4mk0

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
m (Protected "4mk0" [edit=sysop:move=sysop])
Line 1: Line 1:
-
'''Unreleased structure'''
+
{{STRUCTURE_4mk0| PDB=4mk0 | SCENE= }}
 +
===Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative===
 +
{{ABSTRACT_PUBMED_24220010}}
-
The entry 4mk0 is ON HOLD
+
==Function==
 +
[[http://www.uniprot.org/uniprot/ARBK1_HUMAN ARBK1_HUMAN]] 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.<ref>PMID:19306925</ref> [[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.
-
Authors: Homan, K.T., Tesmer, J.J.G.
+
==About this Structure==
 +
[[4mk0]] is a 3 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MK0 OCA].
-
Description: Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative
+
==Reference==
 +
<ref group="xtra">PMID:024220010</ref><references group="xtra"/><references/>
 +
[[Category: Homan, K T.]]
 +
[[Category: Tesmer, J J.G.]]
 +
[[Category: Atp binding]]
 +
[[Category: Hydrolase]]
 +
[[Category: Inhibitor complex]]
 +
[[Category: Peripheral membrane protein]]
 +
[[Category: Phosphorylation]]
 +
[[Category: Protein kinase]]
 +
[[Category: Signaling protein-inhibitor complex]]

Revision as of 06:57, 22 January 2014

Template:STRUCTURE 4mk0

Contents

Crystal structure of G protein-coupled receptor kinase 2 in complex with a a rationally designed paroxetine derivative

Template:ABSTRACT PUBMED 24220010

Function

[ARBK1_HUMAN] 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.[1] [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. [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.

About this Structure

4mk0 is a 3 chain structure. Full crystallographic information is available from OCA.

Reference

  • Homan KT, Wu E, Wilson MW, Singh P, Larsen SD, Tesmer JJ. Structural and functional analysis of g protein-coupled receptor kinase inhibition by paroxetine and a rationally designed analog. Mol Pharmacol. 2014 Feb;85(2):237-48. doi: 10.1124/mol.113.089631. Epub 2013 Nov , 12. PMID:24220010 doi:http://dx.doi.org/10.1124/mol.113.089631
  1. ↑ Aziziyeh AI, Li TT, Pape C, Pampillo M, Chidiac P, Possmayer F, Babwah AV, Bhattacharya M. Dual regulation of lysophosphatidic acid (LPA1) receptor signalling by Ral and GRK. Cell Signal. 2009 Jul;21(7):1207-17. doi: 10.1016/j.cellsig.2009.03.011. Epub, 2009 Mar 21. PMID:19306925 doi:10.1016/j.cellsig.2009.03.011

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/4mk0"
Personal tools