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

Journal of Medicinal Chemistry
John J G TesmerJochen 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.

References

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Citations

Oct 1, 2013·European Journal of Medicinal Chemistry·Alfonso CarotenutoPietro Campiglia
Mar 19, 2011·Journal of Medicinal Chemistry·Nicholas A Meanwell
May 21, 2011·Molecular Pharmacology·David M ThalJohn J G Tesmer
Oct 8, 2011·Cell Communication and Signaling : CCS·David R AdamsPatrick A Kiely
Oct 24, 2014·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Kristoff T HomanJohn J G Tesmer
Sep 10, 2011·Pharmacology & Therapeutics·Eugenia V GurevichVsevolod V Gurevich
Jan 25, 2011·Pharmacology & Therapeutics·Richard Eglen, Terry Reisine
Jul 2, 2014·ACS Chemical Biology·Kristoff T Homan, John J G Tesmer
Apr 1, 2014·Current Opinion in Cell Biology·Kristoff T Homan, John J G Tesmer
Sep 11, 2013·Biochimica Et Biophysica Acta·Irina S Moreira
Jul 1, 2016·Journal of Medicinal Chemistry·Manuela GuccioneSilvana Grasso
Nov 24, 2017·Expert Opinion on Therapeutic Targets·Alessandro CannavoGiuseppe Rengo
Jan 11, 2012·Natural Product Reports·Jing LiuQingsong Liu
Feb 7, 2019·Molecular Pharmacology·Nathaniel A Jeske
Oct 24, 2014·The Journal of Pharmacology and Experimental Therapeutics·Carlos F BurgosLuis G Aguayo
Jun 3, 2015·The Journal of Biological Chemistry·Kristoff T HomanJohn J G Tesmer
Jul 3, 2015·The Journal of Biological Chemistry·Samantha J AllenKevin J Lumb
Dec 13, 2018·Frontiers in Pharmacology·Supachoke MangmoolHitoshi Kurose
Nov 18, 2020·Biomolecules·Andrea Baier, Ryszard Szyszka

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