Recent developments in constitutive receptor activity and inverse agonism, and their potential for GPCR drug discovery

RA Bond, AP IJzerman - Trends in pharmacological sciences, 2006 - cell.com
The concept of constitutively active G-protein-coupled receptors is now firmly rooted in
receptor pharmacology. Many independent research groups have contributed to its …

[HTML][HTML] Experimental design and analysis and their reporting: new guidance for publication in BJP

MJ Curtis, RA Bond, D Spina, A Ahluwalia… - British journal of …, 2015 - ncbi.nlm.nih.gov
This editorial is part of a series describing changes in the guidelines for authors making
submissions to the British Journal of Pharmacology (BJP)(McGrath and Curtis, 2015); …

Cardiac function in mice overexpressing the β-adrenergic receptor kinase or a βARK inhibitor

WJ Koch, HA Rockman, P Samama, RA Hamilton… - Science, 1995 - science.org
Transgenic mice were created with cardiac-specific overexpression of the β-adrenergic
receptor kinase-1 (βARK1) or a βARK inhibitor. Animals overexpressing βARK1 …

Enhanced Myocardial Function in Transgenic Mice Overexpressing the β2-Adrenergic Receptor

CA Milano, LF Allen, HA Rockman, PC Dolber… - Science, 1994 - science.org
Transgenic mice were created with cardiac-specific overexpression of the β2-adrenergic
receptor. This resulted in increased basal myocardial adenylyl cyclase activity, enhanced …

New perspectives regarding β2‐adrenoceptor ligands in the treatment of asthma

JKL Walker, RB Penn, NA Hanania… - British journal of …, 2011 - Wiley Online Library
In the last two decades several significant changes have been proposed in the receptor
theory that describes how ligands can interact with G protein‐coupled receptors (GPCRs) …

Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor

RA Bond, P Leff, TD Johnson, CA Milano, HA Rockman… - Nature, 1995 - nature.com
Abstract G-PROTEIN-COUPLED receptors are thought to have an inactive conformation (R),
requiring an agonist-induced conformational change for receptor/G-protein coupling1–3. But …

Inverse agonism and the regulation of receptor number

G Milligan, RA Bond - Trends in pharmacological sciences, 1997 - cell.com
Inverse agonists are ligands that preferentially stabilize inactive conformations of G protein-
coupled receptors. In a range of systems, sustained treatment with inverse agonists can …

Myocardial expression of a constitutively active alpha 1B-adrenergic receptor in transgenic mice induces cardiac hypertrophy.

CA Milano, PC Dolber, HA Rockman… - Proceedings of the …, 1994 - National Acad Sciences
Transgenic mice were generated by using the alpha-myosin heavy chain promoter coupled
to the coding sequence of a constitutively active mutant alpha 1B-adrenergic receptor (AR) …

Essential role of β-adrenergic receptor kinase 1 in cardiac development and function

M Jaber, WJ Koch, H Rockman… - Proceedings of the …, 1996 - National Acad Sciences
The β-adrenergic receptor kinase 1 (βARK1) is a member of the G protein-coupled receptor
kinase (GRK) family that mediates the agonist-dependent phosphorylation and …

[PDF][PDF] Nebivolol induces endothelium-dependent relaxations of canine coronary arteries

YS Gao, T Nagao, RA Bond, WJ Janssens… - J Cardiovasc …, 1991 - academia.edu
Nebivolol is a new ß,-antagonist that acutely reduces arterial blood pressure without
depressing cardiac function. The present study was designed to determine the effect of …