Literature DB >> 20128603

Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol.

John J G Tesmer1, Valerie M Tesmer, David T Lodowski, Henning Steinhagen, Jochen Huber.   

Abstract

G protein-coupled receptor kinase 2 (GRK2) is a pharmaceutical target for the treatment of cardiovascular diseases such as congestive heart failure, myocardial infarction, and hypertension. To better understand how nanomolar inhibition and selectivity for GRK2 might be achieved, we have determined crystal structures of human GRK2 in complex with Gbetagamma in the presence and absence of the AGC kinase inhibitor balanol. The selectivity of balanol among human GRKs is assessed.

Entities:  

Mesh：

Substances：

Year:  2010        PMID： 20128603      PMCID： PMC3073382          DOI： 10.1021/jm9017515

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  18 in total

1.  Keeping G proteins at bay: a complex between G protein-coupled receptor kinase 2 and Gbetagamma.

Authors:  David T Lodowski; Julie A Pitcher; W Darrell Capel; Robert J Lefkowitz; John J G Tesmer
Journal:  Science       Date:  2003-05-23       Impact factor: 47.728

Review 2.  Protein kinase inhibitors: insights into drug design from structure.

Authors:  Martin E M Noble; Jane A Endicott; Louise N Johnson
Journal:  Science       Date:  2004-03-19       Impact factor: 47.728

Review 3.  GRK mythology: G-protein receptor kinases in cardiovascular disease.

Authors:  Gerald W Dorn
Journal:  J Mol Med (Berl)       Date:  2009-02-20       Impact factor: 4.599

4.  Feedback inhibition of G protein-coupled receptor kinase 2 (GRK2) activity by extracellular signal-regulated kinases.

Authors:  J A Pitcher; J J Tesmer; J L Freeman; W D Capel; W C Stone; R J Lefkowitz
Journal:  J Biol Chem       Date:  1999-12-03       Impact factor: 5.157

5.  Crystal structure of an activated Akt/protein kinase B ternary complex with GSK3-peptide and AMP-PNP.

Authors:  Jing Yang; Peter Cron; Valerie M Good; Vivienne Thompson; Brian A Hemmings; David Barford
Journal:  Nat Struct Biol       Date:  2002-12

6.  Crystal structure of a transition state mimic of the catalytic subunit of cAMP-dependent protein kinase.

Authors:  Pearl Akamine; Nguyen-Huu Xuong; Susan S Taylor
Journal:  Nat Struct Biol       Date:  2002-04

7.  Purification, crystallization and preliminary X-ray diffraction studies of a complex between G protein-coupled receptor kinase 2 and Gbeta1gamma2.

Authors:  David T Lodowski; Jennifer F Barnhill; Julie A Pitcher; W Darrell Capel; Robert J Lefkowitz; John J G Tesmer
Journal:  Acta Crystallogr D Biol Crystallogr       Date:  2003-04-25

8.  Structure-based optimization of novel azepane derivatives as PKB inhibitors.

Authors:  Christine B Breitenlechner; Thomas Wegge; Laurent Berillon; Klaus Graul; Klaus Marzenell; Walter-Gunar Friebe; Ulrike Thomas; Ralf Schumacher; Robert Huber; Richard A Engh; Birgit Masjost
Journal:  J Med Chem       Date:  2004-03-11       Impact factor: 7.446

9.  Crystal structure of the catalytic subunit of cyclic adenosine monophosphate-dependent protein kinase.

Authors:  D R Knighton; J H Zheng; L F Ten Eyck; V A Ashford; N H Xuong; S S Taylor; J M Sowadski
Journal:  Science       Date:  1991-07-26       Impact factor: 47.728

10.  Balanol analogues probe specificity determinants and the conformational malleability of the cyclic 3',5'-adenosine monophosphate-dependent protein kinase catalytic subunit.

Authors:  Pearl Akamine; Laurence L Brunton; Horng D Ou; Jaume M Canaves; Nguyen-huu Xuong; Susan S Taylor
Journal:  Biochemistry       Date:  2004-01-13       Impact factor: 3.162
View more
  25 in total

1.  Molecular mechanism for inhibition of g protein-coupled receptor kinase 2 by a selective RNA aptamer.

Authors:  Valerie M Tesmer; Sabine Lennarz; Günter Mayer; John J G Tesmer
Journal:  Structure       Date:  2012-06-21       Impact factor: 5.006

Review 2.  Structural insights into G protein-coupled receptor kinase function.

Authors:  Kristoff T Homan; John J G Tesmer
Journal:  Curr Opin Cell Biol       Date:  2013-11-26       Impact factor: 8.382

3.  Comparative genomics uncovers novel structural and functional features of the heterotrimeric GTPase signaling system.

Authors:  Vivek Anantharaman; Saraswathi Abhiman; Robson F de Souza; L Aravind
Journal:  Gene       Date:  2010-12-20       Impact factor: 3.688

Review 4.  Understanding molecular recognition by G protein βγ subunits on the path to pharmacological targeting.

Authors:  Yuan Lin; Alan V Smrcka
Journal:  Mol Pharmacol       Date:  2011-07-07       Impact factor: 4.436

Review 5.  G protein-coupled receptor kinases: more than just kinases and not only for GPCRs.

Authors:  Eugenia V Gurevich; John J G Tesmer; Arcady Mushegian; Vsevolod V Gurevich
Journal:  Pharmacol Ther       Date:  2011-08-26       Impact factor: 12.310

6.  Molecular mechanism of selectivity among G protein-coupled receptor kinase 2 inhibitors.

Authors:  David M Thal; Raymond Y Yeow; Christian Schoenau; Jochen Huber; John J G Tesmer
Journal:  Mol Pharmacol       Date:  2011-05-19       Impact factor: 4.436

7.  Evidence for α-helices in the large intracellular domain mediating modulation of the α1-glycine receptor by ethanol and Gβγ.

Authors:  Carlos F Burgos; Patricio A Castro; Trinidad Mariqueo; Marta Bunster; Leonardo Guzmán; Luis G Aguayo
Journal:  J Pharmacol Exp Ther       Date:  2014-10-22       Impact factor: 4.030

8.  Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.

Authors:  Kristoff T Homan; Helen V Waldschmidt; Alisa Glukhova; Alessandro Cannavo; Jianliang Song; Joseph Y Cheung; Walter J Koch; Scott D Larsen; John J G Tesmer
Journal:  J Biol Chem       Date:  2015-06-01       Impact factor: 5.157

9.  Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4.

Authors:  Samantha J Allen; Gopal Parthasarathy; Paul L Darke; Ronald E Diehl; Rachael E Ford; Dawn L Hall; Scott A Johnson; John C Reid; Keith W Rickert; Jennifer M Shipman; Stephen M Soisson; Paul Zuck; Sanjeev K Munshi; Kevin J Lumb
Journal:  J Biol Chem       Date:  2015-07-01       Impact factor: 5.157

10.  The interplay between G protein-coupled receptor kinase 2 (GRK2) and histone deacetylase 6 (HDAC6) at the crossroads of epithelial cell motility.

Authors:  Vanesa Lafarga; Federico Mayor; Petronila Penela
Journal:  Cell Adh Migr       Date:  2012-10-17       Impact factor: 3.405
View more

北京卡尤迪生物科技股份有限公司 © 2022-2023.