Development of a Microscale Thermophoresis-Based Method for Screening and Characterizing Inhibitors of the Methyl-Lysine Reader Protein MRG15
| Autor: | Tanja Bartoschik, Alessandra Feoli, Monica Viviano, Vincenzo Pisapia, Sabrina Castellano, Gianluca Sbardella |
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| Rok vydání: | 2021 |
| Předmět: |
0301 basic medicine
Lysine Drug Evaluation Preclinical Ligands 01 natural sciences Biochemistry Analytical Chemistry Chromodomain 03 medical and health sciences Drug Development biophysics Epigenetics Transcription factor MST epigenetics Chemistry Microscale thermophoresis MRG15 Methylation 0104 chemical sciences 010404 medicinal & biomolecular chemistry 030104 developmental biology Molecular Medicine Protein Binding Transcription Factors Biotechnology |
| Zdroj: | SLAS Discovery. 26:77-87 |
| ISSN: | 2472-5552 |
| Popis: | MRG15 is a transcription factor containing the methyl-lysine reader chromodomain. Despite its involvement in different physiological and pathological states, to date the role of this protein has not been fully elucidated due to the lack of a specific and potent chemical probe.In this work, we report the development of a microscale thermophoresis (MST)-based assay for the study of MRG15-ligand binding interactions. After the development, the assay was validated using a small focused library and UNC1215 as the reference compound, to yield the identification of 10 MRG15 ligands with affinities ranging from 37.8 nM to 59.1 µM.Hence, our method is robust, convenient, and fast and could be applied to other methylation reader domain-containing proteins for the identification of new chemical probes. |
| Databáze: | OpenAIRE |
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