53 results about "Glycolysis Inhibition" patented technology

An improved system for large scale production of proteins and / or polypeptides in cell culture is provided. In accordance with the present invention, cells expressing the protein or polypeptide of interest are grown in media that comprise a glycolysis-inhibiting substance. Additionally and / or alternatively, cells expressing the protein or polypeptide of interest are grown in media in which glutamine is limited. The use of such a system allows high levels of protein or polypeptide production and lessens accumulation of undesirable metabolic waste products such as lactate. Proteins and polypeptides expressed in accordance with the present invention may be advantageously used in the preparation of pharmaceutical, immunogenic, agricultural or other commercial compositions.

Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a fatty acid metabolism inhibitor, a glycolytic inhibitor, and / or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an oxirane carboxylic acid, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and / or an antibody against UCP and / or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.

The present invention generally relates to systems and methods for treating inflammatory and proliferative diseases, and wounds, using a combination of (1) fatty acid metabolism inhibitors and (2) glycolytic inhibitors and / or UCP and / or Fas inhibitors or antibodies. More particularly, the invention combines an oxirane carboxylic acid compound, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and / or an antibody against UCP and / or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers (i.e., cancers resistant to conventional cancer drug therapies).

Glycolytic inhibitors are useful in the treatment of solid tumors by attacking anaerobic cells at the center on the tumor. 2-deoxyglucose, oxamate and various analogs thereof are identified as having a natural selective toxicity toward anaerobic cells, and will significantly increase the efficacy of standard cancer chemotherapeutic and radiation regiments as well as new protocols emerging with anti-angiogenic agents.

Glycolytic inhibitors are useful in the treatment of solid tumors by attacking anaerobic cells at the center on the tumor. 2-deoxyglucose, oxamate and various analogs thereof are identified as having a natural selective toxicity toward anaerobic cells, and will significantly increase the efficacy of standard cancer chemotherapeutic and radiation regiments as well as new protocols emerging with anti-angiogenic agents.

Disclosed is an anticancer pharmaceutical composition comprising phenformin or a pharmaceutically acceptable salt thereof, and a glycolysis inhibitor, particularly, 2-deoxy-D-glucose as active ingredients. These ingredients act in synergy with each other, thus exhibiting more potent inhibitory activity against the growth of cancer cells, compared to individual ingredients. Also, the synergistic anticancer activity allows the individual drugs to be used in lower amounts, which leads to a reduction in the occurrence of adverse effects. In addition, the time-lag release or administration of the ingredients decreases blood lactic acid levels to significantly mitigate the adverse effect of lactic acidosis, as well as exerting high anticancer effects. Particularly, the pharmaceutical composition can be formulated to dosage forms effective for therapy, increasing the drug compliance of the subject.

The present invention discloses anti-cancer compositions, and associated methods, including an anti-cancer composition comprising: a cellular energy inhibitor having the structure according to formula Iwherein X is selected from the group consisting of: a nitro, an imidazole, a halide, sulfonate, a carboxylate, an alkoxide, and amine oxide; and R is selected from the group consisting of: OR′, N(R″)2, C(O)R′″, C1-C6 alkyl, C6-C12 aryl, C1-C6 heteroalkyl, a C6-C12 heteroaryl, H, and an alkali metal; where R′ represents H, alkali metal, C1-C6 alkyl, C6-C12 aryl or C(O)R′″, R″ represents H, C1-C6 alkyl, or C6-C12 aryl, and R′″ represents H, C1-C20 alkyl or C6-C12 aryl. The anti-cancer composition can additionally comprise at least one sugar, which stabilizes the cellular energy inhibitor by substantially preventing the inhibitor from hydrolyzing. Also, the anti-cancer composition can comprise a glycolysis inhibitor. Further, the anti-cancer composition can comprise a biological buffer that is present in an amount sufficient to at least partially deacidify the cellular energy inhibitor and neutralize metabolic by-products of the cellular energy inhibitor.

Methods and products for treating proliferative diseases, and wounds, using as a pharmacon an autophagy inhibitor, a glycolytic inhibitor, and / or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherapeutic agents. In some embodiments, the invention combines a 4-aminoquinoline, exemplified by chloroquine, with a glycolytic inhibitor, exemplified by 2-deoxy-D-glucose and anti-VEGF antibodies. The systems and methods of the invention may be used to treat drug-resistant or multi-drug resistant cancers.

The present invention relates to compositions and methods for treating cancer, by administering a combination comprising a jasmonate derivative (e.g., methyl jasmonate or a compound of any of formulae I through VII or any of the jasmonate derivatives exemplified by such formulae) and at least one other agent selected from a chemotherapeutic agent (e.g., a nitroso-urea, a platinum compound, a taxane derivative, an antitumor antibiotic) and an inhibitor of glycolysis (e.g., 2-deoxy-D-glucose). The jasmonate derivative and the at least one other agent together provide a therapeutic effect, which is preferably synergistic (cooperative).

Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a fatty acid metabolism inhibitor, a glycolytic inhibitor, and / or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherpeutic agents. In preferred embodiments, the invention combines an oxirane carboxylic acid, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and / or an antibody against UCP and / or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.

The invention provides a new application of a glycolytic inhibitor. Based on the increased glycolytic level in a rapamycin target protein highly-activated cell, and the significantly inhibited growth of a mTOR activated cell due to the application of a glycolytic inhibitor, the invention provides an application of the glycolytic inhibitor in preparing medicaments for treating mammal tumors or diseases caused by activation of mammal target protein and an upstream pathway thereof. The glycolytic inhibitor can specifically inhibit the glycolytic pathway, can pertinently treat tumors caused by mTOR activation, and has less toxic side effects, so better curative effect can be achieved.

The invention generally relates to systems and methods for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using a bifunctional compound that inhibits both fatty acid metabolism and glycolysis. Thus, the invention links a fatty acid metabolism inhibitor to a glycolysis inhibitor. More particularly, the invention provides novel bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a glucose derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of 2-deoxy-D-glucose.

The present invention relates to methods, compositions, and diagnostic tests for treating and diagnosing proliferative disorders, such as cancel-, that result in dysregulation of malic enzyme 2. In particular, the methods and compositions include monotherapy with malate, or a derivative thereof, as well as combination therapy, such as malate, or a derivative thereof, combined with another therapeutic agent, such as a malic enzyme 2 inhibitor, an antineoplastic agent, a glycolysis inhibitor, an antiangiogenic agent, an immunomodulatory agent, an antibody, or a cytokine.

The invention relates to an application of an energy metabolism-interfering drug in recurrence of pancreatic cancer. Specifically, the invention discloses a pharmaceutical composition which comprisescarboxyamidotriazole or a pharmaceutically acceptable salt thereof and a glycolytic inhibitor. Carboxyamidotriazole and the glycolysis inhibitor are used for blocking from oxidative phosphorylation and glycolysis ways respectively, so the content of ATP in cells can be significantly reduced, the vitality and self renewal of pancreatic cancer stem cells are seriously destroyed, and thus the recurrence of pancreatic cancer after drug treatment can be delayed.

The invention relates to an ursolic acid derivative and an application thereof, in particular to an ursolic acid derivative having the functions of tumor cell apoptosis resisting and metabolism double targeting and an application thereof. The ursolic acid derivative is formed after dichloroacetylation of the ursolic acid and the derivative of the ursolic acid. Formula I, formula II and formula III of the ursolic acid derivative are as shown in the specification. The invention further provides the application of the ursolic acid derivative to preparation of anti-tumor drugs.

The invention provides an antitumor medicament. The antitumor medicament is a glycolysis inhibitor, and the glycolysis inhibitor is 3-bromacetone acid ester. According to the antitumor medicament, the aim of killing tumor stem cells is fulfilled by efficiently blocking the energy metabolism of the tumor stem cells. The invention further provides application of the glycolysis inhibitor to the preparation of antitumor medicaments, a preparation method of the glycolysis inhibitor and application of the glycolysis inhibitor to tumor treatment.

A method of measuring HbA1c is provided that, even with a whole blood sample after storage, measurement accuracy substantially equal to a whole blood sample right after collection can be maintained. Whole blood is stored in a presence of a glycolytic inhibitor and protease is added to the stored whole blood sample to cleave hemoglobin in the whole blood sample. Then a glycated part of a hemoglobin fragment thereby obtained is treated with fructosyl amine oxidase. Thereafter, a glycation degree of HbA1c is determined by measuring a redox reaction between the glycated part and the fructosyl amine oxidase. Further, instead of storage of the whole blood in a presence of the glycolytic inhibitor, a strong electrolyte substance such as KCl, K2SO4, KNO, NaCl, Na2SO4, NaNO, MgCl2, MgSO4, Mg(NO)2, etc. is added to the whole blood after storage and a protease treatment is performed in a presence of the strong electrolyte substance. According to these methods, fluctuation in a measurement value of HbA1c due to storage of the whole blood can be avoided.

Methods and compositions for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using combination of compounds, or a bifunctional compound, that inhibits both fatty acid metabolism and glycolysis. In particular, the invention combines or links a glycolysis inhibitor that is, or that is derived from, hypoglycin A (also referred to as hypoglycine A) and a fatty acid metabolism inhibitor. Preferably, the invention provides bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a hypoglycin A derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of hypoglycin A.

Methods and compositions for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using combination of compounds, or a bifunctional compound, that inhibits both fatty acid metabolism and glycolysis. In particular, the invention combines or links a glycolysis inhibitor that is, or that is derived from, hypoglycin A (also referred to as hypoglycine A) and a fatty acid metabolism inhibitor. Preferably, the invention provides bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a hypoglycin A derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of hypoglycin A.

The invention discloses application of a glycolysis inhibitor in preparation of a medicine for preventing and treating porcine reproductive and respiratory syndrome virus infection. Researches find that the glycolysis inhibitor can be used for preventing and treating porcine reproductive and respiratory syndrome virus infection; particularly, the replication of the PRRSV in a pig body can be remarkably inhibited by orally taking a lactic dehydrogenase inhibitor, namely sodium oxalyl or pedioxanthin; the new application of the glycolysis inhibitor, especially the lactic dehydrogenase inhibitor(sodium oxalyl or peptin), as the PRRSV antagonist is discovered for the first time, and the anti-PRRSV drug effect of the glycolysis inhibitor is clear in component, controllable in quality, safe andnon-toxic, so that the glycolysis inhibitor has a good application prospect in the aspect of preventing and treating porcine reproductive and respiratory syndrome.

Methods for treating a subject determined to have a cancer comprising a heterozygous inactivation of a housekeeping gene (or a homozygous deletion of a functionally redundant housekeeping gene) by treating the subject with an inhibitor of the gene. For example, a subject having a cancer with an ENO gene deletion can be treated with a glycolysis inhibitor, such as an enolase inhibitor. In some aspects, a subject having a cancer with an ARS gene deletion can be treated with an ARS inhibitor.

The present invention relates to a sweetener composition for preventing or treating obesity containing, as active ingredients, a glucose or D-fructose absorption inhibiting component and a sugar hydrolysis inhibiting sugar or sugar alcohol.

The invention provides a reagent kit for detecting the condition of vascular endothelial cells, a medicine for treating abnormality of the vascular endothelial cells, and a reagent kit which is used for treating diseases relevant to the vascular endothelial cells and includes a glycolysis inhibitor medicine and other medicines for treating the diseases relevant to the vascular endothelial cells. The invention also provides an application of a PFKFB3 enzyme detection reagent to detection of the condition of the vascular endothelial cells and an application of a glycolysis inhibitor to preparation of medicines or reagent kits for treating the abnormality of the vascular endothelial cells of an examinee. The health status or the prognosis prospects can be judged according to the state of thevascular endothelial cells, the abnormality of the vascular endothelial cells can be treated through the glycolysis inhibitor, complications, such as after cancer chemotherapy and hematopoietic stem cell transplantation can be reduced, the treatment risk is reduced, the quality of life is improved, the case-fatality rate is reduced, the medical treatment expenses are reduced, the clinical diagnosis and treatment level of the diseases relevant to the abnormality of the vascular endothelial cells is increased, and prognosis is improved.

A drug combination comprising at least one inhibitor of tyrosine kinase and at least one inhibitor of glycolysis. The drug combination may be used in the treatment of proliferative disorders, such as liver or colon cancer. The inhibitor of tyrosine kinase may be an inhibitor of at least one of the tyrosine kinases Fer and FerT.

The present invention relates to a sweetener composition for preventing or treating obesity containing, as active ingredients, a glucose or D-fructose absorption inhibiting component and a sugar hydrolysis inhibiting sugar or sugar alcohol.