8a66

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== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[8a66]] 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=8A66 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8A66 FirstGlance]. <br>
<table><tr><td colspan='2'>[[8a66]] 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=8A66 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=8A66 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5BS:4-[(5,10-DIMETHYL-6-OXO-6,10-DIHYDRO-5H-PYRIMIDO[5,4-B]THIENO[3,2-E][1,4]DIAZEPIN-2-YL)AMINO]BENZENESULFONAMIDE'>5BS</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=TPO:PHOSPHOTHREONINE'>TPO</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.901&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=5BS:4-[(5,10-DIMETHYL-6-OXO-6,10-DIHYDRO-5H-PYRIMIDO[5,4-B]THIENO[3,2-E][1,4]DIAZEPIN-2-YL)AMINO]BENZENESULFONAMIDE'>5BS</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</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=8a66 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8a66 OCA], [https://pdbe.org/8a66 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8a66 RCSB], [https://www.ebi.ac.uk/pdbsum/8a66 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8a66 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=8a66 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=8a66 OCA], [https://pdbe.org/8a66 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=8a66 RCSB], [https://www.ebi.ac.uk/pdbsum/8a66 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=8a66 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
[https://www.uniprot.org/uniprot/STK3_HUMAN STK3_HUMAN] Stress-activated, pro-apoptotic kinase which, following caspase-cleavage, enters the nucleus and induces chromatin condensation followed by internucleosomal DNA fragmentation. Key component of the Hippo signaling pathway which plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Phosphorylation of YAP1 by LATS2 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. STK3/MST2 and STK4/MST1 are required to repress proliferation of mature hepatocytes, to prevent activation of facultative adult liver stem cells (oval cells), and to inhibit tumor formation. Phosphorylates NKX2-1 (By similarity). Phosphorylates NEK2 and plays a role in centrosome disjunction by regulating the localization of NEK2 to centrosome, and its ability to phosphorylate CROCC and CEP250. In conjunction with SAV1, activates the transcriptional activity of ESR1 through the modulation of its phosphorylation. Positively regulates RAF1 activation via suppression of the inhibitory phosphorylation of RAF1 on 'Ser-259'. Phosphorylates MOBKL1A and RASSF2. Phosphorylates MOBKL1B on 'Thr-74'. Acts cooperatively with MOBKL1B to activate STK38.<ref>PMID:8566796</ref> <ref>PMID:8816758</ref> <ref>PMID:15688006</ref> <ref>PMID:16930133</ref> <ref>PMID:18328708</ref> <ref>PMID:18362890</ref> <ref>PMID:19525978</ref> <ref>PMID:20212043</ref> <ref>PMID:21076410</ref> <ref>PMID:21104395</ref>
[https://www.uniprot.org/uniprot/STK3_HUMAN STK3_HUMAN] Stress-activated, pro-apoptotic kinase which, following caspase-cleavage, enters the nucleus and induces chromatin condensation followed by internucleosomal DNA fragmentation. Key component of the Hippo signaling pathway which plays a pivotal role in organ size control and tumor suppression by restricting proliferation and promoting apoptosis. The core of this pathway is composed of a kinase cascade wherein STK3/MST2 and STK4/MST1, in complex with its regulatory protein SAV1, phosphorylates and activates LATS1/2 in complex with its regulatory protein MOB1, which in turn phosphorylates and inactivates YAP1 oncoprotein and WWTR1/TAZ. Phosphorylation of YAP1 by LATS2 inhibits its translocation into the nucleus to regulate cellular genes important for cell proliferation, cell death, and cell migration. STK3/MST2 and STK4/MST1 are required to repress proliferation of mature hepatocytes, to prevent activation of facultative adult liver stem cells (oval cells), and to inhibit tumor formation. Phosphorylates NKX2-1 (By similarity). Phosphorylates NEK2 and plays a role in centrosome disjunction by regulating the localization of NEK2 to centrosome, and its ability to phosphorylate CROCC and CEP250. In conjunction with SAV1, activates the transcriptional activity of ESR1 through the modulation of its phosphorylation. Positively regulates RAF1 activation via suppression of the inhibitory phosphorylation of RAF1 on 'Ser-259'. Phosphorylates MOBKL1A and RASSF2. Phosphorylates MOBKL1B on 'Thr-74'. Acts cooperatively with MOBKL1B to activate STK38.<ref>PMID:8566796</ref> <ref>PMID:8816758</ref> <ref>PMID:15688006</ref> <ref>PMID:16930133</ref> <ref>PMID:18328708</ref> <ref>PMID:18362890</ref> <ref>PMID:19525978</ref> <ref>PMID:20212043</ref> <ref>PMID:21076410</ref> <ref>PMID:21104395</ref>
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==See Also==
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*[[Serine/threonine protein kinase 3D structures|Serine/threonine protein kinase 3D structures]]
== References ==
== References ==
<references/>
<references/>

Current revision

Crystal structure of MST2 in complex with XMU-MP-1

PDB ID 8a66

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