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Cell-Based Epigenetic Assays

Recent years, the understanding of modular epigenetic regulators containing targeting motives and/or catalytic domains has dramatically increased. Druggable epigenetic modulators undergo oncogenic mutation and are seen as attractive therapeutic targets. Some protein domains such as Plant Homeo Domains (PHD), Bromodomains (BRD) or Malignant Brain Tumors (MBT) direct the proteins to particular binding sites in the chromatin, while others such as Jumonji (JMJ) or Su(var)3-9, Enhancer-of-zeste and Trithorax (SET) domains ensure that an appropriate genomic site is marked with an activating/repressive or cell cycle appropriate mark. However, the essential part of the epigenetic modulators’ functional investigation is the design of robust cellular assays that guide chemical probe development. Given the wide variety of cellular processes epigenetic regulators take part in, functional consequences such as influence on include gene expression, cell cycle progression, genome-wide localization, DNA replication and repair can be assessed.

With years of professional experience in the epigenetic field, Creative Biogene has developed various cell-based epigenetic assays which can be applied to all stages of drug discovery and are ideal for identifying potent and selective small molecule inhibitors to emerging epigenetic targets. Our assays for epigenetic targets enable identification and classification of inhibitors based on potency, selectivity and in vitro efficacy. Moreover, with our primary human cell model systems, phenotypic signatures can be generated to gain insight into the mechanism of action, efficacy and safety-related effects in the context of human diseases.

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Figure 1. Overview of different approaches for cellular characterization of potential epigenetic modulators.

Cell-Based Epigenetic Assays Available

  • Cell-based histone & tubulin deacetylation assays
  • Histone methylation cell assays
  • Histone deacetylase assays
  • NanoBRET assay for epigenetic protein and protein interactions in living cells
  • Cell-based bromodomain & histone methyltransferase binding assays

Advantages

  • High quality intracellular binding data
  • Rank ordering of compounds based on cellular potency
  • Binding mode available
  • Broad applications - primary screening, lead optimization, structure-activity relationship (SAR) optimization
  • Rapid data turnaround

Moreover, Creative Biogene has established long-term assay conditions to yield robust cell line profiling data. Our highly skilled and experienced service team is able to provide you with high quality, reproducible data to help you meet all your project timelines and requirements. If you have any specific needs, please feel free to contact us. Look forward to the cooperation with you in the near future.

Reference:

  1. Hau M, et al. Cellular analysis of the action of epigenetics drugs and probes. Epigenetics, 2017:00-00.

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