5 results about "Histone deacetylase activity" patented technology

The invention discloses a genetic engineering strain of high-yield secondary metabolite Fumagillin as well as a construction method and application of the genetic engineering strain, and the genetic engineering strain is obtained by taking aspergillus fumigatus as a chassis bacterium through hosA gene knockout or hosA catalytic active site mutation. According to the method, a hosA gene knockout strain (delta hosA) and catalytic active site mutation strains (HosAD133A, HosAH175A and HosAD210A) are constructed by means of molecular biology, and the mutant strains are subjected to liquid or solid fermentation under the culture condition of 37 DEG C, so that the yield of Fumagillin can be remarkably increased. According to the method disclosed by the invention, the inhibition on a Fumagillin biosynthetic pathway is relieved and the metabolic flux is enhanced by utilizing the activity change of histone deacetylase caused by hosA defects, and an efficient and directional production method for high-yield Fumagillin is provided, so that the method has an important industrial application value.

The present invention discloses a selective histone deacetylase inhibitor and a preparation method and application thereof. The histone deacetylase inhibitor is a compound with a six-membered cyclic ring as a parent core and a hydrazide as a zinc ion chelating group, and has a structure as shown in the general formula (I). The present invention also provides a preparation method of the compound. The compound of the present invention has a significant inhibitory effect on histone deacetylase 11 (HDAC11), and can be used to prepare drugs for treating diseases related to abnormal expression of histone deacetylase activity, such as tumors, liver diseases, hyperlipidemia, diabetes, cardiovascular diseases, obesity and atherosclerosis.

A histone deacetylase inhibitor and uses thereof are provided. A class of HDAC inhibitors with a novel structure and high efficiency is prepared by introducing a succinimide fragment. The HDAC inhibitor has the beneficial effects of excellent inhibitory activity against HDACs and excellent in vitro anti-tumor activity, providing a new approach for the application of HDAC inhibitors in solid tumors and / or the treatment of diseases associated with uncontrolled histone deacetylase activity.

The objective is to provide a histone deacetylase inhibitor and its use. [Solution] The present invention relates to histone deacetylase inhibitors and their use, and belongs to the field of chemical technology. In this invention, a structurally novel and highly efficient HDACs inhibitor is obtained by introducing a succinimide fragment. An advantageous effect of the present invention is that these compounds exhibit excellent inhibitory activity against HDACs and also have excellent in vitro antitumor activity, providing a new means for the application of HDAC inhibitors to solid tumors or for the treatment of diseases associated with abnormalities in histone deacetylase activity.

A histone deacetylase inhibitor and the use, which belong to the field of medicinal chemistry. A structurally new and highly efficient HDAC inhibitor is obtained by introducing a succinimide fragment, which is as shown in formula (I) below. The beneficial effects thereof involve: having an excellent inhibitory activity on HDACs and also an excellent anti-tumor activity in vitro; and providing a new pathway for the application of the HDAC inhibitor in solid tumors and / or the treatment of diseases related to uncontrolled histone deacetylase activity.