5vlo - Revision history

OCA at 14:11, 13 March 2024

OCA — Wed, 13 Mar 2024 14:11:07 GMT

←Older revision		Revision as of 14:11, 13 March 2024
Line 1:		Line 1:

	==The structure of human CamKII with bound inhibitor==		==The structure of human CamKII with bound inhibitor==
-	<StructureSection load='5vlo' size='340' side='right' caption='[[5vlo]], [[Resolution\|resolution]] 2.05Å' scene=''>	+	<StructureSection load='5vlo' size='340' side='right'caption='[[5vlo]], [[Resolution\|resolution]] 2.05Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
-	<table><tr><td colspan='2'>[[5vlo]] 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=5VLO OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=5VLO FirstGlance]. <br>	+	<table><tr><td colspan='2'>[[5vlo]] 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=5VLO OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5VLO FirstGlance]. <br>
-	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=9EJ:N-[(2S)-2-(diethylamino)propyl]-2-[(2S)-2-(methylcarbamoyl)azetidin-1-yl]-6-[5-(thiophen-2-yl)pyrazolo[1,5-a]pyrimidin-3-yl]pyridine-4-carboxamide'>9EJ</scene>, <scene name='pdbligand=DTT:2,3-DIHYDROXY-1,4-DITHIOBUTANE'>DTT</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]] 2.05Å</td></tr>
-	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CAMK2D, CAMKD ([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=9EJ:N-[(2S)-2-(diethylamino)propyl]-2-[(2S)-2-(methylcarbamoyl)azetidin-1-yl]-6-[5-(thiophen-2-yl)pyrazolo[1,5-a]pyrimidin-3-yl]pyridine-4-carboxamide'>9EJ</scene>, <scene name='pdbligand=DTT:2,3-DIHYDROXY-1,4-DITHIOBUTANE'>DTT</scene></td></tr>
-	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Calcium/calmodulin-dependent_protein_kinase Calcium/calmodulin-dependent protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.17 2.7.11.17] </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=5vlo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5vlo OCA], [https://pdbe.org/5vlo PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5vlo RCSB], [https://www.ebi.ac.uk/pdbsum/5vlo PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5vlo 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=5vlo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5vlo OCA], [~~http~~://pdbe.org/5vlo PDBe], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=5vlo RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/5vlo PDBsum], [~~http~~://prosat.h-its.org/prosat/prosatexe?pdbcode=5vlo ProSAT]</span></td></tr>	+
	</table>		</table>
	== Function ==		== Function ==
-	[~~[http~~://www.uniprot.org/uniprot/KCC2D_HUMAN KCC2D_HUMAN]] Calcium/calmodulin-dependent protein kinase involved in the regulation of Ca(2+) homeostatis and excitation-contraction coupling (ECC) in heart by targeting ion channels, transporters and accessory proteins involved in Ca(2+) influx into the myocyte, Ca(2+) release from the sarcoplasmic reticulum (SR), SR Ca(2+) uptake and Na(+) and K(+) channel transport. Targets also transcription factors and signaling molecules to regulate heart function. In its activated form, is involved in the pathogenesis of dilated cardiomyopathy and heart failure. Contributes to cardiac decompensation and heart failure by regulating SR Ca(2+) release via direct phosphorylation of RYR2 Ca(2+) channel on 'Ser-2808'. In the nucleus, phosphorylates the MEF2 repressor HDAC4, promoting its nuclear export and binding to 14-3-3 protein, and expression of MEF2 and genes involved in the hypertrophic program. Is essential for left ventricular remodeling responses to myocardial infarction. In pathological myocardial remodeling acts downstream of the beta adrenergic receptor signaling cascade to regulate key proteins involved in ECC. Regulates Ca(2+) influx to myocytes by binding and phosphorylating the L-type Ca(2+) channel subunit beta-2 CACNB2. In addition to Ca(2+) channels, can target and regulate the cardiac sarcolemmal Na(+) channel Nav1.5/SCN5A and the K+ channel Kv4.3/KCND3, which contribute to arrhythmogenesis in heart failure. Phosphorylates phospholamban (PLN/PLB), an endogenous inhibitor of SERCA2A/ATP2A2, contributing to the enhancement of SR Ca(2+) uptake that may be important in frequency-dependent acceleration of relaxation (FDAR) and maintenance of contractile function during acidosis. May participate in the modulation of skeletal muscle function in response to exercise, by regulating SR Ca(2+) transport through phosphorylation of PLN/PLB and triadin, a ryanodine receptor-coupling factor.<ref>PMID:16690701</ref> <ref>PMID:17179159</ref>	+	[https://www.uniprot.org/uniprot/KCC2D_HUMAN KCC2D_HUMAN] Calcium/calmodulin-dependent protein kinase involved in the regulation of Ca(2+) homeostatis and excitation-contraction coupling (ECC) in heart by targeting ion channels, transporters and accessory proteins involved in Ca(2+) influx into the myocyte, Ca(2+) release from the sarcoplasmic reticulum (SR), SR Ca(2+) uptake and Na(+) and K(+) channel transport. Targets also transcription factors and signaling molecules to regulate heart function. In its activated form, is involved in the pathogenesis of dilated cardiomyopathy and heart failure. Contributes to cardiac decompensation and heart failure by regulating SR Ca(2+) release via direct phosphorylation of RYR2 Ca(2+) channel on 'Ser-2808'. In the nucleus, phosphorylates the MEF2 repressor HDAC4, promoting its nuclear export and binding to 14-3-3 protein, and expression of MEF2 and genes involved in the hypertrophic program. Is essential for left ventricular remodeling responses to myocardial infarction. In pathological myocardial remodeling acts downstream of the beta adrenergic receptor signaling cascade to regulate key proteins involved in ECC. Regulates Ca(2+) influx to myocytes by binding and phosphorylating the L-type Ca(2+) channel subunit beta-2 CACNB2. In addition to Ca(2+) channels, can target and regulate the cardiac sarcolemmal Na(+) channel Nav1.5/SCN5A and the K+ channel Kv4.3/KCND3, which contribute to arrhythmogenesis in heart failure. Phosphorylates phospholamban (PLN/PLB), an endogenous inhibitor of SERCA2A/ATP2A2, contributing to the enhancement of SR Ca(2+) uptake that may be important in frequency-dependent acceleration of relaxation (FDAR) and maintenance of contractile function during acidosis. May participate in the modulation of skeletal muscle function in response to exercise, by regulating SR Ca(2+) transport through phosphorylation of PLN/PLB and triadin, a ryanodine receptor-coupling factor.<ref>PMID:16690701</ref> <ref>PMID:17179159</ref>
		+
		+	==See Also==
		+	*[[Calcium/calmodulin dependent protein kinase 3D structures\|Calcium/calmodulin dependent protein kinase 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
-	[[Category: ~~Calcium/calmodulin-dependent protein kinase~~]]	+	[[Category: Homo sapiens]]
-	[[Category: ~~Human~~]]	+	[[Category: Large Structures]]
-	[[Category: Somoza~~, J R~~]]	+	[[Category: Somoza JR]]
-	[[Category: Villasenor~~, A G]]~~	+	[[Category: Villasenor AG]]
-	~~[[Category: Camkii]]~~	+
-	~~[[Category: Inhibitor]]~~	+
-	~~[[Category: Kinase]]~~	+
-	~~[[Category: Transferase~~]]	+

OCA at 14:41, 6 November 2017

OCA — Mon, 06 Nov 2017 14:41:40 GMT

←Older revision		Revision as of 14:41, 6 November 2017
Line 1:		Line 1:
-	'''Unreleased structure'''

-	The ~~entry~~ 5vlo is ~~ON HOLD until Oct 25 2018~~	+	==The structure of human CamKII with bound inhibitor==
-		+	<StructureSection load='5vlo' size='340' side='right' caption='[[5vlo]], [[Resolution\|resolution]] 2.05Å' scene=''>
-	~~Authors~~: ~~Somoza~~, J.R., ~~Villasenor~~, A.G.	+	== Structural highlights ==
-		+	<table><tr><td colspan='2'>[[5vlo]] 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=5VLO OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5VLO FirstGlance]. <br>
-	~~Description~~: ~~The structure~~ of ~~human CamKII with bound~~ inhibitor	+	</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=9EJ:N-[(2S)-2-(diethylamino)propyl]-2-[(2S)-2-(methylcarbamoyl)azetidin-1-yl]-6-[5-(thiophen-2-yl)pyrazolo[1,5-a]pyrimidin-3-yl]pyridine-4-carboxamide'>9EJ</scene>, <scene name='pdbligand=DTT:2,3-DIHYDROXY-1,4-DITHIOBUTANE'>DTT</scene></td></tr>
-	[[Category: ~~Unreleased Structures~~]]	+	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">CAMK2D, CAMKD ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr>
-	[[Category: ~~Villasenor, A.G~~]]	+	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Calcium/calmodulin-dependent_protein_kinase Calcium/calmodulin-dependent protein kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.17 2.7.11.17] </span></td></tr>
-	[[Category: Somoza, J.R]]	+	<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=5vlo FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5vlo OCA], [http://pdbe.org/5vlo PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5vlo RCSB], [http://www.ebi.ac.uk/pdbsum/5vlo PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5vlo ProSAT]</span></td></tr>
		+	</table>
		+	== Function ==
		+	[[http://www.uniprot.org/uniprot/KCC2D_HUMAN KCC2D_HUMAN]] Calcium/calmodulin-dependent protein kinase involved in the regulation of Ca(2+) homeostatis and excitation-contraction coupling (ECC) in heart by targeting ion channels, transporters and accessory proteins involved in Ca(2+) influx into the myocyte, Ca(2+) release from the sarcoplasmic reticulum (SR), SR Ca(2+) uptake and Na(+) and K(+) channel transport. Targets also transcription factors and signaling molecules to regulate heart function. In its activated form, is involved in the pathogenesis of dilated cardiomyopathy and heart failure. Contributes to cardiac decompensation and heart failure by regulating SR Ca(2+) release via direct phosphorylation of RYR2 Ca(2+) channel on 'Ser-2808'. In the nucleus, phosphorylates the MEF2 repressor HDAC4, promoting its nuclear export and binding to 14-3-3 protein, and expression of MEF2 and genes involved in the hypertrophic program. Is essential for left ventricular remodeling responses to myocardial infarction. In pathological myocardial remodeling acts downstream of the beta adrenergic receptor signaling cascade to regulate key proteins involved in ECC. Regulates Ca(2+) influx to myocytes by binding and phosphorylating the L-type Ca(2+) channel subunit beta-2 CACNB2. In addition to Ca(2+) channels, can target and regulate the cardiac sarcolemmal Na(+) channel Nav1.5/SCN5A and the K+ channel Kv4.3/KCND3, which contribute to arrhythmogenesis in heart failure. Phosphorylates phospholamban (PLN/PLB), an endogenous inhibitor of SERCA2A/ATP2A2, contributing to the enhancement of SR Ca(2+) uptake that may be important in frequency-dependent acceleration of relaxation (FDAR) and maintenance of contractile function during acidosis. May participate in the modulation of skeletal muscle function in response to exercise, by regulating SR Ca(2+) transport through phosphorylation of PLN/PLB and triadin, a ryanodine receptor-coupling factor.<ref>PMID:16690701</ref> <ref>PMID:17179159</ref>
		+	== References ==
		+	<references/>
		+	__TOC__
		+	</StructureSection>
		+	[[Category: Calcium/calmodulin-dependent protein kinase]]
		+	[[Category: Human]]
		+	[[Category: Somoza, J R]]
		+	[[Category: Villasenor, A G]]
		+	[[Category: Camkii]]
		+	[[Category: Inhibitor]]
		+	[[Category: Kinase]]
		+	[[Category: Transferase]]

OCA at 13:58, 17 May 2017

OCA — Wed, 17 May 2017 13:58:16 GMT

←Older revision		Revision as of 13:58, 17 May 2017
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

-	The entry 5vlo is ON HOLD	+	The entry 5vlo is ON HOLD until Oct 25 2018

	Authors: Somoza, J.R., Villasenor, A.G.		Authors: Somoza, J.R., Villasenor, A.G.

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

OCA — Thu, 04 May 2017 11:27:16 GMT

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

←Older revision

Revision as of 11:27, 4 May 2017

OCA: New page: '''Unreleased structure''' The entry 5vlo is ON HOLD Authors: Somoza, J.R., Villasenor, A.G. Description: The structure of human CamKII with bound inhibitor [[Category: Unreleased Stru...

OCA — Thu, 04 May 2017 11:27:15 GMT

New page: '''Unreleased structure''' The entry 5vlo is ON HOLD Authors: Somoza, J.R., Villasenor, A.G. Description: The structure of human CamKII with bound inhibitor [[Category: Unreleased Stru...

New page

'''Unreleased structure'''

The entry 5vlo is ON HOLD

Authors: Somoza, J.R., Villasenor, A.G.

Description: The structure of human CamKII with bound inhibitor
[[Category: Unreleased Structures]]
[[Category: Villasenor, A.G]]
[[Category: Somoza, J.R]]