18 results about "Cisplatin resistance" patented technology

The application discloses a vanadium-based nano drug capable of reversing cisplatin drug resistance through multiple targets and a preparation method thereof.The preparation method of the drug comprises the following steps: (1) preparation of mesoporous silica; (2) vanadium ion doping; (3) surface amino modification; (4) loading of a Pt(IV) prodrug; and (5) PDGF modification on the surface of the drug-loaded nanoparticles, thereby obtaining the vanadium-based nano drug.The vanadium-based nano drug prepared by the method has excellent performance, can reverse cisplatin drug resistance through multiple targets, and provides a new idea for constructing a lung cancer precision treatment scheme for reversing cisplatin drug resistance through multiple targets.

The invention relates to application of an antibody for detecting phosphorylation of a Tyr165 site of CPT1A protein in preparation of a product for detecting the sensitivity of head and neck squamous cell carcinoma to cis-platinum. The CPT1A protein Tyr165 site is obtained through cisplatin stress and phosphorylation mass spectrometry identification, the phosphorylation level of the CPT1A protein Tyr165 site is increased along with the increase of cisplatin stress time, and the drug resistance degree of the head and neck squamous cell carcinoma to cisplatin is enhanced. Therefore, the CPT1A protein Tyr165 site is phosphorylated to serve as the biomarker of the cis-platinum drug resistance of the head and neck squamous cell carcinoma. The invention further provides a specific antibody for phosphorylation of the Tyr165 site of the CPT1A protein, the antibody is used for detecting whether the Tyr165 site of the CPT1A protein is phosphorylated or not, whether the head and neck squamous cell carcinoma has drug resistance to cis-platinum or not is determined, and a basis is provided for targeted selection of chemotherapeutic drugs for the head and neck squamous cell carcinoma.

The invention discloses application of DNASE1L3, CYP4B1 and / or FAM65B in enhancing the cisplatin sensitivity of nasopharyngeal carcinoma, and belongs to the field of biological medicine. The invention proves that overexpression of the DNASE1L3 gene, the CYP4B1 gene and / or the FAM65B gene can obviously inhibit the activity of nasopharyngeal carcinoma cells and obviously enhance the sensitivity of the nasopharyngeal carcinoma cells to cis-platinum. An in-vivo xenotransplantation tumor model further proves that the in-vivo anti-tumor effect of the cis-platinum can be remarkably enhanced by combining the overexpressed DNASE1L3 gene, the CYP4B1 gene or the FAM65B gene with the cis-platinum, and tumor growth is effectively inhibited. The invention provides a brand new molecular target for overcoming the cisplatin resistance of nasopharynx cancer, provides a new strategy for preparing high-efficiency and low-toxicity nasopharynx cancer treatment drugs and cisplatin sensitizers, and has important clinical application prospects and market values.

The invention belongs to the technical field of biological medicine, and particularly discloses a combined tumor marker for noninvasive detection of oral cancer and application of the combined tumor marker. The invention provides application of a reagent for detecting a biomarker in preparation of a product for diagnosing or predicting oral cancer. The biomarker is an RBMX gene and / or an NEK2 gene. The invention finds that the two oral cancer carcinogenic key molecules are significantly highly expressed in oral cancer tissues, and the activity, migration and invasion ability of oral cancer cells can be inhibited by knocking down the expression of RBMX or NEK2, and the cis-platinum drug resistance of the oral cancer cells can be inhibited. According to the invention, RBMX or NEK2 is taken as a tumor marker to detect the oral cancer and has good diagnostic efficacy, and the RBMX and the NEK2 are combined for use, so that the sensitivity and the specificity of diagnosis can be further improved, and the risk of the oral cancer can be more comprehensively judged. The invention also provides application of the two pathogenic factors as inhibition targets in preparation of drugs for oral cancer.

The present invention relates to a composition for the prevention or treatment of cisplatin-resistant cancer comprising an inhibitor of DUSP23 expression or activity as an active ingredient. It was found that DUSP23 expression is upregulated in cell clusters exhibiting characteristics of cancer stem cells, and that knocking down DUSP23 significantly reduces cell cluster formation as well as decreases the expression of SOX2, a major stem cell marker. Furthermore, DUSP23 expression was increased in lung cancer cells that had developed cisplatin resistance, and it was confirmed that the downregulation of DUSP23 inhibits self-renewal and invasive capabilities during the induction of cancer cell death. In addition, it was confirmed that DUSP23 plays an important role in promoting cancer stem cell characteristics through SOX2 expression. In conclusion, it has been shown that targeting DUSP23 can be a promising therapeutic strategy to overcome anticancer drug resistance in lung cancer, and the composition of the present invention is expected to be usefully utilized as a treatment for lung cancer cells with cisplatin resistance.

The invention discloses a gold (I) complex containing an alkyne ligand, a preparation method of the gold (I) complex and application of the gold (I) complex in preparation of antitumor drugs, the gold (I) complex has a structure as shown in a general formula I, a phosphorus ligand is selected from diphenyl-2-pyridine phosphine or tricyclohexylphosphine, and Rx is an organic group selected from a specific alkyne ligand; according to the preparation method, chloroauric acid is taken as an initial raw material, sequentially reacts with dimethyl sulfide and an organic phosphine ligand, and finally is coupled with an alkyne ligand under an alkaline condition, so that the steps are simple and convenient, the conditions are mild, and the yield is high; in-vitro activity experiments show that the complex shows remarkable proliferation inhibition activity on ovarian cancer, malignant melanoma, non-small cell lung cancer and cisplatin-resistant cell strains thereof, the effect of the complex is superior to that of cisplatin and auronafine, and a candidate compound is provided for developing a novel targeted anti-tumor drug for overcoming the drug resistance of platinum drugs.

The invention belongs to the technical field of biological medicines, and particularly discloses a nano-drug for oral cancer as well as a preparation method and application of the nano-drug. The nano-drug provided by the invention is a drug-loaded mesoporous polydopamine nano-particle wrapped by a lipidosome modified by RGD peptide; wherein the load components of the mesoporous polydopamine nanoparticles comprise a cis-platinum drug and an RBMX gene expression inhibitor. The molecular RBMX related to regulation and control of oral cancer progress and cis-platinum drug resistance is screened, a nano biomimetic material drug loading system is constructed to load si-RBMX and cis-platinum to synergistically resist oral cancer treatment, and a novel nano drug with strong targeting property, good biological safety and excellent tumor lethality is obtained. The invention also provides a preparation method and application of the nano-drug.

The invention belongs to the technical field of tumor drug research, and particularly relates to application of 2-phenyl oxindole in preparation of a drug for reversing cis-platinum drug resistance or treating tumors. In-vitro experiments and in-vivo experiments prove that the 2-phenyl oxoindole can effectively inhibit proliferation of triple negative breast cancer cells and can remarkably improve the sensitivity of the cells to cis-platinum with a series of concentrations, and pathological staining results of visceral organs and tissues of mice show that the 2-phenyl oxoindole can effectively inhibit proliferation of the triple negative breast cancer cells and remarkably improve the sensitivity of the cells to cis-platinum with a series of concentrations. The 2-phenyl oxoindole does not cause obvious injury to main organs such as liver, kidney and the like.

The application discloses an antibody capable of specifically recognizing acetylation of ribosome biogenesis factor 1 protein at the 1147th position, and a preparation method and application thereof. According to the protein sequence and modification type of ribosome biogenesis factor 1, two modified antigen polypeptides A and B are designed. It is detected that the antibody obtained by immunizing animals by using the two polypeptides has high specificity and affinity, and can accurately recognize the acetylation modification form of the 1147th position of BMS1, and avoid recognizing the unmodified form or other modification sites. The antibody is suitable for various immunological detection methods, has high repeatability, low background, has mass production potential, can be industrialized, and is not only used for evaluating the cisplatin resistance in esophageal cancer treatment, but also used for various scenes such as basic research, disease mechanism analysis, biomarker development, drug target screening, and has a wide application range.

The invention discloses gold (I) complexes containing benzene ring ligands, a preparation method of the gold (I) complexes and application of the gold (I) complexes in preparation of antitumor drugs. The gold (I) complex has a structure as shown in a general formula I, wherein Rx in the general formula I is a group containing a benzene ring; the preparation method comprises the following steps: enabling chloroauric acid to react with dimethyl sulfide to obtain an intermediate Au (Me2S) Cl, then enabling the intermediate Au (Me2S) Cl to react with an organic phosphine ligand to generate a phosphine-chlorine-gold intermediate, and finally enabling the phosphine-chlorine-gold intermediate to react with a sulfydryl ligand under an alkaline condition to obtain a target product. The series of complexes show remarkable proliferation inhibition activity on ovarian cancer cells, melanoma cells, non-small cell lung cancer cells and cis-platinum drug-resistant strains thereof in vitro, the effect of the complexes is superior to that of cis-platinum and Jinnofen, and candidate compounds are provided for developing novel anti-drug-resistant tumor drugs.

The invention relates to the technical field of tongue squamous cell carcinoma cis-platinum chemotherapy treatment, and provides application of a DNPEP inhibitor in preparation of a medicine for reducing the tolerance of cis-platinum to tongue squamous cell carcinoma cells. The DNPEP inhibitor is applied to preparation of the medicine for reducing the tolerance of the cis-platinum to the tongue squamous carcinoma cells, and the tolerance of the tongue squamous carcinoma cells to the cis-platinum is reduced by inhibiting expression of DNPEP in the tongue squamous carcinoma cells. The DNPEP can be used as a treatment target for overcoming the chemotherapy drug resistance of the tongue squamous carcinoma, and the DNPEP inhibitor and cis-platinum are combined for treating the tongue squamous carcinoma, especially for treating patients with cis-platinum resistance type tongue squamous carcinoma.

The invention belongs to the technical field of medicinal chemistry, and particularly discloses a platinum (IV) prodrug with a small molecule TrxR inhibitor as a ligand and a preparation method and application of the platinum (IV) prodrug, the synthesized platinum (IV) prodrug shows good anti-proliferative activity on cancer cells such as MDA-MB-231, MCF-7, 4T1 and MDA-MB-231 / CDDP, and the anticancer activity of a compound 6b is optimal. In an in-vivo anti-tumor activity test, the compound 6b can effectively inhibit proliferation of cis-platinum sensitive and cis-platinum drug-resistant triple negative breast cancer xenotransplantation tumors, the tumor inhibition rates of the compound 6b are 73.8% and 66.3%, and the curative effect of the compound 6b is superior to that of a positive drug cis-platinum. In addition, the compound 6b can effectively inhibit proliferation of homotransplantation tumors of mouse breast cancer cells 4T1, and the tumor inhibition rate of the compound 6b is 76.8% and is obviously higher than that of a cis-platinum treatment group. And the compound 6b shows a powerful immunoregulation effect in vivo, which indicates that the design successfully realizes effective combination of chemotherapy and immunotherapy, and the compound disclosed by the invention has potential application prospects in treatment of triple negative breast cancer.

The invention belongs to the technical field of drug delivery systems, and particularly relates to a multifunctional PEG lipid derivative and lipid nanoparticle co-delivery system. The multifunctional PEG (Polyethylene Glycol) lipid derivative is DSPE-PEG2000-R8-FRRG-IMI (Distearoyl Sulfonate Polymer). According to the lipid nanoparticle co-delivery system, lipid nanoparticles serve as a carrier, and siRNA and a cis-platinum prodrug are entrapped in the lipid nanoparticles. Wherein the lipid nanoparticles are prepared from an ionizable cationic lipid, DSPC (Distearoyl Pyrrolidone), cholesterol and a PEG (Polyethylene Glycol) lipid derivative, and the PEG lipid derivative is DSPE-PEG2000-R8-FRRG-IMI (Distearoyl Pyrrolidone Polyethylene Glycol 2000-R8-FRRG-IMI). The lipid nanoparticle co-delivery system not only can realize co-loading of a cis-platinum prodrug and siRNA and overcome cis-platinum drug resistance while killing tumors, but also has an active targeting property, stimulation responsiveness and an efficient intracellular escape function, and has a remarkable treatment effect on lung adenocarcinoma or breast cancer and the like.

This invention discloses the application of CALD1 protein in the preparation of drugs for treating bladder cancer, belonging to the field of biomedical technology. The application of CALD1 protein in the preparation of drugs for treating bladder cancer: This invention, through the construction of drug-resistant cell lines using in vivo animal models and combined with clinical sample analysis, first discovered that CALD1 is highly expressed in cisplatin-resistant bladder cancer cells and is associated with poor patient prognosis, demonstrating that CALD1 is a potential novel target for treating cisplatin resistance in bladder cancer, which is beneficial for further research on the mechanism of tumor chemotherapy resistance caused by abnormal activation of CALD1.

The present invention relates to a composition for preventing or treating cancer, the composition comprising cisplatin and narciclasine or an analog thereof. In the present invention, it was found that co-administration of cisplatin and narciclasine or a narciclasine analog has synergistic anticancer effects. It was found that narciclasine increases cisplatin sensitivity by inducing apoptosis in cisplatin-resistant NSCLC tumor spheroids, and co-administration of cisplatin and narciclasine weakens the efficacy of MCL1 by inhibiting MCL1 translation and promotes the degradation of MCL1 by inducing NOXA. In addition, it was found that co-administration of even low concentrations of cisplatin with narciclasine or a narciclasine analog has excellent anticancer effects, and thus the composition comprising cisplatin and narciclasine or a narciclasine analog according to the present invention can be applied for the purposes of overcoming chemoresistance to cisplatin and improving treatment outcomes.

The application relates to the technical field of biochemical detection, and discloses a nucleic acid detection composition for screening of cisplatin drug resistance of non-small cell lung cancer, which comprises a specific amplification primer pair for targeting an NFAT2 gene, a TaqMan detection probe, a hot-start Taq DNA polymerase and a reaction buffer solution; the reaction buffer solution comprises tetrahydro pyrimidine and tetramethylammonium chloride, and the molar ratio of the two is controlled to be between 3.2:1 and 3.8:1 to construct a micro function phase structure. The application blocks cisplatin through a dense hydration shell layer formed by tetrahydro pyrimidine on the surface of an enzyme, and eliminates the base pair hydrogen bond energy difference of a nucleic acid major groove by using tetramethylammonium chloride, so that efficient protection of polymerase activity and regulation of primer hybridization specificity are simultaneously realized in a single reaction system, and the sensitivity and accuracy of drug resistance gene detection in complex clinical samples are improved.

This invention provides the use of a reagent for detecting LMTK3 protein, a combination drug, and the use of LMTK3 inhibitors in combination with platinum-based drugs, belonging to the field of pharmaceutical technology. This invention is the first to discover that LMTK3 is significantly highly expressed in ovarian cancer patients compared to healthy individuals; and that LMTK3 is significantly highly expressed in cisplatin-resistant ovarian cancer patients compared to cisplatin-sensitive ovarian cancer patients. Detecting the expression level of LMTK3 in ovarian tissue can differentiate between ovarian cancer patients and healthy individuals, as well as between cisplatin-sensitive and cisplatin-resistant ovarian cancer patients. Furthermore, this invention also discovers that combining LMTK3 inhibitors with platinum-based drugs to treat platinum-resistant ovarian cancer can effectively increase the sensitivity of platinum-based drugs to drug-resistant ovarian cancer cells, improve the therapeutic efficacy of platinum-based drugs for ovarian cancer, and lay the foundation for developing new drugs to reverse drug resistance.

The invention belongs to the technical field of biological medicine, and discloses an application of polyphyllin II in preparation of a medicine for treating cis-platinum resistant non-small cell lung cancer, the medicine comprises polyphyllin II as an active component and one or more pharmaceutically acceptable auxiliary materials, the polyphyllin II can effectively inhibit proliferation of cisplatin-resistant non-small cell lung cancer cells, and the action mechanism of the polyphyllin II is to activate integrin pathways, especially integrin alpha1 (ITGA1), integrin alpha5 (ITGA5) and / or integrin alpha11 (ITGA11). A further research shows that the polyphyllin II plays a therapeutic role by inhibiting the phosphorylation level of FAK and / or Src and regulating the expression of cytoskeleton related proteins such as RhoA and Cofilin, specifically, the expression of RhoA protein and the phosphorylation of Cofilin protein are inhibited. The invention provides a new mechanism explanation and theoretical basis for the application of the polyphyllin II in preparing the medicine for treating the cis-platinum drug-resistant non-small cell lung cancer, and provides a new treatment strategy and medicine selection for overcoming the clinical problem of cis-platinum drug resistance.