Human sirtuin 2 inhibitors, their mechanisms and binding modes.
André Berndt PenteadoHaifa HassanieRenan Augusto GomesFlavio da Silva EmeryGustavo Henrique Goulart TrossiniPublished in: Future medicinal chemistry (2023)
The silent information regulator (sirtuin) is a family of enzymes involved in epigenetic processes with lysine deacetylase activity, having as substrates histones and other proteins. They participate in a wide range of cellular and pathologic processes, such as gene expression, cell division and motility, oxidative-induced stress management, metabolic control and carcinogenesis, among others, thus presenting as interesting therapeutic targets. In this article, the authors describe the inhibitory mechanisms and binding modes of the human sirtuin 2 (hSIRT2) inhibitors, which had their complexes with the enzyme structurally characterized. The results help pave the way for the rational designing of new hSIRT2 inhibitors and the development of novel therapeutic agents targeting this epigenetic enzyme.
Keyphrases
- gene expression
- endothelial cells
- dna methylation
- high glucose
- induced pluripotent stem cells
- squamous cell carcinoma
- healthcare
- neoadjuvant chemotherapy
- biofilm formation
- cell therapy
- dna binding
- transcription factor
- stem cells
- drug delivery
- stress induced
- mesenchymal stem cells
- cancer therapy
- drug induced
- bone marrow
- lymph node
- radiation therapy
- oxidative stress
- locally advanced
- social media
- candida albicans