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105 results about "Cathepsin B" patented technology

Cathepsin B is in humans encoded by the CTSB gene. Cathepsin B belongs to a family of lysosomal cysteine proteases and plays an important role in intracellular proteolysis. Upregulation of cathepsin B is found in premalignant lesions and various pathological conditions, as well as cancers.

Micromolecular conjugate based on RGD polypeptide-chemotherapy drug and nanometer prodrug system thereof

The invention relates to a micromolecular conjugate based on RGD polypeptide-chemotherapy drug and a self-assembly nanometer prodrug system thereof, and belongs to the technical field of biological medicine and nanometer medicine. The nanometer prodrug system has the main advantages that (1) the system is formed by RGD polypeptide and an anti-tumor drug through direct covalent connection via micromolecular connecting arms, and the drug loading capacity of the system is improved; (2) the conjugate is self-assembled into a nanometer prodrug using the drug as a hydrophobic inner core and the RGD polypeptide as a hydrophilic outer shell, the active targeting on tumor cells and tumor new vessels is realized through the ligand-receptor mutual action, and the endocytosis is promoted; (3) the stability of the nanometer prodrug system in the body circulation can be ensured through thioether bonds, reduction sensitive bonds and cathepsin B sensitive bonds, and the cytotoxic drug is released when the nanometer prodrug system reaches the tumor microenvironment; and (4) the micromolecular conjugate instead of a macromolecular material is used as a carrier, so that the nanometer prodrug system can favorably and better penetrate into the tumor tissues and cells to achieve better anti-tumor effects.
Owner:PEKING UNIV

Preparation and application of cathepsin B activation type targeted anti-tumor polypeptide

The invention discloses a novel cathepsin B activation type targeted anti-tumor polypeptide m(KLA)-iRGD, the molecular weight is 2570, and the amino acid sequence is D(KLAKLAKKLAKLA)KGGCRGDKGPDC. The polypeptide is formed by KLA peptide and iRGD peptide through flexible connexon Gly-Gly. The sequence of the KLA peptide is KLAKLAKKLAKLAK, and amino acids of the KLAKLAKKLAKLA sequence at the N terminal of the polypeptide are all D-amino acids. The sequence of the iRGD peptide is CRGDKGPDC. The polypeptide has the advantage that the tumor targeted peptide iRGD and the apoptosis promoting peptide KLA are connected into the new polypeptide m(KLA)-iRGD for the first time. The polypeptide m(KLA)-iRGD can be specifically combined with alphaVbeta3 and NRP-1 receptors and enter tumor cells, mitochondrial apoptosis is initiated after the polypeptide is activated by intracellular cathepsin B (CTSB), tumor cells are selectively killed, and growth and migration of tumors are remarkably inhibited. Under the same concentration, a polypeptide m(KLA)-iRGD comparison peptide has higher tumor targeting and higher capacity of inhibiting tumor growth and migration. Meanwhile, the polypeptide m(KLA)-iRGD has no obvious toxicity on mouse weight and vital organs, and a solid foundation is laid for further clinical research and application.
Owner:SUN YAT SEN UNIV

Low-molecular-weight L-polyglutamine-mitomycin C as well as synthesis method and applications thereof

The invention relates to a low-molecular-weight L-polyglutamine-mitomycin C with the structural formula shown in the specification and the molecular weight of 1882Da-5892Da, wherein n is equal to 1500-6000. A synthesis method comprises the following steps: dissolving polyglutamic acid into water, stirring and then separating with sephadex chromatography to take polyglutamic acid with molecular weight of 1500-6000, performing freeze-drying and then adding dioxane, N-hydroxysuccinimide, a condensing agent and an acid-binding agent, evaporating out solvents and dissolving chloroform, washing with diluted hydrochloric acid and then evaporating the chloroform layer to dryness, adding a product to HBS buffer, adding mitomycin C under stirring, and then stirring reaction liquid and concentrating to dryness, and separating by using silicon gel column chromatography to obtain the low-molecular-weight L-polyglutamine-mitomycin C. The mitomycin C is modified by utilizing low-molecular-weight L-polyglutamine, and cannot penetrate cornea due to large molecular weight; the low-molecular-weight L-polyglutamine-mitomycin C can be accumulated in pterygium tissues through EPR effect; and the release of mitomycin C can be mediated by cathepsin B enzyme in the pterygium tissues so as to achieve the treatment effect.
Owner:XIAN MEDICAL UNIV

Fluorescence probe and synthetic method thereof and application of fluorescence probe in circulating tumor cell detection

The invention discloses a fluorescence probe and a synthetic method thereof and an application of the fluorescence probe in circulating tumor cell detection. The fluorescence probe comprises a fluorescence group, a cathepsin B substrate and folic acid molecules, the fluorescence group is connected with the cathepsin B substrate through a self-degradation bond, and then is connected with the folic acid molecules; the fluorescence group is excited by the excitation light under a dissociation state, and then is enable covalent connection with other molecules for quenching. The fluorescence probe is the switching-mode fluorescence probe having a spontaneous cascade amplification function, can be used for avoiding complex operation steps of antibody or nucleic acid detection during a circulating tumor cell detection process, is used for an automatic biochemical analyzer as a matching reagent, is in favor of promoting automation detection of tumor cells, and has the advantages of simple and convenient operation, short time consuming, and low apparatus requirement. The fluorescence probe can be used for positioning minimal tumor cells and tubercle in clinical operation, and has wide application prospect and large market value.
Owner:THE FIFTH AFFILIATED HOSPITAL OF GUANGZHOU MEDICAL UNIV
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