Brain Tumor Drug Development Targeting Epigenetic Genes

Chromatin was the first identified target for cancer therapy. Epigenetic abnormalities are not only associated with the development of certain cancers but may also affect the efficacy and prognosis of anticancer drugs by modifying pharmacokinetic-related genes such as drug absorption, distribution, metabolism, and excretion, as well as pharmacodynamic-related genes such as signaling pathways and targets of action. As research progresses, there is increasing evidence that epigenetic mechanisms have an important impact on the clinical efficacy of many drugs, especially anti-brain tumor drugs.

We provide services for the development of targeted brain tumor drugs targeting epigenetic genes

Drugs that exert anti-brain tumor effects by modulating epigenetic genes are becoming a hot topic of research. Alfa Cytology provides epigenetically targeted drug development services for clients in the field of brain tumor research. Given a large number of potential targets, we have developed a systematic approach to discover and validate potential drug targets to focus on helping our clients in brain tumor drug development and improving drug efficacy.

Other targets that could be developed

• DNMT1, 3A, and 3B. Methylates cytosines on DNA, and mutation can lead to aberrant methylation
• EZH2. Methylates histone H3K27
• DOT1L. Methylates histone H3K79
• KMT2A-D, SETD2, NSDI. Methylate histone lysines
• EP300, CREBBP. Acetylate histone lysines
• TET2. Is the first step in cytosine demethylation, and it is inhibited by 2-hydroxyglutarate (2-HG)
• IDH1, IDH2. Mutated protein produces 2-HG from isocitrate that inhibits TET2 and lysine demethylases
• HDAC1-3, 8 and HDAC6. Deacetylase removes acetyl groups from histone lysines
• KDMIA, KDM6A (UTX). Demethylates histone lysines
• BRD4. Bromodomain proteins read acetyl groups on histone lysines
• CBX family, CHD1. Chromodomain proteins read methyl groups
• ARIDIA, ARID1B, ARID2, SMARCA2, SMARCA4, SMARCBI, CHD1. Proteins in the chromatin remodeling complex use ATP to move nucleosomes away from DNA. The loss-of-function mutations common in cancer
• HIST1H1B, HIST1HIC, HISTIH3B, H3F3A, H3F3B. Structural histone proteins acquire mutations that can be oncogenic
• CTCF, STAG2, RAD21, CHD8. Normal binding to CTCF sites on DNA defines and protects gene neighborhoods from the inappropriate expression

Epigenetic assay development

Disorders of chromatin epigenetic modifications are seen in the pathology of many major diseases such as brain tumors, and cardiovascular and cerebrovascular. Therefore, there is an urgent need for drugs that can intervene in epigenetic modification disorders in disease states. In response to this need, Alfa Cytology offers its clients epigenetically targeted drug development services for brain tumors. You can contact us at any time to receive updates on our services.