Patents
Literature
Hiro is an intelligent assistant for R&D personnel, combined with Patent DNA, to facilitate innovative research.
Hiro

44 results about "Deubiquitinating enzyme" patented technology

Deubiquitinating enzymes (DUBs), also known as deubiquitinating peptidases, deubiquitinating isopeptidases, deubiquitinases, ubiquitin proteases, ubiquitin hydrolases, ubiquitin isopeptidases, are a large group of proteases that cleave ubiquitin from proteins and other molecules. Ubiquitin is attached to proteins in order to regulate the degradation of proteins via the proteasome and lysosome; coordinate the cellular localisation of proteins; activate and inactivate proteins; and modulate protein-protein interactions. DUBs can reverse these effects by cleaving the peptide or isopeptide bond between ubiquitin and its substrate protein. In humans there are nearly 100 DUB genes, which can be classified into two main classes: cysteine proteases and metalloproteases. The cysteine proteases comprise ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU). The metalloprotease group contains only the Jab1/Mov34/Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases.

Cyanopyrrolidines as dub inhibitors for the treatment of cancer

ActiveUS20180194724A1Nervous disorderOrganic chemistry methodsEnzymeUbiquitin C-Terminal Hydrolase
The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1) and ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer and conditions involving mitochondrial dysfunction. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1,R2,R3,R4,R5,R6,R7,R8 and R9 are as defined herein.
Owner:MISSION THERAPEUTICS

Novel compounds

ActiveUS20170247365A1Antibacterial agentsOrganic active ingredientsMedicinal chemistryUbiquitin C-Terminal Hydrolase
The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.
Owner:MISSION THERAPEUTICS

1-cyano-pyrrolidine compounds as usp30 inhibitors

The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (II) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R8, R9, R10, R12, Z, Y and m are as defined herein.
Owner:MISSION THERAPEUTICS LTD

Novel Compounds

The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f, R1g, R2, X, L and A are as defined herein.
Owner:MISSION THERAPEUTICS

1-cyano-pyrrolidine derivatives as dub inhibitors

The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The novel compounds have formula (I): (Formula (I)) or are pharmaceutically acceptable salts thereof, wherein: R1a, R1b, R1c, R1d, R1e and R1f each independently represent hydrogen, optionally substituted C1-C6 alkyl or optionally substituted C3-C4 cycloalkyl, or R1b and R1c together form an optionally substituted C3-C6 cycloalkyl ring, or R1d and R1e together form an optionally substituted C3-C6 cycloalkyl ring; R2 represents hydrogen or optionally substituted C1-C6 alkyl; A represents an optionally further substituted 5 to 10 membered monocyclic or bicyclic heteroaryl, heterocyclyl or aryl ring; L represents a covalent bond or linker; B represents an optionally substituted 3 to 10 membered monocyclic or bicyclic heterocyclyl, heteroaryl, cycloalkyl or aryl ring; and when -A-L-B is at position x attachment to A is via a carbon ring atom of A, and either: A cannot be triazolopyridazinyl, triazolopyridinyl, imidazotriazinyl, imidazopyrazinyl or pyrrolopyrimidinyl; or B cannot be substituted with phenoxyl; or B cannot be cyclopentyl when L is an oxygen atom.
Owner:MISSION THERAPEUTICS

Application of MERS-CoV 3CLpro (Middle East respiratory syndrome coronavirus 3C-like protease) as deubiquitinating enzyme and interferon inhibitor

The invention relates to the field of biomedicine, in particular to application of MERS-CoV 3CLpro (Middle East respiratory syndrome coronavirus 3C-like protease) as a deubiquitinating enzyme and interferon inhibitor. The invention provides a novel deubiquitinating enzyme and interferon inhibitor; the new understanding of the functionality of human coronavirus proteinase can be expanded; theoretical basis can be provided for the research on coronavirus and host antiviral natural immunization and the research on antiviral drugs using viral proteinase as a target.
Owner:ACADEMY OF MILITARY MEDICAL SCI

Application of inhibitor in preparation of drugs for treating cystic echinococcosis

The invention relates to application of an inhibitor in preparation of drugs for treating cystic echinococcosis, and particularly discloses application of an inhibitor for preparing drugs for treatingcystic echinococcosis. The inhibitor is selected from the following inhibitors: a deubiquitinating enzyme inhibitor, an EGFR inhibitor or a combination thereof. The inhibitor can effectively kill echinococcus granulosus (particularly echinococcus granulosus larva), and then the cystic echinococcosis is treated.
Owner:THE FIRST TEACHING HOSPITAL OF XINJIANG MEDICAL UNIVERCITY

Preparation and application of deubiquitinating enzyme inhibitor

The invention aims to provide a compound with single / double inhibitory activity on USP25 and USP28 proteases. The invention provides a compound shown as a formula I and a racemate, a stereoisomer, an isotope label, nitrogen oxide, a solvate, a polymorphic substance, a metabolite, a pharmaceutically acceptable salt or a prodrug of the compound.
Owner:刘丽萍

Biaryl pyridine deubiquitinating enzyme inhibitor as well as preparation method and application thereof

The invention designs and synthesizes a biaryl pyridine deubiquitinating enzyme inhibitor. The biaryl pyridine deubiquitinating enzyme inhibitor has the structure which is shown as a general formula (I). The biaryl pyridine deubiquitinating enzyme inhibitor provided by the invention has good inhibiting activity on deubiquitinating enzyme, and has a good in-vitro proliferation inhibiting effect ontumour cells, such as K562 cells, Hep-G2 cells, HCT-116 cells, WSD-DLCL cells and A549 cells. According to the compound disclosed by the invention, raw materials required for synthesis are easily obtained; a route design is reasonable; reaction conditions are mild; the yield in each step is high; the operation is simple and convenient; the biaryl pyridine deubiquitinating enzyme inhibitor is suitable for industrial production.
Owner:杭州市西溪医院

Thienopyrimidinone compound and medical application thereof

The invention relates to a thienopyrimidinone compound and a medical application thereof. The invention belongs to the field of medicines, and particularly relates to a compound as shown in a formula I, and pharmaceutically acceptable salt, ester, solvate, stereoisomer, tautomer, prodrug, any crystal form, and metabolite thereof or a mixture of the compound, the pharmaceutically acceptable salt, the ester, the solvate, the stereoisomer, the tautomer, the prodrug, any crystal form, and the metabolite. The invention also relates to the medical application of the compound shown in the formula I, the pharmaceutically acceptable salt, the ester, the solvate, the stereoisomer, the tautomer, the prodrug, any crystal form, the metabolite or the mixture of the compound, the pharmaceutically acceptable salt, the ester, the solvate, the stereoisomer, the tautomer, the prodrug and the metabolite. The compound provided by the invention can be used for inhibiting the activity of deubiquitinating enzyme USP7, and can also be used for preventing or treating USP7 regulation related diseases or symptoms (such as cancers).
Owner:SICHUAN KELUN BIOTECH BIOPHARMACEUTICAL CO LTD

Medicine for inhibiting Marek's disease virus replication and preventing or resisting Marek's disease

The invention provides a medicine for inhibiting Marek's disease virus replication, which comprises a deubiquitinating enzyme UL36 inhibitor and a medicine for preventing or resisting Marek's disease. The deubiquitinating enzyme UL36 inhibitor DUBs-IN-1 and the derivative thereof are screened out for the first time through an enzyme activity experiment for inhibiting virus encoding, a drug toxicity experiment on a CEF cell level, a virus CPE inhibition experiment and a chicken Marek's disease model experiment, the activity of UL36 can be inhibited on an enzyme level, replication of Marek's disease viruses can be inhibited on a cell level, and the Marek's disease tumor growth and visceral hemorrhage can be inhibited on the animal level, has the advantages of extremely strong effect and small dosage, and can be widely applied to production practice of Marek's disease prevention in poultry industry as an anti-MD drug.
Owner:JILIN UNIV

Application of deubiquitinating enzyme USP45 in preparation of medicine for treating esophageal cancer

The invention discloses application of deubiquitinating enzyme USP45 in preparation of a medicine for treating esophageal cancer, and belongs to the technical field of biological medicine. The invention finds that the mRNA expression level of the USP45 in esophageal cancer tissues is up-regulated and is related to the total lifetime of esophageal cancer patients, and the protein expression level of the USP45 in the esophageal cancer tissues is increased; uSP45 knock-down can significantly inhibit proliferation of esophageal cancer cells. The invention provides application of USP45 serving as an esophageal cancer molecular diagnosis marker or a prognosis prediction marker and application of USP45 serving as a target spot in preparation of drugs for treating esophageal cancer.
Owner:NANYANG INST OF TECH

Application of deubiquitinating enzyme inhibitor in preparation of medicine for resisting rabies virus

The invention provides application of a deubiquitinating enzyme inhibitor in preparation of a medicine for resisting rabies virus, and relates to the technical field of biological medicine. Experiments show that PR-619 has anti-rabies virus activity for the first time, and it is determined that PR-619 has prevention and treatment effects on rabies virus infection.
Owner:ACAD OF MILITARY SCI PLA CHINA ACAD OF MILITARY MEDICAL SCI INST OF MILITARY VETERINARY MEDICINE

Cyanopyrrolidines as dub inhibitors for the treatment of cancer

The present invention relates to novel compounds and method for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1) and ubiquitin C-terminal hydrolase 30 or ubiquitin specific peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of cancer and conditions involving mitochondrial dysfunction. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein.
Owner:MISSION THERAPEUTICS

Application of deubiquitinating enzyme USP25 in preparation of biomarker for diagnosing breast cancer

The invention provides an application of deubiquitinating enzyme USP25 in preparation of a biomarker for diagnosing breast cancer. The invention also provides application of the reagent for detecting the deubiquitinating enzyme USP25 in a kit for diagnosing breast cancer. The action principle that a homologous recombination repair mechanism regulates and controls breast cancer drug resistance is utilized, it is identified that the deubiquitinating enzyme USP25 is related to a homologous recombination repair pathway, the cell homologous recombination repair capacity can be remarkably improved by knocking out the USP25, and the resistance capacity of breast cancer cells to a PARP inhibitor is remarkably enhanced. Besides, IHC detection proves that USP25 is highly expressed in breast cancer tissues, and database analysis further shows that a breast cancer patient with simultaneous low expression of USP25 and BRCA1 has better HR repair capacity and is more tolerant to chemotherapeutic drugs. Therefore, the invention finds a novel molecular marker for breast cancer diagnosis and personalized treatment.
Owner:SHANGHAI EAST HOSPITAL EAST HOSPITAL TONGJI UNIV SCHOOL OF MEDICINE

Application of OTU Domain-Containing Deubiquitinase 1 in preparation of medicines for treating fatty liver and related diseases

The invention discloses an application of OTU Domain-Containing Deubiquitinase 1 in preparation of medicines for treating fatty liver and related diseases. According to the invention, a normal human hepatocyte L02 cell line is taken as a research object, lentivirus can be used for constructing an OTUD1 knockout and overexpression vector system, and an OTUD1 gene knockout or overexpressed L02 cellis obtained. The function of the OTUD1 gene in fatty degeneration is researched through a palmitic acid (PA) and oleic acid (OA) combination-induced fatty liver cell model. The result displays that under same PA+OA stimulation, compared with the L02 cell normally expressed by the OTUD1 gene, the red fat droplets in the L02 cell knockouted by the OTUD1 gene are large and multiple; and on the contrary, and the red fat droplets in the L02 cell overexpressed by the OTUD1 gene are small and less. The result shows that the OTUD1 gene can obviously inhibit liver lipid deposition and inhibit generation of fatty liver.
Owner:WUHAN UNIV

Compounds

The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 30 or Ubiquitin Specific Peptidase 30 (USP30). The invention further relates to the use of DUB inhibitors in the treatment of conditions involving mitochondrial dysfunction and cancer. Compounds of the invention include compounds having the formula (I): (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c, R1d, R1e, R1f, R1g, R2, X, L and A are as defined herein.
Owner:MISSION THERAPEUTICS

Methodologies for measuring isopeptidase activity in biological samples in a high throughput manner

The present invention relates to materials and methods for high throughput monitoring of target engagement of isopeptidases, such as deubiquitylating enzymes by, inter alia, small molecule inhibitors. In particular the invention relates to development of high throughput assays to measure isopeptidase activity in biological samples, such as cells, animal tissues, animal tumours, human tissue or patient-derived biopsies.
Owner:MISSION THERAPEUTICS

A class of biarylpyridine deubiquitinase inhibitors, its preparation method and application

The present invention designs and synthesizes a class of biarylpyridine deubiquitinase inhibitors, which have the structure of general formula (I): Formula (I) The biarylpyridine deubiquitinase inhibitors provided by the present invention have Sutinase has good inhibitory activity, and has good in vitro proliferation inhibitory effect on tumor cells such as K562 cells, Hep‑G2 cells, HCT‑116 cells, WSD‑DLCL2 cells and A549 cells. The raw materials required for the synthesis of the compound of the invention are easily available, the route design is reasonable, the reaction conditions are mild, the yield of each step is high, the operation is simple and convenient, and the method is suitable for industrial production.
Owner:杭州市西溪医院

A method for inhibiting the myogenic differentiation of bovine skeletal muscle satellite cells by interfering with uch-l3 expression

ActiveCN110951783BRegulates the process of development and differentiationInhibition of myogenic differentiation processActivity regulationVector-based foreign material introductionSkeletal Muscle Satellite CellsDeubiquitinating enzyme
The invention relates to a method for inhibiting the myogenic differentiation of bovine skeletal muscle satellite cells by interfering with the expression of UCH-L3, wherein the method is to suppress the myogenic differentiation of bovine skeletal muscle satellite cells by interfering with the expression of UCH-L3, wherein the The genome base sequence of UCH‑L3 is: SEQ NO.1. The method of the present invention regulates the myogenic differentiation process of bovine muscle satellite cells by changing the expression of UCH-L3, which can provide enlightenment for the research on deubiquitinating enzymes of muscle development and differentiation, and provide clinical research, diagnosis and treatment for muscle development and differentiation and injury repair Provide new ideas and references.
Owner:TIANJIN AGRICULTURE COLLEGE

Application of deubiquitinase 1 containing otu functional domain in the preparation of drugs for the treatment of fatty liver and related diseases

The invention discloses an application of OTU Domain-Containing Deubiquitinase 1 in preparation of medicines for treating fatty liver and related diseases. According to the invention, a normal human hepatocyte L02 cell line is taken as a research object, lentivirus can be used for constructing an OTUD1 knockout and overexpression vector system, and an OTUD1 gene knockout or overexpressed L02 cellis obtained. The function of the OTUD1 gene in fatty degeneration is researched through a palmitic acid (PA) and oleic acid (OA) combination-induced fatty liver cell model. The result displays that under same PA+OA stimulation, compared with the L02 cell normally expressed by the OTUD1 gene, the red fat droplets in the L02 cell knockouted by the OTUD1 gene are large and multiple; and on the contrary, and the red fat droplets in the L02 cell overexpressed by the OTUD1 gene are small and less. The result shows that the OTUD1 gene can obviously inhibit liver lipid deposition and inhibit generation of fatty liver.
Owner:WUHAN UNIV

Application of deubiquitinating enzymes USP42 as drug target in preparation of drugs

The invention relates to application of deubiquitinating enzymes USP42 as a drug target in preparation of drugs, in particular to a mechanism of the deubiquitinating enzymes USP42 for promoting lung cancer growth by regulating and controlling mRNA variable splicing through phase separation and application of the deubiquitinating enzymes USP42 in treatment of lung cancer. It is found through research that USP42 is positioned in a cell nucleus and is in a liquid phase separation state, a carbon-end disordered region with positive charges of USP42 drives phase separation to occur and enter a nuclear spot, and the activity of the deubiquitinating enzymes USP42 plays an important role in the process. The deficiency of USP42 can inhibit growth of tumor cells. USP42 regulates and controls the phase separation state of a splicing body component PLRG1 and mRNA splicing, and therefore gene expression participating in cell function regulation is affected. In conclusion, inhibition of USP42 can serve as a potential mode for tumor treatment.
Owner:DALIAN MEDICAL UNIVERSITY

Application of AgDT compound

The invention discloses application of [Ag(S2CN(C2H5)2)]6 to preparation of a medicine for preventing and curing tumor as well as application of the [Ag(S2CN(C2H5)2)]6 serving as deubiquitinating enzyme to preparation of a medicine for preventing and treating inflammation, tissue ischemia-reperfusion injury and myocardial hypertrophy diseases. The invention also provides the medicine for preventing and curing tumor, inflammation, tissue ischemia-reperfusion injury and myocardial hypertrophy diseases, which takes the [Ag(S2CN(C2H5)2)]6 as an active component, so that more choices are provided for clinical aspect.
Owner:GUANGZHOU MEDICAL UNIV

Application of deubiquitinating enzyme OTUD6A in preparation of medicine for preventing and treating prostatic cancer

The invention discloses application of deubiquitinating enzyme OTUD6A in preparation of a medicine for preventing and treating prostatic cancer, and discloses the application of the deubiquitinating enzyme OTUD6A as a regulatory molecule of the prostatic cancer and application of the OTUD6A as a target in preparation of the medicine for treating the prostatic cancer. Specifically, the invention discloses expression change of the OTUD6A in a prostatic cancer patient, the regulation and control effect of the OTUD6A for the proliferation and energy metabolism process of prostatic cancer cells, and the regulation and control effect of the OTUD6A in a tumor formation process of the prostatic cancer cell. Therefore, the invention provides the application of the OTUD6A serving as a prostatic cancer molecular diagnosis marker and the application of the OTUD6A serving as the target in screening and preparation of medicines for treating and preventing the prostatic cancer.
Owner:XI AN JIAOTONG UNIV +1
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products