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- Rob Leurs, Paul Louis Chazot, Fiona C. Shenton, Herman D. Lim, Iwan J.P. de Esch
- British journal of pharmacology
- 2009
The elucidation of the human genome has had a major impact on histamine receptor research. The identification of the human H4 receptor by several groups has been instrumental for a new appreciation… (More)
- Herman D. Lim, Rogier A. Smits, Remko A. Bakker, Cindy M E van Dam, Iwan J.P. de Esch, Rob Leurs
- Journal of medicinal chemistry
- 2006
During an in-house database screen, we identified S-(2-guanidylethyl)-isothiourea as a high affinity agonist for the histamine H4 receptor, with a 33-fold selectivity over the histamine H3 receptor… (More)
- Radovan Spurny, Joachim Ramerstorfer, +13 authors Chris Ulens
- Proceedings of the National Academy of Sciences…
- 2012
GABA(A) receptors are pentameric ligand-gated ion channels involved in fast inhibitory neurotransmission and are allosterically modulated by the anxiolytic, anticonvulsant, and sedative-hypnotic… (More)
- Albert J. Kooistra, Sebastiaan Kuhne, Iwan J.P. de Esch, Rob Leurs, Chris de Graaf
- British journal of pharmacology
- 2013
BACKGROUND AND PURPOSE
Chemogenomics focuses on the discovery of new connections between chemical and biological space leading to the discovery of new protein targets and biologically active… (More)
- Iwan J.P. de Esch, Robin L. Thurmond, Aldo Jongejan, Rob Leurs
- Trends in pharmacological sciences
- 2005
Following the sequencing of the human genome, data-mining efforts have revealed the existence of a new histamine receptor that is expressed at high levels in mast cells and leukocytes. The histamine… (More)
- Oscar P J van Linden, Albert J. Kooistra, Rob Leurs, Iwan J.P. de Esch, Chris de Graaf
- Journal of medicinal chemistry
- 2014
Protein kinases regulate the majority of signal transduction pathways in cells and have become important targets for the development of designer drugs. We present a systematic analysis of… (More)
- Maikel Wijtmans, Rob Leurs, Iwan J.P. de Esch
- Expert opinion on investigational drugs
- 2007
The neurotransmitter histamine exerts its action through four distinct histamine receptors. The histamine H(1) and H(2) receptor are well established drug targets, whereas the histamine H(4) receptor… (More)
- Rob Leurs, Henry F. Vischer, Maikel Wijtmans, Iwan J.P. de Esch
- Trends in pharmacological sciences
- 2011
With the recognition of two new histamine receptors at the start of the new millennium, the field of histamine research has seen a clear revival. In the last 10 years, many academic and industrial… (More)
- Sylvain Célanire, Maikel Wijtmans, Patrice E Talaga, Rob Leurs, Iwan J.P. de Esch
- Drug discovery today
- 2005
Antagonists of the histamine H(1) and H(2) receptors have been successful as blockbuster drugs for treating allergic conditions and gastric ulcers, respectively. As such, histamine receptors have… (More)
- Dennis Verzijl, Stefania Storelli, +10 authors Rob Leurs
- The Journal of pharmacology and experimental…
- 2008
The chemokine receptor CXCR3 is involved in various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, psoriasis, and allograft rejection in transplantation patients. The CXCR3… (More)