Seifert, Roland and Strasser, Andrea and Schneider, Erich H. and Neumann, Detlef and Dove, Stefan and Buschauer, Armin (2013) Molecular and cellular analysis of human histamine receptor subtypes. TRENDS IN PHARMACOLOGICAL SCIENCES, 34 (1). pp. 33-58. ISSN 0165-6147, 1873-3735
Full text not available from this repository. (Request a copy)Abstract
The human histamine receptors hH(1)R and hH(2)R constitute important drug targets, and hH(3)R and hH(4)R have substantial potential in this area. Considering the species-specificity of pharmacology of HxR orthologs, it is important to analyze hH(x)Rs. Here, we summarize current knowledge of hH(x)Rs endogenously expressed in human cells and hH(x)Rs recombinantly expressed in mammalian and insect cells. We present the advantages and disadvantages of the various systems. We also discuss problems associated with the use of hH(x)R antibodies, an issue of general relevance for G-protein-coupled receptors (GPCRs). There is much greater overlap in activity of 'selective' ligands for other hH(x)Rs than the cognate receptor subtype than generally appreciated. Studies with native and recombinant systems support the concept of ligand-specific receptor conformations, encompassing agonists and antagonists. It is emerging that for characterization of hH(x)R ligands, one cannot rely on a single test system and a single parameter. Rather, multiple systems and parameters have to be studied. Although such studies are time-consuming and expensive, ultimately, they will increase drug safety and efficacy.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | G-ACYLATED IMIDAZOLYLPROPYLGUANIDINES; COMMERCIALLY AVAILABLE ANTIBODIES; DIFFERENTIATED HL-60 CELLS; SITE-DIRECTED MUTAGENESIS; INCREASES CYTOSOLIC CA2+; IN-VITRO PHARMACOLOGY; H-4 RECEPTOR; CONSTITUTIVE ACTIVITY; HUMAN EOSINOPHILS; G-PROTEINS; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy > Alumni or Retired Professors > Pharmaceutical/Medicinal Chemistry II (Prof. Buschauer) |
| Depositing User: | Petra Gürster |
| Date Deposited: | 27 May 2020 07:38 |
| Last Modified: | 27 May 2020 07:38 |
| URI: | https://pred.uni-regensburg.de/id/eprint/17484 |
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