6b3e: Difference between revisions

Line 1:

~~'''Unreleased structure'''~~

~~The entry~~ 6b3e is ~~ON HOLD~~ ~~until Paper Publication~~

==Crystal structure of human CDK12/CyclinK in complex with an inhibitor==

~~Authors~~:

== Structural highlights ==

<table><tr><td colspan='2'>[[6b3e]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6B3E OCA]. For a guided tour on the structure components use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6B3E FirstGlance].

~~Description~~:

</td></tr><tr id='ligand'><td class="sblockLbl">[[Ligand|Ligands:]]</td><td class="sblockDat"><scene name='pdbligand=CJM:2-[(2S)-1-(6-{[(4,5-difluoro-1H-benzimidazol-2-yl)methyl]amino}-9-ethyl-9H-purin-2-yl)piperidin-2-yl]ethan-1-ol'>CJM</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>

[[Category: ~~Unreleased Structures~~]]

<tr id='NonStdRes'><td class="sblockLbl">[[Non-Standard_Residue|NonStd Res:]]</td><td class="sblockDat"><scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>

<tr id='resources'><td class="sblockLbl">Resources:</td><td class="sblockDat">[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6b3e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6b3e OCA], [http://pdbe.org/6b3e PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6b3e RCSB], [http://www.ebi.ac.uk/pdbsum/6b3e PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6b3e ProSAT]</td></tr>

</table>

== Disease ==

[[http://www.uniprot.org/uniprot/CDK12_HUMAN CDK12_HUMAN]] Chromosomal aberrations involving CDK12 may be a cause gastric cancer. Deletions within 17q12 region producing fusion transcripts with ERBB2, leading to CDK12-ERBB2 fusion leading to trunctated CDK12 protein not in-frame with ERBB2.

== Function ==

[[http://www.uniprot.org/uniprot/CDK12_HUMAN CDK12_HUMAN]] Cyclin-dependent kinase which displays CTD kinase activity and is required for RNA splicing. Has CTD kinase activity by hyperphosphorylating the C-terminal heptapeptide repeat domain (CTD) of the largest RNA polymerase II subunit RPB1, thereby acting as a key regulator of transcription elongation. Required for RNA splicing, possibly by phosphorylating SRSF1/SF2. Involved in regulation of MAP kinase activity, possibly leading to affect the response to estrogn inhibitors.<ref>PMID:11683387</ref> <ref>PMID:19651820</ref> <ref>PMID:20952539</ref> [[http://www.uniprot.org/uniprot/CCNK_HUMAN CCNK_HUMAN]] May play a role in transcriptional regulation. In vitro, is associated with a kinase activity toward both RNA polymerase II C-terminal domain and CDK2 (CAK).<ref>PMID:10574912</ref>

== References ==

__TOC__

</StructureSection>

[[Category: Ferguson, A D]]

[[Category: Complex]]

[[Category: Inhibitor]]

[[Category: Kinase]]

[[Category: Transferase]]

[[Category: Transferase-inhibitor complex]]

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-'''Unreleased structure'''
-The entry 6b3e is ON HOLD  until Paper Publication
+==Crystal structure of human CDK12/CyclinK in complex with an inhibitor==
+<StructureSection load='6b3e' size='340' side='right' caption='[[6b3e]], [[Resolution|resolution]] 3.06&Aring;' scene=''>
-Authors:
+== Structural highlights ==
+<table><tr><td colspan='2'>[[6b3e]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6B3E OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6B3E FirstGlance]. <br>
-Description:
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=CJM:2-[(2S)-1-(6-{[(4,5-difluoro-1H-benzimidazol-2-yl)methyl]amino}-9-ethyl-9H-purin-2-yl)piperidin-2-yl]ethan-1-ol'>CJM</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene></td></tr>
-[[Category: Unreleased Structures]]
+<tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><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'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6b3e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6b3e OCA], [http://pdbe.org/6b3e PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6b3e RCSB], [http://www.ebi.ac.uk/pdbsum/6b3e PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6b3e ProSAT]</span></td></tr>
+</table>
+== Disease ==
+[[http://www.uniprot.org/uniprot/CDK12_HUMAN CDK12_HUMAN]] Chromosomal aberrations involving CDK12 may be a cause gastric cancer. Deletions within 17q12 region producing fusion transcripts with ERBB2, leading to CDK12-ERBB2 fusion leading to trunctated CDK12 protein not in-frame with ERBB2.
+== Function ==
+[[http://www.uniprot.org/uniprot/CDK12_HUMAN CDK12_HUMAN]] Cyclin-dependent kinase which displays CTD kinase activity and is required for RNA splicing. Has CTD kinase activity by hyperphosphorylating the C-terminal heptapeptide repeat domain (CTD) of the largest RNA polymerase II subunit RPB1, thereby acting as a key regulator of transcription elongation. Required for RNA splicing, possibly by phosphorylating SRSF1/SF2. Involved in regulation of MAP kinase activity, possibly leading to affect the response to estrogn inhibitors.<ref>PMID:11683387</ref> <ref>PMID:19651820</ref> <ref>PMID:20952539</ref>  [[http://www.uniprot.org/uniprot/CCNK_HUMAN CCNK_HUMAN]] May play a role in transcriptional regulation. In vitro, is associated with a kinase activity toward both RNA polymerase II C-terminal domain and CDK2 (CAK).<ref>PMID:10574912</ref>
+== References ==
+<references/>
+__TOC__
+</StructureSection>
+[[Category: Ferguson, A D]]
+[[Category: Complex]]
+[[Category: Inhibitor]]
+[[Category: Kinase]]
+[[Category: Transferase]]
+[[Category: Transferase-inhibitor complex]]