3psc - Revision history

OCA at 10:00, 6 September 2023

2023-09-06T10:00:55Z

← Older revision		Revision as of 10:00, 6 September 2023
Line 3:		Line 3:
	<StructureSection load='3psc' size='340' side='right'caption='[[3psc]], [[Resolution\|resolution]] 2.67Å' scene=''>		<StructureSection load='3psc' size='340' side='right'caption='[[3psc]], [[Resolution\|resolution]] 2.67Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3psc]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/~~Bovin Bovin~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PSC FirstGlance]. <br>		<table><tr><td colspan='2'>[[3psc]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PSC FirstGlance]. <br>
	</td></tr><tr id='~~NonStdRes~~'><td class="sblockLbl"><b>[[~~Non-Standard_Residue~~\|~~NonStd Res~~:]]</b></td><td class="sblockDat"~~><scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</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]] 2.67Å</td></tr>
	~~<tr~~ id~~='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class~~="~~sblockDat~~">~~<div style='overflow: auto; max~~-~~height: 3em;'>[[1omw\|1omw]]~~, [[~~3pvu~~\|~~3pvu]], [[3pvw\|3pvw]], [[3krw\|3krw]], [[3krx\|3krx]], [[3cik\|3cik~~]]~~</div>~~</td></tr>		<tr id='ligand'><td class="sblockLbl"><b>[[Ligand\|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</scene></td></tr>
	<tr id='~~gene~~'><td class="sblockLbl"><b>[[~~Gene~~\|~~Gene~~:]]</b></td><td class="sblockDat"~~>ADRBK1, GRK2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&~~id=9913 BOVIN]), GNB1 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 BOVIN]), GNG2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 BOVIN])</td><~~/tr>~~
	~~<tr id~~='~~activity'><td class~~=~~"sblockLbl"><b>Activity~~:~~</b></td><td class="sblockDat"><span class='plainlinks~~'>~~[https://en.wikipedia.org/wiki/[Beta-adrenergic-receptor]_kinase [Beta-adrenergic-receptor] kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.15 2.7.11.15]~~ </~~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=3psc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3psc OCA], [https://pdbe.org/3psc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3psc RCSB], [https://www.ebi.ac.uk/pdbsum/3psc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3psc 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=3psc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3psc OCA], [https://pdbe.org/3psc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3psc RCSB], [https://www.ebi.ac.uk/pdbsum/3psc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3psc ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[https://www.uniprot.org/uniprot/ARBK1_BOVIN ARBK1_BOVIN]] Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner (By similarity). [[https://www.uniprot.org/uniprot/GBG2_BOVIN GBG2_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. [[https://www.uniprot.org/uniprot/GBB1_BOVIN GBB1_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.		[https://www.uniprot.org/uniprot/ARBK1_BOVIN ARBK1_BOVIN] Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner (By similarity).
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 29:		Line 27:
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Bovin~~]]		[[Category: Bos taurus]]
	[[Category: Large Structures]]		[[Category: Large Structures]]
	[[Category: Tesmer~~, J J~~]]		[[Category: Tesmer JJ]]
	[[Category: Thal~~, D M]]~~		[[Category: Thal DM]]
	~~[[Category: Atp-binding]]~~
	~~[[Category: Kinase]]~~
	~~[[Category: Membrane]]~~
	~~[[Category: Serine/threonine-protein kinase]]~~
	~~[[Category: Transferase-signaling protein complex~~]]

OCA at 08:53, 25 May 2022

2022-05-25T08:53:01Z

← Older revision		Revision as of 08:53, 25 May 2022
Line 1:		Line 1:

	==Bovine GRK2 in complex with Gbetagamma subunits==		==Bovine GRK2 in complex with Gbetagamma subunits==
	<StructureSection load='3psc' size='340' side='right' caption='[[3psc]], [[Resolution\|resolution]] 2.67Å' scene=''>		<StructureSection load='3psc' size='340' side='right'caption='[[3psc]], [[Resolution\|resolution]] 2.67Å' scene=''>
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3psc]] is a 3 chain structure with sequence from [~~http~~://en.wikipedia.org/wiki/~~Bos_taurus Bos taurus~~]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA]. For a <b>guided tour on the structure components</b> use [~~http~~://~~oca~~.~~weizmann.ac.il/oca-docs~~/fgij/fg.htm?mol=3PSC FirstGlance]. <br>		<table><tr><td colspan='2'>[[3psc]] is a 3 chain structure with sequence from [https://en.wikipedia.org/wiki/Bovin Bovin]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3PSC FirstGlance]. <br>
	</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</scene></td></tr>		</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</scene></td></tr>
	<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1omw\|1omw]], [[3pvu\|3pvu]], [[3pvw\|3pvw]], [[3krw\|3krw]], [[3krx\|3krx]], [[3cik\|3cik]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat"><div style='overflow: auto; max-height: 3em;'>[[1omw\|1omw]], [[3pvu\|3pvu]], [[3pvw\|3pvw]], [[3krw\|3krw]], [[3krx\|3krx]], [[3cik\|3cik]]</div></td></tr>
	<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ADRBK1, GRK2 ([~~http~~://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 ~~Bos taurus~~]), GNB1 ([~~http~~://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 ~~Bos taurus~~]), GNG2 ([~~http~~://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 ~~Bos taurus~~])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ADRBK1, GRK2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 BOVIN]), GNB1 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 BOVIN]), GNG2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 BOVIN])</td></tr>
	<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[~~http~~://en.wikipedia.org/wiki/[Beta-adrenergic-receptor]_kinase [Beta-adrenergic-receptor] kinase], with EC number [~~http~~://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.15 2.7.11.15] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/[Beta-adrenergic-receptor]_kinase [Beta-adrenergic-receptor] kinase], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.15 2.7.11.15] </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=3psc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3psc OCA], [~~http~~://www.rcsb.org/pdb/explore.do?structureId=3psc RCSB], [~~http~~://www.ebi.ac.uk/pdbsum/3psc PDBsum]</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=3psc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3psc OCA], [https://pdbe.org/3psc PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3psc RCSB], [https://www.ebi.ac.uk/pdbsum/3psc PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3psc ProSAT]</span></td></tr>
	</table>		</table>
	== Function ==		== Function ==
	[[~~http~~://www.uniprot.org/uniprot/ARBK1_BOVIN ARBK1_BOVIN]] Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner (By similarity). [[~~http~~://www.uniprot.org/uniprot/GBG2_BOVIN GBG2_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. [[~~http~~://www.uniprot.org/uniprot/GBB1_BOVIN GBB1_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.		[[https://www.uniprot.org/uniprot/ARBK1_BOVIN ARBK1_BOVIN]] Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner (By similarity). [[https://www.uniprot.org/uniprot/GBG2_BOVIN GBG2_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. [[https://www.uniprot.org/uniprot/GBB1_BOVIN GBB1_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 19:		Line 20:
	From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>
			<div class="pdbe-citations 3psc" style="background-color:#fffaf0;"></div>

	==See Also==		==See Also==
	*[[~~Guanine nucleotide-binding protein~~\|~~Guanine nucleotide-binding protein~~]]		*[[Beta adrenergic receptor kinase 3D structures\|Beta adrenergic receptor kinase 3D structures]]
	*[[Transducin\|Transducin]]		*[[Transducin 3D structures\|Transducin 3D structures]]
	== References ==		== References ==
	<references/>		<references/>
	__TOC__		__TOC__
	</StructureSection>		</StructureSection>
	[[Category: ~~Bos taurus~~]]		[[Category: Bovin]]
			[[Category: Large Structures]]
	[[Category: Tesmer, J J]]		[[Category: Tesmer, J J]]
	[[Category: Thal, D M]]		[[Category: Thal, D M]]

OCA at 18:15, 25 December 2014

2014-12-25T18:15:16Z

← Older revision		Revision as of 18:15, 25 December 2014
Line 3:		Line 3:
	== Structural highlights ==		== Structural highlights ==
	<table><tr><td colspan='2'>[[3psc]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PSC FirstGlance]. <br>		<table><tr><td colspan='2'>[[3psc]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PSC FirstGlance]. <br>
	</td></tr><tr><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</scene></td></tr>		</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</scene></td></tr>
	<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1omw\|1omw]], [[3pvu\|3pvu]], [[3pvw\|3pvw]], [[3krw\|3krw]], [[3krx\|3krx]], [[3cik\|3cik]]</td></tr>		<tr id='related'><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1omw\|1omw]], [[3pvu\|3pvu]], [[3pvw\|3pvw]], [[3krw\|3krw]], [[3krx\|3krx]], [[3cik\|3cik]]</td></tr>
	<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ADRBK1, GRK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus]), GNB1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus]), GNG2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus])</td></tr>		<tr id='gene'><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ADRBK1, GRK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus]), GNB1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus]), GNG2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus])</td></tr>
	<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/[Beta-adrenergic-receptor]_kinase [Beta-adrenergic-receptor] kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.15 2.7.11.15] </span></td></tr>		<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/[Beta-adrenergic-receptor]_kinase [Beta-adrenergic-receptor] kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.15 2.7.11.15] </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=3psc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3psc OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3psc RCSB], [http://www.ebi.ac.uk/pdbsum/3psc 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=3psc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3psc OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3psc RCSB], [http://www.ebi.ac.uk/pdbsum/3psc PDBsum]</span></td></tr>
	<table>		</table>
			== Function ==
			[[http://www.uniprot.org/uniprot/ARBK1_BOVIN ARBK1_BOVIN]] Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors, probably inducing a desensitization of them. Key regulator of LPAR1 signaling. Competes with RALA for binding to LPAR1 thus affecting the signaling properties of the receptor. Desensitizes LPAR1 and LPAR2 in a phosphorylation-independent manner (By similarity). [[http://www.uniprot.org/uniprot/GBG2_BOVIN GBG2_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction. [[http://www.uniprot.org/uniprot/GBB1_BOVIN GBB1_BOVIN]] Guanine nucleotide-binding proteins (G proteins) are involved as a modulator or transducer in various transmembrane signaling systems. The beta and gamma chains are required for the GTPase activity, for replacement of GDP by GTP, and for G protein-effector interaction.
	<div style="background-color:#fffaf0;">		<div style="background-color:#fffaf0;">
	== Publication Abstract from PubMed ==		== Publication Abstract from PubMed ==
Line 15:		Line 17:
	Molecular Mechanism of Selectivity Among G Protein-Coupled Receptor Kinase 2 Inhibitors.,Thal DM, Yeow RY, Schoenau C, Huber J, Tesmer JJ Mol Pharmacol. 2011 May 19. PMID:21596927<ref>PMID:21596927</ref>		Molecular Mechanism of Selectivity Among G Protein-Coupled Receptor Kinase 2 Inhibitors.,Thal DM, Yeow RY, Schoenau C, Huber J, Tesmer JJ Mol Pharmacol. 2011 May 19. PMID:21596927<ref>PMID:21596927</ref>

	From ~~MEDLINEÂ®~~/~~PubMedÂ®~~, a database of the U.S. National Library of Medicine.<br>		From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
	</div>		</div>

	==See Also==		==See Also==
	*[[Guanine nucleotide-binding protein\|Guanine nucleotide-binding protein]]		*[[Guanine nucleotide-binding protein\|Guanine nucleotide-binding protein]]
			*[[Transducin\|Transducin]]
	== References ==		== References ==
	<references/>		<references/>
Line 25:		Line 28:
	</StructureSection>		</StructureSection>
	[[Category: Bos taurus]]		[[Category: Bos taurus]]
	[[Category: Tesmer, J J.]]		[[Category: Tesmer, J J]]
	[[Category: Thal, D M.]]		[[Category: Thal, D M]]
	[[Category: Atp-binding]]		[[Category: Atp-binding]]
	[[Category: Kinase]]		[[Category: Kinase]]

OCA at 05:32, 4 June 2014

2014-06-04T05:32:24Z

← Older revision		Revision as of 05:32, 4 June 2014
Line 1:		Line 1:
	[[~~Image~~:~~3psc~~.~~png~~\|~~left~~\|~~200px~~]]		==Bovine GRK2 in complex with Gbetagamma subunits==
			<StructureSection load='3psc' size='340' side='right' caption='[[3psc]], [[Resolution\|resolution]] 2.67Å' scene=''>
			== Structural highlights ==
			<table><tr><td colspan='2'>[[3psc]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3PSC FirstGlance]. <br>
			</td></tr><tr><td class="sblockLbl"><b>[[Non-Standard_Residue\|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=CMT:O-METHYLCYSTEINE'>CMT</scene></td></tr>
			<tr><td class="sblockLbl"><b>[[Related_structure\|Related:]]</b></td><td class="sblockDat">[[1omw\|1omw]], [[3pvu\|3pvu]], [[3pvw\|3pvw]], [[3krw\|3krw]], [[3krx\|3krx]], [[3cik\|3cik]]</td></tr>
			<tr><td class="sblockLbl"><b>[[Gene\|Gene:]]</b></td><td class="sblockDat">ADRBK1, GRK2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus]), GNB1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus]), GNG2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9913 Bos taurus])</td></tr>
			<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/[Beta-adrenergic-receptor]_kinase [Beta-adrenergic-receptor] kinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.11.15 2.7.11.15] </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=3psc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3psc OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3psc RCSB], [http://www.ebi.ac.uk/pdbsum/3psc PDBsum]</span></td></tr>
			<table>
			<div style="background-color:#fffaf0;">
			== Publication Abstract from PubMed ==
			G protein-coupled receptors (GPCRs) are key regulators of cell physiology and control processes ranging from glucose homeostasis to contractility of the heart. A major mechanism for the desensitization of activated GPCRs is their phosphorylation by GPCR kinases (GRKs). Overexpression of GRK2 is strongly linked to heart failure, and GRK2 has long been considered a pharmaceutical target for the treatment of cardiovascular disease. Several lead compounds developed by Takeda Pharmaceuticals show high selectivity for GRK2 and therapeutic potential for the treatment of heart failure. To understand how these drugs achieve their selectivity, we determined crystal structures of the bovine GRK2-Gbetagamma complex in the presence of two of these inhibitors. Comparison with the apoGRK2-Gbetagamma structure demonstrates that the compounds bind in the kinase active site in a manner similar to the AGC kinase inhibitor balanol. Both balanol and the Takeda compounds induce a slight closure of the kinase domain, the degree of which correlates with the potencies of the inhibitors. Based on our crystal structures and homology modeling, we indentified five amino acids surrounding the inhibitor-binding site that we hypothesized could contribute to inhibitor selectivity. However, our results indicate that these residues are not major determinants of selectivity among GRK subfamilies. Rather, selectivity is achieved by the stabilization of a unique inactive conformation of the GRK2 kinase domain.

	<!--		Molecular Mechanism of Selectivity Among G Protein-Coupled Receptor Kinase 2 Inhibitors.,Thal DM, Yeow RY, Schoenau C, Huber J, Tesmer JJ Mol Pharmacol. 2011 May 19. PMID:21596927<ref>PMID:21596927</ref>
	~~The line below this paragraph~~, ~~containing "STRUCTURE_3psc"~~, ~~creates the "Structure Box" on the page~~.
	~~You may change the PDB parameter (which sets the PDB file loaded into the applet)~~
	~~or the SCENE parameter (which sets the initial scene displayed when the page is loaded),~~
	~~or leave the SCENE parameter empty for the default display~~.
	-->
	~~{{STRUCTURE_3psc\| PDB=3psc \| SCENE= }}~~

	~~===Bovine GRK2 in complex with Gbetagamma subunits===~~		From MEDLINEÂ®/PubMedÂ®, a database of the U.S. National Library of Medicine.<br>
			</div>

			==See Also==
	~~<!--~~		*[[Guanine nucleotide-binding protein\|Guanine nucleotide-binding protein]]
	~~The line below this paragraph, {{ABSTRACT_PUBMED_21596927}}, adds the Publication Abstract to the page~~		== References ==
	~~(as it appears on PubMed at http://www.pubmed.gov), where 21596927 is the PubMed ID number.~~		<references/>
	~~-->~~		__TOC__
	~~{{ABSTRACT_PUBMED_21596927}}~~		</StructureSection>

	==~~About this Structure~~==
	[[~~3psc]] is a 3 chain structure with sequence from [http://en.wikipedia.org/wiki/Bos_taurus Bos taurus~~]~~. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3PSC OCA~~].

	==~~Reference~~==
	<~~ref group="xtra">PMID:021596927<~~/~~ref~~><~~references group="xtra"~~/>
	[[Category: Bos taurus]]		[[Category: Bos taurus]]
	[[Category: Tesmer, J J.]]		[[Category: Tesmer, J J.]]

OCA at 05:17, 27 July 2011

2011-07-27T05:17:44Z

← Older revision		Revision as of 05:17, 27 July 2011
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	[[Image:3psc.~~jpg~~\|left\|200px]]		[[Image:3psc.png\|left\|200px]]

	<!--		<!--
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	[[Category: Tesmer, J J.]]		[[Category: Tesmer, J J.]]
	[[Category: Thal, D M.]]		[[Category: Thal, D M.]]
			[[Category: Atp-binding]]
			[[Category: Kinase]]
			[[Category: Membrane]]
			[[Category: Serine/threonine-protein kinase]]
			[[Category: Transferase-signaling protein complex]]

OCA at 05:45, 1 June 2011

2011-06-01T05:45:30Z

@@ Line 1: / Line 1: @@
-'''Unreleased structure'''
+[[Image:3psc.jpg|left|200px]]
-The entry 3psc is ON HOLD  until Paper Publication
+<!--
-Authors: Thal, D.M., Tesmer, J.J.
+===Bovine GRK2 in complex with Gbetagamma subunits===
-Description: Bovine GRK2 in complex with Gbetagamma subunits

OCA: Protected "3psc" [edit=sysop:move=sysop]

2011-02-09T05:46:22Z

Protected "3psc" [edit=sysop:move=sysop]

← Older revision	Revision as of 05:46, 9 February 2011
(No difference)

OCA at 05:46, 9 February 2011

2011-02-09T05:46:21Z

← Older revision		Revision as of 05:46, 9 February 2011
Line 1:		Line 1:
	'''Unreleased structure'''		'''Unreleased structure'''

	The entry 3psc is ON HOLD		The entry 3psc is ON HOLD until Paper Publication

	Authors: Thal, D.M., Tesmer, J.J.		Authors: Thal, D.M., Tesmer, J.J.

	Description: Bovine GRK2 in complex with Gbetagamma subunits		Description: Bovine GRK2 in complex with Gbetagamma subunits

	~~''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Dec 8 11:33:34 2010''~~

OCA: New page: '''Unreleased structure''' The entry 3psc is ON HOLD Authors: Thal, D.M., Tesmer, J.J. Description: Bovine GRK2 in complex with Gbetagamma subunits ''Page seeded by [http://oca.weizma...

2010-12-08T08:21:30Z

New page: '''Unreleased structure''' The entry 3psc is ON HOLD Authors: Thal, D.M., Tesmer, J.J. Description: Bovine GRK2 in complex with Gbetagamma subunits ''Page seeded by [http://oca.weizma...

New page

'''Unreleased structure'''

The entry 3psc is ON HOLD

Authors: Thal, D.M., Tesmer, J.J.

Description: Bovine GRK2 in complex with Gbetagamma subunits

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Dec 8 11:33:34 2010''