Histone acetyltransferases (HATs) transfer an acetyl group from acetyl coenzyme A (CoA) to lysine residue that reside on histone tails. This process generally results in gene activation by inducing a euchromatin conformation and recruiting bromodomain-containing transcription factors for genes proximal to the acetylated histone. Abnormal histone acetylation profiles have been shown to correlate with disease progression. Current work is focused on the identification of specific epigenetic regulators that lead to aberrant acetylation profiles, to develop specific inhibitors and activators of HATs. Histone deacetylases (HDACs) and sirtuins (SIRTs) work opposite to HATs by removing acetyl group and restoring the positive charge of the lysine residue tail. HDACs modification could lead to a more tightly compacted, heterochromatin conformation, thus negatively regulating gene expression. Cancers and neurological disorders are closely related with abnormal HDAC activity, and herein HDAC has been an attractive drug target. Several HDAC inhibitors have been approved by FDA as anti-cancer drugs.

Creative BioMart offers rapid and dependable biochemical screening service for small molecule inhibitors against HATs or HDACs by IC₅₀ (half maximal inhibitory concentration) determination. Highly sensitive and reproducible chemiluminescent-based and fluorogenic-based functional assays are provided at Creative BioMart to minimize false positives and negatives, which is ideal for accelerating your drug discovery program with right drug candidates being selected and progressed through the pipeline. In addition to a panel of HAT&HDAC screening assays, there are also a full suite of active HAT, HDAC and SIRT proteins, assay kits, as well as a number of inhibitors and substrates to meet your research goals.

HAT & HDAC Screening Services at Creative BioMart

Histone Acetyltransferase Screening
HATs are tightly involved in critical cellular processes and the disruption in the equilibrium of histone acetylation leads to tumorigenesis and cancer progression. The identification of histone acetylation would provide useful information for the development of HAT-targeted drugs. Creative BioMart is experienced in performing HAT screening assay that support your compounds to advance speedily through the discovery pipeline.

Histone Deacetylase/SIRT Screening
Site-specific histone deacetylation has been shown to repress eukaryotic gene transcription, and HDACs are involved in cell differentiation, proliferation, apoptosis, and senescence. Aberrant HDAC expression is detected in various diseases, especially cancer, and thereby HDAC has become a novel target for the treatment of cancer. HDAC/SIRT screening assays at Creative BioMart is specifically designed to meet your specific needs in epigenetic drug development process.

HAT & HDAC screening services at Creative BioMart assure the high-tech platform and quality data that you seek in development of epigenetics-related therapy. The selection of method or protocol will depend on the question you are trying to answer. Our well-trained project team is also ready to give advice about your choice of technology and substrates, providing more flexibility to meet your drug discovery needs. contact us today for more information about our HAT & HDAC screening and profiling services.