Kymera Therapeutics Inc. has described proteolysis targeting chimera (PROTACs) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a signal transducer and activator of transcription 6 (STAT6)-targeting moiety.
Shenzhen Zhongge Biotechnology Co. Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to an interleukin-1 receptor-associated kinase 4 (IRAK-4) targeting moiety via a linker reported to be useful for the treatment of cancer, autoimmune disorders, inflammatory disorders, transplant rejection, thromboembolism, atherosclerosis, myocardial infarction and metabolic syndrome.
Katalytic Therapeutics Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a phosphodiesterase PDE4-targeting moiety reported to be useful for the treatment of arthritis, Behçet’s disease, chronic obstructive pulmonary disease, non-small-cell lung cancer, inflammatory disorders, inflammatory bowel disease, psoriasis and rheumatoid arthritis.
Scientists at Guangzhou Imd Therapeutics Co. Ltd. and Pamplona Therapeutics (Shenzhen) Co. Ltd. have described proteolysis targeting chimeric (PROTAC) compounds comprising cereblon (CRBN) ligands covalently linked to an interleukin-1 receptor-associated kinase 4 (IRAK-4) targeting moiety through a linker reported to be useful for the treatment of atopic dermatitis, autoimmune disease, cancer, cardiovascular, eye and inflammatory disorders, rheumatoid arthritis and inflammatory bowel disease, among others.
Haisco Pharmaceutical Group Co. Ltd. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to an androgen receptor (AR) targeting moiety acting as AR degradation inducers reported to be useful for the treatment of prostate cancer.
Biotheryx Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a son of sevenless homolog 1 (SOS1) targeting moiety reported to be useful for the treatment of cancer.
Humanwell Healthcare (Group) Co. Ltd. has described proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to an interleukin-1 receptor-associated kinase 4 (IRAK-4) targeting moiety via a linker reported to be useful for the treatment of cancer, rheumatoid arthritis, renal disorders, multiple sclerosis, alopecia areata, urticaria, psoriasis and chronic obstructive pulmonary disease (COPD), among others.
Enhanced quantity and functionality of natural killer (NK) cells in hepatocellular carcinoma (HCC) have been associated with improved prognosis and survival. Therefore, NK cell-based immunotherapy has been proposed for treating HCC, relying on the activation of NK cell receptors like natural cytotoxicity receptors (NCRs), which recognize specific ligands on HCC cells. However, the effectiveness of this approach remains low due to tumor immune evasion.
Targeted protein degradation (TPD) is an alternative to conventional protein inhibition that is gaining attention due to advantages such as ensuring complete elimination of the target protein, reduced off-target effects or the potential to target previously inaccessible or “undruggable” proteins. Proteolysis targeting chimeras (PROTACs) are agents used for TPD that have proven effective for degradation of histone deacetylase (HDAC), among other different proteins.
Researchers from Wuyi University presented the discovery and preclinical characterization of kinesin spindle protein (KSP) degraders developed using proteolysis-targeting chimera (PROTAC) technology.