53 results about "PKM2" patented technology

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

The invention discloses a series of aminodithioformate compounds, a preparation method therefor and use of aminodithioformate compounds in preparation of antitumor drugs. Through carrying out activity screening on a micromolecular compound library, a novel structure type of PKM2 inhibitors are discovered from the micromolecular compound library, and a series of aminodithioformate compounds with a structure represented by a general formula I shown in the description are designed and synthesized according to the inhibitors. Proven by enzyme activity tests, the compounds have remarkable superior PKM2 inhibiting activity and selectivity to those of currently available PKM2 inhibitors. Through separately carrying out killing effect test on pyruvate kinase M2 and M2 subtypes and four kinds of tumor cell lines, i.e., MCF-7, HCT116, Hela and H1299 by using the compounds disclosed by the invention, activity tests prove that the compounds have a remarkable tumor cell proliferation inhibiting action.

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

The invention described herein features methods, compositions, and kits for the use of activators of PKM2 for the treatment, prevention, or amelioration of diseases related to PKM2 function, including, e.g., cancer, diabetes, atherosclerosis, restenosis, obesity, autoimmune disorders, and proliferative disorders.

Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

The invention described herein features methods, compositions, and kits that utilize activators of pyruvate kinase M2 (PKM2) for the treatment or amelioration of disorders related to PKM2 function and characterized by abnormally low levels of serine.

This invention provides a method of treating lung cancer including administering a therapeutically effective amount of a compound of 0089-0022 formula I to a subject in need thereof. The compound activates pyruvate kinase M2 isoform (PKM2) to treat the lung cancer. In one example, the lung cancer is Non-Small Cell Lung Cancer (NSCLC).

The present invention relates to prevention of congenital deformations. The invention further relates to cancer inhibition and prevention. The invention further relates to methods and compositions to modulate, antagonize, or agonize disparate signaling pathways that may converge to regulate patterning events and gene expression during prenatal development, post-natal development, and during development in the adult organism. The invention also relates to activators or deactivators of pyruvate kinase M2 (PKM2) for the treatment, prevention, or amelioration of diseases related to PKM2 function.

Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

The invention relates to nucleic acid molecules and compositions for specific post-transcriptional inhibition of PKM2 expression. Methods for specific inhibition of PKM2 expression in a target cell, for example a cancer cell, are also provided.

Disclosed are pyruvate kinase M2 activators, which are bis sulfonamide piperazinyl and piperidinyl compounds of Formula (I), 2,4-disubstituted 4H-thieno[3,2-c]pyrrole-2-(substituted benzyl)pyridazin-3(2H)-ones of Formula (II) and 6-(3,4-dimethylphenylaminosulfonyl)-3,4-dihydro-1H-quinolin-2-one of formula (III), wherein L, R1, R2, R11 to R16, R21 and R22 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia.

The invention discloses an anti-tumor polypeptide targeting PKM2 protein and application of the anti-tumor polypeptide. The amino acid sequence of the polypeptide is at least one of KG-pY-EQ, KG-pY-IW, HW-pY-KW, NK-pY-GE, RD-pY-LY, HV-pY-SR, PE-pY-YR and DE-pY-FQ, wherein pY represents phosphorylated tyrosine. The anti-tumor polypeptide targeting the PKM2 protein has an inhibiting effect on growthand proliferation of liver cancer cells and breast cancer cells, and can be used for treating tumors.

The invention discloses application of a scutellarin biotin-labeled probe and a related PKM2 kinase inhibitor. The PKM2 kinase inhibitor is characterized in that a target of an active group is found by the scutellarin biotin-labeled probe; a scutellarin aglycone derivative is prepared by the found target protein; then, the scutellarin aglycone derivative is applied to a tumor treating medicine preparation.

The invention provides a small molecular activator taking human M2 type pyruvate kinase (M2 type pyruvate kinase, PKM2) as a target spot and application of the small molecular activator, and belongs to the technical field of pharmacy. According to the small molecular activator, the PKM2 is taken as the target spot, and the small molecule activator is screened by combining virtual screening based on butt joint and in-vitro biological activity evaluation. In-vitro activity test results show that two screened compounds have good PKM2 activation activity and good cancer cell inhibition activity, and discovered small molecules can provide a basis for research and development of new drugs for treating PKM2 related diseases, such as cervical cancer, breast cancer, ovarian cancer, prostate cancer,liver cancer, lung cancer, pancreatic cancer, colorectal cancer, leukemia, melanoma and multiple myeloma. A lead compound of the small molecular activator can be further optimized in structure, and arelatively good application prospect is achieved.

Compounds of general Formula (I), and compositions comprising compounds of general formula I that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

The invention discloses application of piperidine-1-dithioformate-3-methyl-1, 4-dioxo-1, 4-dihydronaphthalene-2-methyl ester in treatment of Parkinson's disease. Experimental results show that a Parkinson's model (PD) mouse is given PKM2-IN-1 in an intragastric administration mode, and the medicine can remarkably relieve PD related symptoms, such as recovering the number of dopaminergic neurons at the substantia nigra part, improving expression of tyrosine hydroxylase at the midbrain part and improving the motor ability and the olfactory function of the mouse.

The invention provides an inhibitor of M2 type pyruvate kinase (PKM2)-a type of carbamic acid alkannin ester compound. Compound 3 is the currently reported M2 type pyruvate kinase inhibitor. The inhibition effect of carbamic acid alkannin ester on PKM2 is found to be higher than that of the Compound 3. Therefore, as an inhibitor of pyruvic acid, the carbamic acid alkannin ester has important application value. A type of new pyruvate kinase inhibitor-carbamic acid alkannin ester is provided, provides basis for selection of new medicaments and has important application prospect.

The invention relates to the field of biotechnology and oncology, in particular to a biological sample marker relative to benign and malignant differential diagnosis of thyroid nodule and applicationthereof. The invention provides the biological sample (FNA sample) marker relative to preoperative benign and malignant differential diagnosis of thyroid nodule and application of the biological sample (FNA sample) marker in benign and malignant differentiation and prognosis evaluation of thyroid nodule, and provides a detection kit for preoperative benign and malignant differentiation of thyroidnodule. The marker is PKM2 mRNA in a preoperative FNA sample of thyroid nodule. Studies find that expression of the PKM2 mRNA in the preoperative FNA sample of papillary thyroid carcinoma (PTC) increases, and the fact that the PKM2 mRNA is relative to formation and development of thyroid malignancy is shown. The FNA sample is used for detecting the PKM2 mRNA, and as a new method for differentiating benign and malignant of thyroid nodule, the method is beneficial for avoiding diagnostic surgery when a definite diagnosis cannot be made by cytologic diagnosis.

The invention relates to a polypeptide aggregate molecule as well as a preparation method and an application thereof. The polypeptide aggregate molecule comprises serine, an enzyme specific hydrolysis part, an assembly driving part and an aggregation-induced emission part, and the serine, the enzyme specific hydrolysis part, the assembly driving part and the aggregation-induced emission part are connected to form the polypeptide aggregate molecule. The polypeptide aggregate molecule can be specifically hydrolyzed in tumor cells, the action of serine and dimer PKM2 is exposed, the polypeptide aggregate molecule is promoted to be converted into tetramer PKM2, and therefore tumor inhibition is achieved, in addition, the aggregation-induced luminescence effect is achieved through assembling, the progress and migration of tumors can be monitored in real time, and meanwhile the long-acting retention effect is achieved.

Compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.

The invention provides an inhibitor for pyruvate kinase M2 (PKM2), namely a carbamic acid alkannin ester compound. A pyruvate kinase M2 inhibitor which has been reported at present comprises Compound 3, but the invention discovers that the effect of carbamic acid alkannin ester on the inhibition of the PKM2 is higher than that of the Compound 3. Therefore, the carbamic acid alkannin ester serving as an inhibitor for pyruvic acid has important application value. The invention has the advantages that: a novel pyruvate kinase inhibitor, namely the carbamic acid alkannin ester is provided, so that the basis is provided for the screening of novel medicines; and the inhibitor has an important application prospect.