23 results about "Histone Acetyltransferases" patented technology

The invention relates to an application of a histone H3K18 lactic acid modification related target in preparation of a medicine for preventing or treating atherosclerosis. The invention belongs to the field of biological medicine, and discloses histone acetyltransferase P300 and application of histone H3K18 lactylation (H3K18la) modification mediated by the histone acetyltransferase P300 as a new target spot for treating atherosclerosis (AS). Researches find that in the AS process, lactic acid accumulation in vascular smooth muscle cells (VSMCs) up-regulates H3K18la through P300 catalysis, and then the pathological phenotype of the VSMCs is induced, and plaque development is promoted. H3K18la can be reduced and the phenotype can be improved by inhibiting LDHA and MCT1 in vitro or knocking out a P300 gene; the P300 for in-vivo targeted inhibition of the VSMCs can significantly reduce the artery plaque. Therefore, the P300 and H3K18la inhibitors can be used for preparing the anti-atherosclerosis medicine.

Small molecules compounds and methods of their synthesis are provided. Small molecules identified can inhibit histone acetyltransferase 1 activity. Formulations and medicaments are also provided that are directed to the treatment of human disorders and conditions, such as, for example, neoplasms, cancers, viral, fungal, and parasitic infections, and aging. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration.

Compounds and compositions comprising compounds that modulate histone acyltransferase (HAT). Methods of treating neurodegenerative disorders, conditions associated with amyloid-beta peptide deposit accumulation, Tau protein levels, and / or alpha-synuclein accumulation, and cancer by administering to a subject a compound that modulates HAT.

The invention belongs to the technical field of biological medicines, and particularly discloses application of a KAT6A inhibitor in preparation of a medicine for treating diabetic cardiomyopathy. Specifically, the invention relates to an application of a histone acetyltransferase inhibitor in preparation of drugs for treating or preventing diabetic cardiomyopathy. The invention discloses an application of a KAT6A inhibitor in preparation of a medicine for treating diabetic cardiomyopathy, which is used for treating or preventing diabetic cardiomyopathy by inhibiting acetylation modification of dihydrolipoamide transacetylase protein and inhibiting cell copper death.

Provided are a compound defined by chemical formula 1, a stereoisomer thereof, a tautomer thereof, and a pharmaceutically acceptable salt thereof. In chemical formula 1, R is a site which binds to a histone acetyl transferase region of EP300. The compound of the present invention can reduce the intracellular level of EP300. [Chemical formula 1]

Cell culture media comprising luteinizing hormone, follicle-stimulating hormone and at least one histone acetyltransferase inhibitor or reverse transcriptase inhibitor are provided. Methods of in vitro maturing a human oocyte, determining suitability for in vitro maturation, as well as kits comprising media, luteinizing hormone, follicle-stimulating hormone and at least one histone acetyltransferase inhibitor or reverse transcriptase inhibitor are also provided.

The disclosure, in one aspect, relates to methods for treating cancer in a subject, the methods including at least the steps of administering at least one drug from each of at least two classes selected from an inhibitor of poly-ADP ribose polymerase (PARP inhibitor), an inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs inhibitor), an inhibitor of wild-type isocitrate dehydrogenase (IDH inhibitor), an inhibitor of histone acetyltransferase (HAT inhibitor), an inhibitor of histone deacetylase (HDAC inhibitor), an inhibitor of DNA polymerase Θ (POLΘ inhibitor), an inhibitor of platelet-derived growth factor receptor (PDGFR inhibitor), and a DNA alkylating agent to the subject. In any of these aspects, the disclosed method allows for administering lower doses of the drugs in combination compared to administration as single drugs while preventing the recurrence of the cancer, preventing drug resistance of the cancer, and reducing side effects associated with cancer treatment.

The invention discloses a diagnostic marker for the drug resistance of kidney cancer sunitinib. The diagnostic marker for the drug resistance of kidney cancer sunitinib is selected from a group consisting of histone acetyltransferase KAT2A. The invention further discloses a kit for detecting the sunitinib drug resistance of the kidney cancer. The kit comprises a reagent for detecting the expression quantity of KAT2A. The KAT2A provided by the invention is used as a renal cancer sunitinib drug resistance diagnosis marker, has good specificity and high sensitivity, provides a new diagnosis and treatment means for renal cancer sunitinib drug resistance, is beneficial to drug resistance monitoring and avoids further invalid treatment, and has a good medical conversion prospect.

The invention provides a diagnostic reagent for lung adenocarcinoma radiotherapy prognosis, which comprises a reagent for detecting the expression level of histone acetyltransferase 1 (HAT1) and / or a reagent for detecting the lactylation level of replication protein A1 (Replication Protein A1, RPA1). The invention also provides application of the diagnostic reagent. The invention provides application of HAT1-mediated RAP1 protein lactylation modification to evaluation of radiotherapy resistance characteristics of lung adenocarcinoma patients and a targeting strategy, and provides more diversified and personalized means for LUAD clinical diagnosis and treatment.

Addressing the challenges of low genome editing efficiency and low efficiency in producing plants with mutations introduced into target genes, this research aims to provide plant genome editing technology with higher genome editing efficiency. [Solution] A method for producing genome-edited plants, comprising introducing a histone acetyltransferase expression cassette and a site-specific nuclease expression cassette into a plant.

Disclosed is a method of treating diffuse midline glioma (DMG), such as diffuse intrinsic pontine glioma (DIPG), with a compound that possesses inhibitory activity against histone acetyltransferase p300 (EP300) and CREB-binding protein (CBP).

The disclosure, in one aspect, relates to methods for treating cancer in a subject, the methods including at least the steps of administering at least one drug from each of at least two classes selected from an inhibitor of poly-ADP ribose polymerase (PARP inhibitor), an inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs inhibitor), an inhibitor of wild-type isocitrate dehydrogenase (IDH inhibitor), an inhibitor of histone acetyltransferase (HAT inhibitor), an inhibitor of histone deacetylase (HDAC inhibitor), an inhibitor of DNA polymerase Θ (POLΘ inhibitor), an inhibitor of platelet-derived growth factor receptor (PDGFR inhibitor), and a DNA alkylating agent to the subject. In any of these aspects, the disclosed method allows for administering lower doses of the drugs in combination compared to administration as single drugs while preventing the recurrence of the cancer, preventing drug resistance of the cancer, and reducing side effects associated with cancer treatment.

Provided are compounds of Formula (I):and pharmaceutically acceptable salts and compositions thereof, which are useful for treating a variety of conditions associated with histone acetyltransferase (HAT).

The application belongs to the technical field of biological medicine, and provides application of a peptide in a histone acetyltransferase MOF biological activity inhibitor, and an amino acid sequence of the peptide is PYQRRGYGKF, as shown in SEQ ID No. 1. The application finds a biological activity domain of the histone acetyltransferase MOF, identifies an amino acid sequence capable of inhibiting the biological activity of the MOF, and proves that the sequence small molecule peptide can play a role in inhibiting the biological function and acetylation catalytic activity of the MOF, and can be applied as the MOF inhibitor to alleviate or treat diseases caused by the increase of the biological activity of the MOF.

Methods to identify modulators of histone acetyltransferases are described. Modulators of histone acetyltransferases can be used to treat individuals. In some instances, modulators of histone acetyltransferases are utilized to treat individuals having a neoplasm.

The invention provides application of histone acetyltransferase GhGCN5 in regulation and control of cotton fiber development, and relates to the technical field of molecular breeding. After the GhGCN5 gene is edited in cotton, both the initial number of fibers and the length of mature fibers are increased; the overexpression GhGCN5 gene can significantly inhibit the growth of cotton fibers in the initial and elongation stages, and leads to the reduction of the length and quantity of mature fibers. The GhGCN5 gene capable of regulating and controlling the development of the cotton fibers, provided by the invention, provides new gene resources and theoretical support for the quality improvement of the cotton fibers.

The invention relates to a kit for detecting clear cell renal cell carcinoma. The kit comprises: a) at least one reagent capable of inhibiting aldolase A (ALDOA) K230 site lactic acid modification; b) at least one agent capable of modulating the activity of histone acetyltransferase CBP (CREB binding protein); and / or c) at least one agent capable of modulating the activity of the deacetylase SIRT7.

The invention relates to a compound used as a histone acetyltransferase p300 / CBP bromodomain inhibitor and a preparation method and application thereof. The compound has a structure as shown in the following formula I: # imgabs0 #, wherein R1 to R3, X and Y1 to Y3 are defined in the specification. The invention also relates to a pharmaceutical composition containing the compound or the derivative thereof and application of the pharmaceutical composition as a p300 / CBP bromodomain inhibitor. The compound and the derivative thereof can significantly inhibit the activity of histone acetyltransferase p300 / CBP, have very strong proliferation inhibition activity on multiple myeloma cells OPM-2, prostate cancer cells 22RV1 and the like, have good metabolic stability, safety and drug-likeness, and can be used as an antitumor drug.

Disclosed herein are heterobifunctional compounds comprising a BCL6 binding moiety and a moiety that binds to a bromodomain of a histone acetyltransferase (HAT) wherein the two moieties are linked by a linker. Also disclosed herein are pharmaceutical compositions comprising the compounds, and methods of using the compounds, for example, to treat proliferative diseases, such as cancer.

The disclosure, in one aspect, relates to methods for treating cancer in a subject, the methods including at least the steps of administering at least one drug from each of at least two classes selected from an inhibitor of poly-ADP ribose polymerase (PARP inhibitor), an inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs inhibitor), an inhibitor of wild-type isocitrate dehydrogenase (IDH inhibitor), an inhibitor of histone acetyltransferase (HAT inhibitor), an inhibitor of histone deacetylase (HDAC inhibitor), an inhibitor of DNA polymerase Θ (POLΘ inhibitor), an inhibitor of platelet-derived growth factor receptor (PDGFR inhibitor), and a DNA alkylating agent to the subject. In any of these aspects, the disclosed method allows for administering lower doses of the drugs in combination compared to administration as single drugs while preventing the recurrence of the cancer, preventing drug resistance of the cancer, and reducing side effects associated with cancer treatment.

The disclosure, in one aspect, relates to methods for treating cancer in a subject, the methods including at least the steps of administering at least one drug from each of at least two classes selected from an inhibitor of poly-ADP ribose polymerase (PARP inhibitor), an inhibitor of DNA-dependent protein kinase catalytic subunit (DNA-PKcs inhibitor), an inhibitor of wild-type isocitrate dehydrogenase (IDH inhibitor), an inhibitor of histone acetyltransferase (HAT inhibitor), an inhibitor of histone deacetylase (HDAC inhibitor), an inhibitor of DNA polymerase Θ (POLΘ inhibitor), an inhibitor of platelet-derived growth factor receptor (PDGFR inhibitor), and a DNA alkylating agent to the subject. In any of these aspects, the disclosed method allows for administering lower doses of the drugs in combination compared to administration as single drugs while preventing the recurrence of the cancer, preventing drug resistance of the cancer, and reducing side effects associated with cancer treatment.