Shenzhen Targetrx Inc. has disclosed proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety covalently linked to a Bcr-Abl (Bcr-Abl1) kinase and its mutant targeting moiety through a linker reported to be useful for the treatment of cancer and immunological disorders.
Ascentage Pharma (Suzhou) Co. Ltd. and China Pharmaceutical University have identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase-binding moiety coupled to B-cell lymphoma 6 protein (BCL6)-targeting moiety through a linker reported to be useful for the treatment of cancer.
Amphista Therapeutics Ltd. has developed and presented data for AMX-883, a novel orally bioavailable bromodomain-containing protein 9 (BRD9) degradation inducer for acute myeloid leukemia (AML)
treatment.
Nikang Therapeutics Inc. has divulged proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a cyclin-dependent kinase 2 (CDK2)- and/or CDK4-targeting moiety through a linker reported to be useful for the treatment of cancer.
Uppthera Inc. has identified proteolysis targeting chimera (PROTAC) compounds comprising an E3 ubiquitin ligase binding moiety covalently linked to a serine/threonine-protein kinase PLK1 (STPK13)-targeting moiety reported to be useful for the treatment of cancer.
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.
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