399 results about "Anticancer drug" 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 field of bioinformatics, and relates to an anti-cancer drug response prediction method based on an attention mechanism. The method comprises the following steps: firstly, capturing uniform-dimension drug and cancer cell line characteristics through a multi-layer perceptron; secondly, fusing drug characteristics by adopting a Transform encoder, and constructing a cell encoder for cancer cell line characteristic polymerization; then, designing a cross-modal cross fusion module to promote information interaction between the two; and finally, predicting a semi-suppressed concentration value subjected to logarithmic transformation between the two through a multi-layer perceptron. Experimental results show that compared with an existing optimal method, the method has the advantage that the RMSE is reduced by 2.9%. According to the method, accurate prediction of the anti-cancer drug response is achieved by integrating drug and cancer cell line data, screening of potential anti-cancer drugs can be accelerated, personalized treatment schemes can be optimized, the cure rate of cancer patients is further increased, and the method has great significance in cancer treatment.

The invention discloses a drug-combined anticancer composition and application of the composition in preparation of anticancer drugs. According to the present invention, the drug combination composition comprises the PARP inhibitor Olaparib and the calcium ion antagonist amlodipine maleate, the PARP inhibitor Olaparib and the calcium ion antagonist amlodipine maleate provide the synergistic effect, and compared with the single PARP inhibitor, the drug combination composition has characteristics of high stomach cancer sensitivity, significant gastric cancer efficiency improving, and wide application prospect. The Amlodipine in the drug combination composition provided by the invention enhances the curative effect of the PARP inhibitor Olaparib on the gastric cancer.

This invention relates to the field of anticancer drugs, and more particularly to an indole-3-aryl ketone derivative, its preparation method, and its applications. The indole-3-aryl ketone derivative is compound I-VI, which can be used to prepare drugs for the prevention and / or treatment of cancer, including at least one of breast cancer, liver cancer, lung cancer, colorectal cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, cervical cancer, ovarian cancer, kidney cancer, and esophageal cancer. This invention screened the activity of various compounds and, for the first time, discovered that compound I-VI exhibits excellent inhibitory activity against multiple different types of human cancer cells, providing a potential option for broad-spectrum anticancer drugs.

The invention discloses a synthetic lethal prediction method based on non-generality forgetting and low-rank interaction multi-mode adaptive fusion, and relates to the technical field of bioinformatics, computational biology and drug target screening. The method comprises the following steps: firstly, constructing a multi-view gene embedding expression based on a gene graph structure, a hypergraph structure and a knowledge graph; then constructing a difference vector and an interaction vector for any gene pair so as to characterize the difference and potential complementary relationship between the genes; multi-source information fusion is realized by using a deep learning model containing interactive attention, a forgetting gate and a multi-modal fusion mechanism; on this basis, multi-task optimization is carried out through joint classification loss, modal interaction loss and redundancy suppression loss, and optimal discrimination is realized through a dynamic threshold search strategy; and finally, outputting a sorting result of the candidate synthetic lethal gene pairs according to the prediction score. According to the method, the accuracy and generalization ability of synthetic lethal relationship prediction can be effectively improved, and a high-reliability calculation auxiliary tool is provided for anti-cancer drug target screening and gene therapy strategy design.

The invention belongs to the technical field of medicines, and discloses preparation and application of a paclitaxel-loaded liposome nano targeting preparation. The paclitaxel-entrapped nano-particles are prepared by adopting a film dispersion method, and micromolecular hyaluronic acid is entrapped on the surfaces of the lipid nano-particles by utilizing the charge effect. The bionic nano-drug provided by the invention is helpful for solving the problems of poor solubility, low bioavailability, high toxicity and the like of the anticancer drug paclitaxel. The hyaluronic acid has affinity with a glycoprotein CD44 receptor on the surface of a tumor cell, so that the nanoparticles are targeted and concentrated at a tumor part, the anti-tumor effect is improved, and the systemic toxicity of paclitaxel is reduced. The preparation process is simple, the cost is low, the stability is good, the repeatability is high, and the preparation method also has a better development prospect in the aspect of clinical application transformation.

The invention provides an anticancer drug collaborative prediction method MultiFusion Syn based on multi-scale feature fusion, and relates to the technical field of anticancer drug collaborative prediction. According to the method, synergistic effect prediction is converted into a multi-scale feature fusion classification task: a pre-trained graph neural network DGCL is utilized to extract drug fine-grained structure features, ChemBERTa is combined to obtain semantic features, and adaptive fusion is carried out through an attention mechanism; meanwhile, a residual network is adopted to extract biological characteristics of the cell line, drug-cell bidirectional interaction is constructed by means of double-end cross attention, and fine fusion is performed through a gating network; the model introduces a pre-training encoder and realizes knowledge migration in combination with parameter freezing. On a reference data set, MultiFusionSyn is evaluated by indexes such as AUC, PRAUC, ACC and BACC, and the performance of MultiFusionSyn is superior to that of an existing advanced method through verification of an independent test set.

The invention relates to the field of antitumor drugs, in particular to a thiophene acetyl tetrahydro-beta-carboline compound and application thereof. The thiophene acetyl tetrahydro-beta-carboline compound or the pharmaceutically acceptable salt thereof, and the pharmaceutical composition containing the compound can be used for preparing medicines for preventing and / or treating various cancers. The cancer is at least one of breast cancer, lung cancer, osteosarcoma, melanoma, gastric cancer, pancreatic cancer, kidney cancer, glioma and ovarian cancer. Activity screening is carried out on various compounds, it is found for the first time that the 12 compounds provided by the invention have remarkable broad-spectrum inhibitory activity on various human cancer cell lines, and key candidate compounds are provided for developing novel anti-cancer drugs.

METHODS OF TREATING CANCER BY ADMINISTERING MCL-1 INHIBITORS AND ANTI-CANCER AGENTS SOLUTION: The present disclosure relates generally to methods for treating cancer by administering an MCL-1 inhibitor and an anti-cancer agent. As is explained in detail in the present specification and as is specifically demonstrated, according to the present invention, a remarkable effect is achieved, which could not be easily expected by those skilled in the art from the prior art.SELECTED DRAWING: Figure 5

The application relates to the frontiers of nanomaterials and drug screening fields, and discloses a fluorescent probe material for drug screening and a drug screening method. The fluorescent probe material realizes screening of anticancer drug efficacy of a to-be-detected drug by detecting the concentration of an NAD+ (nicotinamide adenine dinucleotide) active marker of lactate dehydrogenase, the fluorescent probe material comprises an A agent and a B agent, the A agent is a covalent organic framework material loaded with carbon dots with reducibility, and is denoted as COF@CDs, and the B agent is a transition metal hydride; the transition metal hydride can make NAD+ hydrogenated and reduced into NADH in the presence of the COF@CDs; the product after hydrogen loss of the transition metal hydride can be combined with the COF@CDs, and the COF@CDs can emit fluorescence under excitation light, and the fluorescence is quenched.

Disclosed are a CD24 antibody or an antigen-binding fragment thereof and the medical use thereof. Further, disclosed are a chimeric antibody comprising CDRs of the CD24 antibody, a humanized antibody, a pharmaceutical composition comprising the CD24 antibody or the antigen-binding fragment thereof, and the use thereof as an anticancer drug.

The present invention relates to a pharmaceutical composition for preventing or treating tumors, which contains a novel pyrazolopyrimidine compound or a pharma- ceutical acceptable salt thereof as an active ingredient, and which can be usefully used as a composition for preventing or treating cancer by administering it in combination with other anticancer agents.

The invention belongs to the field of anti-cancer drugs, and particularly relates to an anti-cancer porphyrin molecular cage structure and cytotoxic application of the anti-cancer porphyrin molecular cage structure to liver cancer. The invention discloses two coordination molecular cages Pd-TMPP (Cu) and Pd-TMPP (Zn), and detailed and accurate verification is carried out on the structural characteristics and element composition of the two coordination molecular cages through a series of tests. And then the two compounds are modified by hyaluronic acid so as to obtain targeting and water solubility. Experimental results show that the Pd-TMPP (Zn) has concentration-dependent cytotoxicity to HuH-7, Hep-G2 and PLC / PRF / 5, and the cytotoxicity is remarkably enhanced after the Pd-TMPP (Zn) is irradiated by infrared light.

The application relates to the technical field of natural medicinal chemistry, and specifically discloses a triterpenoid compound and application, and a preparation method of the compound. The preparation method comprises the following steps: drying and crushing schisandra chinensis roots to obtain dried and crushed schisandra chinensis roots, extracting the dried and crushed schisandra chinensis roots by using 70% ethanol water solution under negative pressure cavitation, combining and concentrating the extract to obtain a crude extract, separating the crude extract by using a D101 macroporous adsorption resin, eluting the crude extract by using water, 30% ethanol, 70% ethanol and 90% ethanol in sequence, collecting a 70% ethanol elution part, performing MCI column chromatography on the 70% ethanol elution part, performing gradient elution on the 70% ethanol elution part by using methanol-water, collecting a depigmentation sample, performing ODS column chromatography on the depigmentation sample, performing gradient elution on the depigmentation sample by using water-methanol, collecting a target component, and purifying the target component by using a preparative high performance liquid chromatograph to obtain the target compound. The application separates a novel triterpenoid compound from schisandra chinensis roots for the first time, expands the development range of medicinal resources of schisandra chinensis plants, simultaneously provides a novel structure mother nucleus and a candidate active molecule for anticancer drug research and development, and enriches the research and development reserves of antitumor natural medicines.

This invention proposes a mechanism-aware synergistic anticancer drug combination prediction method and system, belonging to the field of biomedical technology. It includes: extracting node-level feature representations of the first and second drugs through a drug encoder, and extracting molecular representations of the cell line through a cell line encoder; generating an attention tensor based on a trilinear cross-modal synergistic strategy using a trilinear attention network to explicitly capture the synergistic dependencies of the drug combination in a specific cellular environment, and updating and enhancing the features through context fusion; finally, concatenating the enhanced features and outputting a synergistic score via a multilayer perceptron. This invention can directly model the joint interaction relationship between the first drug, the second drug, and the cell line, thereby accurately predicting the synergistic effect of the anticancer drug combination.

This disclosure describes how to treat and / or improve pancreatic cancer using a novel proteomic profile of the pancreatic cancer. In some embodiments, the treatment includes removing cancerous tissue after taking a biopsy from the patient. Optionally, the treatment includes administering anticancer agents to suppress the progression of pancreatic cancer. In further or alternative embodiments, the novel proteomic profile is used to monitor disease progression or remission.

This invention discloses a polysubstituted indole[1,2-a]quinoxaline compound, its preparation method, and its applications. The structural formula of the polysubstituted indole[1,2-a]quinoxaline compound of this invention is or , where R 1 Selected from -H or -F, R 2 The compounds are selected from phenyl, 4-methylphenyl, 4-methoxyphenyl, or 4-fluorophenyl. The polysubstituted indole[1,2-a]quinoxaline compounds of this invention have novel structures and significant antitumor activity, making them suitable for the synthesis of anticancer drugs. Furthermore, their preparation methods offer advantages such as readily available and inexpensive catalysts, broad substrate applicability, good functional group tolerance, simple operation, mild reaction conditions, and high step economy, making them suitable for large-scale industrial production and application.

The invention relates to application of (E)-2-(4-(dimethylamino) styryl)-6-methoxy-3-methylbenzo [d] thiazole-3-onium in preparation of anti-cancer drugs, and belongs to the technical field of medical application, the structure of (E)-2-(4-(dimethylamino) styryl)-6-methoxy-3-methylbenzo [d] thiazole-3-onium is as shown in the following formula I, the (E)-2-(4-(dimethylamino) styryl)-6-methoxy-3-methylbenzo [d] thiazole-3-onium can inhibit the growth of gastric cancer cells, inhibit the proliferation, invasion and migration of the gastric cancer cells by promoting the autophagy and mitochondrial rupture of AGS and HGC-27 cells of the gastric cancer cells, and block the gastric cancer cells in the G1 stage. Furthermore, in-vivo experiments of mice prove that ZWK-3 can inhibit tumor growth of the mice, shows obvious dose dependence, and does not influence the body weight and visceral indexes of the mice at the same time. Formula I.

The invention relates to the technical field of anti-cancer drugs, and provides a traditional Chinese medicine multi-component nano drug delivery system as well as a preparation method and application thereof. According to the invention, honokiol (HN) is entrapped by adopting lipid nanoparticles formed by a berberine (BR)-disulfide bond-caprylic capric triglyceride compound, the surface of the lipid nanoparticles is coated with a gelatin layer, and quercetin (QE) is entrapped in the gelatin layer, so that simultaneous delivery of HN, BR and QE and programmed release outside and inside cells are realized. Furthermore, the surface of the gelatin layer is modified with PEG, so that the long circulation of the drug delivery system in blood is improved; furthermore, cRGD is connected to PEG, and the synergistic lung cancer resisting effect of HN, BR and QE is greatly improved through the targeting effect of cRGD. In conclusion, the drug delivery system provided by the invention can give full play to the effect of synergistically treating lung cancer by HN, QE and BR, and has a wide application prospect.

The invention provides an anti-cancer medicine and food homologous composition and a preparation method thereof. The composition is prepared from the following components in parts by weight: 5 to 10 parts of lipoic acid, 30 to 50 parts of nano curcumin, 2 to 7 parts of berberine, 50 to 100 parts of beta-glucan, 15 to 35 parts of polymethylacrylic acid, 15 to 25 parts of herba hedyotidis diffusae extract, 7 to 15 parts of scutellaria barbata baicalein, 25 to 55 parts of astragalus polysaccharide, 8 to 18 parts of coix seed ester and 10 to 15 parts of cordyceps cicadae. Through a space-time targeting synergistic release mechanism of a bionic nanocellulose skeleton and in combination with pH / enzyme double-response intelligent regulation and control, three-stage precise synergistic effects of oxidation resistance, apoptosis promotion and immune activation are realized, the limitation that a traditional medicinal and edible composition is poor in targeting property, low in synergistic efficiency and uncontrollable in toxicity is broken through, and the medicinal and edible composition has a broad application prospect. High-efficiency and low-toxicity tumor multi-channel synergistic intervention is achieved in a natural component system for the first time, and the actual effect of the whole medicinal and edible composition on cancer and swelling resistance is improved.

The present invention relates to a composition for preventing, ameliorating, or treating neuropathic pain, comprising syringaresinol or a pharmaceutically acceptable salt thereof as an active ingredient. The composition of the present invention may be administered to a subject for which administration of an anticancer agent is scheduled or to which an anticancer agent has been administered, or to a subject which has suffered peripheral nerve damage, to thereby prevent, ameliorate, or treat neuropathic pain.

The application relates to a synthesis method of red luminescent carbon dots with a targeting diagnosis and treatment potential of hepatocellular carcinoma, which comprises the following steps: 1) adding 5-fluorouracil and indocyanine green into deionized water, uniformly mixing, and forming a uniform mixed solution; 2) heating the mixed solution obtained in the step 1) at 160-200 DEG C for 5-9 h, and cooling to room temperature; 3) filtering and dialyzing the solution obtained in the step 2), and obtaining a pure 5-FICD solution; and 4) freeze-drying the solution obtained in the step 3), and obtaining the product. The method takes anticancer drug 5-fluorouracil and photosensitizer indocyanine green as precursors, synthesizes a low-toxicity red light carbon dot through a simple hydrothermal method, improves the shortcoming that a chemotherapy drug has a large side effect, and realizes the targeted killing of hepatocellular carcinoma cells.

The invention belongs to the technical field of bioengineering, and discloses a UBXN10 active polypeptide, a carrier thereof and application of the UBXN10 active polypeptide in anti-cancer drugs. The amino acid sequence of the UBXN10 active polypeptide is as shown in SEQ ID NO: 1, and the nucleotide sequence for coding the UBXN10 active polypeptide is as shown in SEQ ID NO: 2. According to the invention, a plurality of functional means are utilized to analyze the transcriptional activity of cancer promoting beta-catenin in colorectal cancer cells and the antagonism of cancer cell proliferation and stem cell nature. The cell biology level proves that the UBXN10 active polypeptide has the potential of antagonizing beta-catenin mediated proliferation and stem cell gene expression and inhibiting colorectal cancer cell proliferation and stem cell property.

This invention discloses a class of pentacyclic triterpenoid derivatives with diverse B-ring modifications, their preparation methods, and applications. This invention utilizes a chemical enzymatic method to expand the chemical space of the B-ring in pentacyclic triterpenoids, obtaining a series of pentacyclic triterpenoid derivatives with diverse B-ring modifications. Pharmacological activity screening of these pentacyclic triterpenoid derivatives revealed their good tumor-suppressive activity, providing a promising application prospect for the prevention and treatment of tumors. This invention achieves the efficient synthesis of pentacyclic triterpenoid derivatives with diverse B-ring modifications, structures that are difficult to obtain using traditional chemical methods. Systematic antiproliferative activity screening identified candidate molecules with broad-spectrum and highly efficient inhibitory effects against various human tumor cell lines. These molecules show good drug development potential, providing novel lead compounds for the innovative development of anticancer drugs.

Provided are compositions for preventing or treating cancer including Asarum maculatum Nakai extracts, or a fraction thereof. According to an aspect, an Asarum maculatum Nakai extract has an excellent anticancer efficacy against various cancers including diffuse-type gastric cancer, and a cancer treatment agent having an excellent effect may be developed by using the extract as an active ingredient.

The invention discloses an intelligent synergistic administration composition and a preparation method thereof, and belongs to the technical field of pharmaceutical preparations and delivery. The composition takes lipidosome as a carrier, the surface of the lipidosome is modified with a peelable PEG protective layer with'enzyme / pH dual gating 'responsiveness, and the lipidosome is used for being activated under specific conditions of a tumor microenvironment to realize accurate targeting. The interior of the composition is covalently connected with a synergistic auxiliary drug for overcoming multi-drug resistance through chemical bonds sensitive to acid, and a main-effect anti-cancer drug is physically entrapped. After entering the target cell, the auxiliary drug is preferentially and rapidly released in the lysosome by means of the acid-sensitive bond so as to inhibit the drug efflux pump function; and then the main-effect medicine is slowly released, so that programmed sequential administration is realized. Through the collaborative design of intelligent shelling and sequential release, the technical problems of poor targeting property and difficulty in overcoming drug resistance in drug delivery are solved, and the collaborative anti-tumor effect is remarkable.

This invention provides a combination for use in treating cancers that express prostate-specific membrane antigen (PSMA). [Solution] A combination comprising a PD-1 inhibitor, a CTLA-4 inhibitor, and a radiolabeled compound of formula Ia for use in treating PSMA-expressing cancer in the subject. JPEG2026049728000042.jpg45132 The aforementioned combination comprises one or more further anticancer agents, wherein the further anticancer agents are selected from octreotide, lanreotide, vapreotide, pasireotide, satreotide, everolimus, temozolomide, telotristat, sunitinib, sulfatinib, ribociclib, entinostat, and pazopanib.

The invention relates to an anticancer drug combination synergistic effect prediction method. Comprising the following steps: learning low-dimensional feature representation of drugs and cell lines through an automatic encoder of a self-attention mechanism; inputting the low-dimensional feature representation into a hybrid expert network, and constructing interactive feature representation of the drug and the cell line from multiple angles; through a self-attention gating network, multiple interactive feature representations constructed by a hybrid expert layer are efficiently fused, and enhanced interactive feature representations are generated; inputting the enhanced interaction feature representation into a prediction layer, introducing a weight coefficient to adjust a loss function, and realizing drug synergy and single-drug treatment sensitivity prediction; and through a self-attention gating network, feature representation is efficiently fused, and the internal relationship between the drug and cell line features is captured, so that the prediction precision of the synergistic effect of the anti-cancer drug combination is improved.

The present invention provides anti-CD73 binding molecules, such as antibodies and their antigen-binding fragments. [Solution] Provided are isolated binding molecules or antigen-binding fragments thereof that contain an antibody VL and specifically bind to CD73 having a specific sequence. Furthermore, pharmaceutical formulations comprising the disclosed composition, as well as methods for diagnosing and treating diseases associated with CD73 expression, such as cancer, are also provided. Such diseases can be treated, for example, by direct therapy with the disclosed anti-CD73 binding molecule (e.g., a naked antibody or antibody-drug conjugate that binds to CD73), by adjuvant therapy with other antigen-binding anticancer agents such as immune checkpoint inhibitors (e.g., anti-CTLA-4 and anti-PD-1 monoclonal antibodies), and / or by combination therapy in which the anti-CD73 molecule is administered before, after, or concurrently with chemotherapy.