Aryl-1,3,5-triazine derivatives as histamine H4 receptor ligands

Łażewska, Dorota; Więcek, Małgorzata; Ner, Joanna; Kamińska, Katarzyna; Kottke, Tim; Schwed, J. Stephan; Zygmunt, Małgorzata; Karcz, Tadeusz; Olejarz, Agnieszka; Kuder, Kamil; Latacz, Gniewomir; Grosicki, Marek; Sapa, Jacek; Karolak‐Wojciechowska, J.; Stark, Holger; Kieć‐Kononowicz, Katarzyna

doi:10.1016/j.ejmech.2014.06.032

Cited by 47 publications

(42 citation statements)

References 28 publications

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“…For the studies, previously described histamine H 4 R model, was used [21] built on the basis of crystal structure of histamine H 1 receptor (PDB entry: 3RZE), paying attention to mutagenesis data described by Jongejan et al [36]. Histamine H 4 R models based on the crystal structure of histamine H 1 R could be more reliable than rhodopsin-based H 4 R models and could help to identify potential H 4 R ligands through virtual screening [37,38].…”

Section: Docking Studiesmentioning

confidence: 99%

“…The luminescence signal was measured with a microplate reader in luminescence mode (PerkinElmer). The IC 50 value of the reference compound -ketoconazole (Sigma-Aldrich) was determined as we described previously [21]. The final concentrations of 6 were 0.025-25 µM and for CYP3A4 inhibitorketoconazole 0.025-10 µM.…”

Section: Metabolic Stability and Interaction With Cyp3a4mentioning

confidence: 99%

“…Efficacy of selected compounds was determined in cAMP accumulation assay, as already described elsewhere [21]. Briefly, CHO cells stably expressing human H 4 R were incubated (30 min, room temperature) with histamine (140 nM), forskolin (10 µM) and evaluated compounds (10 appropriate concentrations in a range spanning over 5 log units) in presence of phosphodiesterase inhibitor (RO-201724, 100µM).…”

Section: Camp Accumulation Assay In Cells Expressing Hh 4 Rmentioning

confidence: 99%

See 2 more Smart Citations

(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands

Kamińska

Ziemba

Ner

et al. 2015

European Journal of Medicinal Chemistry

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Section: Docking Studiesmentioning

confidence: 99%

Section: Metabolic Stability and Interaction With Cyp3a4mentioning

confidence: 99%

Section: Camp Accumulation Assay In Cells Expressing Hh 4 Rmentioning

confidence: 99%

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(2-Arylethenyl)-1,3,5-triazin-2-amines as a novel histamine H4 receptor ligands

Kamińska

Ziemba

Ner

et al. 2015

European Journal of Medicinal Chemistry

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“…In another study, the binding mode of 2-amino-4-(4-methylpiperazin-1-yl)-1,3,5-triazine derivatives with different aryl substituents in the 6-position was investigated at the H4R binding site [59]. The authors used a H1R based homology model of H4R following the protocol of Feng et al [57].…”

Section: H4 Receptormentioning

confidence: 99%

Structure-based discovery and binding site analysis of histamine receptor ligands

Kingsford-Adaboh

Keserü

2016

Expert Opinion on Drug Discovery

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Introduction: Application of structure-based drug discovery in histamine receptor projects was previously hampered by the lack of experimental structures. The publication of the first X-ray structure of the histamine H1 receptor has been followed by several successful virtual screens and binding site analysis studies of H1-antihistamines. This structure together with several other recently solved aminergic G-protein coupled receptors (GPCRs) enabled the development of more realistic homology models for H2, H3 and H4 receptors. Areas covered: In this paper, we review the development of histamine receptors models and their application on drug discovery. Expert opinion: In our opinion, the application of atomistic histamine receptor models played a significant role in understanding key ligand-receptor interactions as well as in the discovery of novel chemical starting points. The recently solved H1 receptor structure is a major milestone in structure-based drug discovery, however our analysis also demonstrate that for building H3 and H4 receptor homology models other GPCRs may be more suitable as a template. For these receptors we envisage that the development of higher quality homology models will significantly contribute to the discovery and optimization of novel H3 and H4 ligands.

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“…al [57]. synthesized and evaluated a series of novel triazine derivatives with different aryl substituents at 6-position for histamine H4 receptor (H4R) affinity in Sf9 cells, expressing human H4R co-expressed with G-protein subunits.…”

mentioning

confidence: 99%