3qql - Revision history

OCA at 11:55, 14 March 2024

OCA — Thu, 14 Mar 2024 11:55:08 GMT

←Older revision		Revision as of 11:55, 14 March 2024
Line 3:		Line 3:
	<StructureSection load='3qql' size='340' side='right'caption='[[3qql]], [[Resolution\|resolution]] 1.85Å' scene=''>		<StructureSection load='3qql' size='340' side='right'caption='[[3qql]], [[Resolution\|resolution]] 1.85Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3qql]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Human Human~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QQL FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3qql]] 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=3QQL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QQL FirstGlance]. <br>
-	</td></tr><tr id='~~ligand~~'><td class="sblockLbl"><b>[[~~Ligand~~\|~~Ligands~~:]]</b></td><td class="sblockDat" id="~~ligandDat~~">~~<scene name='pdbligand=X03:(5R)~~-~~5-(2-METHYLBUTAN-2-YL)-4~~,~~5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</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]] 1.85Å</td></tr>
-	~~<tr id='related'><td class="sblockLbl"><b>~~[[~~Related_structure~~\|~~Related:~~]]~~</b></td><td class="sblockDat"><div style='overflow: auto~~; max-height: 3em;'>[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</div></td></tr>	+	<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene></td></tr>
-	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat"~~>CDK2 ([https://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'>[https~~:~~//en.wikipedia.org/wiki/Cyclin~~-~~dependent_kinase Cyclin~~-~~dependent kinase], with EC number [https://www.brenda~~-~~enzymes.info/php/result_flat.php4?ecno=~~2.7~~.11.22 2.7.11.22]~~ </~~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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [https://pdbe.org/3qql PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [https://www.ebi.ac.uk/pdbsum/3qql PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qql 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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [https://pdbe.org/3qql PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [https://www.ebi.ac.uk/pdbsum/3qql PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qql ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[https://www.uniprot.org/uniprot/CDK2_HUMAN CDK2_HUMAN]] Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression; controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Crucial role in orchestrating a fine balance between cellular proliferation, cell death, and DNA repair in human embryonic stem cells (hESCs). Activity of CDK2 is maximal during S phase and G2; activated by interaction with cyclin E during the early stages of DNA synthesis to permit G1-S transition, and subsequently activated by cyclin A2 (cyclin A1 in germ cells) during the late stages of DNA replication to drive the transition from S phase to mitosis, the G2 phase. EZH2 phosphorylation promotes H3K27me3 maintenance and epigenetic gene silencing. Phosphorylates CABLES1 (By similarity). Cyclin E/CDK2 prevents oxidative stress-mediated Ras-induced senescence by phosphorylating MYC. Involved in G1-S phase DNA damage checkpoint that prevents cells with damaged DNA from initiating mitosis; regulates homologous recombination-dependent repair by phosphorylating BRCA2, this phosphorylation is low in S phase when recombination is active, but increases as cells progress towards mitosis. In response to DNA damage, double-strand break repair by homologous recombination a reduction of CDK2-mediated BRCA2 phosphorylation. Phosphorylation of RB1 disturbs its interaction with E2F1. NPM1 phosphorylation by cyclin E/CDK2 promotes its dissociates from unduplicated centrosomes, thus initiating centrosome duplication. Cyclin E/CDK2-mediated phosphorylation of NPAT at G1-S transition and until prophase stimulates the NPAT-mediated activation of histone gene transcription during S phase. Required for vitamin D-mediated growth inhibition by being itself inactivated. Involved in the nitric oxide- (NO) mediated signaling in a nitrosylation/activation-dependent manner. USP37 is activated by phosphorylation and thus triggers G1-S transition. CTNNB1 phosphorylation regulates insulin internalization.<ref>PMID:10499802</ref> <ref>PMID:11051553</ref> <ref>PMID:10995386</ref> <ref>PMID:10995387</ref> <ref>PMID:10884347</ref> <ref>PMID:11113184</ref> <ref>PMID:15800615</ref> <ref>PMID:18372919</ref> <ref>PMID:20147522</ref> <ref>PMID:20079829</ref> <ref>PMID:20935635</ref> <ref>PMID:20195506</ref> <ref>PMID:19966300</ref> <ref>PMID:21262353</ref> <ref>PMID:21596315</ref> <ref>PMID:21319273</ref> <ref>PMID:17495531</ref>	+	[https://www.uniprot.org/uniprot/CDK2_HUMAN CDK2_HUMAN] Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression; controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Crucial role in orchestrating a fine balance between cellular proliferation, cell death, and DNA repair in human embryonic stem cells (hESCs). Activity of CDK2 is maximal during S phase and G2; activated by interaction with cyclin E during the early stages of DNA synthesis to permit G1-S transition, and subsequently activated by cyclin A2 (cyclin A1 in germ cells) during the late stages of DNA replication to drive the transition from S phase to mitosis, the G2 phase. EZH2 phosphorylation promotes H3K27me3 maintenance and epigenetic gene silencing. Phosphorylates CABLES1 (By similarity). Cyclin E/CDK2 prevents oxidative stress-mediated Ras-induced senescence by phosphorylating MYC. Involved in G1-S phase DNA damage checkpoint that prevents cells with damaged DNA from initiating mitosis; regulates homologous recombination-dependent repair by phosphorylating BRCA2, this phosphorylation is low in S phase when recombination is active, but increases as cells progress towards mitosis. In response to DNA damage, double-strand break repair by homologous recombination a reduction of CDK2-mediated BRCA2 phosphorylation. Phosphorylation of RB1 disturbs its interaction with E2F1. NPM1 phosphorylation by cyclin E/CDK2 promotes its dissociates from unduplicated centrosomes, thus initiating centrosome duplication. Cyclin E/CDK2-mediated phosphorylation of NPAT at G1-S transition and until prophase stimulates the NPAT-mediated activation of histone gene transcription during S phase. Required for vitamin D-mediated growth inhibition by being itself inactivated. Involved in the nitric oxide- (NO) mediated signaling in a nitrosylation/activation-dependent manner. USP37 is activated by phosphorylation and thus triggers G1-S transition. CTNNB1 phosphorylation regulates insulin internalization.<ref>PMID:10499802</ref> <ref>PMID:11051553</ref> <ref>PMID:10995386</ref> <ref>PMID:10995387</ref> <ref>PMID:10884347</ref> <ref>PMID:11113184</ref> <ref>PMID:15800615</ref> <ref>PMID:18372919</ref> <ref>PMID:20147522</ref> <ref>PMID:20079829</ref> <ref>PMID:20935635</ref> <ref>PMID:20195506</ref> <ref>PMID:19966300</ref> <ref>PMID:21262353</ref> <ref>PMID:21596315</ref> <ref>PMID:21319273</ref> <ref>PMID:17495531</ref>

	==See Also==		==See Also==
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	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Cyclin-dependent kinase]]~~	+	[[Category: Homo sapiens]]
-	~~[[Category: Human~~]]	+
	[[Category: Large Structures]]		[[Category: Large Structures]]
-	[[Category: Alam, R]]	+	[[Category: Alam R]]
-	[[Category: Becker, A]]	+	[[Category: Becker A]]
-	[[Category: Betzi, S]]	+	[[Category: Betzi S]]
-	[[Category: Han, H]]	+	[[Category: Han H]]
-	[[Category: Schonbrunn, E]]	+	[[Category: Schonbrunn E]]
-	~~[[Category: Inhibitor]]~~	+
-	~~[[Category: Protein kinase]]~~	+
-	~~[[Category: Transferase-transferase inhibitor complex~~]]	+

OCA at 06:19, 8 June 2022

OCA — Wed, 08 Jun 2022 06:19:54 GMT

←Older revision		Revision as of 06:19, 8 June 2022
Line 1:		Line 1:

	==CDK2 in complex with inhibitor L3==		==CDK2 in complex with inhibitor L3==
-	<StructureSection load='3qql' size='340' side='right' caption='[[3qql]], [[Resolution\|resolution]] 1.85Å' scene=''>	+	<StructureSection load='3qql' size='340' side='right'caption='[[3qql]], [[Resolution\|resolution]] 1.85Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3qql]] 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=3QQL OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3QQL FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3qql]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3QQL FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene></td></tr>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene></td></tr>
-	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</div></td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK2 ([~~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">CDK2 ([https://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/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [~~http~~://pdbe.org/3qql PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3qql PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=3qql 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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [https://pdbe.org/3qql PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [https://www.ebi.ac.uk/pdbsum/3qql PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3qql ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
-	[[~~http~~://www.uniprot.org/uniprot/CDK2_HUMAN CDK2_HUMAN]] Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression; controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Crucial role in orchestrating a fine balance between cellular proliferation, cell death, and DNA repair in human embryonic stem cells (hESCs). Activity of CDK2 is maximal during S phase and G2; activated by interaction with cyclin E during the early stages of DNA synthesis to permit G1-S transition, and subsequently activated by cyclin A2 (cyclin A1 in germ cells) during the late stages of DNA replication to drive the transition from S phase to mitosis, the G2 phase. EZH2 phosphorylation promotes H3K27me3 maintenance and epigenetic gene silencing. Phosphorylates CABLES1 (By similarity). Cyclin E/CDK2 prevents oxidative stress-mediated Ras-induced senescence by phosphorylating MYC. Involved in G1-S phase DNA damage checkpoint that prevents cells with damaged DNA from initiating mitosis; regulates homologous recombination-dependent repair by phosphorylating BRCA2, this phosphorylation is low in S phase when recombination is active, but increases as cells progress towards mitosis. In response to DNA damage, double-strand break repair by homologous recombination a reduction of CDK2-mediated BRCA2 phosphorylation. Phosphorylation of RB1 disturbs its interaction with E2F1. NPM1 phosphorylation by cyclin E/CDK2 promotes its dissociates from unduplicated centrosomes, thus initiating centrosome duplication. Cyclin E/CDK2-mediated phosphorylation of NPAT at G1-S transition and until prophase stimulates the NPAT-mediated activation of histone gene transcription during S phase. Required for vitamin D-mediated growth inhibition by being itself inactivated. Involved in the nitric oxide- (NO) mediated signaling in a nitrosylation/activation-dependent manner. USP37 is activated by phosphorylation and thus triggers G1-S transition. CTNNB1 phosphorylation regulates insulin internalization.<ref>PMID:10499802</ref> <ref>PMID:11051553</ref> <ref>PMID:10995386</ref> <ref>PMID:10995387</ref> <ref>PMID:10884347</ref> <ref>PMID:11113184</ref> <ref>PMID:15800615</ref> <ref>PMID:18372919</ref> <ref>PMID:20147522</ref> <ref>PMID:20079829</ref> <ref>PMID:20935635</ref> <ref>PMID:20195506</ref> <ref>PMID:19966300</ref> <ref>PMID:21262353</ref> <ref>PMID:21596315</ref> <ref>PMID:21319273</ref> <ref>PMID:17495531</ref>	+	[[https://www.uniprot.org/uniprot/CDK2_HUMAN CDK2_HUMAN]] Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression; controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Crucial role in orchestrating a fine balance between cellular proliferation, cell death, and DNA repair in human embryonic stem cells (hESCs). Activity of CDK2 is maximal during S phase and G2; activated by interaction with cyclin E during the early stages of DNA synthesis to permit G1-S transition, and subsequently activated by cyclin A2 (cyclin A1 in germ cells) during the late stages of DNA replication to drive the transition from S phase to mitosis, the G2 phase. EZH2 phosphorylation promotes H3K27me3 maintenance and epigenetic gene silencing. Phosphorylates CABLES1 (By similarity). Cyclin E/CDK2 prevents oxidative stress-mediated Ras-induced senescence by phosphorylating MYC. Involved in G1-S phase DNA damage checkpoint that prevents cells with damaged DNA from initiating mitosis; regulates homologous recombination-dependent repair by phosphorylating BRCA2, this phosphorylation is low in S phase when recombination is active, but increases as cells progress towards mitosis. In response to DNA damage, double-strand break repair by homologous recombination a reduction of CDK2-mediated BRCA2 phosphorylation. Phosphorylation of RB1 disturbs its interaction with E2F1. NPM1 phosphorylation by cyclin E/CDK2 promotes its dissociates from unduplicated centrosomes, thus initiating centrosome duplication. Cyclin E/CDK2-mediated phosphorylation of NPAT at G1-S transition and until prophase stimulates the NPAT-mediated activation of histone gene transcription during S phase. Required for vitamin D-mediated growth inhibition by being itself inactivated. Involved in the nitric oxide- (NO) mediated signaling in a nitrosylation/activation-dependent manner. USP37 is activated by phosphorylation and thus triggers G1-S transition. CTNNB1 phosphorylation regulates insulin internalization.<ref>PMID:10499802</ref> <ref>PMID:11051553</ref> <ref>PMID:10995386</ref> <ref>PMID:10995387</ref> <ref>PMID:10884347</ref> <ref>PMID:11113184</ref> <ref>PMID:15800615</ref> <ref>PMID:18372919</ref> <ref>PMID:20147522</ref> <ref>PMID:20079829</ref> <ref>PMID:20935635</ref> <ref>PMID:20195506</ref> <ref>PMID:19966300</ref> <ref>PMID:21262353</ref> <ref>PMID:21596315</ref> <ref>PMID:21319273</ref> <ref>PMID:17495531</ref>
		+
		+	==See Also==
		+	*[[Cyclin-dependent kinase 3D structures\|Cyclin-dependent kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
Line 18:		Line 21:
	[[Category: Cyclin-dependent kinase]]		[[Category: Cyclin-dependent kinase]]
	[[Category: Human]]		[[Category: Human]]
		+	[[Category: Large Structures]]
	[[Category: Alam, R]]		[[Category: Alam, R]]
	[[Category: Becker, A]]		[[Category: Becker, A]]

OCA at 22:22, 4 August 2016

OCA — Thu, 04 Aug 2016 22:22:08 GMT

←Older revision		Revision as of 22:22, 4 August 2016
Line 1:		Line 1:
		+
	==CDK2 in complex with inhibitor L3==		==CDK2 in complex with inhibitor L3==
	<StructureSection load='3qql' size='340' side='right' caption='[[3qql]], [[Resolution\|resolution]] 1.85Å' scene=''>		<StructureSection load='3qql' size='340' side='right' caption='[[3qql]], [[Resolution\|resolution]] 1.85Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[3qql]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/~~Homo_sapiens Homo sapiens~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QQL FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[3qql]] 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=3QQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QQL FirstGlance]. <br>
	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene></td></tr>		</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 ~~Homo sapiens~~])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK2 ([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/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [http://www.ebi.ac.uk/pdbsum/3qql 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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [http://pdbe.org/3qql PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [http://www.ebi.ac.uk/pdbsum/3qql PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=3qql ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
Line 16:		Line 17:
	</StructureSection>		</StructureSection>
	[[Category: Cyclin-dependent kinase]]		[[Category: Cyclin-dependent kinase]]
-	[[Category: ~~Homo sapiens~~]]	+	[[Category: Human]]
	[[Category: Alam, R]]		[[Category: Alam, R]]
	[[Category: Becker, A]]		[[Category: Becker, A]]

OCA at 20:11, 24 December 2014

OCA — Wed, 24 Dec 2014 20:11:41 GMT

←Older revision		Revision as of 20:11, 24 December 2014
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3qql]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QQL FirstGlance]. <br>		<table><tr><td colspan='2'>[[3qql]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QQL FirstGlance]. <br>
-	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene><br>	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene></td></tr>
-	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</td></tr>	+	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</td></tr>
-	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
-	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </span></td></tr>	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [http://www.ebi.ac.uk/pdbsum/3qql 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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [http://www.ebi.ac.uk/pdbsum/3qql PDBsum]</span></td></tr>
-	<table>	+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/CDK2_HUMAN CDK2_HUMAN]] Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, NPAT, EZH2. Interacts with cyclins A, B1, B3, D, or E. Triggers duplication of centrosomes and DNA. Acts at the G1-S transition to promote the E2F transcriptional program and the initiation of DNA synthesis, and modulates G2 progression; controls the timing of entry into mitosis/meiosis by controlling the subsequent activation of cyclin B/CDK1 by phosphorylation, and coordinates the activation of cyclin B/CDK1 at the centrosome and in the nucleus. Crucial role in orchestrating a fine balance between cellular proliferation, cell death, and DNA repair in human embryonic stem cells (hESCs). Activity of CDK2 is maximal during S phase and G2; activated by interaction with cyclin E during the early stages of DNA synthesis to permit G1-S transition, and subsequently activated by cyclin A2 (cyclin A1 in germ cells) during the late stages of DNA replication to drive the transition from S phase to mitosis, the G2 phase. EZH2 phosphorylation promotes H3K27me3 maintenance and epigenetic gene silencing. Phosphorylates CABLES1 (By similarity). Cyclin E/CDK2 prevents oxidative stress-mediated Ras-induced senescence by phosphorylating MYC. Involved in G1-S phase DNA damage checkpoint that prevents cells with damaged DNA from initiating mitosis; regulates homologous recombination-dependent repair by phosphorylating BRCA2, this phosphorylation is low in S phase when recombination is active, but increases as cells progress towards mitosis. In response to DNA damage, double-strand break repair by homologous recombination a reduction of CDK2-mediated BRCA2 phosphorylation. Phosphorylation of RB1 disturbs its interaction with E2F1. NPM1 phosphorylation by cyclin E/CDK2 promotes its dissociates from unduplicated centrosomes, thus initiating centrosome duplication. Cyclin E/CDK2-mediated phosphorylation of NPAT at G1-S transition and until prophase stimulates the NPAT-mediated activation of histone gene transcription during S phase. Required for vitamin D-mediated growth inhibition by being itself inactivated. Involved in the nitric oxide- (NO) mediated signaling in a nitrosylation/activation-dependent manner. USP37 is activated by phosphorylation and thus triggers G1-S transition. CTNNB1 phosphorylation regulates insulin internalization.<ref>PMID:10499802</ref> <ref>PMID:11051553</ref> <ref>PMID:10995386</ref> <ref>PMID:10995387</ref> <ref>PMID:10884347</ref> <ref>PMID:11113184</ref> <ref>PMID:15800615</ref> <ref>PMID:18372919</ref> <ref>PMID:20147522</ref> <ref>PMID:20079829</ref> <ref>PMID:20935635</ref> <ref>PMID:20195506</ref> <ref>PMID:19966300</ref> <ref>PMID:21262353</ref> <ref>PMID:21596315</ref> <ref>PMID:21319273</ref> <ref>PMID:17495531</ref>
		+	== References ==
		+	<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: Cyclin-dependent kinase]]		[[Category: Cyclin-dependent kinase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]
-	[[Category: Alam, R.]]	+	[[Category: Alam, R]]
-	[[Category: Becker, A.]]	+	[[Category: Becker, A]]
-	[[Category: Betzi, S.]]	+	[[Category: Betzi, S]]
-	[[Category: Han, H.]]	+	[[Category: Han, H]]
-	[[Category: Schonbrunn, E.]]	+	[[Category: Schonbrunn, E]]
	[[Category: Inhibitor]]		[[Category: Inhibitor]]
	[[Category: Protein kinase]]		[[Category: Protein kinase]]
	[[Category: Transferase-transferase inhibitor complex]]		[[Category: Transferase-transferase inhibitor complex]]

OCA at 07:09, 9 June 2014

OCA — Mon, 09 Jun 2014 07:09:54 GMT

←Older revision		Revision as of 07:09, 9 June 2014
Line 1:		Line 1:
-	~~[[Image:3qql.jpg\|left\|200px]]~~	+	==CDK2 in complex with inhibitor L3==
-		+	<StructureSection load='3qql' size='340' side='right' caption='[[3qql]], [[Resolution\|resolution]] 1.85Å' scene=''>
-	~~{{STRUCTURE_3qql\| PDB=3qql \| SCENE= }}~~	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[3qql]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3QQL FirstGlance]. <br>
-	===CDK2 in complex with inhibitor L3===	+	</td></tr><tr><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=X03:(5R)-5-(2-METHYLBUTAN-2-YL)-4,5,6,7-TETRAHYDRO-1H-INDAZOLE-3-CARBOHYDRAZIDE'>X03</scene><br>
-		+	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[3ql8\|3ql8]], [[3qqf\|3qqf]], [[3qqg\|3qqg]], [[3qqh\|3qqh]], [[3qqj\|3qqj]], [[3qqk\|3qqk]], [[3qrt\|3qrt]], [[3qru\|3qru]], [[3qtq\|3qtq]], [[3qtr\|3qtr]], [[3qts\|3qts]], [[3qtu\|3qtu]], [[3qtw\|3qtw]], [[3qtx\|3qtx]], [[3qtz\|3qtz]], [[3qu0\|3qu0]], [[3qwj\|3qwj]], [[3qwk\|3qwk]], [[3qx2\|3qx2]], [[3qx4\|3qx4]], [[3qxo\|3qxo]], [[3qxp\|3qxp]], [[3qzf\|3qzf]], [[3qzg\|3qzg]], [[3qzh\|3qzh]], [[3qzi\|3qzi]], [[3r1q\|3r1q]], [[3r1s\|3r1s]], [[3r1y\|3r1y]], [[3r28\|3r28]], [[3r6x\|3r6x]], [[3r71\|3r71]], [[3r73\|3r73]], [[3r7e\|3r7e]], [[3r7i\|3r7i]], [[3r7u\|3r7u]], [[3r7v\|3r7v]], [[3r7y\|3r7y]], [[3r83\|3r83]], [[3r8l\|3r8l]], [[3r8m\|3r8m]], [[3r8p\|3r8p]], [[3r8u\|3r8u]], [[3r8v\|3r8v]], [[3r8z\|3r8z]], [[3r9d\|3r9d]], [[3r9h\|3r9h]], [[3r9n\|3r9n]], [[3r9o\|3r9o]], [[3rah\|3rah]], [[3rai\|3rai]], [[3rak\|3rak]], [[3ral\|3ral]], [[3rjc\|3rjc]], [[3rk5\|3rk5]], [[3rk7\|3rk7]], [[3rk9\|3rk9]], [[3rkb\|3rkb]], [[3rm6\|3rm6]], [[3rm7\|3rm7]], [[3rmf\|3rmf]], [[3rni\|3rni]], [[3roy\|3roy]], [[3rpo\|3rpo]], [[3rpr\|3rpr]], [[3rpv\|3rpv]], [[3rpy\|3rpy]], [[3rzb\|3rzb]], [[3s00\|3s00]], [[3s0o\|3s0o]], [[3s1h\|3s1h]], [[3sqq\|3sqq]]</td></tr>
-		+	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CDK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr>
-	==~~About this Structure~~==	+	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Cyclin-dependent_kinase Cyclin-dependent kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.22 2.7.11.22] </span></td></tr>
-	[[3qql]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA].	+	<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=3qql FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3qql OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3qql RCSB], [http://www.ebi.ac.uk/pdbsum/3qql PDBsum]</span></td></tr>
		+	<table>
		+	__TOC__
		+	</StructureSection>
	[[Category: Cyclin-dependent kinase]]		[[Category: Cyclin-dependent kinase]]
	[[Category: Homo sapiens]]		[[Category: Homo sapiens]]

OCA at 05:24, 8 August 2012

OCA — Wed, 08 Aug 2012 05:24:25 GMT

←Older revision		Revision as of 05:24, 8 August 2012
Line 1:		Line 1:
-	~~'''Unreleased structure'''~~	+	[[Image:3qql.jpg\|left\|200px]]

-	~~The entry~~ 3qql ~~is ON HOLD~~ ~~until Aug 15 2013~~	+	{{STRUCTURE_3qql\| PDB=3qql \| SCENE= }}

-	~~Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.~~	+	===CDK2 in complex with inhibitor L3===

-	~~Description: CDK2 in complex~~ with inhibitor L3	+
		+	==About this Structure==
		+	[[3qql]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3QQL OCA].
		+	[[Category: Cyclin-dependent kinase]]
		+	[[Category: Homo sapiens]]
		+	[[Category: Alam, R.]]
		+	[[Category: Becker, A.]]
		+	[[Category: Betzi, S.]]
		+	[[Category: Han, H.]]
		+	[[Category: Schonbrunn, E.]]
		+	[[Category: Inhibitor]]
		+	[[Category: Protein kinase]]
		+	[[Category: Transferase-transferase inhibitor complex]]

OCA at 04:45, 18 July 2012

OCA — Wed, 18 Jul 2012 04:45:53 GMT

←Older revision		Revision as of 04:45, 18 July 2012
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3qql is ON HOLD until Aug 01 2013	+	The entry 3qql is ON HOLD until Aug 15 2013

	Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.		Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.

	Description: CDK2 in complex with inhibitor L3		Description: CDK2 in complex with inhibitor L3

OCA at 06:40, 1 February 2012

OCA — Wed, 01 Feb 2012 06:40:18 GMT

←Older revision		Revision as of 06:40, 1 February 2012
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3qql is ON HOLD until ~~Paper Publication~~	+	The entry 3qql is ON HOLD until Aug 01 2013

	Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.		Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.

	Description: CDK2 in complex with inhibitor L3		Description: CDK2 in complex with inhibitor L3

OCA at 06:45, 23 March 2011

OCA — Wed, 23 Mar 2011 06:45:25 GMT

←Older revision		Revision as of 06:45, 23 March 2011
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 3qql is ON HOLD	+	The entry 3qql is ON HOLD until Paper Publication

	Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.		Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.

	Description: CDK2 in complex with inhibitor L3		Description: CDK2 in complex with inhibitor L3

OCA at 06:41, 2 March 2011

OCA — Wed, 02 Mar 2011 06:41:39 GMT

←Older revision		Revision as of 06:41, 2 March 2011
Line 5:		Line 5:
	Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.		Authors: Betzi, S., Alam, R., Han, H., Becker, A., Schonbrunn, E.

-	Description: CDK2 ~~IN COMPLEX WITH INHIBITOR~~ L3	+	Description: CDK2 in complex with inhibitor L3