[HTML][HTML] The histamine H3 receptor: from gene cloning to H3 receptor drugs

R Leurs, RA Bakker, H Timmerman… - Nature reviews Drug …, 2005 - nature.com
Since the cloning of the histamine H 3 receptor cDNA in 1999 by Lovenberg and co-workers,
this histamine receptor has gained the interest of many pharmaceutical companies as a …

Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 …

HD Lim, RM van Rijn, P Ling, RA Bakker… - … of Pharmacology and …, 2005 - ASPET
The histamine H 4 receptor (H 4 R) is involved in the chemotaxis of leukocytes and mast
cells to sites of inflammation and is suggested to be a potential drug target for asthma and …

Histamine H1-receptor activation of nuclear factor-κB: roles for Gβγ-and Gαq/11-subunits in constitutive and agonist-mediated signaling

RA Bakker, SBJ Schoonus, MJ Smit, H Timmerman… - Molecular …, 2001 - ASPET
Nuclear factor κB (NF-κB) is an important transcription factor in inflammation that has obtained
a great interest as a drug target for the treatment of various allergic conditions. In this study…

[HTML][HTML] Constitutive signaling of the human cytomegalovirus-encoded chemokine receptor US28

P Casarosa, RA Bakker, D Verzijl, M Navis… - Journal of Biological …, 2001 - ASBMB
Previously it was shown that the HHV-8-encoded chemokine receptor ORF74 shows
considerable agonist-independent, constitutive activity giving rise to oncogenic transformation (…

Constitutive activity of the histamine H1 receptor reveals inverse agonism of histamine H1 receptor antagonists

RA Bakker, K Wieland, H Timmerman… - European journal of …, 2000 - Elsevier
Transient expression of the wild-type human histamine H 1 receptor in SV40-immortalised
African green monkey kidney cells resulted in an agonist-independent elevation of the basal …

Pharmacogenomic and structural analysis of constitutive G protein–coupled receptor activity

MJ Smit, HF Vischer, RA Bakker… - Annu. Rev …, 2007 - annualreviews.org
G protein–coupled receptors (GPCRs) respond to a chemically diverse plethora of signal
transduction molecules. The notion that GPCRs also signal without an external chemical trigger…

Molecular aspects of the histamine H3 receptor

G Bongers, RA Bakker, R Leurs - Biochemical pharmacology, 2007 - Elsevier
The cloning of the histamine H 3 receptor (H 3 R) cDNA in 1999 by Lovenberg et al. [10]
allowed detailed studies of its molecular aspects and indicated that the H 3 R can activate …

Characterization of the Histamine H4 Receptor Binding Site. Part 1. Synthesis and Pharmacological Evaluation of Dibenzodiazepine Derivatives

RA Smits, HD Lim, B Stegink, RA Bakker… - Journal of medicinal …, 2006 - ACS Publications
A series of dibenzodiazepine derivatives was synthesized to probe the binding site of the
recently discovered histamine H 4 receptor (H 4 R). Optimization of the lead structure clozapine …

Synthesis and structure–activity relationships of indole and benzimidazole piperazines as histamine H4 receptor antagonists

N Terzioglu, RM van Rijn, RA Bakker… - Bioorganic & medicinal …, 2004 - Elsevier
We describe the structure–activity relationships for a series of ligands structurally related to
the recently identified (5-chloro-1H-indol-2-yl)-(4-methyl-piperazin-1-yl)-methanone (1) as …

Linking agonist binding to histamine H1 receptor activation

…, JA Ballesteros, E Haaksma, RA Bakker… - Nature chemical …, 2005 - nature.com
G protein–coupled receptors (GPCRs) constitute a large and functionally diverse family of
transmembrane proteins. They are fundamental in the transfer of extracellular stimuli to …