117 results about "Prostate cancer cell" patented technology

The invention relates to the field of natural products, in particular to a dimer compound of guaiane type sesquiterpenes and uric acid as well as an extraction and separation method and application of the dimer compound. According to the invention, a new dimer compound of guaiane type sesquiterpene and uric acid is extracted and separated from carpesium abrotanoides in Guizhou, and it is found that the dimer compound has relatively strong anti-tumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharynx cancer, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an optional scheme for broad-spectrum anti-cancer drugs. Moreover, in human prostate cancer cells PC3, human cervical cancer cells Hela, human liver cancer cells HepG2 and human glioma cells U87 which are resistant to paclitaxel, the compound also shows strong anti-cancer activity, which indicates that the compound has the potential of treating patients resistant to paclitaxel.

The invention relates to a 5, 9-di-tert-butyl naphtho-indolizine phenothiazine compound as well as a preparation method and medical application thereof. The compound is efficiently synthesized through Ullmann coupling and palladium-catalyzed intramolecular arylation reaction. In-vitro anti-tumor activity research shows that the compound has remarkable selective inhibitory activity on various human tumor cell lines, and particularly, the inhibitory effect on non-small cell lung cancer A549 cells (IC50 = 0.21 mu M) is improved by two orders of magnitude compared with that of cis-platinum; iC50 (half maximal inhibitory concentration) of other cell lines are as follows: 1.26 mu M of prostate cancer PC-3 cells, 6.78 mu M of liver cancer HepG2 cells, 7.99 mu M of cervical cancer Hela cells and 25.46 mu M of breast cancer MCF-7 cells. Preliminary toxicity experiments prove that the compound has the characteristic of low cytotoxicity. The compound can be used as a novel high-efficiency low-toxicity anti-tumor lead compound, and provides an important structural basis for the development of anti-cancer drugs.

The invention discloses application of a small molecular compound secalonic acid B in inhibiting Skp2 protein and resisting prostate cancer cell metastasis, and belongs to the technical field of medicines. The research finds that secalonic acid B can obviously reduce the half-life period of Skp2, accelerate the degradation speed of Skp2 and reduce the protein level of Skp2 in DU145 cells by enhancing the polyubiquitination process on Skp2 protein. The secalonic acid B induces proteasome degradation of Skp2 through a multi-ubiquitination pathway of a K48 chain, so that tumor cell metastasis is inhibited, and the effect of resisting prostatic cancer is achieved. The invention discloses an action mechanism of secalonic acid B in inhibiting Skp2 protein and resisting prostate cancer cell metastasis, lays a theoretical foundation for research and development of drugs for inhibiting Skp2 protein and treating prostate cancer, and provides a new strategy for treatment of prostate cancer.

The invention discloses an application of a PGK1 inhibitor in preparation of a medicine for treating MYC (myelodysplastic cancer) oncogene amplification type prostate cancer, it is found for the first time that PGK1 is a stable target for patent medicine, the PGK1 inhibitor NG-52 can effectively inhibit growth of MYC oncogene amplification type prostate cancer cells, and the target targets a glycolytic pathway, has small influence on aerobic respiratory metabolism of normal cells in a body, and can be used for preparing a medicine for treating MYC oncogene amplification type prostate cancer. The safety is higher; the mechanism of the target is different from that of current advanced prostate cancer chemotherapy drugs and endocrine therapy drugs, and the target has great potential of combined treatment with current first-line drugs, is easy to popularize and use clinically, and provides better prognosis for MYC gene amplification type prostate cancer patients.

The present invention belongs to the field of biomedicine technology, and relates to the application of the Lnc-FLJ gene in the treatment of castration-resistant prostate cancer. The application of the Lnc-FLJ gene inhibitor in the preparation of prostate cancer drugs. The present invention discovered for the first time that Lnc-FLJ can inhibit the proliferation and autophagy of castration-resistant prostate cancer. Lnc-FLJ is more highly expressed in castration-resistant prostate cancer cells and prostate cancer tissues with higher malignancy. Inhibiting Lnc-FLJ can inhibit the occurrence and development of castration-resistant prostate cancer. The preparation of Lnc-FLJ small molecule inhibitor shRNA is used to treat castration-resistant prostate cancer and cancer insensitive to enzalutamide, thereby inhibiting the AR signaling pathway. The present invention provides new ideas for further studying the pathogenesis of castration-resistant prostate cancer and the function of the Lnc-FLJ gene, and provides a new direction for the development of castration-resistant prostate cancer drugs.

The invention discloses a double-target chimeric antigen receptor capable of simultaneously targeting TLL1 and B7H3, a CAR-T cell and application of the double-target chimeric antigen receptor. The chimeric antigen receptor is a fusion protein which is sequentially composed of Omburt-scFv (SEQ ID NO: 1) targeting B7H3, a CD8 alpha hinge region and transmembrane region, a 4-1BB costimulatory domain, a CD3 zeta signal domain and TLL1-scFv (SEQ ID NO: 6) targeting TLL1 from an N terminal to a C terminal. The TLL1-scFv can be efficiently combined with TLL1 protein, can inhibit a TGF-beta signal channel and block prostate cancer cell migration, and is integrated into CAR of targeted B7H3, so that the double-target CAR-T cell with direct killing and immune microenvironment regulation functions is successfully constructed. The CAR-T cell has a remarkable killing effect on a prostate cancer cell line DU145, can be strongly activated after being co-cultured with a target cell and secretes a large amount of IFN-gamma and TNF-alpha, and shows high immunocompetence. The invention provides a new synergistic immunotherapy strategy for the B7H3-positive prostate cancer with the TGF-beta signal channel activated.

The invention relates to the technical field of biological medicine, and discloses an anti-human 5T4 single-chain antibody, the antibody has the capability of specifically binding to human 5T4 protein, the human 5T4 protein corresponds to TPBG / WAIF1, and the GenBank login number is NP001018111.1; the antibody also has the capability of specifically binding and expressing human 5T4 protein tumor cells, and the human 5T4 protein tumor cells are breast cancer cells MCF-7, prostate cancer cells PC3 or gastric cancer cells MGC-803. By combining single B cell culture with a magnetic bead sorting technology, natural pairing of a heavy chain and a light chain of an antibody can be reserved, and the defect that pairing is damaged by a traditional hybridoma technology is overcome; meanwhile, false positive clones are effectively eliminated through double positive screening of detecting protein binding activity through ELISA and detecting cell binding activity through FACS, the finally obtained targeting 5T4 monoclonal antibody can be specifically combined with human 5T4 protein and tumor cells expressing the protein, and a high-quality targeting molecular basis is provided for research and development of subsequent antibody drugs and CAR-T cell treatment products.

The present application relates to the technical field of biological medicine, in particular to a curcumin analogue, a synthetic method and application thereof. The present application takes curcumin as a lead compound, introduces cyclopropylmethyl, n-butyl and isobutyl in acetylacetone, introduces 4-acetylamino, 3,4-dimethoxy, 2-fluoro and 3-trifluoromethyl on a benzene ring, and designs and synthesizes a series of curcumin analogues. In vitro cytotoxicity experiments show that the killing effect of the newly synthesized curcumin analogue on prostate cancer cells is stronger than that of dimethyl curcumin, and the androgen receptor inhibition effect is also stronger than that of dimethyl curcumin.

The BTK-C isoform is expressed in human breast and prostate cancer cells and it plays a crucial role in epithelial cancer cell survival. BTK-C has a 34 amino acid extension to the n-terminus that facilitate it being palmitoylated on two cysteine residues. This modification localizes BTK-C closer to the cell membrane where it plays a role in improving cancer cell survival, as compared to BTK-A. BTK-C is not found to be expressed in healthy adult cells, whereas BTK-A is necessary for immune cell production. Disclosed herein are alternative kinases besides BTK having similar attributes, which present therapeutic opportunities for the treatment of cancers, especially for solid tumors.

This invention belongs to the technical field of chemical drug synthesis, specifically relating to an indole alkaloid compound, its preparation method, and its application. The indole alkaloid compound, whose structural formula is shown in Formula I, is synthesized from 7-bromoindole and a boric acid ester as starting materials. The preparation process is simple and easy, and the resulting indole alkaloid compound or a pharmaceutically acceptable salt thereof exhibits highly effective targeted inhibition of STEAP1, inhibiting STEAP1 at both the protein and cellular levels and demonstrating potent anti-proliferative effects against prostate cancer cells in animals.

The present invention belongs to the field of biochemistry and discloses a polypeptide comprising: (I) an amino acid sequence as shown in SEQ ID No. 1; or (II) an amino acid sequence formed by adding one or more amino acids before or after the amino acid sequence as shown in (I); or (III) a cell-penetrating polypeptide obtained by combining the polypeptide shown in (I) or (II) with a cell-penetrating peptide. The polypeptide significantly inhibits the growth and proliferation of two prostate cancer cell lines (DU145 and PC3), as well as RNA alternative splicing. The present invention also discloses a drug containing the polypeptide and its uses.

The present application belongs to the field of medicine, and particularly relates to betulinic acid nucleoside derivatives for preventing or treating cancer. Some compounds provided by the present application exhibit excellent inhibitory activity on test cancer cells, and particularly have unexpected inhibitory activity on colon cancer or prostate cancer cells. The compounds provided by the present application are expected to be used for preventing or treating colon cancer, prostate cancer and other cancers or symptoms related thereto.

The invention discloses application of 6-methylcoumarin in preparation of a medicine for treating prostatic cancer, and relates to the technical field of medicines. The technical problem to be solved is to provide application of 6-methylcoumarin in preparation of drugs, health care products and functional food for treating prostatic cancer. The key point of the technical scheme is as follows: 6-methylcoumarin is used as an efficient ligand of an olfactory receptor OR51E2 to regulate prostate cancer cells so as to treat prostate cancer. In the prostate cancer cells LNCaP highly expressed by OR51E2, the 6-methylcoumarin can significantly inhibit cell proliferation, the inhibition effect of the 6-methylcoumarin is positively correlated with the action concentration of the 6-methylcoumarin, a new molecular target and a technical path are provided for prostate cancer treatment, the adopted 6-methylcoumarin has good chemical stability and application safety, and the 6-methylcoumarin has good application prospects. The potential of further drug development and transformation application is realized.

The present invention relates to a composition for the treatment of castration resistant prostate cancer, the composition comprising (i) a first active ingredient comprising a CDK9 degrading agent; and (ii) a second active ingredient, wherein the second active ingredient comprises olaparib. The effects of inhibiting tumor cell proliferation and promoting cell apoptosis of the composition are obviously higher than those of a single drug under the same dosage.

The present invention provides a pyrazolo[1,5-a]pyrimidine-7-oxide compound, a preparation method and uses thereof, belonging to the field of chemical drugs. The structure of the pyrazolo[1,5-a]pyrimidine-7-oxide compound is shown in Formula I. Experimental results show that such compounds can effectively inhibit the growth of various tumor cells including lung cancer cells, breast cancer cells, prostate cancer cells, bladder cancer cells, and esophageal cancer cells, and have broad application prospects in the preparation of drugs for preventing and / or treating tumors.

The invention belongs to the technical field of biomedicine, and particularly relates to application of ADH-6 in preparation of a medicine for treating prostatic cancer. The invention provides application of ADH-6 in preparation of a product for preventing, relieving or / and treating prostatic cancer. The ADH-6 specifically targets the prostatic cancer with p53 mutation, the p53 mutation comprises p53 contact mutation and p53 structural mutation, the conformation of the p53 mutation is remodeled to restore the transcriptional activity of the wild type p53, the expression of downstream target genes P21CDKN1A, BAX and PUMA of the p53 is enhanced, and finally, the proliferation of the prostatic cancer cells is inhibited, and the apoptosis of the prostatic cancer cells is promoted.

This invention provides a peptide targeting the degradation of P300, a drug for the prevention and treatment of prostate cancer, a preparation method, and its applications, belonging to the field of protein peptide drug technology. The amino acid sequence of the peptide targeting the degradation of P300 is shown in SEQ ID NO: 1, and its binding constant to P300 protein is 78.3 nM, indicating a strong binding ability to P300 protein. Delivery of the peptide targeting the degradation of P300 to prostate cancer cells can significantly inhibit the proliferation of prostate cancer cells. Simultaneously, the peptide also has the ability to degrade P300. Compared with existing targeted drugs, the peptide drug conjugated with selenium nanoparticles of this invention provides a treatment strategy for drug-resistant and advanced castration-resistant prostate cancer, especially addressing the practical problem of a lack of therapeutic drugs for neuroendocrine prostate cancer.

The present invention relates to a salt of cinnamate, its preparation method, and its application, and belongs to the field of chemical medicine technology. The cinnamate salt of the present invention comprises an alkaline salt and an acidic salt. The cinnamate salt is prepared using cinnamate acid through a one-step reaction, with a purity of ≥95% and a yield of 70% or more. The reaction conditions are not demanding, the equipment requirements are simple, and there is no reliance on special equipment. The production process is simple and controllable, making it more suitable for industrial production. The cinnamate salt of the present invention has anti-inflammatory activity and a significant inhibitory effect on the inflammatory response of microglia. It also has anti-tumor activity and can significantly inhibit the proliferation of large cell lung cancer cells, triple-negative breast cancer cells, colon cancer cells, and prostate cancer cells.

The application discloses application of UFSP2 as a target point in preparation of a prostate cancer treatment product. The application relates to the field of biological medicine, and research finds that UFM1 specific protease 2 (UFSP2) is highly expressed in prostate cancer tissues, and the protein level is higher than that of paracancerous tissues, and is positively correlated with the expression of proliferation related molecules c-Myc and CyclinD1. Function experiments further show that inhibition of UFSP2 expression can significantly inhibit the proliferation, clone formation and migration of prostate cancer cells, and inhibit the growth and metastasis of prostate cancer in vivo; on the contrary, overexpression of UFSP2 can promote the proliferation of prostate cancer cells, indicating that UFSP2 can be used as a prostate cancer treatment target and can be used for screening of anti-prostate cancer drugs. The application provides application of an UFSP2 expression inhibitor and / or a function inhibitor in preparation of a prostate cancer treatment product, and provides a new drug development direction and a targeted intervention strategy for prostate cancer treatment.

This invention relates to the field of biopharmaceutical technology, and in particular to the application of myrotoxin A in the preparation of drugs for treating prostate cancer. This invention is the first to discover the function of myrotoxin A in inducing ferroptosis in DU145 prostate cancer cells by targeting and inhibiting ACSL3 protein, and its inhibitory effect on prostate cancer proliferation. Specific embodiments of this invention reveal for the first time that myrotoxin A can precisely utilize the unique metabolic vulnerability of prostate cancer cells, significantly downregulating the expression of ACSL3 protein in DU145 cells at the protein level. This, in turn, by relieving the inhibition of ferroptosis by ACSL3 protein, specifically induces ferroptosis in prostate cancer cells, ultimately effectively inhibiting tumor cell growth and achieving the therapeutic goal of targeting prostate cancer development.

The application belongs to the technical field of biological medicine, and discloses application of a MYLK3 gene inhibitor in preparation of a drug for treating castration-resistant prostate cancer. The biological function of MYLK3 in prostate cancer is confirmed for the first time, an intervention means with the gene as a target point is provided, and it is confirmed that the MYLK3 inhibitor can improve the sensitivity of castration-resistant prostate cancer to androgen receptor antagonists. A gene therapy drug with the human MYLK3 gene as a treatment target point is specially provided, which is suitable for the treatment of prostate cancer (especially castration-resistant prostate cancer), and can also be combined with other targeted drugs to improve the treatment effect. By designing a reasonable RNAi target sequence for the target gene, a retrovirus vector plasmid containing the target sequence is successfully constructed, which has a significant inhibitory effect on the proliferation ability of prostate cancer cells, and significantly increases the sensitivity of prostate cancer cells to AR antagonists.

The invention belongs to the field of chemical medicines, and particularly relates to a combined medicine for preventing and / or treating neuroendocrine prostate cancer, application of the combined medicine and a medicine composition. The combined medicine disclosed by the invention is prepared from the fluphenazine and the illliseme-copper chloride; wherein the fluoroperphenazine can be used for treating neuroendocrine prostate cancer (NEPC) by improving the oxygen consumption of NEPC cells and reducing the glycolytic ability of the NEPC cells; the invention relates to a pharmaceutical composition for treating prostatic cancer with NEPC phenotype, in particular to a pharmaceutical composition for treating prostatic cancer with NEPC phenotype, and ilisimus-copper chloride has no obvious killing effect on prostatic cancer cells with NEPC phenotype, but after fluphenazine and ilisimus-copper chloride are combined for use, the pharmaceutical composition has obvious treatment effect on prostatic cancer with NEPC phenotype, and shows synergistic interaction. The invention opens up a new direction for treating the neuroendocrine prostate cancer, and has a wide application prospect.

The present application belongs to the field of chemical medicine, and particularly relates to a combined drug for preventing and / or treating neuroendocrine prostate cancer, use thereof and a pharmaceutical composition. The combined drug of the present application is fluphenazine and ilesidomosine-copper chloride; wherein fluphenazine can be used for treating neuroendocrine prostate cancer (NEPC) by increasing the oxygen consumption of NEPC cells and reducing the glycolytic capacity of NEPC cells; and ilesidomosine-copper chloride has no obvious killing effect on prostate cancer cell lines with NEPC phenotype, but when fluphenazine is combined with ilesidomosine-copper chloride, the combination has a significant therapeutic effect on prostate cancer with NEPC phenotype, and shows synergistic effect. The present application opens up a new direction for treating neuroendocrine prostate cancer, and has a broad application prospect.

The present invention discloses an application of a bromodomain protein 4 active compound based on a water network strategy. The bromodomain protein 4 active compound can be used to prepare a drug that inhibits the activity of bromodomain protein 4, and can be used to prepare a pharmaceutically acceptable salt. In addition, the bromodomain protein 4 active compound and the pharmaceutically acceptable salt prepared therefrom can also be used to prepare a bromodomain protein 4 inhibitor and the pharmaceutically acceptable salt prepared therefrom, as well as a pharmaceutical composition for preparing a prostate cancer cell proliferation inhibitor, an anti-prostate tumor drug, and a pharmaceutical composition for treating bromodomain protein 4-related diseases. The bromodomain protein 4 inhibitor prepared based on the bromodomain protein 4 active compound having obvious inhibitory activity of the present invention is applied to the treatment of diseases related to bromodomain protein 4, has high reliability, is easy to promote and popularize, and utilizes the potential advantages of the bromodomain protein 4 active compound as a drug or pharmaceutical composition, opening up a new approach for the treatment of related diseases.

The invention discloses an abiraterone acetate self-nanoemulsion liquid-filled capsule as well as a preparation method and application thereof. The abiraterone acetate self-nanoemulsion liquid-filled capsule is good in self-nanoemulsion effect, controllable in preparation quality and remarkable in killing effect on prostate cancer cells, the bioavailability of the capsule is improved by 12.54 times compared with that of commercially available tablets, the influence of food on the bioavailability of drugs is reduced, the limitation of abiraterone tablets in clinical application is expected to be overcome, and the capsule is worthy of popularization and application. The research has important scientific significance and potential clinical application value.

The invention discloses application of FBXO2 in treatment of prostatic cancer, and belongs to the field of prostatic cancer treatment. According to the application of the FBXO2 accelerant in preparation of the medicine for treating the prostatic cancer, specifically, expression of the FBXO2 in prostatic cancer tissue is remarkably reduced, and the high expression level of the FBXO2 is in positive correlation with good prognosis of a patient; fBXO2 overexpression can effectively inhibit prostate cancer cell proliferation and metastasis and induce apoptosis; mechanism research finds that FBXO2 is specifically combined with m6A reading protein YTHDF2 through a carboxyl terminal structural domain of the FBXO2, mediates the m6A reading protein YTHDF2 to generate ubiquitination modification at a K286 site and promotes proteasome dependent degradation of the m6A reading protein YTHDF2. The YTHDF2 is used as a high-expression cancer promoting protein in prostatic cancer, and the degradation of the YTHDF2 can be accelerated by regulating m6A methylation modification of CDKN1C mRNA, so that the tumor progression is driven. A theoretical basis is provided for developing a novel prognostic marker and a treatment strategy.

The invention relates to an indole maleimide derivative and application thereof, belongs to the technical field of synthesis of heterocyclic compounds, and solves the problem that the types of existing medicines for treating cancers are not rich enough. The indole maleimide derivative disclosed by the invention has a structure as shown in a structural formula 4 and / or has a structure as shown in a structural formula 3. The indole maleimide derivative disclosed by the invention has an obvious inhibition effect on the proliferation of human leukemia cells (K562) and prostate cancer cells (PC-3).

The invention relates to the technical field of biological medicine, and particularly discloses a bicyclic peptide for targeted degradation of FOXA1 protein and a preparation method and application thereof, and the amino acid sequence of the bicyclic peptide for targeted degradation of FOXA1 protein is as shown in SEQ ID NO.1. The bicyclic peptide capable of degrading the FOXA1 protein in the targeted manner, provided by the invention, can effectively degrade the FOXA1 protein, and shows the capability of remarkably inhibiting prostate cancer cell proliferation.

The invention discloses an anthraquinone compound as well as a preparation method and application thereof in resisting prostatic cancer. The structure of the anthraquinone compound 1 is shown as a formula (I). According to the present invention, the solid fermentation extract product of Aspergillus versicola SCSIO 41323 is subjected to separation and purification so as to obtain the compound Nidurufin (1), wherein the compound Nidurufin (1) is obtained from the solid fermentation extract product of Aspergillus versicola SCSIO 41323; prostate cancer cell activity evaluation finds that the compound 1 can significantly inhibit the activity of prostate cancer cells and inhibit cell proliferation, protein expression of AR, KLK3, MBOAT2 and the like can be significantly inhibited by increasing ROS activity and inducing ferroptosis of prostate cancer cells, and the Nidurfin (1) can inhibit growth of prostate cancer cells in vitro and in vivo, and can inhibit growth of prostate cancer cells in vitro and in vivo. The method is of great significance to development and utilization of deep sea abyssal and other extreme environment source microbial resources.

The invention relates to an androgen receptor antagonist with a disubstituted-N-(substituted polynary fused cyclo-2-yl) propanamide structure as well as a preparation method and application of the androgen receptor antagonist, the androgen receptor antagonist is shown in a general formula I, and the androgen receptor antagonist inhibits growth and proliferation of prostate cancer cells by inhibiting AR activity and blocking an androgen signal channel. Compared with the traditional AR antagonist, the novel compound provided by the invention has a novel action mechanism, and effectively overcomes the problem of drug resistance of the existing drug.