5 results about "Protein kinase A" patented technology

The application discloses a covalent polypeptide inhibitor targeting protein kinase A, a conjugate, a kit, a pharmaceutical composition and application. The general formula of the covalent polypeptide inhibitor is Z1-Seq-Z2; wherein Seq is an amino acid sequence; the C-terminal of Seq comprises a pseudo-substrate recognition motif recognized by protein kinase A, a non-natural amino acid with a covalent reaction group, and can be covalently crosslinked with a Cys200 residue on a catalytic subunit of protein kinase A; Z1 is selected from hydrogen, an acyl group, a fluorescent group, biotin, an isotopic tag or a biological ortho-reaction group; and Z2 is selected from a hydroxyl group, an amino group, a cell-penetrating peptide or a stabilization modification group. The covalent polypeptide inhibitor can strongly and irreversibly inhibit PKA activity, and can be used as an active probe to specifically label active PKA in a complex biological sample, and is used for biological research and drug development.

The present invention relates to a method for treating cancer exhibiting high expression of SFRP4. In particular, the present invention was developed through intensive research to identify a highly reliable treatment method for stem cell-type gastric cancer that has the worst prognosis and for which effective therapeutic agents are difficult to develop. As a result, it was confirmed that the cancer stem cell properties decreased when Wnt protein was injected to the MKN1 gastric cancer cell line, which exhibits high expression of SFRP4. In addition, it was confirmed that secreted frizzled-related protein 4 (SFRP4), phosphorylated and secreted by protein kinase A (PKA) can form a complex with β-catenin and TCF4 to increase transcription of Wnt target genes, and by inhibiting PKA to prevent phosphorylation of SFRP4, a decrease in cancer stem cell properties was observed, which leads to the completion of the present invention. The invention can be advantageously used as a novel therapeutic agent for stem cell-type gastric cancer.

The compounds and methods of the present disclosure exhibit induce Ucp1 transcription, enhance of mitochondrial respiration, activate protein kinase A, increase lipolysis, and increase p38 MAPK phosphorylation in cells, particularly brown adipocytes and white adipocytes. They also protect primary cardiomyocytes against hypertrophy induced by adrenergic agonists. Such compounds and methods are useful in the treatment and prevention of conditions such as obesity and associated complex metabolic, endocrine, and hemodynamic changes, as well as related conditions as dyslipidemias, cardiovascular disease, and type 2 diabetes.

This invention discloses a logic-responsive biomolecule carrier based on a phase separation system, its construction method, and its applications. The carrier is based on the attraction between cationic peptides with different logic responses and negatively charged biomolecules such as DNA or RNA, driving liquid-liquid phase separation and forming droplet-like particle structures. The carrier of this invention can selectively use protein kinase A (PKA) to phosphorylate peptides and use matrix metalloproteinases (MMPs) or glutathione (GSH) to cleave the peptide chain, thereby changing the charge density of the peptide to control the controlled release of biomolecules. It exhibits excellent biocompatibility, resistance to enzymatic degradation, and transfection efficiency, enabling effective delivery of biomolecules.

The present invention relates to protein kinase A (PKA) for use in diagnosing autism spectrum disorder (ASD) phenotype 1 in an ASD patient wherein PKA levels are measured in a sample of the patient and wherein ASD phenotype 1 is diagnosed if the measured levels are lower than PKA levels in an age and sex-matched control sample. Additionally, the present invention relates to PKA for use in monitoring variation in ASD severity in an ASD patient, wherein PKA levels are measured in a sample of the patient and an increase in ASD severity is characterized by a decrease of PKA levels compared to PKA levels measured in previous samples of the patient. The present invention also relates to PKA for use in monitoring efficacy of an ASD treatment in an ASD phenotype 1 patient, wherein PKA levels are measured in a sample of the patient and wherein a positive response to the ASD treatment is characterized by an increase of PKA levels in comparison to baseline PKA levels of the patient prior to treatment. Furthermore, the present invention is directed to methods of diagnosing ASD phenotype 1 as well as kits comprising means to measure PKA levels.