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3 results about "Thymidylate synthase" patented technology
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Thymidylate synthase (TS) (EC 2.1.1.45) is an enzyme that catalyzes the conversion of deoxyuridine monophosphate (dUMP) to deoxythymidine monophosphate (dTMP). Thymidine is one of the nucleotides in DNA. With inhibition of TS, an imbalance of deoxynucleotides and increased levels of dUMP arise. Both cause DNA damage.
Pharmaceutical composition for realizing co-inhibition of tk1 / ts dual targets and use thereof
The application provides a drug composition for realizing TK1 / TS double-target co-inhibition and application thereof. The creativity is derived from the key mechanism disclosed by the inventors for the first time, that is, thymidine kinase 1 (TK1) and thymidylate synthase (TS) present co-expression up-regulation in the DNA synthesis period. In-vivo experiments show that the tumor inhibition rate of the drug composition is significantly higher than that of any single drug, synergistic effect is realized, and the drug composition can be used for treating solid tumors or hematological malignancies.
Owner:NANKAI UNIV
Thymidylate synthase targeting PROTAC molecule and application thereof
PendingCN121991079ANovel and diverse structureEfficient degradationOrganic active ingredientsOrganic chemistryDiseaseFolic acid antagonist
The invention provides preparation and application of a PROTAC molecule for targeted degradation of thymidylate synthetase, and relates to the field of medicine. The invention relates to a novel folic acid PROTAC molecule which is prepared based on a pyrrolo [2, 3-d] pyrimidine multi-target folic acid antagonist by utilizing connection chains with different lengths and types to be connected with an E3 ligase Cerebron (CRBN) ligand, and an application of the novel folic acid PROTAC molecule in folic acid related diseases such as cancers. The compound has a structure as shown in a general formula I,
Owner:HEBEI MEDICAL UNIVERSITY
Pharmaceutical composition for realizing TK1 / TS double-target co-inhibition and application thereof
ActiveCN121371188AOrganic active ingredientsAntineoplastic agentsIn vivo experimentPharmaceutical drug
The invention provides a pharmaceutical composition for realizing TK1 / TS double-target co-inhibition and application of the pharmaceutical composition. The pharmaceutical composition is creatively derived from a key mechanism disclosed by the inventor for the first time: thymidine kinase 1 (TK1) and thymidylate synthase (TS) present up-regulated co-expression in a DNA synthesis period, in vivo experiments show that the tumor inhibition rate of the pharmaceutical composition is significantly higher than that of any single drug, synergistic interaction is achieved, and the pharmaceutical composition can be used for treating solid tumors or hematological malignant tumors.
Owner:NANKAI UNIV