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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

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

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

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

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 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
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