9 results about "Ubiquitin ligase binding" patented technology

Provided here are IRE1 degrader compounds comprising a protein target moiety covalently attached by a linker to an E3 ubiquitin ligase-binding moiety. Also provided are intermediate compositions for the preparation of IRE 1 degrader compounds and methods of treating diseases and disorders such as cancer with the IRE1 degrader compounds.

The present disclosure provides bifunctional compounds comprising a target protein binding moiety and a E3 ubiquitin ligase binding moiety, and associated methods of use.

Disclosed herein is a molecule, or a pharmaceutically acceptable salt thereof, that has a formula M1DO1-L-ME3, M1DO1 is a moiety that binds to IDO1, L is a linker covalently attaching M1DO1 and ME3, and ME3 is a moiety that binds to an E3 ubiquitin ligase. Disclosed herein are also the uses of the molecule, or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same, in a method of treating cancer in a subject in need thereof.

This disclosure provides a bifunctional compound comprising a target protein binding moiety and an E3 ubiquitin ligase binding moiety, and related methods of use.

The application belongs to the technical field of biological medicine, and provides application of astragaloside IV in preparation of a medicine for treating advanced ovarian cancer. The application analyzes and studies a targeting effect of AS-IV on CD276, determines a molecular mode of covalent combination of AS-IV and CD276, identifies a molecular mechanism of combination of AS-IV and CD276 through an E3 ubiquitin ligase and activation of an mTORC1 pathway of NK cells, and determines application potential of AS-IV in enhancement of NK cell anti-tumor immunity in preparation of an OC immunotherapy medicine.

The present invention relates to bifunctional compounds, which find utility to degrade and (inhibit) one or more of the following kinases: DYRK1A, DYRK1B, DYRK2, DYRK3, CLKI, CLK2, CLK3, CLK4, and HASPIN. In particular, the present invention is directed to compounds, which contain on one end an E3 ubiquitin ligase binding moiety which binds to an E3 ubiquitin ligase and on the other end a moiety which binds one or more of the following kinases: DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK3, CLK4, and HASPIN, such that the one or more kinases is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of the one or more kinases. The bifunctional compounds serve as therapeutics for the treatment of Alzheimer's disease, down syndrome, diabetes, an autoimmune disease, an inflammatory disorder (e.g., airway inflammation, osteoarthritis (e.g., knee related osteoarthritis)), cancer (e.g., glioblastoma, prostate cancer, metastatic breast cancer, metastatic lung cancer, multiple myeloma, secondary metastatic tumors of the brain, colorectal cancer), a viral infection (e.g., SARS-COV-2 infection (e.g., COVID-19)), and other diseases.

Bifunctional compounds comprising a GDC-0068 analog that binds AKT isoforms AKT1, 2 and 3 and a degron which represents a moiety that binds an E3 ubiquitin ligase, covalently attached to each other by a linker, pharmaceutical compositions, and methods for treating diseases or conditions mediated by dysfunctional AKT activity.

The invention relates to a compound which is a Proteolysis Targeting Chimera (PROTAC) or a pharmaceutically acceptable salt thereof, wherein the PROTAC has the structure:wherein U is an E3 ubiquitin ligase binding moiety, LINK is a moiety that covalently links M and U, and M is an MLLT1 and / or MLLT3 binder of formula (I):wherein:wherein Z1, Z2, Y1, Y2, Y3, R1, R2, R8, X, L and Hy are as defined herein, and either R8 is a bond to LINK, or M is bonded to LINK via a C or N atom within group R8 or ring Hy such that a hydrogen atom on the C or N atom within group R8 or ring Hy is replaced with a bond to LINK. The compounds are useful in the treatment of cancer.

To provide quinoline compounds or salts thereof. [Solution] A quinoline compound or a salt thereof having a structure represented by a specific formula (I): a compound having a structure in which an E3 ubiquitin ligase binding domain is linked to the 6th position of the quinoline skeleton via a linker, a compound having a structure in which an E3 ubiquitin ligase binding domain is linked to the 5th position of the quinoline skeleton via a linker, or a compound having a structure in which an E3 ubiquitin ligase binding domain is linked to the 8th position of the quinoline skeleton via a linker.