[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 …
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 …
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…
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 (…
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 …
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…
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 …
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 …
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 …
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 …
transmembrane proteins. They are fundamental in the transfer of extracellular stimuli to …