48 results about "HDAC1" patented technology

Compounds represented by formula (1) have strong inhibitory activity that is selective towards HDAC1 and HDAC4. Therefore, the compounds of the present invention are useful as pharmaceutical agents for treating or preventing diseases caused by HDAC1 and HDAC4.

Compounds represented by formula (1) have strong inhibitory activity that is selective towards HDAC1 and HDAC4. Therefore, the compounds of the present invention are useful as pharmaceutical agents for treating or preventing diseases caused by HDAC1 and HDAC4.

This invention is based in part on the discovery that miR-34 is independent of p53. It has been discovered that miR-34 functions in a TP53 -independent tumor suppression pathway. Specifically, miR-34-induced inhibition of cancer cell growth was found to be the same in p53-normal and p53-deficient cells. Thus, miR-34 has a more central role during tumor suppression that is uncoupled from p53. In the absence of p53, miR-34, unlike certain other miRNAs, is sufficient to induce an up-regulation of genes known to be regulated by p53, including but not limited to p21<CIP1 / WAF1>(CDKN1A), PUMA, BAX, NOXA, PHLDA3, and MDM2 and a down-regulation of HDAC1. Therefore, these biomarkers can be used as biomarkers of miR-34 activity. The invention is further based on the discovery that some of these biomarkers are indispensable for a therapeutic response to miR-34 activity, and are thus prerequisite biomarkers of miR-34 activity.

A method for treating cancer is described using combination therapies comprising the use of hyperbaric oxygen with histone deacetylase inhibitors, with and without glycolytic therapies. The patient is subjected to a hyperbaric environment of substantially pure oxygen. A predetermined dose of one or more HDACI substances is administered to the patient. In addition, glycolitic inhibitors may also be administered. Dosages, pressures, and durations are selected as described herein to have a therapeutic effect on the patient.

The invention discloses a saussurea-obvallata effective part and a preparing method and application thereof, and belongs to the technical field of plant extract. The saussurea-obvallata effective part is selected from the mixture of any mass ratio of one or two above of a saussurea-obvallata petroleum ether part, a saussurea-obvallata ethyl acetate part, a saussurea-obvallata n-butyl alcohol part and a saussurea-obvallata aqueous phase extraction part. The preparing method includes the steps that saussurea-obvallata whole plant is smashed, an ethanol solution with the mass percent concentration of 65% to 95% is added and subjected to reflux extraction, the obtained extracted liquid is concentrated and dried, and extract is obtained; the extract is dispersed in distilled water, extract dispersion liquid is obtained, petroleum ether, ethyl acetate and n-butyl alcohol are sequentially used as a solvent to extract the extract dispersion liquid, and after the solvent is volatilized, the saussurea-obvallata petroleum ether part, the saussurea-obvallata ethyl acetate part and the saussurea-obvallata n-butyl alcohol part are obtained; the extracted extract dispersion liquid is concentrated and dried, and the saussurea-obvallata aqueous phase extraction part is obtained. The saussurea-obvallata effective part has an application to preparing medicine for inhibiting a HDAC1 enzyme, and can be used for preparing antitumor medicine.

A method for treating cancer is described using combination therapies comprising the use of hyperbaric oxygen with histone deacetylase inhibitors, with and without glycolytic therapies. The patient is subjected to a hyperbaric environment of substantially pure oxygen. A predetermined dose of one or more HDACI substances is administered to the patient. In addition, glycolitic inhibitors may also be administered. Dosages, pressures, and durations are selected as described herein to have a therapeutic effect on the patient.

The present invention provides three-dimensional structural information from the hyperthermophilic bacterium Aquifex aeolicus which is a histone deacetylase-like protein (HDLP). HDLP shares 35.2% amino acid sequence identity with human histone deacetylase (HDAC1). The present invention further provides three-dimensional structural information of HDLP bound by inhibitor molecules. The three-dimensional structural information of the present invention is useful to design, isolate and screen deacetylase inhibitor compounds capable of inhibiting HDLP, HDAC family members and HDLP-related molecules. The invention also relates to nucleic acids encoding a mutant HDLP which facilitates the determination of the three-dimensional structure of HDLP in the presence of a zinc atom.

The invention discloses a corydalis pygmaea effective part, as well as a preparation method and application thereof, and belongs to the technical field of a plant extract. The corydalis pygmaea effective part is mixture of one or more than one of a corydalis pygmaea petroleum ether part, a corydalis pygmaea ethyl acetate part and a corydalis pygmaea aqueous extraction part in an arbitrary mass ratio. The preparation method comprises the following steps: grinding whole grass of corydalis pygmaea, refluxing and extracting with an ethanol solution having a volume percentage concentration of 65-95 percent, concentrating and drying the extract to obtain an extract; dispersing the extract with distilled water to obtain an extract dispersant, extracting the extract dispersant sequentially with petroleum ether, ethyl acetate and n-butyl alcohol, and volatizing solvent to obtain a corydalis pygmaea petroleum ether part and a corydalis pygmaea ethyl acetate part; and concentrating and drying the extracted extract dispersant to obtain a corydalis pygmaea water-phase extraction part. The corydalis pygmaea effective part can be applied to preparation of medicines for inhibiting HDAC1 enzyme, and can be used for preparing anti-tumor medicines.

The present invention provides three-dimensional structural information from the hyperthermophilic bacterium Aquifex aeolicus which is a histone deacetylase-like protein (HDLP). HDLP shares 35.2% amino acid sequence identity with human histone deacetylase (HDAC1). The present invention further provides three-dimensional structural information of HDLP bound by inhibitor molecules. The three-dimensional structural information of the present invention is useful to design, isolate and screen deacetylase inhibitor compounds capable of inhibiting HDLP, HDAC family members and HDLP-related molecules. The invention also relates to nucleic acids encoding a mutant HDLP which facilitates the determination of the three-dimensional structure of HDLP in the presence of a zinc atom.

The invention discloses a composition for detecting chemoradiotherapy sensitivity of rectal cancers, a micro array and a computer system. The composition of the invention includes oligonucleotides that are specifically bound to a part of contiguous regions of a gene selected from a group consisting of ABL1, AR, CDK1, HDAC1, IRF1, JUN, PRKCB, RELA-3, STAT1-2, SUMO1-3, ACTB, CSNK1G2, FARP1, GAPDH, and RPLP0. The composition can be used to detect the relative expression level of each gene. In addition, based on expression level differences, and a sensitivity index (RSI) is obtained via a specificalgorithm, and can be used to effectively determine the chemotherapy sensitivity of a detection sample.

The invention provides a histone deacetylase inhibitor and use thereof. Specifically, the present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein the definitions of each group are as described in the specification. The present invention also provides a preparation method of such compounds. The compounds of formula (I) of the present invention can be used for the treatment of histone deacetylases (HDACs) by inhibiting histone deacetylases (HDACs), especially class I histone deacetylases (subtypes such as HDAC1, HDAC3, etc.). A series of diseases mediated, including the treatment of solid tumors, leukemia and other tumor diseases, and neurodegenerative diseases.

The invention relates to a class of 2-aryl-4-(1H-pyrazole-3-yl)pyridine LSD1 / HDAC dual-target inhibitors, its preparation method and its application in the preparation of antitumor drugs, belonging to medicinal chemistry technology field. The compound has the following general formula: wherein, R 1 CH is preferred 3 、OCH 3 and H; R 2 F and H are preferred. The compounds of the present invention have strong inhibitory activity on both LSD1 and HDAC, and the IC on HDAC1 50 The value is less than 5 nM, significantly better than the positive drug SAHA. It shows good in vitro anti-tumor activity against human acute myeloid leukemia THP‑1 cell line, which is better than the positive drug SAHA, which provides a basis for the development of LSD1 / HDAC dual-target inhibitor drugs and can be used as a candidate for further development Or lead compounds are used to develop anti-tumor therapeutic drugs.