177 results about "Arrestin" patented technology

Provided are a c-Myc protein inhibitor, and a preparation method therefor and use thereof. The c-Myc protein inhibitor selectively inhibits c-Myc protein. Therefore, the inhibitor can be used for prevention and treatment of diseases related to c-Myc protein disorders, such as cancers, cardiovascular and cerebrovascular diseases, diseases related to virus infection.

The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers.

The invention discloses application of an NR1D1 protein phosphorylation site in preparation of cerebral hemorrhage treatment drugs, and belongs to the technical field of molecular biology. According to the invention, the specific phosphorylation site and phosphorylation modification level of the NR1D1 protein are determined for the first time, and the NR1D1 protein can be used as a key marker for evaluating the secondary nerve injury degree of the hemorrhagic cerebral apoplexy and developing treatment and / or alleviation of the hemorrhagic cerebral apoplexy; a specific antigen peptide and an antibody for accurately detecting the NR1D1 protein phosphorylation site are further constructed, and an efficient tool is provided for molecular evaluation of hemorrhagic stroke secondary nerve injury; meanwhile, polypeptide molecules capable of inhibiting NR1D1 protein phosphorylation are researched and developed, through the dual effects of specifically blocking the phosphorylation process and reducing protein degradation, necrosis of brain tissues around hematoma after hemorrhagic cerebral apoplexy is relieved, secondary dyskinesia is improved, and the effect of inhibiting NR1D1 protein phosphorylation is achieved. And a brand new scheme is provided for molecular evaluation and targeted intervention of hemorrhagic stroke secondary nerve injury.

The invention discloses an antibody specifically bound with novel coronavirus nucleocapsid protein or an antigen binding fragment thereof and application thereof. The antibody or the antigen binding fragment thereof comprises a heavy chain variable region and a light chain variable region, the heavy chain variable region comprises a CDR1 of which the amino acid sequence is shown as SEQ ID NO: 5, a CDR2 of which the amino acid sequence is shown as SEQ ID NO: 6 and a CDR3 of which the amino acid sequence is shown as SEQ ID NO: 7; the light chain variable region comprises CDR1 of which the amino acid sequence is as shown in SEQ ID NO: 8, CDR2 of which the amino acid sequence is as shown in SEQ ID NO: 9 and CDR3 of which the amino acid sequence is as shown in SEQ ID NO: 10. The antibody provided by the scheme of the invention can specifically recognize the novel coronavirus nucleocapsid protein, and has the capability of inhibiting SARS-CoV-2 N protein from inducing excessive complement activation.

Provided herein are compounds of Formula (II) (e.g., Formula (II-a), (II-b), (II-a1), (II-b1), (II-a2), (II-b2), (II-3), (II-a3), (II-4), (II-a4), (II-5), (II-a5), (II-6), (II-a6), (II-7), (II-a7), (II-7), or (II-a8)), Formula (III) (e.g., Formula (III-1), (III-2), (III-3), (III-4), (III-5), (III-6), (III-7), or (III-8)), Formula (IV) (e.g., Formula (IV-a), (IV-b), (IV-c), (IV-a1), (IV-b1), (IV-a2), (IV-b2), (IV-a3), (IV-b3), (IV-a4), (IV-b4), (IV-a5), (IV-b5), (IV-a6), (IV-b6), (IV-a7), (IV-b7), (IV-a8), or (IV-b8)), Formula (V) (e.g., Formula (V-a) or (V-b), (V-a1), (V-c), (V-d), (V-b1), (V-a2), (V-b2), (V-a3), or (V-b3)), Formula (VI) (e.g., Formula (VI-a), (VI-b), (VI-c), (VI-d), or (VI-e))), or Formula (A) (e.g., Formula (I-a1)), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein (e.g., a dysregulated KRas protein (e.g., a mutated or amplified KRas protein)). This disclosure also provides compositions containing the compounds as provided herein, or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

The present invention relates to carbamate compounds of formula (I), as further detailed herein, for use in inhibiting the SARM1 protein, as well as compositions comprising these compounds and methods of treatment by administration of the compounds and compositions.

The invention belongs to the technical field of biological medicine, and relates to a small molecule compound for targeted inhibition of STRAP protein and application of the small molecule compound in colorectal cancer treatment. The invention discovers that the compound Y502-6036 can inhibit STRAP protein expression or / and function for the first time; moreover, it is found through cellular level experiment research that the compound Y502-6036 can inhibit proliferation, migration or / and invasion of colorectal cancer cells, and also can inhibit tumor globular formation ability; in-vivo experimental research finds that the compound Y502-6036 can inhibit the growth of colorectal cancer tumors, so that the compound Y502-6036 can be used for preparing medicines for preventing, relieving or / and treating colorectal cancer. Besides, the compound Y502-6036 and the anti-PD-1 antibody are combined for administration, so that the synergistic interaction effect is achieved, and the inhibition effect on the colorectal cancer is remarkably improved.

The invention discloses application of a substance for inhibiting MED10 protein activity and / or expression quantity in treatment of liver cancer. Experiments prove that the expression quantity of the MED10 protein and the encoding gene thereof in liver tissues or plasma of liver cancer patients is obviously higher than that of healthy people; by inhibiting the activity and / or expression quantity of the MED10 protein, proliferation of liver cancer cells can be inhibited, growth of the liver cancer cells can be inhibited, apoptosis of the liver cancer cells can be promoted, diffusion of the liver cancer cells can be inhibited, and metastasis of the liver cancer cells can be inhibited, so that the liver cancer can be treated. The method has an important application value.

Disclosed are inhibitors of a protein-protein interaction between protein arginine methyltransferase 5 (PRMT5) and methylosome protein 50 (MEP50) based on isoxazolyl methoxyphenyl derivatives. Further disclosed are pharmaceutical compositions comprising PRMT5:MEP50 inhibitors and methods of inhibiting protein arginine methyltransferase 5 (PRMT5) using PRMT5.MEP50 inhibitors or pharmaceutical compositions comprising PRMT5:MEP50 inhibitors.

Provided herein is a method of decreasing a-syn levels and / or decreasing a-syn toxicity in a cell, the method comprising contacting the cell with a charged multivesicular body protein 2B: a-synuclein (CHMP2B:a-syn) inhibitor and a method of inhibiting neural degeneration, the method comprising administering to a subject in need thereof a charged multivesicular body protein 2B: a-synuclein (CHMP2B:a-syn) inhibitor.

The application provides application of PAI-1 protein in detection and treatment of NEC patients and FNEC patients. The inventor of the application, in combination with years of experience and a large amount of research screening, obtains a biomarker capable of quickly assisting in diagnosis of NEC patients and identifying FNEC patients and Non-FNEC patients, and the biomarker is PAI-1 protein. The PAI-1 protein can be used for auxiliary diagnosis of NEC patients and early screening of FNEC patients, and FNEC patients are identified in time, so that intervention measures are taken in time, and mortality is reduced. Moreover, inhibition of expression of the PAI-1 protein can effectively relieve intestinal villus injury of a NEC model animal, and significantly reduce mortality. Therefore, the PAI-1 protein can be used as a potential target for treating NEC patients, and an agent for inhibiting expression of the PAI-1 protein can be used as a potential drug for treating NEC patients.

The present invention relates to a method of determining the responsiveness of a cancer patient to treatment with a compound that inhibits a KRAS protein or a KRAS protein mutant or treatment with a compound that inhibits the interaction between MDM2 and p53, the method comprising measuring the survivin level in a first sample obtained from the patient prior to treatment with the compound, measuring the level of survivin in a second sample obtained from the patient during or after treatment with the compound, comparing the level of survivin in the second sample to the level of survivin in the first sample, and determining the level of survivin in the second sample when compared to the level of survivin in the first sample. When the survivin level in the second sample decreases, it is determined that the patient is responsive to treatment with the compound. The invention further relates to the use of survivin in compounds for determining the inhibition of KRAS protein or KRAS protein mutants, or in compounds for inhibiting the interaction between MDM2 and p53, or a pharmaceutical formulation comprising said compound that inhibits a KRAS protein or a KRAS protein mutant or said compound that inhibits an interaction between MDM2 and p53 in a method of treating cancer.

A compound represented by formula (I). The compound has good agonistic activity on an APJ receptor, can effectively inhibit the production of cAMP, has weak ability to recruit β-arrestin, and has good pharmacokinetic properties.

Provided herein are compounds of Formula (II) (e.g., Formula (II-a), (II-b), (II-a1), (II-b1), (II-a2), (II-b2), (II-3), (II-a3), (II-4), (II-a4), (II-5), (II-a5), (II-6), (II-a6), (II-7), (II-a7), (II-7), or (II-a8)), Formula (III) (e.g., Formula (III-1), (III-2), (III-3), (III-4), (III-5), (III-6), (III-7), or (III-8)), Formula (IV) (e.g., Formula (IV-a), (IV-b), (IV-c), (IV-a1), (IV-b1), (IV-a2), (IV-b2), (IV-a3), (IV-b3), (IV-a4), (IV-b4), (IV-a5), (IV-b5), (IV-a6), (IV-b6), (IV-a7), (IV-b7), (IV-a8), or (IV-b8)), Formula (V) (e.g., Formula (V-a) or (V-b), (V-a1), (V-c), (V-d), (V-b1), (V-a2), (V-b2), (V-a3), or (V-b3)), Formula (VI) (e.g., Formula (VI-a), (VI-b), (VI-c), (VI-d), or (VI-e))), or Formula (A) (e.g., Formula (I-a1)), or pharmaceutically acceptable salts thereof, that inhibit a KRas protein (e.g., a dysregulated KRas protein (e.g., a mutated or amplified KRas protein)). This disclosure also provides compositions containing the compounds as provided herein, or pharmaceutically acceptable salts thereof, as well as methods of using and making the same.

This invention discloses a polypeptide that inhibits the desimilarization activity of tau protein and its applications, belonging to the field of biomedical technology. The polypeptide of this invention is tau. 438 The peptide is obtained through endogenous tau protein synthesis. The peptide provided by this invention can inhibit tau protein desimulation and increase tau mimicry, exhibiting high specificity and safely and effectively improving cognitive and memory function in AD model mice.

The invention relates to a group of antisense oligonucleotides for specifically inhibiting an androgen receptor and application thereof, the length of the antisense oligonucleotides is 14-22 basic groups, and the antisense oligonucleotides (ASO) are applied as follows: (1) preparing a preparation for inhibiting the expression quantity of AR protein; (2) preparing a medicine or a medicine composition for treating androgen-induced alopecia; or (3) preparing a medicine or a medicine composition for treating androgen-induced acne; or (4) inhibiting expression or activation of AR protein; and (5) treating diseases caused by overexpression or transition activation of the AR protein, wherein the diseases comprise but are not limited to tumors, alopecia or acne caused by overexpression or transition activation of the AR protein.

Disclosed herein are 2-amino imidazole derivatives. These compounds inhibit Protein Arginine N-Methyl Transferase 5 (PRMT5) activity. In addition to the compounds, disclosed herein are pharmaceutical compositions containing the compounds, and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.

The invention provides a pilot small-molecule compound and application thereof, the structural formula of the pilot small-molecule compound is shown in the specification, and application of the small-molecule compound in preparation of a preparation for inhibiting FGL2 activity. The pilot small molecule compound provided by the invention can be combined with FGL2 protein to play a role in inhibiting the FGL2 protein, so that the development process of tumors is slowed down.

Compounds comprising an amide-linked coumarin scaffold, compositions comprising same, and method of using such compounds and compositions to inhibit tubulin-associated unit (tau) protein aggregation or alpha-synuclein ( α-syn) protein aggregation in a subject having, or at risk for, tau protein aggregation or α-syn protein aggregation, respectively.

The present application relates to a kind of FOXM1 protein phosphorylation modification interfering peptide and its application, belong to the field of biological medicine technology. Specifically, the present application is found in research, the transcriptional activity of FOXM1 protein depends on the condensate formed by its polymerization, destroying the polymerization of FOXM1 can effectively inhibit the occurrence and development of tumor, and the phosphorylation of the 376th amino acid of FOXM1 protein can also inhibit polymerization to some extent, thereby inhibiting the transcriptional activation of FOXM1 protein. Therefore, the present application designs an interfering peptide, and introduces phosphorylation modification in appropriate position, obtains a kind of phosphorylation modification interfering peptide FIP4 targeted to FOXM1 protein polymerization domain, the interfering peptide plays a significant role in inhibiting the transcriptional activation of FOXM1 protein in cell and animal in vivo, and can be used for treating tumor-related diseases.

To provide a protein adsorption inhibitor that can suppress the adsorption of proteins to surfaces such as immunoreaction vessels and measuring instruments to a high degree, while also reducing variability between measurements. [Solution] Formula (1): Z-{O-[(PO) a (EO) b ]-(AO) c -H]} x A protein adsorption inhibitor comprising an alkylene oxide derivative represented by (the definition of the symbols in the formula is as described in the specification), wherein the cloud point of a 1% by mass aqueous solution of the alkylene oxide derivative is 0°C or higher and 30°C or lower.

The present invention provides, inter alia, apelin receptor agonists having increased half-life, reduced desensitization, improved apelin receptor signaling properties (e.g., bias of G a signaling over arrestin signaling), enhanced stability, and / or enhanced binding to apelin receptors.

The application discloses an EZH2 and BRD4 double-target inhibitor and application thereof, wherein the double-target inhibitor is obtained by coupling a structural fragment for inhibiting a BRD4 protein and a structural fragment for inhibiting an EZH2 protein through a linker. The inventors find that the structural fragment for inhibiting the EZH2 protein and the structural fragment for inhibiting the BRD4 protein are restructured, coupled together through the linker, and the length of the linker is adjusted, so that the obtained EZH2 and BRD4 double-target inhibitor has an unexpected anti-tumor effect, the anti-tumor effect is better than that of an individual EZH2 inhibitor or BRD4 inhibitor, and is also better than that of a combination of the two under the same conditions.

This invention provides a polypeptide, a polypeptide product comprising the same, a kit, and applications. The polypeptide, particularly those shown in SEQ ID NO:1 to SEQ ID NO:8, specifically binds to the spike protein of SARS-CoV-2, thereby competitively inhibiting the binding of the SARS-CoV-2 spike protein to hACE2. These polypeptides can competitively reduce or inhibit the binding of the S protein to the ACE2 protein, and therefore can serve as drugs or potential drugs to weaken or inhibit the infectivity of SARS-CoV-2 in humans.

The present application relates to RAS inhibitors. The invention features macrocyclic compounds capable of inhibiting Ras proteins and pharmaceutical compositions and protein complexes thereof, and their use in the treatment of cancer.

The present invention relates to a compound that may be useful for inhibiting RAS protein. More specifically, the present invention relates to a compound for inhibiting broad-spectrum KRAS mutant protein. Therefore, the compound of the present invention can be used to treat conditions mediated by KRAS protein. For example, the compound can be used to treat cancer.

The application provides a screening device and method and application of small molecules for inducing or inhibiting protein polymerization, adopts a solid-state quartz nanopore as a core detection device, drives target proteins or complexes of the target proteins and small molecules to pass through a nanoscale pore, records ion current changes caused by each time of perforation event in real time, analyzes peak current and residence time characteristic values of each event, and can identify whether the proteins are in monomer, oligomer, aggregation or LLPS state. Meanwhile, the nanopore sensing is combined with small molecule processing, a mapping relationship between current signal changes and aggregation state regulation is established, and screening of small molecules for inducing or destroying protein aggregation behavior is realized. The technology has multiple advantages of label-free, single molecule, real-time monitoring and adaptation to multiple protein aggregation states, and breaks through the bottleneck of throughput and resolution capacity of existing methods.

The present invention relates to novel compounds for inhibiting protein kinases and pharmaceutical compositions comprising the same. More particularly, the compound according to the present invention can effectively inhibit various protein kinases, and thus can be effectively used for developing a therapeutic agent for protein kinase-related diseases, particularly cancer.