Differential Role of Serines and Threonines in Intracellular Loop 3 and C-Terminal Tail of the Histamine H4 Receptor in β-Arrestin and G Protein-Coupled Receptor …

EWE Verweij, B Al Araaj, WR Prabhata… - ACS pharmacology & …, 2020 - ACS Publications
The histamine H4 receptor (H4R) activates Gαi-mediated signaling and recruits β-arrestin2
upon stimulation with histamine. β-Arrestins play a regulatory role in G protein-coupled …

Roles of phosphorylation-dependent and-independent mechanisms in the regulation of histamine H2 receptor by G protein-coupled receptor kinase 2

N Fernandez, FL Gottardo, MN Alonso… - Journal of Biological …, 2011 - ASBMB
It is widely assumed that G protein-coupled receptor kinase 2 (GRK2)-mediated specific
inhibition of G protein-coupled receptors (GPCRs) response involves GRK-mediated …

Bimodal regulation of the human H1 histamine receptor by G protein-coupled receptor kinase 2

K Iwata, J Luo, RB Penn, JL Benovic - Journal of Biological Chemistry, 2005 - ASBMB
The H1 histamine receptor (H1HR) is a member of the G protein-coupled receptor
superfamily and regulates numerous cellular functions through its activation of the G q/11 …

Modulation of histamine H2 receptor signalling by G‐protein‐coupled receptor kinase 2 and 3

MS Rodriguez‐Pena, H Timmerman… - British journal of …, 2000 - Wiley Online Library
To evaluate the role of G‐protein‐coupled receptor kinases (GRK) in the desensitization of
the histamine H2 receptor, the H2 receptor was transiently cotransfected with GRK2, 3, 5 or …

Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins

EM Rosethorne, SJ Charlton - Molecular pharmacology, 2011 - ASPET
The Gi/o-coupled histamine H4 receptor is highly expressed in hemopoietic cells and is a
promising new target for the treatment of chronic inflammatory diseases. 1-[(5-Chloro-1 H …

[HTML][HTML] Ligand-directed biased agonism at human histamine H3 receptor isoforms across Gαi/o-and β-arrestin2-mediated pathways

SN Rahman, F Imhaouran, R Leurs… - Biochemical …, 2023 - Elsevier
The histamine H 3 receptor (H 3 R) is a neurotransmitter receptor that is primarily found in
the brain, where it controls the release and synthesis of histamine, as well as the release of …

Histamine H2 receptor desensitization: involvement of a select array of G protein-coupled receptor kinases

C Shayo, N Fernandez, BL Legnazzi, F Monczor… - Molecular …, 2001 - ASPET
The histamine H2 receptor (H2r) belongs to the heptahelical receptor family; upon agonist
binding, members of this family activate a G protein and the downstream effector adenylyl …

Isoform-specific biased agonism of histamine H3 receptor agonists

DM Riddy, AE Cook, NA Diepenhorst, S Bosnyak… - Molecular …, 2017 - ASPET
The human histamine H3 receptor (hH3R) is subject to extensive gene splicing that gives
rise to a large number of functional and nonfunctional isoforms. Despite the general …

Differential regulation of histamine H1 receptor-mediated ERK phosphorylation by Gq proteins and arrestins

S Michinaga, A Nagata, R Ogami, Y Ogawa… - Biochemical …, 2023 - Elsevier
G q protein-coupled histamine H 1 receptors play crucial roles in allergic and inflammatory
reactions, in which the phosphorylation of extracellular signal-regulated kinase (ERK) …

Analysis of multiple histamine H4 receptor compound classes uncovers Gαi protein-and β-arrestin2-biased ligands

S Nijmeijer, HF Vischer, EM Rosethorne… - Molecular …, 2012 - ASPET
After the recent description of β-arrestin2 recruitment to the human histamine H4 receptor
(hH4R) in response to the well known H4R antagonist 1-[(5-chloro-1 H-indol-2-yl) carbonyl] …