Receptor-interacting protein kinase 1 (RIPK1) helps promote the survival of cancer cells, and degrading it can sensitize tumors to immunotherapy against PD-1. Degrading the entire protein seems to be essential: merely blocking its kinase activity does not sensitize tumors.
Qingdao Putaike Biomedical Technology Co. Ltd. has divulged hydrophobic tag-based degraders comprising heat shock protein 90 (HSP90) ligands covalently linked to an androgen receptor (AR)-targeting moiety through a linker acting as AR degradation inducers reported to be useful for the treatment of acne, androgenic alopecia, hirsutism, metabolic disorders, breast cancer and prostate cancer.
LRRK2 plays a key role in the biology of multiple neurodegenerative disorders, including Parkinson’s disease (PD) and progressive supranuclear palsy (PSP), where mutations or altered activity are associated with impaired cellular signaling and neuronal decline.
In a study published in Molecular Therapy, researchers from H. Lee Moffitt Cancer Center and Research Institute and the University of South Florida developed an E6-targeting proteolysis targeting chimera (PROTAC) that inhibits the growth of human papillomavirus (HPV)-positive tumors. HPV is the most prevalent sexually transmitted infection worldwide, with persistent infections causing up to six different types of cancer.
CCNK is frequently upregulated in diverse tumor types, where its increased expression promotes proliferation and its depletion triggers apoptosis. Researchers from Guangdong Pharmaceutical University reported the discovery and preclinical characterization of a novel series of CCNK molecular glue degraders with antitumor activity.
G1 to S phase transition 1 (GSPT1) is a protein involved in cell cycle progression, translation termination, and protein homeostasis, and its overexpression has been implicated in various cancers. Although GSPT1 is considered a promising therapeutic target, the lack of conventional ligand-binding pockets has historically rendered it undruggable.
Raqualia Pharma Inc.’s Fimecs Inc. subsidiary has agreed with Astellas Pharma Inc. to add two new targets under their ongoing joint research. They entered into an agreement in 2022 to conduct joint research on targeted protein degradation.
Gluetacs Therapeutics (Shanghai) Co. Ltd. has synthesized molecular glue degraders comprising cereblon (CRBN) binding agents and protein degradation moieties reported to be useful for the treatment of cancer, infections, autoimmune diseases, anemia, transplant rejection, diabetes, cardiovascular disorders and inflammatory disorders, among others.
Blueprint Medicines Corp. has disclosed PROTAC compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a cyclin-dependent kinase 4 (CDK4)-targeting moiety potentially useful for the treatment of cancer.
In an effort to develop more effective estrogen receptor α (ERα) inhibitors, researchers at Nanjing University of Chinese Medicine and collaborators aimed to develop a proteolysis targeting chimera (PROTAC) against the receptor.
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