409 results about "Cell cycle" patented technology

A KIF18 inhibitor having a structure as shown in formula (I) and a synthesis method therefor. The compound can be used to adjust the KIF18A protein, thereby affecting a cell cycle and cell proliferation process for the treatment of cancer and cancer-related diseases. Further disclosed are a pharmaceutical composition containing the compound, and a method for the treatment of conditions associated with KIF18A activity.

The invention discloses application of chrysin-7-0-beta-D-glucuronide in treatment of ischemic heart disease or an LRP6 inhibitor, and belongs to the technical field of treatment of ischemic heart disease. The invention provides a new application of a small molecular compound chrysin-7-0-beta-D-glucuronide, the compound realizes regulation and control on a cardiac muscle cell cycle by inhibiting LRP6, and finally promotes repair of cardiac muscle cells and inhibits apoptosis. According to the invention, by exploring the function of inhibiting LRP6 protein of a small molecule drug, a powerful repair reaction is guided after myocardial ischemia reperfusion, so that effective treatment of myocardial infarction is realized. Therefore, finding of an LRP6 inhibitor not only has a potential curative effect on promoting myocardial cells to enter a cell cycle, but also has important significance on treatment of MI.

The invention relates to application of an ACBD3 inhibitor in preparation of a medicine for treating lung cancer and gRNA for inhibiting ACBD3 gene expression, and belongs to the field of bioengineering.199 binding proteins of ACBD3 are obtained through co-immunoprecipitation and mass spectrum identification, new biological functions of ACBD3 are excavated through GO analysis and KEGG pathway analysis of the binding proteins of ACBD3, and the application of the ACBD3 inhibitor in preparation of the medicine for treating lung cancer is developed. The ACBD3 is used for regulating and controlling a KEGG pathway enrichment map of a differential gene, and the ACBD3 is found to participate in the occurrence and development of cancers; the ACBD3 is successfully knocked out by designing gRNA, and tests prove that the multiple effects of slowing down A549 lung cancer cell proliferation, inhibiting lung cancer cell migration, inhibiting A549 lung cancer cell invasion, retarding A549 cell cycle G1 phase and reducing tumorigenicity can be achieved by knocking out the ACBD3.

The invention relates to the field of molecular targeted therapy, and discloses an application of an SLC16A5 (MCT6) small-molecule inhibitor MCT6-Ai7-2 in preparation of a medicine for treating acute myeloid leukemia (AML). The inhibitor takes an SLC16A5 protein structure predicted by Alphafold as a target spot, and is obtained through compound database screening, molecular docking and druggability optimization. An in-vitro experiment proves that MCT6-Ai7-2 can remarkably inhibit proliferation of AML cell lines such as U937 and MOLM-13, induce cell apoptosis and retard a cell cycle, has an inhibiting effect on a primary AML patient specimen and is relatively low in toxicity to normal cells; in-vivo experiments show that the compound is effective and has good safety in AML model mice. In addition, the MCT6-Ai7-2 and the vinca can be combined to synergistically enhance the inhibition effect on vinca drug-resistant cells, and by reducing the expression of anti-apoptotic protein MCL-1, the activation of pro-apoptotic factors BIM and tBID is promoted to play a role. The invention provides a novel targeting drug and strategy for treatment of AML (especially drug-resistant or recurrent patients).

Provided is a compound having a structure of formula (I) or a pharmaceutically acceptable salt, stereoisomer, isotope isomer, prodrug, hydrate or solvate thereof. The compounds are capable of modulating the KIF18A protein, thereby affecting the cell cycle and cell proliferation processes to treat cancer and cancer-related diseases. Also provided are methods of synthesis of the compounds, pharmaceutical compositions comprising the compounds, and methods for treating conditions associated with KIF18A activity.

The invention discloses an application of CD132 in treatment of AML (acute myeloid leukemia). The CD132 is differentially expressed in the AML, the expression level of the CD132 is related to the malignant degree of the AML and the total survival rate of AML patients, and CD132 knock-down can inhibit the proliferation capacity of AML cells, influence the cell cycle of the AML cells and promote cell apoptosis of the AML cells.

The invention discloses an application of LDLR in screening or preparing a medicine for treating acute myelogenous leukemia, the expression level of the LDLR in acute myelogenous leukemia cells is detected for the first time so as to characterize the conditions of proliferation, apoptosis, cycle and the like of the acute myelogenous leukemia cells, and the LDLR is taken as a target spot; by knocking down the expression quantity of the LDLR, the proliferation of acute myelogenous leukemia cells can be inhibited, the apoptosis of the acute myelogenous leukemia cells can be promoted, the cycle of the acute myelogenous leukemia cells can be retarded in the S phase, the in-vitro proliferation of the acute myelogenous leukemia cells can be accurately and effectively inhibited, and the application prospect is wide. A new thought and a new direction are provided for screening or preparing the medicine for diagnosing and treating the acute myelogenous leukemia.

The invention relates to application of piRNA as a target spot in preparation of a medicine for treating lung cancer or lung injury caused by tobacco exposure, and belongs to the technical field of biomedicine. The invention provides application of piR-2850767 and / or piR-157618 as a target spot in preparation of a medicine for treating lung cancer or lung injury caused by tobacco exposure, and particularly relates to application of an expression inhibitor of piR-2850767 and / or an overexpression reagent of piR-157618 in preparation of a medicine for treating lung cancer or lung injury caused by tobacco exposure. The inhibitor and the overexpression preparation can cause growth inhibition of lung cancer representative cells A549 and cause apoptosis of the lung cancer representative cells A549, and can recover cell cycle arrest, cell apoptosis, cell proliferation and motor ability decline of lung epithelial cells caused by tobacco exposure as a preventive drug for lung injury caused by tobacco exposure.

The invention discloses a limonin compound and application thereof in preparation of a medicine for preventing and / or treating cancers. The structure of the limonin compound is shown as a formula I or II. The cancer is at least one of breast cancer, liver cancer, gastric cancer, esophageal cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, prostatic cancer, nasopharynx cancer, cervical cancer, ovarian cancer, kidney cancer and skin cancer. According to the invention, activity screening is carried out on various natural product extracts, it is found for the first time that limonin compounds with structural formulas I and II have excellent inhibitory activity on various different types of human cancer cells, and an optional scheme is provided for broad-spectrum anti-cancer drugs. Related results also show that the compound provided by the invention can inhibit migration and invasion ability of breast cancer cells, promote cell apoptosis and retard a cell cycle. The limonin compound applied in the invention is derived from mallotus oblongifolius, the source is wide, and the production cost is low.

The invention relates to the technical field of cell engineering, and particularly discloses a construction method and application of a sika deer immortalized renal epithelial cell line, and the construction method comprises the following steps: taking renal epithelial primary cells from healthy sika deer renal cortex tissues to obtain primary renal epithelial cells; treating the primary renal epithelial cells with trypsin to obtain a cell suspension; inoculating the cell suspension into a complete culture medium, and transfecting with lentivirus loaded with SV40 large T antigen genes to obtain transfected cells; 3 [mu] g / mL puromycin is applied to the transfected cells for selective culture, so that non-transfected cells are eliminated, and drug-resistant cells are obtained; carrying out continuous passage on the drug-resistant cells for at least 30 generations to obtain the immortalized renal epithelial cell line of the sika deer; according to the invention, through a specific action mechanism (inhibiting a p53 / pRb pathway and blocking cell cycle exit) of the SV40 large T antigen, a proliferation limit caused by inhibition of telomerase activity of primary cells of the cervidae animals is overcome, and a cell resource library capable of realizing continuous passage is established.

The invention relates to the technical field of antitumor drugs, in particular to a Ru (II) complex and a preparation method and application thereof, and the Ru (II) complex has a structure as shown in a formula I. The Ru (II) complex synthesized by the method disclosed by the invention not only has relatively high cytotoxicity, but also has good photodynamic antitumor activity. After the complex is illuminated, the efficiency of the complex entering cells in an active transportation mode can be accelerated, mitochondria and endoplasmic reticulum are targeted at the same time, mitochondrial membrane potential decline and endoplasmic reticulum stress are caused to form a dual organelle damage effect, immunogenic cell death is caused, the tumor microenvironment is adjusted, and the tumor cell immunogenicity is improved. The enrichment of dendritic cells (DCs) in tumor cells is realized, the chemotactic activity of effector T cells is improved, the proportion of CD4 < + > and Foxp3 < + > cell populations is reduced, and finally the anti-tumor immune response is activated. Meanwhile, the complex provided by the invention can also induce the cell to generate pan apoptosis, retard the cell cycle in the G2 / M period and enhance the effect of the complex in inhibiting tumor proliferation.

The invention discloses application of a Lys35 site of a PC4 protein as a target spot in preparation of tumor diagnosis and treatment products. The invention provides application of a Lys35 site of a PC4 protein as a target spot in preparation of a tumor diagnosis product. The research shows that the Lys35 site methylation of the PC4 protein can promote the cell cycle progress of tumor cells and promote the proliferation growth and malignant progression of the tumor cells, and the scheme for inhibiting the site methylation can be used for developing tumor treatment drugs. Therefore, the Lys35 site of the PC4 protein can be used as a key target to be applied to development of tumor diagnosis products and targeted therapy drugs. The invention further develops the PC4 protein Lys35 methylation antigen peptide and the antibody capable of specifically recognizing the PC4 protein Lys35 methylation site, and the PC4 protein Lys35 methylation antigen peptide and the antibody can be applied to regulation and control of tumor cell proliferation or growth, can be used for developing diagnostic products and targeted therapy drugs for clinical tumor diseases, and have good clinical application value.

Compounds of formula (I): (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

The invention discloses an MSC culture medium composition and a culture method, and belongs to the field of biological medicine. Aiming at the problems of low MSC amplification efficiency and poor function maintenance in the prior art, the invention provides the MSC culture medium combination, which comprises a basic culture medium and functional factors, and the functional factors comprise an activation functional factor, an amplification functional factor and a steady-state functional factor which are sequentially added according to a preset time interval; wherein the activating functional factors comprise b-FGF, EGF and TGF-beta 1; the amplification functional factors comprise b-FGF (Fibroblast Growth Factor), PDGF-BB (Platelet Derived Growth Factor The steady-state functional factors comprise a b-FGF (Fibroblast Growth Factor) and IGF-1. The cell cycle is quickly started by activating the functional factors, differentiation is inhibited, and the functional factors are amplified to promote large-scale cell amplification; steady-state functional factor equilibrium amplification and dryness maintenance are carried out; and different functional factors are sequentially added according to a preset time interval, and the concentration of the factors is dynamically adjusted, so that differentiation tendency or aging acceleration caused by long-time high-concentration stimulation of a single factor is avoided, long-term efficient amplification of the MSC is realized, and the multifunctionality of the MSC is kept.

The invention belongs to the technical field of traditional Chinese medicines, and particularly relates to application of a traditional Chinese medicine composition in preparation of anti-hepatoma medicines. The traditional Chinese medicine composition comprises red ginseng, ox horn tip, musk, borneol, safflower, bezoar, radix aconiti lateralis praeparata slice, venenum bufonis, pseudo-ginseng, benzoin and pearl. Experimental results show that the traditional Chinese medicine composition can induce apoptosis and necrosis of liver cancer cells and inhibit proliferation of the liver cancer cells; and liver cancer cells are retarded to be in a G1 cell cycle. Therefore, the invention provides a new therapeutic drug for clinical treatment of liver cancer, and the raw materials are natural medicinal materials, have wide sources and have good application prospects.

The invention discloses a bacterial strain with an anti-tumor effect and application of the bacterial strain, the bacterial strain is Lactobacillus paracasei Biohalo 27, the bacterial strain is preserved in the China General Microbiological Culture Collection Center (CGMCC), and the preservation number is CGMCC NO.34917; the preservation time is June 16, 2025; the screened strain with the anti-tumor effect has the effects of inhibiting proliferation and migration of rectal cancer cells and breast cancer cells, retarding the cell cycle and promoting cell apoptosis, so that the anti-tumor purpose is achieved, and the strain can be used as a potential application value of probiotic adjuvant therapy.

The invention discloses an application of an ALK / LTK inhibitor in preparation of a product for treating and / or preventing chronic lymphocytic leukemia. Cell tests prove that the ALK / LTK inhibitor can inhibit an AKT signal channel at the downstream of LTK, so that the cell cycle of tumor cells is stopped, cell apoptosis is promoted, and finally the inhibiting effect on CLL cell proliferation is achieved; in a mouse model, the ALK / LTK inhibitor is proved to be capable of remarkably prolonging the survival time of tumor-bearing mice; the invention provides more drug choices for clinical treatment of CLL.

The invention discloses a polypeptide targeting NPAT protein and application of the polypeptide in inhibition of tumor cell proliferation, and relates to the technical field of biological medicines. The polypeptide provided by the invention is found in research on a regulatory mechanism formed by a membrane-free organelle-histone matrix in a cell nucleus. The polypeptide is over-expressed in cells, NPAT condensation in the cells can be effectively inhibited, then formation of a histone matrix is inhibited, and expression of a histone gene is down-regulated. A CCK8 experiment and a clone formation experiment can be used for observing that the polypeptide has an obvious effect of inhibiting tumor cell proliferation. The polypeptide is 1-50 amino acid sequences at the N end of NPAT protein, and can effectively interfere the normal function of NPAT for regulating histone transcription and hinder the normal process of the cell cycle. The compound has an application prospect in the field of medicines, and a new design idea can be provided for developing medicines for inhibiting abnormal proliferation of tumor cells.

The invention discloses a ganoderma lucidum lipid exosome containing a liver protection component and a preparation method and application thereof.The preparation method comprises the steps that the liver protection component is wrapped with a coarsely extracted ganoderma lucidum exosome, then the liver protection component is wrapped with lipidosome, and therefore a lipidosome-exosome-liver protection component three-layer structure is formed from outside to inside; in the three-layer structure, the outer layer liposome can protect the storage of the liver protection component and can improve the transmembrane transport efficiency, the middle layer exosome serves as a carrier and can reach a designated position to be released, and the inner layer contains the liver protection component and can improve the transmembrane transport efficiency. Cell cycle arrest can be prevented, antioxidant enzyme activity can be improved, cell membranes can be protected from oxidative damage, and redox steady state can be maintained to relieve cell aging. The prepared ganoderma lucidum lipid exosome containing the liver protection component realizes slow release synergy through a three-layer structure, and the action time of the active component is remarkably prolonged.

The invention provides a compound shown in a formula (I), and the compound can regulate KIF18A protein, so that the cell cycle and the cell proliferation process are influenced to treat cancers and cancer-related diseases. The invention also includes pharmaceutical compositions comprising the compounds and methods for treating conditions associated with KIF18A activity. # imgabs0 #

The invention discloses an application of 2, 3-dihydroxybenzoic acid in preparation of an antitumor drug. Researches find that 2, 3-dihydroxybenzoic acid can inhibit proliferation, migration and invasion of colorectal cancer cells in vitro and promote cell cycle arrest and cell apoptosis, and 2, 3-dihydroxybenzoic acid can inhibit growth of mouse transplanted tumors in vivo and promote cell apoptosis; the 2, 3-dihydroxybenzoic acid has a remarkable treatment effect on mouse colon cancer and can improve the immunotherapy effect; moreover, the 2, 3-dihydroxybenzoic acid small molecule substance, as an inhibitor of fatty acid synthase (FASN), plays an important role in inhibiting colorectum.

The present invention relates to the technical field of stem cell detection, and particularly relates to a determination method for purity and population doubling time of human umbilical cord mesenchymal stem cells (hUC-MSCs). The cultured hUC-MSCs are mixed with the buffer solution to obtain cell suspension; the cell suspension is mixed and incubated with a fluorescein-labeled antibody to obtain an incubated substance; and the incubated substance is centrifuged, and the precipitate obtained is cleaned and then mixed with the buffer solution to obtain a substance to be tested. The present invention analyzes cell surface markers and cell cycles by using a flow cytometer and monoclonal antibodies labeled with different fluoresceins of hUC-MSCs as well as PI staining, and further defines a determination method for purity and population doubling time of hUC-MSCs.

The present invention relates to chemical compounds having a general formula (I), as defined herein, and synthetic intermediates thereof, which are capable of modulating KIF18A protein thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of KIF18A.

The invention relates to rapamycin-loaded bionic nanoparticles as well as a preparation method and application thereof. The bionic nanoparticle loaded with the rapamycin comprises RZ NPs loaded with the rapamycin and a tumor cell membrane, the tumor cell membrane is coated with the RZ NPs loaded with the rapamycin; the rapamycin is modified in pores of the RZ NPs; and the RZ NPs has a crystal structure of ZIF8. The preparation method of the rapamycin-loaded bionic nano-particles comprises the following steps: preparing RZ NPs loaded with rapamycin, and modifying the RZ NPs by using a tumor cell membrane to prepare the RZM NPs. The RZM NPs provided by the invention has the capability of external irradiation sensitization on tumors, and due to the fact that rapamycin has potential influence possibility on cell cycles, tumor cells can be stagnated in a stage which is more sensitive to external irradiation, so that the radiotherapy effect is improved.

Metastatic uveal melanomas are highly resistant to all existing treatments. To identify actionable vulnerabilities, the inventors conducted a CRISPR-Cas9 knockout screen using a library composed of chromatin remodelers. They revealed that the histone H3 methyltransferase SETDB1 plays a critical role in metastatic uveal melanoma cell proliferation and survival. Functionally, SETDB1 knockdown triggers decreased expression of genes related to replication and cell cycle and promotes growth arrest associated with increased markers for DNA damage and senescence entry. Using pre-clinical model, they further demonstrated that anti-SETDB1 therapy tumor growth in vivo. The inventors identify SETDB1 as a new relevant therapeutic target for the treatment of metastatic uveal melanomas. The present invention relates to a method for treating uveal melanoma in a subject in need thereof comprising a step of administering said subject with a therapeutically effective amount of SETDB1 inhibitor.

The invention belongs to the technical field of animal gene engineering, and particularly relates to a down producing goat lncRNA, an interference vector and application of the interference vector to regulation and control of down producing goat hair follicle development, the down producing goat lncRNA is lncRNA TCONS-00237214 and is used for regulating and controlling down producing goat hair follicle development; the nucleotide sequence of the lncRNA TCONS-00237214 is as shown in SEQ ID NO. 1 (sequence identifier number 1). According to the invention, the hair papilla cells are selected for subsequent experimental verification, and the cell cycle, cell proliferation and cell migration of the hair papilla cells are detected by constructing an interference lncRNA TCONS-00237214 stable transformation hair papilla cell line. Results of the invention show that melatonin can regulate and control expression of lncRNA TCONS-00237214, participate in cell cycle transformation, promote proliferation and migration of hair papilla cells and inhibit apoptosis of the hair papilla cells, thereby affecting generation and development of hair follicles.

The invention discloses cell-penetrating peptide modified enzyme-sensitive PDC type PROTAC as well as a preparation method and application thereof, and belongs to the technical field of tumor targeted therapy. The cell-penetrating peptide modified enzyme-sensitive PDC type PROTAC is obtained by modifying a target protein ligand with a cell-penetrating peptide and an enzyme-sensitive Linker (GFLG) as an antitumor drug, has the capability of releasing the PDC type PROTAC under the catalysis of cathepsin B, has small influence on the cell activity of U251 cells, U87 cells and HEK293 cells, has proliferation inhibition activity on the U251 cells and the U87 cells, and can be used for preparing an antitumor drug. The polypeptide can degrade target proteins in U251 cells and U87 cells, can induce apoptosis of the U251 cells and the U87 cells, has an influence on the cycle of the U251 cells, can be used for preparing antitumor drugs (in the aspects of targeted protein degradation and membrane permeation), has a good application prospect in preparation of drugs targeting human brain glioma cells, and can be used in another important field of PROTAC drug development.

The invention provides application of tea catechin in preparation of a medicine for preventing and treating bortezomib-induced peripheral neuropathy. A plurality of in-vitro model results show that tea catechin can be used as a copper death inhibitor, remarkably improves related indexes of bortezomib-induced peripheral neuropathy, improves survival rates of Schwanton cells and SH-SY5Y, improves mitochondrial functions and cell cycle abnormalities of the Schwanton cells, reduces intracellular copper ion, cuprous ion and ATP levels, and can be used for preparing the copper death inhibitor for the peripheral neuropathy of the Bortezomib-induced peripheral neuropathy of the Bortezomib-induced peripheral neuropathy. Meanwhile, the death of Schwann cells and SH-SY5Y induced by the copper death inducer is reduced. In-vivo experiments show that the tea catechin plays a role in protecting functional damage of the bortezomib, and the tea catechin remarkably improves mechanical hyperalgesia, gait abnormality and pathological changes of myelin sheath and axon of mice caused by peripheral neuropathy induced by the bortezomib. The tea catechin can be used as a medicine for peripheral neuropathy induced by bortezomib, and has high clinical application value and development prospect.

The invention relates to an application of Avasimibe in preparation of a medicine for treating nasopharynx cancer or oral cancer, and belongs to the field of tumor targeted therapy. An in-vitro cell experiment and an in-vivo animal model experiment verify the anti-tumor effect of the compound. Experiments show that Avasimibe can significantly inhibit the activity, proliferation ability, healing ability and cloning ability of nasopharynx cancer cells and oral cancer cells, can regulate cell cycle arrest in a dose-dependent manner, and induces cell apoptosis. In vivo experiments, the tumor volume of nude mice in an Avasimibe treatment group is remarkably reduced, serum cholesterol is remarkably reduced, and serum biochemical analysis shows that compared with a control group, the Avasimibe treatment group has no statistical difference in indexes such as aspartate transaminase (AST) / glutamic-pyruvic transaminase (ALT) and creatinine (Cr). The invention provides a new indication for resisting nasopharynx cancer and oral cancer for the existing compound Avassimibe, has the clinical advantages of low toxicity and capability of overcoming drug resistance, and provides a new treatment choice for patients with nasopharynx cancer and oral cancer.

The invention provides an application of an ANGPT2 monoclonal antibody in preparation of a medicine for treating non-small cell lung cancer of a subject subjected to heavy ion treatment. Research results show that the promotion effect of the combined treatment of the nevapsumab and the heavy ion irradiation on ANGPT2 overexpression A549 cell cycle arrest and cell apoptosis rate and the inhibition effect on cell invasion, migration and clone forming ability are obviously better than those of the single treatment of the nevapsumab and the heavy ion irradiation. In a nude mouse transplantation tumor model, the inhibition effect of the combined treatment on the growth of ANGPT2 overexpression A549 cell transplantation tumor is more obvious than that of the single treatment of nevapsumab and heavy ion irradiation, and the negative influence on the physiological state of a host is smaller. A new strategy is provided for clinical treatment of the non-small cell lung cancer, and it is indicated that combined application of heavy ion treatment and ANGPT2 monoclonal antibody is expected to improve the treatment effect, prolong the lifetime of a patient and reduce treatment-related side effects, so that the life quality of the patient is remarkably improved.