Introduction
Inhibition of BRPF1
There are two types of BRPF1 inhibitors reported on the basis of structures: 1, 3-dimethylbenzimidazolone and N-methylquinoline-2-ketone. GSK6853 is a BRPF1 bromodomain inhibitor with high selectivity developed by GSK and other companies. The physicochemical properties of GSK6853 and good cellular activity will contribute to its cellular and in vivo studies as a chemical probe molecule for the biological functions of BRPF1 bromodomain. The N-methylquinoline-2-ketone compound NI-57 is a BRPF bromodomain inhibitor with Kd values of 31, 110 and 410 nmol/L for BRPF1, BRPF2 and BRPF3, respectively. Experiments indicated that NI-57 showed an activity of submicromolar concentration on tumor and inflammatory models.
BRPF1 and disease
Epigenetic mechanisms regulate gene expression, which when altered can lead to disease, especially tumors. There are three main mechanisms for initiating and maintaining epigenetic changes: DNA methylation, RNA-induced gene silencing, and histone modifications. It is reported that BRPF1 is responsible for the assembly of histone acetyltransferase complexes. Therefore, BRPF1 may be a new target for cancer therapy as the epigenetic function of BRPF proteins is closely related to diseases such as tumors. Researchers are supposed to spare more effort in identifying its physiological function and its role in tumor to obtain more information about BRPF1 as a potential drug target.
There are two types of BRPF1 inhibitors reported on the basis of structures: 1, 3-dimethylbenzimidazolone and N-methylquinoline-2-ketone. GSK6853 is a BRPF1 bromodomain inhibitor with high selectivity developed by GSK and other companies. The physicochemical properties of GSK6853 and good cellular activity will contribute to its cellular and in vivo studies as a chemical probe molecule for the biological functions of BRPF1 bromodomain. The N-methylquinoline-2-ketone compound NI-57 is a BRPF bromodomain inhibitor with Kd values of 31, 110 and 410 nmol/L for BRPF1, BRPF2 and BRPF3, respectively. Experiments indicated that NI-57 showed an activity of submicromolar concentration on tumor and inflammatory models.
BRPF1 and disease
Epigenetic mechanisms regulate gene expression, which when altered can lead to disease, especially tumors. There are three main mechanisms for initiating and maintaining epigenetic changes: DNA methylation, RNA-induced gene silencing, and histone modifications. It is reported that BRPF1 is responsible for the assembly of histone acetyltransferase complexes. Therefore, BRPF1 may be a new target for cancer therapy as the epigenetic function of BRPF proteins is closely related to diseases such as tumors. Researchers are supposed to spare more effort in identifying its physiological function and its role in tumor to obtain more information about BRPF1 as a potential drug target.
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