40 results about "Inhibitory molecules" patented technology

The invention relates to application of mitogen-activated protein kinase PiPmk1 in screening molecules for inhibiting formation of a phytophthora infestans infection structure. The invention finds that the molecular marker plays a key role in the development of a phytophthora infestans cyst bud tube and / or the formation of an infection structure, which indicates that the molecular marker has the potential of serving as a target for inhibiting phytophthora infestans infection, and a corresponding molecular screening method and a generative prediction model are further developed and utilized; rapid and accurate prediction and screening of phytophthora infestans infection inhibitory molecules are realized, the research and development period and cost are greatly shortened, and a new thought and a new method are provided for development of accurate targeted green pesticides.

Compositions and methods for treating diseases associated with expression of a cancer associated antigen are disclosed. The invention also relates to chimeric antigen receptor (CAR) specific to a cancer associated antigen as described herein, SHP inhibitory molecules, vectors encoding the same, and recombinant immune effector cells comprising the CARs and SHP inhibitory molecules. Methods of administering a genetically modified immune effector cell expressing a CAR that comprises an antigen binding domain that binds to a cancer associated antigen and a SHP inhibitory polypeptide are also disclosed.

The present invention relates to the use of compounds of formula (I) as RAS inhibitors and as a medicament, in particular for use in treating proliferative disorders, inflammatory diseases and / or genetic disorders. The present invention relates further to a pharmaceutical composition comprising the compounds of formula (I). Moreover, the present invention relates to a method of inhibiting growth, proliferation or metastasis of cancer cells in a subject in need thereof, in particular which may encompass subsets of patients defined by their mutational status of the RAS oncogene or patients who might have developed resistance to the standard of care or treatment with RAS mutation specific inhibitors. The present invention also relates to a method of inhibiting RAS molecules in treating genetic disorders like RASopathies or inflammatory disorders like Adenomyosis where KRAS gene is mutationally activated. In addition, the present invention relates to a method of inhibiting proliferation and or secretion of factors from a cell population sensitive towards inhibiting RAS activation in vitro, in particular sensitive towards inhibiting KRAS. HRAS and NRAS activation in vitro. Furthermore, the present invention relates to a kit containing a formulation comprising a pharmaceutical composition comprising a compound of formula (I).

The present invention refers to a composition comprising an inhibitory molecule capable of inhibiting the expression of a gene selected from any of the list consisting of SMPD1, ARAP1, CST3, GSN, HDAC5, PACS1, TOM1L2, TSC22D3 and USP20 or homologues thereof and increasing the levels of endogenous SMN1 and / or SMN2 proteins, or a mixture of two or more of said molecules, for use in the treatment of Spinal Muscular Atrophy (SMA) in a subject in need thereof.

A combination therapy comprising a semaphorin-4D inhibitory molecule and Flt3 ligand or a FLT3 agonist with or without a checkpoint inhibitor for treating cancer is disclosed.

The present invention relates to the use of compounds of formula (I) as RAS inhibitors and as a medicament, in particular for use in treating proliferative disorders, inflammatory diseases and / or genetic disorders. The present invention relates further to a pharmaceutical composition comprising the compounds of formula (I). Moreover, the present invention relates to a method of inhibiting growth, proliferation or metastasis of cancer cells in a subject in need thereof, in particular which may encompass subsets of patients defined by their mutational status of the RAS oncogene or patients who might have developed resistance to the standard of care or treatment with RAS mutation specific inhibitors. The present invention also relates to a method of inhibiting RAS molecules in treating genetic disorders like RASopathies or inflammatory disorders like Adenomyosis where KRAS gene is mutationally activated. In addition, the present invention relates to a method of inhibiting proliferation and / or secretion of factors from a cell population sensitive towards inhibiting RAS activation in vitro, in particular sensitive towards inhibiting KRAS, HRAS and NRAS activation in vitro. Furthermore, the present invention relates to a kit containing a formulation comprising a pharmaceutical composition comprising a compound of formula (I).

The present invention relates to a planar amide derivative thermally activated delayed fluorescence material represented by formula (1), and its preparation method and application. The compound has a highly twisted molecular structure, and such molecules have high molecular rigidity, which is beneficial to inhibiting intra-molecular and inter-molecular vibrational and rotational relaxations, achieving high light efficiency. In addition, it also has a small singlet-triplet energy gap (<0.2 eV), enabling the planar amide derivative of the present invention to possess thermally activated delayed fluorescence properties. Compared with the commercial iridium complex Flrpic, the electroluminescent device prepared using the planar amide derivative thermally activated delayed fluorescence material of the present invention has a higher external quantum efficiency.

The application relates to a novel triarylamine compound with two carbazole units introduced on a biphenyl-triarylamine and application thereof, wherein, by fixing one of the carbazole units at the ortho position of the biphenyl in the triarylamine, a twisted structure is formed, thus effectively inhibiting the aggregation of the molecule, so that a stable dense film is formed; by changing the position of the other carbazole and the structure of the other two aryl groups of the triarylamine, the energy level barrier and the hole mobility can be effectively regulated, and the efficiency and the service life of the device are improved. Meanwhile, the double-carbazole system can more effectively inhibit the diffusion of electrons from the light-emitting layer to the hole side, so that the service life of the device is further improved.

The present invention improves an effect of killing or an effect of inhibiting the growth of cancer cells. The present invention comprises: a binding domain that includes a first antigen-binding site that binds to a cancer cell and a second antigen-binding site that binds to a T cell; a cleavable sequence that is linked to the binding domain; and a masking moiety that is linked to the N-terminus of a single-chain antibody via the cleavable sequence when the binding domain is composed of the single-chain antibody, and that is linked to the C-terminus of each light chain via the cleavable sequence when the binding domain is composed of heavy chains and light chains. In a state in which the cleavable sequence is cleaved, the masking moiety functions as an agonist of a co-stimulatory molecule for the T cell or an antagonist of a co-inhibitory molecule for the T cell.

The invention discloses a piRNA marker related to colorectal cancer and application of the piRNA marker. The nucleotide sequence of the piRNA is shown as SEQ ID NO: 1. The piRNA molecule provided by the invention can be used as a marker for diagnosing the colorectal cancer, and the colorectal cancer can be accurately detected by detecting the piRNA molecule; meanwhile, by inhibiting expression of piRNA molecules, proliferation, invasion and metastasis of colorectal cancer cells can be effectively inhibited, and a novel powerful molecular biological tool is provided for treatment of colorectal cancer. The method has profound clinical significance and important popularization and application prospects.

The present invention relates to an inhibitor of heat shock protein 90, and discloses a bivalent inhibitor based on heat shock protein 90, a preparation method, and an application thereof. The compound has a structural formula as shown in Formula I: A-L-B Formula I, or a pharmaceutically acceptable salt, solvate, or optical isomer thereof, wherein A and B are ATP inhibitors of heat shock protein 90, and the motif structure of L is a flexible linking group of PEG and alkane, or a rigid linking group having an aryl, heteroalkyl, or heteroaryl group. The bivalent inhibitor can effectively inhibit the activity of the molecular chaperone protein HSP90, hinder the folding and modification of substrate proteins, degrade substrate proteins through the ubiquitin-proteasome pathway, induce non-native dimerization of HSP90, and interfere with protein-protein interactions associated with HSP90. At the same time, it also reduces the heat shock effect caused by HSP90 inhibition, and exhibits potent activity in degrading substrate proteins.

The present disclosure relates to a cell-based assay for determining in vitro tumor killing activity of immune cells expressing a chimeric antigen. The present disclosure provides an in vitro method for determining the potency (e.g., cytotoxicity) of immune cells expressing a chimeric antigen receptor (CAR) molecule. In a test sample, the CAR-expressing immune cells are incubated with target cells that express an antigen that interacts with the CAR. In a control sample, the CAR-expressing immune cells are incubated with the target cells and an inhibitory molecule that prevents the interaction between the CAR and the target cells. The amount of target cell death is determined in both the test sample and the control sample and compared.

The present invention provides compositions and methods comprising an activator of interleukin-18 (IL-18) activity for use in therapeutic and non-therapeutic applications. The activator provides IL-18 signaling activity even in the presence of an inhibitory molecule 5 such as IL-18 binding protein (IL-18BP).

The present invention relates to the use of compounds of formula (I) as RAS inhibitors and as a medicament, in particular for use in treating proliferative disorders, inflammatory diseases and / or genetic disorders. The present invention relates further to a pharmaceutical composition comprising the compounds of formula (I). Moreover, the present invention relates to a method of inhibiting growth, proliferation or metastasis of cancer cells in a subject in need thereof, in particular which may encompass subsets of patients defined by their mutational status of the RAS oncogene or patients who might have developed resistance to the standard of care or treatment with RAS mutation specific inhibitors. The present invention also relates to a method of inhibiting RAS molecules in treating genetic disorders like RASopathies or inflammatory disorders like Adenomyosis where KRAS gene is mutationally activated. In addition, the present invention relates to a method of inhibiting proliferation and / or secretion of factors from a cell population sensitive towards inhibiting RAS activation in vitro, in particular sensitive towards inhibiting KRAS, HRAS and NRAS activation in vitro. Furthermore, the present invention relates to a kit containing a formulation comprising a pharmaceutical composition comprising a compound of formula (I).

The present invention relates to lipid-based nanoparticles comprising an antigen-binding domain capable of specifically binding to a target expressed on the surface of activated immune cells, and one or more mRNA molecules encoding an inhibitory protein of the activated immune cells, and to the use thereof.

The invention belongs to the field of organic photoelectric materials and biomedical treatment, and discloses a preparation method and application of an intramolecular proton transfer fluorescent material. The fluorescent molecule is constructed by constructing different receptor units on the basis of donor-receptor configuration. Ar is 3-(ethylidene amino) naphthalene-2-alcohol # imgabs 1 #. According to the invention, imino indole and cyano indanone groups are introduced to one end of a donor, so that a donor-acceptor and a charge transfer state are constructed, and meanwhile, non-radiative transition and intermolecular pi-pi accumulation of molecules in an aggregation state are inhibited; and meanwhile, the material also retains the excellent light response property of the molecular motor, and the introduction of OH bonds enables the material to inhibit the non-radiative transition process of the molecular motor through intramolecular proton transfer, so that the ratio of radiative transition is greatly increased. A thought is provided for the design of the molecules.

The present invention relates to the use of compounds of formula (I) as RAS inhibitors and as a medicament, in particular for use in treating proliferative disorders inflammatory diseases and / or genetic disorders. The present invention relates further to a pharmaceutical composition comprising the compounds of formula (I). Moreover, the present invention relates to a method of inhibiting growth, proliferation or metastasis of cancer cells in a subject in need thereof, in particular which may encompass subsets of patients defined by their mutational status of the RAS oncogene or patients who might have developed resistance to the standard of care or treatment with RAS mutation specific inhibitors. The present invention also relates to a method of inhibiting RAS molecules in treating genetic disorders like RASopathies or inflammatory disorders like Adenomyosis where KRAS gene is mutationally activated. In addition, the present invention relates to a method of inhibiting proliferation and or secretion of factors from a cell population sensitive towards inhibiting RAS activation in vitro, in particular sensitive towards inhibiting KRAS, HRAS and NRAS activation in vitro. Furthermore, the present invention relates to a kit containing a formulation comprising a pharmaceutical composition comprising a compound of formula (I).

To provide an NK inhibitory molecule that can significantly suppress the killing action of NK cells in the subject's body, thereby reducing the risk of HvGD, compared to conventional genetically modified immune cells, and to provide a genetically modified immune cell that expresses the molecule.SOLUTION: Provided is an NK inhibitory molecule comprising one or more NK inhibitory ligands, a transmembrane domain and a co-stimulatory domain, the NK inhibitory ligand specifically binding to an NK inhibitory receptor and inhibiting NK cells from killing genetically modified immune cells that express the NK inhibitory molecule. Provided is a genetically modified immune cell that expresses an NK inhibitory molecule of the invention, the expression of at least one MHC-associated gene being inhibited or silenced. Provided is use of the genetically modified immune cells in the treatment of cancer, infectious disease or autoimmune disease.SELECTED DRAWING: Figure 1

The disclosure relates to methods for treating cognitive decline or selecting subjects for treatment with an anti-semaphorin-4D antibody using the subject's Mini-Mental State Exam (MMSE) score and / or an equivalent cognitive assessment test score as a patient biomarker.

This invention belongs to the field of biomedicine and discloses the application of palmitoyltransferase ZDHHC21 in the preparation of drugs for treating breast cancer. This invention demonstrates that ZDHHC21 knockdown upregulates RIPK1 expression, which is related to signal feedback induced by CD82 palmitoylation deficiency. Depalmitoylated CD82 competitively binds to RIPK1 inhibitory molecules, thereby releasing the regulation of RIPK1, promoting the interaction and phosphorylation activation of RIPK1 and RIPK3, and subsequently upregulating MLKL expression and inducing its activation. Downstream activation of Caspase-3 ultimately initiates necroptosis. A specific regulatory axis of "ZDHHC21–CD82–pan-apoptosis" is established. This provides a potential novel therapeutic target for triple-negative breast cancer and offers a theoretical and experimental basis for therapeutic strategies targeting tumor cell death. Further research can explore the role of this regulatory axis in vivo, providing support for clinical translation.

The invention discloses a pharmaceutical composition containing an antibody drug conjugate and application of the pharmaceutical composition. The invention provides a pharmaceutical composition 1 which comprises a compound C, a histidine buffer agent, a saccharide stabilizer, a surfactant and water, and the pH value of the pharmaceutical composition 1 is 6.0-6.5; wherein the compound C is A-(B) n. The pharmaceutical composition provided by the invention can be stably stored in a liquid form for a long time without freeze-drying, can effectively inhibit ADC molecule aggregation and degradation, has excellent biological activity and safety, and greatly improves the convenience of clinical application while reducing the production cost. Meanwhile, the pharmaceutical composition disclosed by the invention can maintain good stability after being subjected to freeze-drying treatment and redissolution, so that more choices are provided for clinical application.

This invention discloses a near-infrared II photothermal therapeutic agent, its preparation method, and its application, belonging to the field of optical diagnostics and treatment technology. To address the problems of insufficient light absorption, fluorescence quenching, and inadequate molecular structure optimization in existing photothermal therapeutic agents, this invention proposes a molecular design strategy of "central plane + peripheral twisting," developing a novel NIR-II photothermal therapeutic agent, 4TPE-TB, which is a near-infrared II photothermal therapeutic agent. This invention enhances the light absorption capacity of the near-infrared II photothermal therapeutic agent by strengthening the conjugation of the molecular core, and utilizes the peripheral twisted structure to suppress intermolecular stacking, significantly improving photothermal conversion efficiency and fluorescence performance, thereby achieving a comprehensive improvement in the therapeutic agent's performance.

The present invention provides compositions and methods comprising an activator of interleukin-18 (IL-18) activity for use in therapeutic and non-therapeutic applications. The activator provides IL-18 signaling activity even in the presence of an inhibitory molecule 5 such as IL-18 binding protein (IL-18BP).

The present invention provides compositions and methods comprising an activator of interleukin-18 (IL-18) activity for use in therapeutic and non-therapeutic applications. The activator provides IL-18 signaling activity even in the presence of an inhibitory molecule such as IL-18 binding protein (IL-18BP).

The application discloses a kind of drug composition containing antibody drug conjugate and application thereof.The application provides a kind of drug composition 1, it includes compound C, histidine buffer, saccharide stabilizer, surfactant and water, the pH of the described drug composition 1 is 6.0-6.5;Wherein, the compound C is A-(B) n The drug composition of the application can be long-term stably stored in liquid form without freeze-drying, can effectively inhibit the aggregation and degradation of ADC molecules, has excellent biological activity and safety, greatly improves the convenience of clinical application while reducing the production cost.Meanwhile, the drug composition of the application can also maintain good stability after freeze-drying treatment and reconstitution, providing more options for clinical application.

The present invention relates to the use of compounds of formula (I) as RAS inhibitors and as pharmaceutical agents, particularly for the treatment of proliferative, inflammatory, and / or genetic disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I). Furthermore, the present invention relates to methods for inhibiting the growth, proliferation, or metastasis of cancer cells in a subject in need thereof, which may include, in particular, a subset of patients defined by their RAS oncogene mutation status, or patients who have developed resistance to standard treatment or treatment with RAS mutation-specific inhibitors. The present invention also relates to methods for inhibiting RAS molecules in the treatment of genetic disorders such as RAS syndromes or inflammatory diseases such as adenomyosis in which the KRAS gene is activated by mutations. The present invention also relates to methods for inhibiting the proliferation and / or secretion of factors from cell populations sensitive to in vitro inhibition of RAS activation, particularly cell populations sensitive to in vitro inhibition of KRAS, HRAS, and NRAS activation. Furthermore, the present invention relates to kits containing formulations of pharmaceutical compositions containing compounds of formula (I).

The invention discloses a pharmaceutical composition containing an antibody drug conjugate and application of the pharmaceutical composition. The invention provides a pharmaceutical composition 1 which comprises a compound C, a histidine buffer agent, a saccharide stabilizer, a surfactant and water, and the pH value of the pharmaceutical composition 1 is 6.0-6.5; wherein the compound C is A-(B) n. The pharmaceutical composition provided by the invention can be stably stored in a liquid form for a long time without freeze-drying, can effectively inhibit ADC molecule aggregation and degradation, has excellent biological activity and safety, and greatly improves the convenience of clinical application while reducing the production cost. Meanwhile, the pharmaceutical composition disclosed by the invention can maintain good stability after being subjected to freeze-drying treatment and redissolution, so that more choices are provided for clinical application.

The invention belongs to the field of organic photoelectric materials, and discloses preparation and application of a D-A type organic molecular motor stimulation material. Based on a donor-receptor configuration, the compound has the following structure: # imgabs0 #, wherein Ar is N, N-dimethylaniline and a derivative thereof. According to the invention, an imino indole group is introduced to one end of a donor N, N-dimethylaniline and a derivative thereof, so that a donor-acceptor and a charge transfer state are constructed, and meanwhile, non-radiative transition of molecules in an aggregation state is inhibited, so that the material is endowed with the property of AIE. In addition, due to the introduction of a C = N bond, the material shows an excellent molecular motor characteristic, and has a photoresponse phenomenon of donor rotation under optical excitation. After the trifluoroacetic acid proton-donating acidic material is added, the absorption spectrum is faded or the absorption wavelength is subjected to red shift. The material provided by the invention has efficient light and acid response capability, and has good application prospects in the aspects of information storage, optical signal transmission and information encryption.