| Autor: |
Enade P, Istyastono, Chris, de Graaf, Iwan J P, de Esch, Rob, Leurs |
| Rok vydání: |
2010 |
| Předmět: |
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| Zdroj: |
Current topics in medicinal chemistry. 11(6) |
| ISSN: |
1873-4294 |
| Popis: |
The deorphanization of the histamine H₄ receptor (H₄R) has led to a significant number of scientific publications and patent applications. Whereas some histamine H₁, H₂ and H₃ receptor ligands were found to have significant affinity for H₄R, several agonists and antagonists with high affinity for H₄R and selectivity over the other histamine receptors were successfully designed and synthesized. Moreover, site-directed mutation studies on H₄R have been performed and reveal detailed information on receptor-ligand interactions. This review will focus on the most important H₄R ligand scaffolds and their structure-activity relationships and selectivity over other histamine receptors and specific H₄R functional activity. Experimental data are used to construct and validate high resolution three-dimensional receptor-ligand models and, vice versa, in silico models are used to design and rationalize experimental studies to probe receptor-ligand interactions. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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