5I5Z OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5I5Z FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=68U:N-METHYL-8-(1-METHYL-2,2-DIOXO-2,3-DIHYDRO-1H-2LAMBDA~6~,1-BENZOTHIAZOL-5-YL)-1,6-NAPHTHYRIDINE-2-CARBOXAMIDE'>68U</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</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]] 2.6Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK8 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), CCNC ([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=68U:N-METHYL-8-(1-METHYL-2,2-DIOXO-2,3-DIHYDRO-1H-2LAMBDA~6~,1-BENZOTHIAZOL-5-YL)-1,6-NAPHTHYRIDINE-2-CARBOXAMIDE'>68U</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene></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=5i5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i5z OCA], [~~http~~://pdbe.org/5i5z PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5i5z RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5i5z PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5i5z 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=5i5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i5z OCA], [https://pdbe.org/5i5z PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5i5z RCSB], [https://www.ebi.ac.uk/pdbsum/5i5z PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5i5z ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/CDK8_HUMAN CDK8_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex. Phosphorylates CCNH leading to down-regulation of the TFIIH complex and transcriptional repression. Recruited through interaction with MAML1 to hyperphosphorylate the intracellular domain of NOTCH, leading to its degradation.<ref>PMID:10993082</ref> <ref>PMID:15546612</ref> [[http://www.uniprot.org/uniprot/CCNC_HUMAN CCNC_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Binds to and activates cyclin-dependent kinase CDK8 that phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex.<ref>PMID:8700522</ref> <ref>PMID:16595664</ref>	+	[https://www.uniprot.org/uniprot/CDK8_HUMAN CDK8_HUMAN] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex. Phosphorylates CCNH leading to down-regulation of the TFIIH complex and transcriptional repression. Recruited through interaction with MAML1 to hyperphosphorylate the intracellular domain of NOTCH, leading to its degradation.<ref>PMID:10993082</ref> <ref>PMID:15546612</ref>
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 27:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Human~~]]	+	[[Category: Homo sapiens]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Blagg, J]]	+	[[Category: Blagg J]]
-	[[Category: Mallinger, A]]	+	[[Category: Mallinger A]]
-	[[Category: Musil, D]]	+	[[Category: Musil D]]
-	~~[[Category: Cdk8 kinase / cyclin c]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 07:06, 3 June 2020

2020-06-03T07:06:06Z

←Older revision		Revision as of 07:06, 3 June 2020
Line 1:		Line 1:

	==CDK8-CYCC IN COMPLEX WITH 8-(1-Methyl-2,2-dioxo-2,3-dihydro-1H-2l6-benzo[c]isothiazol-5-yl)-[1,6]naphthyridine-2-carboxylic acid methylamide==		==CDK8-CYCC IN COMPLEX WITH 8-(1-Methyl-2,2-dioxo-2,3-dihydro-1H-2l6-benzo[c]isothiazol-5-yl)-[1,6]naphthyridine-2-carboxylic acid methylamide==
-	<StructureSection load='5i5z' size='340' side='right' caption='[[5i5z]], [[Resolution\|resolution]] 2.60Å' scene=''>	+	<StructureSection load='5i5z' size='340' side='right'caption='[[5i5z]], [[Resolution\|resolution]] 2.60Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5i5z]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I5Z OCA]. For a <b>guided tour on the structure components</b> use [http://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5I5Z FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5i5z]] 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=5I5Z OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5I5Z FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=68U:N-METHYL-8-(1-METHYL-2,2-DIOXO-2,3-DIHYDRO-1H-2LAMBDA~6~,1-BENZOTHIAZOL-5-YL)-1,6-NAPHTHYRIDINE-2-CARBOXAMIDE'>68U</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=68U:N-METHYL-8-(1-METHYL-2,2-DIOXO-2,3-DIHYDRO-1H-2LAMBDA~6~,1-BENZOTHIAZOL-5-YL)-1,6-NAPHTHYRIDINE-2-CARBOXAMIDE'>68U</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene></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=5i5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i5z OCA], [http://pdbe.org/5i5z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i5z RCSB], [http://www.ebi.ac.uk/pdbsum/5i5z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5i5z ProSAT]</span></td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK8 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN]), CCNC ([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'>[http://proteopedia.org/fgij/fg.htm?mol=5i5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i5z OCA], [http://pdbe.org/5i5z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i5z RCSB], [http://www.ebi.ac.uk/pdbsum/5i5z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5i5z ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 18:		Line 19:
	</div>		</div>
	<div class="pdbe-citations 5i5z" style="background-color:#fffaf0;"></div>		<div class="pdbe-citations 5i5z" style="background-color:#fffaf0;"></div>
		+
		+	==See Also==
		+	*[[Cyclin 3D structures\|Cyclin 3D structures]]
		+	*[[Cyclin-dependent kinase 3D structures\|Cyclin-dependent kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
		+	[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Blagg, J]]		[[Category: Blagg, J]]
	[[Category: Mallinger, A]]		[[Category: Mallinger, A]]

OCA at 17:46, 12 July 2016

2016-07-12T17:46:40Z

←Older revision		Revision as of 17:46, 12 July 2016
Line 5:		Line 5:
	<table><tr><td colspan='2'>[[5i5z]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I5Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I5Z FirstGlance]. <br>		<table><tr><td colspan='2'>[[5i5z]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I5Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I5Z FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=68U:N-METHYL-8-(1-METHYL-2,2-DIOXO-2,3-DIHYDRO-1H-2LAMBDA~6~,1-BENZOTHIAZOL-5-YL)-1,6-NAPHTHYRIDINE-2-CARBOXAMIDE'>68U</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=68U:N-METHYL-8-(1-METHYL-2,2-DIOXO-2,3-DIHYDRO-1H-2LAMBDA~6~,1-BENZOTHIAZOL-5-YL)-1,6-NAPHTHYRIDINE-2-CARBOXAMIDE'>68U</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene></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=5i5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i5z OCA], [http://pdbe.org/5i5z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i5z RCSB], [http://www.ebi.ac.uk/pdbsum/5i5z 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=5i5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i5z OCA], [http://pdbe.org/5i5z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i5z RCSB], [http://www.ebi.ac.uk/pdbsum/5i5z PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5i5z ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[http://www.uniprot.org/uniprot/CDK8_HUMAN CDK8_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex. Phosphorylates CCNH leading to down-regulation of the TFIIH complex and transcriptional repression. Recruited through interaction with MAML1 to hyperphosphorylate the intracellular domain of NOTCH, leading to its degradation.<ref>PMID:10993082</ref> <ref>PMID:15546612</ref> [[http://www.uniprot.org/uniprot/CCNC_HUMAN CCNC_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Binds to and activates cyclin-dependent kinase CDK8 that phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex.<ref>PMID:8700522</ref> <ref>PMID:16595664</ref>		[[http://www.uniprot.org/uniprot/CDK8_HUMAN CDK8_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex. Phosphorylates CCNH leading to down-regulation of the TFIIH complex and transcriptional repression. Recruited through interaction with MAML1 to hyperphosphorylate the intracellular domain of NOTCH, leading to its degradation.<ref>PMID:10993082</ref> <ref>PMID:15546612</ref> [[http://www.uniprot.org/uniprot/CCNC_HUMAN CCNC_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Binds to and activates cyclin-dependent kinase CDK8 that phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex.<ref>PMID:8700522</ref> <ref>PMID:16595664</ref>
		+	<div style="background-color:#fffaf0;">
		+	== Publication Abstract from PubMed ==
		+	We demonstrate a designed scaffold-hop approach to the discovery of 2,8-disubstituted-1,6-naphthyridine- and 4,6-disubstituted-isoquinoline-based dual CDK8/19 ligands. Optimized compounds in both series exhibited rapid aldehyde oxidase-mediated metabolism, which could be abrogated by introduction of an amino substituent at C5 of the 1,6-naphthyridine scaffold or at C1 of the isoquinoline scaffold. Compounds 51 and 59 were progressed to in vivo pharmacokinetic studies, and 51 also demonstrated sustained inhibition of STAT1(SER727) phosphorylation, a biomarker of CDK8 inhibition, in an SW620 colorectal carcinoma human tumor xenograft model following oral dosing.
		+
		+	2,8-Disubstituted-1,6-Naphthyridines and 4,6-Disubstituted-Isoquinolines with Potent, Selective Affinity for CDK8/19.,Mallinger A, Schiemann K, Rink C, Sejberg J, Honey MA, Czodrowski P, Stubbs M, Poeschke O, Busch M, Schneider R, Schwarz D, Musil D, Burke R, Urbahns K, Workman P, Wienke D, Clarke PA, Raynaud FI, Eccles SA, Esdar C, Rohdich F, Blagg J ACS Med Chem Lett. 2016 Mar 28;7(6):573-8. doi: 10.1021/acsmedchemlett.6b00022., eCollection 2016 Jun 9. PMID:27326329<ref>PMID:27326329</ref>
		+
		+	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
		+	</div>
		+	<div class="pdbe-citations 5i5z" style="background-color:#fffaf0;"></div>
	== References ==		== References ==
	<references/>		<references/>

OCA at 11:30, 12 May 2016

2016-05-12T11:30:07Z

←Older revision		Revision as of 11:30, 12 May 2016
Line 1:		Line 1:
-	'''Unreleased structure'''

-	~~The entry 5i5z is ON HOLD until Paper Publication~~	+	==CDK8-CYCC IN COMPLEX WITH 8-(1-Methyl-2,2-dioxo-2,3-dihydro-1H-2l6-benzo[c]isothiazol-5-yl)-[1,6]naphthyridine-2-carboxylic acid methylamide==
-		+	<StructureSection load='5i5z' size='340' side='right' caption='[[5i5z]], [[Resolution\|resolution]] 2.60Å' scene=''>
-	~~Authors: Musil, D., Blagg, J., Mallinger, A.~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[5i5z]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5I5Z OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5I5Z FirstGlance]. <br>
-	~~Description:~~ CDK8-CYCC IN COMPLEX WITH 8-(1-Methyl-2,2-dioxo-2,3-dihydro-1H-2l6-benzo[c]isothiazol-5-yl)-[1,6]naphthyridine-2-carboxylic acid methylamide	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=68U:N-METHYL-8-(1-METHYL-2,2-DIOXO-2,3-DIHYDRO-1H-2LAMBDA~6~,1-BENZOTHIAZOL-5-YL)-1,6-NAPHTHYRIDINE-2-CARBOXAMIDE'>68U</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene></td></tr>
-	[[~~Category~~: ~~Unreleased Structures~~]]	+	<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=5i5z FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5i5z OCA], [http://pdbe.org/5i5z PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5i5z RCSB], [http://www.ebi.ac.uk/pdbsum/5i5z PDBsum]</span></td></tr>
-	[[~~Category~~: ~~Musil~~, D]]	+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/CDK8_HUMAN CDK8_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex. Phosphorylates CCNH leading to down-regulation of the TFIIH complex and transcriptional repression. Recruited through interaction with MAML1 to hyperphosphorylate the intracellular domain of NOTCH, leading to its degradation.<ref>PMID:10993082</ref> <ref>PMID:15546612</ref> [[http://www.uniprot.org/uniprot/CCNC_HUMAN CCNC_HUMAN]] Component of the Mediator complex, a coactivator involved in regulated gene transcription of nearly all RNA polymerase II-dependent genes. Mediator functions as a bridge to convey information from gene-specific regulatory proteins to the basal RNA polymerase II transcription machinery. Mediator is recruited to promoters by direct interactions with regulatory proteins and serves as a scaffold for the assembly of a functional preinitiation complex with RNA polymerase II and the general transcription factors. Binds to and activates cyclin-dependent kinase CDK8 that phosphorylates the CTD (C-terminal domain) of the large subunit of RNA polymerase II (RNAp II), which may inhibit the formation of a transcription initiation complex.<ref>PMID:8700522</ref> <ref>PMID:16595664</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
	[[Category: Blagg, J]]		[[Category: Blagg, J]]
	[[Category: Mallinger, A]]		[[Category: Mallinger, A]]
		+	[[Category: Musil, D]]
		+	[[Category: Cdk8 kinase / cyclin c]]
		+	[[Category: Transferase]]

OCA at 13:25, 2 March 2016

2016-03-02T13:25:22Z

←Older revision		Revision as of 13:25, 2 March 2016
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 5i5z is ON HOLD	+	The entry 5i5z is ON HOLD until Paper Publication

	Authors: Musil, D., Blagg, J., Mallinger, A.		Authors: Musil, D., Blagg, J., Mallinger, A.

OCA: Protected "5i5z" [edit=sysop:move=sysop]

2016-02-26T16:49:57Z

Protected "5i5z" [edit=sysop:move=sysop]

←Older revision

Revision as of 16:49, 26 February 2016

OCA: New page: '''Unreleased structure''' The entry 5i5z is ON HOLD Authors: Musil, D., Blagg, J., Mallinger, A. Description: CDK8-CYCC IN COMPLEX WITH 8-(1-Methyl-2,2-dioxo-2,3-dihydro-1H-2l6-benzo[...

2016-02-26T16:49:56Z

New page: '''Unreleased structure''' The entry 5i5z is ON HOLD Authors: Musil, D., Blagg, J., Mallinger, A. Description: CDK8-CYCC IN COMPLEX WITH 8-(1-Methyl-2,2-dioxo-2,3-dihydro-1H-2l6-benzo[...

New page

'''Unreleased structure'''

The entry 5i5z is ON HOLD

Authors: Musil, D., Blagg, J., Mallinger, A.

Description: CDK8-CYCC IN COMPLEX WITH 8-(1-Methyl-2,2-dioxo-2,3-dihydro-1H-2l6-benzo[c]isothiazol-5-yl)-[1,6]naphthyridine-2-carboxylic acid methylamide
[[Category: Unreleased Structures]]
[[Category: Musil, D]]
[[Category: Blagg, J]]
[[Category: Mallinger, A]]