240 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 belongs to the technical field of medicinal chemistry, and particularly relates to a series of substituted oxadiazole compounds as well as a preparation method and application thereof. Pharmacological tests show that the series of compounds have strong selectivity and inhibition effect on SphK2, and have anti-proliferation effect on cervical cancer cells, prostate cancer cells and colon cancer cells.

The invention discloses a class of radiopharmaceutical labeled precursors targeting prostate specific membrane antigens, the structure of the radiopharmaceutical labeled precursors is shown as the following: # imgabs0 #, a precursor reagent RESCA-PSMA-1802 targeting prostate specific membrane antigens is synthesized for the first time, the reagent can be labeled by using an 18F-Al method to prepare a positron imaging agent 18FAl-RESCA-PSMA-1802, and the reagent can be used for preparing the prostate specific membrane antigens. The polymer has good stability and biological activity in vivo and in vitro, has good targeting property on prostate cancer cells, can reflect tumor recurrence or metastasis conditions, and is very suitable for PET imaging.

The invention discloses a drug-resistant marker for treating prostatic cancer olaparib and application of the drug-resistant marker, and relates to the technical field of medicine, and the marker is a PCAR1 gene. Research finds that the PCAR1 gene is remarkably and highly expressed in prostate cancer Olaparil drug-resistant cells and clinical drug-resistant samples, and can be used as a key marker for judging the drug resistance of prostate cancer patients to Olaparil. By detecting the expression level of the PCAR1 gene, the treatment reaction of a patient to the olaparil can be effectively predicted, and a basis is provided for clinically and accurately selecting a treatment scheme. Meanwhile, the specific siRNA designed aiming at the PCAR1 gene can obviously inhibit the expression of the PCAR1 gene, and can effectively reduce the drug resistance of cancer cells to olaparione, promote the apoptosis of the cancer cells and inhibit the proliferation of the cancer cells when being combined with the olaparione for use. Based on the siRNA, the invention prepares a pharmaceutical composition containing the siRNA and olaparil, and provides a new drug combination scheme for the treatment of prostatic cancer.

Provided are a compound, or a stereoisomer, or pharmaceutically acceptable salt, or deuterated compound, or tautomer, or polymorphic substance, or solvate, or N-oxide, or isotope labeled compound, or metabolite, or prodrug thereof, and a use thereof. The structure of the compound is as shown in formula 0, and the compound serves as an AR regulator and has better castration-resistant prostate cancer cell proliferation inhibition activity, better AR protein degradation activity, and better oral bioavailability.

The invention discloses application of atypical retinoid A-7 in preparation of androgen receptor inhibitors and antitumor drugs, and belongs to the technical field of medicines. It is proved for the first time that AR can be degraded through a CMA pathway, and the atypical retinoid A-7 serving as an AR inhibitor can obviously reduce the AR protein level in prostate cancer cells; in addition, the Atypic retinoids 7 can be used for inhibiting the growth and proliferation capacity of the prostate cancer cells LNCaP; in addition, the invention further provides an anti-tumor medicine composition, the anti-tumor medicine composition comprises the Atypic retinoid-7 and Enzalutamide, and the anti-tumor medicine composition can be used for treating the prostatic cancer and has important clinical significance.

The invention provides an application of chimeric SFT2D2-TBX19 in diagnosis and treatment of prostatic cancer, and particularly relates to an application of the chimeric SFT2D2-TBX19 as a marker in diagnosis and treatment of prostatic cancer. The nucleotide sequence of the chimeric SFT2D2-TBX19 disclosed by the invention is as shown in SEQ ID NO.1. The overexpression of the chimeric SFT2D2-TBX19 promotes the proliferation, migration and invasion of prostate cancer cells; the chimeric SFT2D2-TBX19 is used for encoding the TBX19-202 protein, the TBX19-202 protein encoded by the chimeric SFT2D2-TBX19 has a carcinogenic effect similar to that of a parent TBX19 in the aspect of promoting the progress of prostatic cancer, and the amino acid sequence of the TBX19-202 protein is shown as SEQ ID NO. 4. Specific high expression of the chimeric SFT2D2-TBX19 in a neuroendocrine prostate cancer (NEPC) cell line is found for the first time, and a new target spot is provided for diagnosis and treatment of related diseases, so that a clinician is guided to provide a prevention method or a treatment scheme for a subject.

The invention discloses an extraction method and application of an aza-sesquiterpenoid compound which is derived from marine fungi and has anti-prostatic cancer activity. The structure of the aza-sesquiterpenoid compound is shown as a formula I-3 or pharmaceutical salt of the aza-sesquiterpenoid compound: # imgabs0 #, wherein the compound 1 is pyripyropene E, the compound 2 is pyripyropene O, and the compound 3 is 11-deacetylated pyripyropene A (11-deacetylated PPPA). The invention further discloses a preparation method of the aza-sesquiterpenoid compound with the anti-prostatic cancer activity and application of the aza-sesquiterpenoid compound with the anti-prostatic cancer activity and application of the aza-sesquiterpenoid compound with the anti-prostatic cancer activity. Molecular docking analysis shows that the compound shows anti-prostatic cancer activity, further experiments find that the compound pyripyroene O (compound 2) has remarkable cytotoxic activity on prostatic cancer cells, an alternative compound is provided for developing new prostatic cancer treatment, and the compound 2 has important significance on development of marine drug resources in China.

The invention belongs to the field of medicines, relates to a heterocyclic compound of a bifunctional chimera for targeted degradation of an androgen receptor and application of the heterocyclic compound, and particularly provides a compound as shown in a formula (I), or a stereoisomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound, and their use in the treatment of diseases associated with androgen receptors. The compound provided by the invention can degrade androgen receptors in prostate cancer cells in a targeted manner and inhibit proliferation of the prostate cancer cells, and also shows good metabolic stability and pharmacokinetic properties. # imgabs0 #

The invention relates to an application of an ezetimibe derivative in preparation of an anti-prostatic cancer drug, and belongs to the technical field of medicinal chemistry. The general formula structure of the ezetimibe derivative L14 is # imgabs0. The ezetimibe derivative L14 can be used for preparing new drugs for treating CRPC and NEPC without depending on an androgen receptor pathway, the clinical curative effect is improved, and the clinical drug selection is increased. The micromolecule L14-8 (R1 = R2 =-C (O) CH = CH2) can specifically inhibit proliferation of prostate cancer cells in vitro and can also inhibit growth of prostate tumors in vivo; in the aspect of drug combination, the AR antagonist and the low-dose small molecule L14-8 are combined for use, so that the sensitivity of CRPC and NEPC to the AR antagonist can be remarkably improved, the drug resistance induced by the AR antagonist can be possibly inhibited, and the clinical benefits of the AR antagonist can be improved.

The invention discloses an RGD modified crocetin-paclitaxel co-drug-loaded compound liposome and a preparation method and application thereof, and belongs to the technical field of biological medicines.The RGD modified crocetin-paclitaxel co-drug-loaded compound liposome comprises the following components: an RGD modified liposome, paclitaxel and crocetin, wherein the RGD modified lipidosome is used as a drug carrier, paclitaxel and crocetin are delivered to prostate tumor cells in a targeted manner, and the RGD modified lipidosome is prepared through a film dispersion method or a reverse evaporation method. The prostate cancer targeted compound liposome prepared by the invention can increase the uptake of prostate cancer cells, improve the in-vitro cytotoxicity of the prostate cancer cells to the prostate cancer cell line RM-1, inhibit the growth of RM-1 ectopic solid tumors in mice, and do not cause obvious damage to other tissues.

The invention provides an extraction method of flavone in folium turpiniae and application of the flavone in preparation of prostate cancer drugs. Through the methods of grinding, degreasing, enzymolysis, fermentation and the like, the extraction rate of flavone in turpinia arguta leaves is increased, and meanwhile, the anti-cancer activity of the flavone-containing extract is improved; the flavone-containing extract obtained by the method provided by the invention has a relatively strong inhibition effect on proliferation of prostatic cancer PC-3 cells, a theoretical basis can be provided for an anti-tumor effect of turpinia formosana leaf flavone, and development and application of turpinia formosana leaves are promoted.

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 belongs to the technical field of protein polypeptides, and particularly relates to a polypeptide targeting BRCA2 protein, application of the polypeptide and a medicine for treating prostatic cancer. The amino acid sequence of the polypeptide is shown as SEQ ID NO.1, the polypeptide has high binding capacity with BRCA2 protein, cell proliferation and tumor growth can be effectively inhibited when the polypeptide is delivered to prostatic cancer, and meanwhile the polypeptide has the capacity of degrading BRCA2 in a targeted mode. The combined application of the polypeptide and the PARP inhibitor can enhance the sensitivity of prostate cancer cells to the PARP inhibitor. Therefore, the polypeptide can be applied to preparation of a medicine for treating metastatic castration-resistant prostate cancer or preparation of a reagent for degrading the BRCA2 protein. The BRCA2 targeting PROTAC medicine can provide a new treatment strategy for prostatic cancer treatment, and the PARP targeting inhibitor is combined to provide a PARP inhibitor synthesis lethal treatment effect for metastatic castration resistant prostatic cancer patients.

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 described herein pertains to the diagnosis, imaging, and / or treatment of pathogenic cell populations. In particular, the invention described herein pertains to the diagnosis, imaging, and / or treatment of diseases caused by PSMA expressing cells, such as prostate cancer cells, using compounds capable of targeting PSMA expressing cells.

The invention relates to a difunctional chimera heterocyclic compound for targeted degradation of an androgen receptor and application of the difunctional chimera heterocyclic compound, and particularly provides a compound shown in a formula (I), or an isotope compound of the compound, or an optical isomer of the compound, or a tautomer of the compound, or a pharmaceutically acceptable salt of the compound, or a prodrug of the compound, or a solvate of the compound, aRB is an androgen receptor recognition / combination part, L is a linking part, and U is a ubiquitin protease recognition / combination part; the three parts are connected through chemical bonds. The compound provided by the invention can degrade androgen receptors in prostate cancer cells in a targeted manner and inhibit proliferation of the prostate cancer cells, and also shows good metabolic stability and pharmacokinetic properties. The compound provided by the invention has a good application prospect in preparation of a protein degradation targeting chimera of an androgen receptor and in preparation of drugs for treating related diseases (including prostatic cancer, breast cancer and Kenildie disease) regulated and controlled by the androgen receptor. # imgabs0 #

The present invention belongs to the field of biomedicine, and particularly relates to an lncRNA ENST00000510619 for the treatment of prostate cancer and its application. The cDNA sequence of lncRNA ENST00000510619 is shown as SEQ ID NO.1. The present invention discovers that the expression of lncRNA ENST00000510619 in mCRPC and mHSPC prostate cancer tissues is significantly higher than that in normal prostate tissues, and the expression of lncRNA ENST00000510619 in mCRPC prostate cancer tissues is significantly higher than that in mHSPC prostate cancer tissues; inhibiting / knocking out lncRNA ENST00000510619 can inhibit the proliferation, migration and invasion of prostate cancer cells, and enhance the sensitivity of docetaxel-induced apoptosis of prostate cancer cells. Therefore, lncRNA ENST00000510619 can be used as a therapeutic target for 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 discloses a 1, 8-disubstituted tryptanthrin derivative and application of the 1, 8-disubstituted tryptanthrin derivative to prevention and treatment of phytopathogen and anti-tumor activity, the general formula of the derivative is shown in (I), and the test result of the compound shown in the general formula on the bacterial activity of phytopathogen shows that the compound has a good antibacterial effect on Xanthomonas oryzae pv. Oryzae, Xanthomonas citri pv. Citri and the like, and can be used for preventing and treating the phytopathogen. The method can be used for developing novel agricultural bactericides. Meanwhile, results of the compound shown in the general formula on tumor cells show that the compound has good in-vitro anti-tumor activity on human chronic myelogenous leukemia cells K562, human lung cancer cell lines A549, human liver cancer cells HepG2, human prostate cancer cells PC3 and the like, and can be used for researching novel anti-tumor drugs. # imgabs0 #

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 provides a netupitant derivative as well as a preparation method and application thereof. The netupitant derivative has a structure as shown in a formula (I). Researches show that the netupitant derivative has a remarkable inhibition effect on non-small cell lung cancer and prostate cancer cells, and can remarkably inhibit proliferation, activity and clone formation of the non-small cell lung cancer and the prostate cancer cells, inhibit expression of RORC genes, inhibit AR and ROR gamma protein expression levels and promote cell apoptosis; the traditional Chinese medicine composition has very good effects of resisting non-small cell lung cancer and prostatic cancer. The compound can be synthesized through simple chemical synthesis steps, the cost is low, large-scale industrial production is easy to realize, and the compound has important application value in the aspect of development of non-small cell lung cancer and prostate cancer anticancer drugs.

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.