Histone Deacetylase Assay Services

Creative Biolabs is the leading supplier of histone deacetylase assay services for the aim of histone deacetylase drug development. We offer top-notch sirtuin and histone deacetylase testing at the most competitive pricing because to our many years of experience.

While transcriptional repressors and corepressors typically associate with histone deacetylases (HDACs), resulting in promoter histone deacetylation and transcriptional repression, recruitment of transcriptional activators and coactivator complexes, including histone acetyltransferases, has been linked to promoter histone acetylation and gene activation. Numerous processes contribute to aberrant transcriptional suppression in cancer, some of which can be addressed with HDAC inhibitor (HDACI) therapy. This type of HDACI-based cancer treatment has been called epigenetic or transcriptional therapy. It has been demonstrated that HDACIs can cause apoptosis, differentiation, or cell cycle arrest. HDACIs are harmful to tumor cells only. Investigations into the mechanisms underlying this tumor selectivity are ongoing, and they may involve both transcriptional and nontranscriptional processes. A growing number of studies have shown that acetylation of nonhistone proteins has critical effects on their function. In response to HDACIs, many nonhistone proteins are hyperacetylated, including some of the proteins most important in maintaining the malignant phenotype.

Fig.1. Fluorescence based activity assay for HDAC.¹

Targets of Demethylase Assay Services

Histones are the most well-studied HDAC substrates because they are fundamental parts of the nucleosome, which is the fundamental structural motif of chromatin. The nucleosome core particle is composed of two copies of each of the four core histones, H2A, -2B, -3, and -4. It has 146 double-stranded DNA nucleotide pairs wrapped around it in a 1.65-turn pattern. Linker DNA, which can range in length from a few nucleotide pairs to approximately 80, and its associated linker histone H1 are located on either side of the nucleosome core particle. Histone acetylation has been linked to higher transcriptional activity potential in vivo, alleviation of transcriptional inhibition, and enhanced accessibility of nucleosomal DNA to transcription factors. Creative Biolabs' histone deacetylase assays aim to achieve the following targets:

Creative Biolabs offers the most reasonably priced histone deacetylase assay services in this sector. We are confident that we can be your trustworthy partner and are dedicated to identifying your inhibitors or activators against HDAC targets with the highest chance of success. We will work directly with your scientists to provide the quickest answer for your HDAC-based drug discovery project. Please contact us for more information.

Reference

1. Zessin, Matthes, et al. "Continuous Sirtuin/HDAC (histone deacetylase) activity assay using thioamides as PET (Photoinduced Electron Transfer)–based fluorescence quencher." Bioorganic Chemistry 117 (2021): 105425.