Histone Acetyltransferase Screening

Histone acetyltransferases (HATs) are critical in controlling H3 lysine acetylation and are tightly associated with cell cycle regulation, cell proliferation, and apoptosis. Histone acetylation also has impact on the regulation of chromatin structure and the recruitment of transcription factors to gene promoters. A disrupted equilibrium of histone acetylation is correlated with diseases ranging from cancers and inflammatory diseases to neurological disorders. The investigation of histone acetylation pattern leads to a better understanding of epigenetic regulation of gene activation, and helps to develop drugs targeting HAT. Although some HAT inhibitors have been developed, there still remains a large gap between the biological activity of inhibitors in in vitro studies and their potential use as therapeutic agents.

Creative BioMart supplies a rapid, flexible profiling and screening service for potential drug inhibitors against HATs, including small molecules, peptides, and antibodies. Two assay platforms, chemiluminescent assays and fluorogenic based functional assays are available at Creative BioMart, both of which are highly sensitive and reproducible to rapidly identify potential therapeutics, predict potency, and narrow down a large school of candidates to a much smaller number. High-throughput screening and practical strategies for assay optimization and validation are also provided to make our services more efficient and trustable. Creative BioMart also owns a large portfolio of acetyltransferase research tools, including active purified enzymes, assay kits, and inhibitors/activators.

Procedure of Histone Acetyltransferase Screening at Creative BioMart

a. Chemiluminescent Assay

The chemiluminescent technology is on the basis of HAT-catalyzed transfer of an acetyl group from acetyl-CoA to a histone substrate that is coated onto a 96-well plate. The acetylated histone is further detected by a highly specific primary antibody, followed by a horseradish peroxidase (HRP)-labeled secondary antibody. Finally, a chemiluminescence reader is employed to measure the chemiluminescence produced by HRP.

General procedure of chemiluminescent method for HAT screening assay

Figure 1. General procedure of chemiluminescent method for HAT screening assay

b. Fluorogenic-based Method

The assay based on fluorescence is simple, sensitive, and rapid to screen potential inhibitors of HAT. HAT is incubated with acetyl coenzyme A (CoA), inhibitor and histone substrate, generating an acetylated substrate and CoA-SH with a free thiol group. Then a pre-chilled isopropyl alcohol is added to stop the reaction, followed by the addition of fluorescence developing solution. The presence of specific inhibitors could inhibit the enzymatic activity and result in a decrease or total loss of fluorescence.

Schematic procedure of fluorometrical method for HAT screening assay

Figure 2. Schematic procedure of fluorometrical method for HAT screening assay

Benefits of Histone Acetyltransferase Screening Services at Creative BioMart

  1. A huge library of HATs targets
  2. Compare potency with IC50 (half maximal inhibitory concentration) determination
  3. Receive data with high quality within fast turnaround time
  4. Get project guidance in a time-efficient manner

With years of professional experience in HATs field, Creative BioMart can work with you to identify potential compounds through an effective screening approach with high sensitivity, high reproducibility, quick turnaround, and minimum false positives and negatives. Creative BioMart is also capable of streamlining the platform processes and designing a customized process that meets your specific needs. If you want to learn more about our custom services, please feel free to contact us.

1. Zhang, R. K.; et al. Identification of novel inhibitors of histone acetyltransferase hMOF through high throughput screening. Eur J Med Chem. 2018, 157: 867-876.

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