Abstract
An artificial polypeptide receptor (APR) library was created by using the self-organization of N-lipidated peptides attached to cellulose via m-aminophenylamino-1,3,5-triazine. The response of the library was probed using a series of novel H3 receptor ligands. Since no guidelines on how to design an APRs selective vs certain receptor types exist, a diverse set of amino acids (Ala, Trp, Pro, Glu, His, Lys and Ser) were used and coupled with one of three gating fatty acids (palmitic, ricinoleic or capric). A competitive adsorption-desorption of an appropriate reporter dye was used for the indirect visualization of the interactions of guests with particular receptors. The resulted library response to individual inhibitors was then arranged in a matrix, preprocessed and analyzed using the principal component analysis (PCA) and partial least squares (PLS) method. The most important conclusion obtained from the PCA analysis is that the library differentiates the probed compounds according to the lipophilicity of the gating unit. The PC3 with a dominant absolute contribution of the receptors containing Glu allowed for the best separation of the ligands with respect to their activity. This conclusion is in agreement with the fact that Glu 206 is a genuine ligand counterpart in the natural histamine receptor.
Keywords: Diagnostic platform, exploratory analysis, molecular recognition, peptide artificial receptor library, triazine.
Combinatorial Chemistry & High Throughput Screening
Title:Probing an Artificial Polypeptide Receptor Library Using a Series of Novel Histamine H3 Receptor Ligands
Volume: 17 Issue: 2
Author(s): Andrzej Bak, Michal Daszykowski, Zbigniew Kaminski, Katarzyna Kiec-Kononowicz, Kamil Kuder, Justyna Fraczyk, Beata Kolesinska, Patrycja Ciosek and Jaroslaw Polanski
Affiliation:
Keywords: Diagnostic platform, exploratory analysis, molecular recognition, peptide artificial receptor library, triazine.
Abstract: An artificial polypeptide receptor (APR) library was created by using the self-organization of N-lipidated peptides attached to cellulose via m-aminophenylamino-1,3,5-triazine. The response of the library was probed using a series of novel H3 receptor ligands. Since no guidelines on how to design an APRs selective vs certain receptor types exist, a diverse set of amino acids (Ala, Trp, Pro, Glu, His, Lys and Ser) were used and coupled with one of three gating fatty acids (palmitic, ricinoleic or capric). A competitive adsorption-desorption of an appropriate reporter dye was used for the indirect visualization of the interactions of guests with particular receptors. The resulted library response to individual inhibitors was then arranged in a matrix, preprocessed and analyzed using the principal component analysis (PCA) and partial least squares (PLS) method. The most important conclusion obtained from the PCA analysis is that the library differentiates the probed compounds according to the lipophilicity of the gating unit. The PC3 with a dominant absolute contribution of the receptors containing Glu allowed for the best separation of the ligands with respect to their activity. This conclusion is in agreement with the fact that Glu 206 is a genuine ligand counterpart in the natural histamine receptor.
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Bak Andrzej, Daszykowski Michal, Kaminski Zbigniew, Kiec-Kononowicz Katarzyna, Kuder Kamil, Fraczyk Justyna, Kolesinska Beata, Ciosek Patrycja and Polanski Jaroslaw, Probing an Artificial Polypeptide Receptor Library Using a Series of Novel Histamine H3 Receptor Ligands, Combinatorial Chemistry & High Throughput Screening 2014; 17 (2) . https://dx.doi.org/10.2174/13862073113169990054
DOI https://dx.doi.org/10.2174/13862073113169990054 |
Print ISSN 1386-2073 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5402 |
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